Article

Lipid metabolism in trained rats: Effect of guarana (Paullinia cupana Mart.) supplementation

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Abstract

Guarana is widely consumed by athletes, either in supplements or in soft drinks, under the belief that it presents ergogenic and "fat burning" effects. We examined the effect of guarana supplementation (14 days) upon aspects of lipid metabolism in sedentary (C) and trained rats (T). To isolate the effect of caffeine from that of other components of guarana, we adopted two different doses of whole extract (G1-0.130 g/kg; G2-0.325 g/kg) or decaffeinated extract (DG1, DG2). Body weight, food and water intake; muscle fat content, oleate incorporation, glycogen content, and carnitine palmitoyltransferase I (CPT I) activity and mRNA expression; along with plasma lactate concentration, were assessed. Muscle oleate incorporation was decreased in rats receiving decaffeinated guarana in relation to G1 and G2; as was CPT I mRNA expression in the gastrocnemius. Whole extract supplementation, but not DG induced reduced plasma lactate concentration in trained rats. G1 showed higher muscle glycogen content compared with all other groups. The results show an effect of guarana on aspects of lipid metabolism, which is abolished by decaffeination. The changes in lipid metabolism of supplemented rats herein reported are associated with the methylxanthine content of guarana.

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... Paullinia cupana, commonly known as Guarana, is a climbing evergreen vine with small fruits and is native to the Amazon region [1,2]. Paullinia cupana seed extracts have been used in folk medicine since pre-Columbian times as stimulants, aphrodisiacs, and tonics [2]. ...
... Indeed, Paullinia cupana (Guarana) containing products are popular among athletes because of their ergogenic and "fat burning" effects [6]. Some studies have shown that Paullinia cupana positively affects lipid metabolism [1], enhances weight loss [7,8], and increases basal energy expenditure [4,9]. Thus, these data suggest that Paullinia cupana has antiobesity effects [4,[7][8][9]. ...
... Paullinia cupana extract (from seed) is approved in the United States as a food additive and is considered a dietary supplement, [3]; Paullinia cupana is also listed in the official Brazilian Pharmacopoeia [12]. Therefore, it is not surprising that Paullinia cupana (Guarana) is found today in a wide variety of drinks, foods, dietary/herbal supplements, and pharmaceuticals [1,12]. Consequently, perhaps concerned about the widespread use or potential abuse of Paullinia cupana-based products, the Committee on Herbal Medicinal Products (HMPC) of European Medicines Agency has recently launched a call to encourage the submission of scientific data on Paullinia cupana (Guarana) in order to prepare the corresponding herbal monograph [13]. ...
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Paullinia cupana is used in weight-loss programs as a constituent of medicinal/dietary supplements. This study aimed to assess a potential herb-drug interaction among a standardized (certified) Paullinia cupana extract and amiodarone (narrow therapeutic index drug) in rats. In a first pharmacokinetic study rats were simultaneously coadministered with a single dose of Paullinia cupana (821 mg/kg, p.o.) and amiodarone (50 mg/kg, p.o.), and in a second study rats were pretreated during 14 days with Paullinia cupana (821 mg/kg/day, p.o.) receiving amiodarone (50 mg/kg, p.o.) on the 15th day. Rats of the control groups received the corresponding volume of vehicle. Blood samples were collected at several time points after amiodarone dosing, and several tissues were harvested at the end of the experiments (24 h after dose). Plasma and tissue concentrations of amiodarone and its major metabolite (mono-N-desethylamiodarone) were measured and analysed. A significant reduction in the peak plasma concentration (73.2%) and in the extent of systemic exposure (57.8%) to amiodarone was found in rats simultaneously treated with Paullinia cupana and amiodarone; a decrease in tissue concentrations was also observed. This paper reports for the first time an herb-drug interaction between Paullinia cupana extract and amiodarone, which determined a great decrease on amiodarone bioavailability in rats.
... Other studies, using both aqueous extracts ( Barbosa and Mello, 2004;Campos et al., 2011) and hydroalcoholic extracts ( Lima et al., 2005;Bittencourt et al., 2013;Portella et al., 2013) revealed quan- tities of constituents similar. The caffeine ranged from 1.2 to 7.97% and the tannins from 1.5 to 12%. ...
... Guarana was placed alongside the plants with psychoanalep- tic activity (stimulants), with emphasis on anorexigenic or weight reduction properties. Although the consumption of guarana can induce changes in lipid metabolism, these effects have been asso- ciated with the methylxanthine content of the extract ( Lima et al., 2005). Guaraná showed anti-adipogenic potential due to its ability to modulate miRNAs and genes related to this process ( Lima et al., 2017) or an increase in energetic metabolism and stimulation of mitochondrial biogenesis, contributing to control of weight gain, even when associated with high-fat diet ( Lima et al., 2018). ...
... In addition, ground guarana seeds or their extracts may be used in association with other herbal drugs, usually in commer- cially available formulations ( Antunes et al., 2001;Boozer et al., 2001;Campos et al., 2004;Bérubé-Parent et al., 2005;Opala et al., 2006;Ruxton et al., 2007;Kennedy et al., 2008;Bulku et al., 2010;Pomportes et al., 2015aPomportes et al., , 2017. Several studies have reported on an extract obtained using a controlled temperature, defined extraction time and standardized amount of solvent ( Bydlowski et al., 1988;Bydlowski et al., 1991;Miura et al., 1998;Barbosa and Mello, 2004;Basile et al., 2005;Lima et al., 2005;Haskell et al., 2007;Jippo et al., 2009;Portella et al., 2013;Machado et al., 2015). Other authors grind the intact seed and subsequently extract it with organic sol- vents and then semi-purify these extracts, commonly by means of partitions with different solvents (Otobone et al., 2005(Otobone et al., , 2007Antonelli-Ushirobira et al., 2007;Yamaguti-Sasaki et al., 2007;Roncon et al., 2011;Dalonso and Petkowicz, 2012;Rangel et al., 2013;Matsuura et al., 2015) or other types of extraction, for exam- ple, supercritical extraction ( Mehr et al., 1996;Saldã na et al., 2002;Marques et al., 2016). ...
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Seeds of guarana (Paullinia cupana Kunth, Sapindaceae) feature diverse pharmacological functions, for example, antimicrobial, antioxidant, anticarcinogenic, stimulating, and cognitive functions, as well as liver protection and weight loss. Many of these actions are probably due to the high content of methylxanthines and tannins in its seeds. In Brazil, the world's largest producer of guarana, the plant material is predominantly used in the soft drinks industry, although it is also used in the cosmetic and pharmaceutical industries. Although the Amazon region has the largest cropping area, the state of Bahia is the main guarana producer in Brazil (71%). This review focuses mainly on the possible pharmacological actions of guarana that have been investigated. Moreover, it discusses less-considered topics, such as the toxicology and quality control of seeds and extractives of guarana that will ultimately influence the safety of its use. In addition, it presents a detailed discussion of the methods used to prepare herbal drugs and their extracts, focusing on the importance of standardization and on the direct impact of preparatory factors, on the pharmacological properties of guarana extracts.
... As primeiras evidências demonstrando a importância do complexo CPT na oxidação de lipídios foram destacadas por Frityz e Yue (6) , que através da incubação de cardiomiócitos, mostraram evidências do papel do complexo CPT no transporte de AG para o interior da mitocôndria em conjunto com a carnitina. Atualmente, acredita-se que a enzima CPT I esteja envolvida na regulação da oxidação de lipídios, limitando a entrada de AG de cadeia longa para o interior da mitocôndria, tendo a sua atividade e expressão gênica moduladas pelo treinamento físico (4)(5)(6)(7)(8) . ...
... Sabe-se que o treinamento pode aumentar a eficiência do transporte de ácidos graxos de cadeia longa através da membrana mitocondrial pela otimização no funcionamento do complexo CPT (5)(6)(7)(8) , por meio da diminuição da concentração de malonil-CoA, inibidor reversível da atividade da CPT I, que se encontra diminuído no músculo esquelético durante a realização do exercício, explicando dessa maneira o aumento na oxidação de AG promovida pelo treinamento (44) . A acetil-CoA caboxilase (ACC) é a enzima que cataliza a formação de malonil-CoA. ...
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Fatty acids are an important source of energy for the skeletal muscle. During exercise, their mobilization is increased to supply the muscle energetic needs. Many points of regulation act in the fatty acids metabolism, where the carnitine palmytoiltransferase (CPT) complex is the main control system. Three compounds named CPT I, CPT II and carnitine acyl carnitine translocase (CACT) are components of this system. Its function is to control the influx of fatty acids inside the mitochondria for posterior oxidation and energy production. There is a pronounced increase in both activity and gene expression of CPT I in the skeletal muscle in response to exercise. Due to its importance in lipid metabolism, the controlling mechanisms are reviewed in the present study. The modulation of gene expression by peroxisome proliferator-activated receptors (PPARs) alpha and beta during the physical training is also discussed in this review.
... Guarana extract can also prevent ventricular fibrillation.43 These studies demonstrate the multipronged role played by guarana seed extract in cell metabolism.38–41 ...
... Guarana is a rich source of caffeine, and it is a source of energy in STG. However, it also helps stimulate the metabolic rate, and can improve thermogenesis.38 The amount of caffeine present in STG is about the same as half a cup of coffee (45 mg). ...
Article
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A novel dietary supplement composed of three well-known phytochemicals, namely, Salvia officinalis (sage) extract, Camellia sinensis (oolong tea) extract, and Paullinia cupana (guarana) extract, and two prominent vitamins (thiamine and niacin) was designed to provide nutritional support by enhancing metabolism and maintaining healthy weight and energy. The present study evaluated the safety of this dietary supplement (STG; S=sage; T=tea; G=guarana) and assessed changes in target organ antioxidant enzymes (liver, kidneys and heart), serum chemistry profiles and organ histopathology in Fisher 344 rats. Adult male and female Fisher 344 rats were fed control (no STG) or STG containing (1X and 7X, 1X=daily human dose) diets and sacrificed after 2 and 4 months. Serum chemistry analysis and histopathological examination of three vital target organs disclosed no adverse influence on protein, lipid and carbohydrate profiles, genomic integrity of the liver and/or the tissue architecture. However, analysis of the most important antioxidant components in the liver, kidney and heart homogenates revealed a dramatic increase in total glutathione concentrations, glutathione peroxidase and superoxide dismutase enzyme activities. Concomitantly, oxidative stress levels (malondialdehyde accumulation) in these three organs were less than control. Organ specific serum markers (ALT/AST for the liver; CPK/AST for the heart; BUN/creatinine for kidneys) and the genomic integrity disclosed no STG-induced alteration. Some of the serum components (lipid and protein) showed insignificant changes. Overall, STG-exposed rats were more active, and the results suggest that STG exposure produces normal serum chemistry coupled with elevated antioxidant capacity in rats fed up to seven times the normal human dose and does not adversely influence any of the vital target organs. Additionally, this study reiterates the potential benefits of exposure to a pharmacologically relevant combination of phytochemicals compared to a single phytochemical entity.
... The authors concluded that botanical stimulants using guaraná as a caffeine source presented characteristics similar to those of their pharmaceutical counterparts. These results support the several biological actions of guaraná that are described in the literature, including positive effects on metabolic variables associated with cardiovascular diseases risks factors, such as obesity [6][7][8], and decreases in the lipid parameters [9]. an additional investigation using in vitro and in vivo assays showed that guaraná decreases the oxidation of lDl cholesterol [10]. ...
... *p < 0.05; **p < 0.01; ***p < 0.001 as metabolic disorders, including obesity, are associated with low-grade inflammation and other immune dysfunctions [23,24], the potential effect of guaraná on blood inflammation biomarkers was tested here. However, it is difficult to isolate the potential immunomodulatory, antiobesogenic effect of guaraná that has been suggested by previous studies [6][7][8][9]25]. Because the inflammatory response is generally acute and does not require a large intervention time for evaluation, the present investigation analysed the effect of guaraná on the levels of blood cytokines independent of body weight loss. ...
Article
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Emerging evidences suggest that biological effects of chemical molecules could to be differentially modulated by gene polymorphisms of several pathways including oxidative-inflammatory metabolism. Guarana (Paullinia cupana) a plant traditionally consumed by Amazon indigenous communities and nowadays used as caffeine source of energetic beverages presents antiinflammatory effect [1]. On the other hand, the same inflammatory cytokines modulated by guarana (G) are also influenced by genetic polymorphism in the superoxide dismutase manganese-dependent gene (SOD2), which an alanine (Ala) is substituted by valine (Val) in 16 codon [2]. In this polymorphism, VV genotype presents less enzyme efficiency and has being associated with several metabolic diseases associated with systemic inflammation. Therefore, we performed an in vitro assay to test the potential Ala16Val-SOD2 polymorphism effects on level of inflammatory (IL-1β, IL = 6, TNFα, Igγ) and antiinflammatory (IL-10) cytokines of human peripheral blood mononuclear cells (PBMCs) treated with G extract at different concentrations (1 – 20 mg/mL guaraná). The experimental conditions (Ala16Val-SOD2 genotyping by PCR protocol, cell culture and evaluation of cytokines by ELISA immunoassay) were similar to described previously [1,2]. The inflammatory cytokines levels decreased at 10 mg/mL G concentration independent of genotypes, with exception of IL-1β. This cytokine maintained similar values between control (C) and G treatments in AA-PBMCs. However, the IL-1β level of AA-PBMCs was lower than other genotypes (C-AA 24 ± 1/G-AA 22 ± 1; C-VV = 99 ± 2; G-VV = 88 ± 3; C-AV = 54 ± 3; G-AV = 44 ± 2 pg/mL, p= 0.001) and this condition could to explain this result. The antiinflammatory IL-10 cytokine increased in all cells G-treated. In conclusion, our results suggest a slight influence of Ala16Val-SOD2 on antiinflammatory effect induced by guaraná and a potential benefice including VV cells that present high levels of inflammatory cytokines.
... The authors concluded that botanical stimulants using guaraná as a caffeine source presented characteristics similar to those of their pharmaceutical counterparts. These results support the several biological actions of guaraná that are described in the literature, including positive effects on metabolic variables associated with cardiovascular diseases risks factors, such as obesity [6][7][8], and decreases in the lipid parameters [9]. an additional investigation using in vitro and in vivo assays showed that guaraná decreases the oxidation of lDl cholesterol [10]. ...
... *p < 0.05; **p < 0.01; ***p < 0.001 as metabolic disorders, including obesity, are associated with low-grade inflammation and other immune dysfunctions [23,24], the potential effect of guaraná on blood inflammation biomarkers was tested here. However, it is difficult to isolate the potential immunomodulatory, antiobesogenic effect of guaraná that has been suggested by previous studies [6][7][8][9]25]. Because the inflammatory response is generally acute and does not require a large intervention time for evaluation, the present investigation analysed the effect of guaraná on the levels of blood cytokines independent of body weight loss. ...
Article
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Guarana powder is an antiobesogenic supplement; however, its effect on inflammatory biomarkers has not yet been determined. Therefore, this study analysed whether guarana supplementation can differentially modulate the levels of proinflammatory cytokines [interleukin 6 (IL-6), tumour necrosis factor-alpha, interleukin 1 beta (IL-1 beta), interferon-gamma (Ig-gamma)] and anti-inflammatory interleukin 10 (IL-10) from in vitro and in vivo protocols. In the pilot in vitro protocol, human peripheral blood mononuclear cells were exposed to guarana, as well as to resveratrol, quercetin and ascorbic acid as positive controls. The effect of guarana on cytokine levels was also evaluated in culture medium supplemented with glucose and insulin. A randomised, placebo-controlled in vivo assay was also performed to evaluate the potential influence of guarana on the blood cytokine levels of 14 healthy volunteers supplemented for 14 days. The effect of guarana was similar to that of resveratrol, a known anti-inflammatory molecule, decreasing IL-1 beta, IL-10 and Ig-gamma levels and increasing IL-10 levels compared to those of the control group. The in vitro insulin supplementation potentiated the effect of guarana on some cytokines. A decreasing effect on the blood inflammatory cytokine levels, along with an increase in IL-10 levels, was also observed in volunteers supplemented with guarana. In conclusion, guarana positively modulates cytokines associated with inflammatory metabolism.
... 89 Extracts of seeds from the fruit of guaraná contain caffeine at concentrations that vary from 2% to as high as 15% of the dry weight. 90,91 Guaraná extracts also contain saponins and tannins, 92 which exert antioxidant effects, 93 and the flavonoids catechin and epicatechin, which reduce platelet aggregation. 94 Several studies with rodents have compared the behavioral effects of guaraná with caffeine in an attempt to clarify whether any observed effects were due to the caffeine content alone or to other active ingredients. ...
... The effect of the caffeine content in guaraná on lipid metabolism in trained and sedentary rats was examined by comparing normal and decaffeinated extracts of the plant powder. 91 Measures of lipid metabolism, which included muscle oleate incorporation, carnitine palmitoyltransferase activity, and mRNA expression and plasma lactate concentrations during exercise, were unchanged following consumption of the decaffeinated guaraná extract, but they were indicative of increased fatty acid oxidation with the consumption of the normal extract. The findings imply that these effects were due to the caffeine content of the intact extract. ...
Article
Energy drinks (EDs) contain caffeine and are a new, popular category of beverage. It has been suggested that EDs enhance physical and cognitive performance; however, it is unclear whether the claimed benefits are attributable to components other than caffeine. A typical 235 mL ED provides between 40 and 250 mg of caffeine, equating to doses that improve cognitive and, at the higher levels, physical performance. EDs often contain taurine, guaraná, ginseng, glucuronolactone, B-vitamins, and other compounds. A literature search using PubMed, Psych Info, and Google Scholar identified 32 articles that examined the effects of ED ingredients alone and/or in combination with caffeine on physical or cognitive performance. A systematic evaluation of the evidence-based findings in these articles was then conducted. With the exception of some weak evidence for glucose and guaraná extract, there is an overwhelming lack of evidence to substantiate claims that components of EDs, other than caffeine, contribute to the enhancement of physical or cognitive performance. Additional well-designed, randomized, placebo-controlled studies replicated across laboratories are needed in order to assess claims made for these products.
... Previous experimental investigations have suggested that guaraná has positive effects on lipid metabolism [7], in body weight loss [8], and increases basal energy expenditure [9]. Furthermore, studies suggested that guaraná exhibits a cardioprotective effect by inhibiting platelet aggregation [10]. ...
... This positive effect of guaraná could be confirmed by in vitro results which showed an increased resistance to LDL oxidation. It was due to high content of polyphenolic compounds, which may act to prevent atherogenesis through a combination of effects, including the other positive effects of guaraná on lipid metabolism [7], in body weight loss [8], and increases basal energy expenditure [9], besides the lower prevalence of hypertension, metabolic syndrome, and lower cholesterol and AOPP levels in GI subjects [11]. Considering these results, our study indicates that consumption of guaraná regularly or its possible inclusion in diet-based therapies could yield certain health benefits and potential defense against oxidative stress and metabolic disorders. ...
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Background Previous experimental investigations have suggested that guaraná (Paullinia cupana Kunth, supplied by EMBRAPA Oriental) consumption is associated with a lower prevalence of cardiovascular metabolic diseases and has positive effects on lipid metabolism, mainly related to low density lipoprotein (LDL) levels. As LDL oxidation is an important initial event in the development of atherosclerosis, we performed in vitro and in vivo studies to observe the potential effects of guaraná on LDL and serum oxidation. Methods The in vivo protocol was performed using blood samples from 42 healthy elderly subjects who habitually ingested guaraná (GI) or never ingested guaraná (NG). The formation of conjugated dienes (CDs) was analyzed from serum samples. The in vitro protocols were performed using LDL obtained from 3 healthy, non-fasted, normolipidemic voluntary donors who did not habitually ingest guaraná in their diets. The LDL samples were exposed to 5 different guaraná concentrations (0.05, 0.1, 0.5, 1, and 5 μg/mL). Results GI subjects demonstrated lower LDL oxidation than did NG subjects (reduction of 27%, p < 0.0014), independent of other variables. In the GI group the total polyphenols was positively associated with LDL levels. Also, guaraná demonstrated a high antioxidant activity in vitro, mainly at concentrations of 1 and 5 μg/mL, demonstrated by suppression of CDs and TBARS productions, tryptophan destruction and high TRAP activity. Conclusions Guaraná, similar to other foods rich in caffeine and catechins such as green tea, has some effect on LDL oxidation that could partially explain the protective effects of this food in cardiometabolic diseases.
... In addition to the psychoactive effects, the use of guarana for metabolic disorders has been widely studied because it possesses functional properties similar to green tea, which is also rich in catechins. Studies have shown that guarana positively affects lipid metabolism, increases basal energy and weight loss and may be useful for obesity treatments (Boozer et al., 2001;Lima et al., 2005;Opala et al., 2006;Krewer et al., 2011b). ...
... Guarana has been suggested to improve cognitive performance, mental fatigue, and mood at physiologically relevant dosages; an effect supported by several research studies (Scholey and Haskell, 2008). Guarana has also been associated with inducing lipid metabolism, probably due to its methylxanthine content (Lima et al., 2005). Additionally, guarana has been shown to exert no toxic effects when consumed both in acute high dosages as well as in chronic lower dosages (Mattei et al., 1998). ...
Article
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In recent years, there has been an increase in the consumption of energy drinks, containing besides calories, other ingredients suspected to boost mental, emotional and physical alertness of the consumers. Such drinks are widely consumed by young people for a variety of reasons. However, from a public health point of view, little seems to be understood of the health benefits and other implications of these drinks by their consumers. Therefore, the understanding that energy drinks have stimulating properties that can boost heart beat rate and blood pressure, dehydrate the body, aggravate the effects of other stimulants, and prevent sleep may help as a decision making tools for the consumers of such products. This review examines some of the important active ingredients of energy drinks, their origins, sources, benefits and side effects. It is concluded that energy drinks, despite the variations in brand name contain bio-active ingredients; therefore further research is needed on their potential hazards.
... Caffeine also has a stimulatory effect on thermogenesis (Acheson and others 1980; Dulloo and others 1989; Astrup and others 1990; Bracco and others 1995). In addition, caffeine consumption has also been linked to reduced food intake (Tremblay and others 1988; Racotta and others 1994; Lima and others 2005) and to promote lipolysis in both animals and humans (Hasegawa and Mori 2000; Zheng and others 2004; Kobayashi-Hattori and others 2005; Lopez-Garcia and others 2006). A review regarding caffeine consumption concluded that among the healthy adult population, a moderate daily caffeine intake of ≤400 mg (equivalent to 6 mg/kg/d for a 65 kg person) was not associated with any adverse effects (Nawrot and others 2003). ...
Article
  The consumption of energy drinks is rapidly increasing, as demonstrated by their large market growth. The targeted demographic group is teenagers, young adults, 18 to 34 y old; although expansion into nontraditional markets is also occurring. It is claimed that energy drinks can offer an increased energy boost related to their ingredient profile of caffeine, taurine, herbal extracts, and vitamins. Research suggests that energy drink formulations, in addition to increasing energy utilization, may also improve mood, enhance physical endurance, reduce mental fatigue, and increase reaction time. However, in most cases, the corresponding mechanisms of action are not clear. In addition, concerns have been raised over their safety and with a currently weak regulatory environment, efforts need to be made to ensure consumer safety. The objective of this article is to review the current U.S. energy drink market with emphasis on its market size, target demographic, active ingredients, potential benefits, safety, and regulations.
... Moreover, during ketogenic diet periods, athletes assumed 1 caplet in of a multivitamin-mineral supplement each morning ([19,25,26]. The composition of the caplets was: Extracts A, ml/day 20 Durvillea antarctica, black radish, mint, liquorice, artichoke, horsetail, burdock, dandelion, rhubarb, gentian, lemon balm, chinaroot, juniper, spear grass, elder, fucus, anise, parsley, bearberry, horehound Extracts B, ml/day 20 Serenoa, Red clover, Chervil, Bean, Elder, Dandelion, Uncaria, Equisetum, Horehound, Rosemary Extracts C, ml/day 50 Horsetail, asparagus, birch, cypress, couch grass, corn, dandelion, grape, fennel, elder, rosehip, anise Extracts D, ml/day (only weeks 1 and 2) 40 Eleuthero, eurycoma longifolia, ginseng, corn, miura puama, grape, guaranà, arabic coffee, ginger C Equisetum Antioxidant [32] Dandelion diuretic [33] (Taraxacum officinale glycemic control [34] D Ginseng Ameliorate the commonly [35] Miura Puama reported symptoms of [36] Guaranà weakness and tiredness during the 1 st phase of ketosis (1/2 weeks) [37] During the second period of the study, the athletes themselves assumed the function of a control group and consumed their usual diet that is very close to the present US diet western diet (WD) [38] with the exception of fat origin (monounsaturated fats, i.e. olive oil in our subjects vs. saturated fats in the typical US diet). The diet consumed was composed mainly of potatoes, whole grains (bread, pasta, whole wheat, rice, and potatoes), meat, fish, eggs, poultry, vegetables, legumes, fruits, condiments (mainly olive oil), whole milk and wine. ...
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Background: Despite the increasing use of very low carbohydrate ketogenic diets (VLCKD) in weight control and management of the metabolic syndrome there is a paucity of research about effects of VLCKD on sport performance. Ketogenic diets may be useful in sports that include weight class divisions and the aim of our study was to investigate the influence of VLCKD on explosive strength performance. Methods: 8 athletes, elite artistic gymnasts (age 20.9 ± 5.5 yrs) were recruited. We analyzed body composition and various performance aspects (hanging straight leg raise, ground push up, parallel bar dips, pull up, squat jump, countermovement jump, 30 sec continuous jumps) before and after 30 days of a modified ketogenic diet. The diet was based on green vegetables, olive oil, fish and meat plus dishes composed of high quality protein and virtually zero carbohydrates, but which mimicked their taste, with the addition of some herbal extracts. During the VLCKD the athletes performed the normal training program. After three months the same protocol, tests were performed before and after 30 days of the athletes' usual diet (a typically western diet, WD). A one-way Anova for repeated measurements was used. Results: No significant differences were detected between VLCKD and WD in all strength tests. Significant differences were found in body weight and body composition: after VLCKD there was a decrease in body weight (from 69.6 ± 7.3 Kg to 68.0 ± 7.5 Kg) and fat mass (from 5.3 ± 1.3 Kg to 3.4 ± 0.8 Kg p < 0.001) with a non-significant increase in muscle mass. Conclusions: Despite concerns of coaches and doctors about the possible detrimental effects of low carbohydrate diets on athletic performance and the well known importance of carbohydrates there are no data about VLCKD and strength performance. The undeniable and sudden effect of VLCKD on fat loss may be useful for those athletes who compete in sports based on weight class. We have demonstrated that using VLCKD for a relatively short time period (i.e. 30 days) can decrease body weight and body fat without negative effects on strength performance in high level athletes.
... Por lo anterior, no se recomienda en individuos con hipertensión arterial, enfermedad coronaria, obesidad e intolerancia a los carbohidratos (29). En cuanto a la pérdida de peso, se ha evidenciado que este efecto puede lograrse por la capacidad anorexígena del guaraná (30)(31). . Neuro-psiquiátrico: los estudios sugieren que después de la administración de guaraná hay mejoría en el desempeño cognitivo, velocidad de atención y memoria, memoria secundaria, memoria de trabajo, razonamiento lógico y razonamiento abstracto. ...
Article
Background. Energy drinks can be found almost everywhere; their consumption has increased due to ease of access to them, their stimulant properties and the idea that they are harmless. Scarce knowledge about their characteristics has led to them being confused with rehydrating drinks and thus their indiscriminate use, even though rehydrating drinks seek to prevent dehydration and energy drinks have a stimulant effect. Objective. Describing energy drinks' components and analysing their effects, undesired reactions and precautions regarding their use. Materials and methods. The literature in Pubmed was reviewed using the MeSH terms «caffeine» OR «taurine» OR «gluconates» combined with the term «energy drinks» with specifiers, 42 articles being found. The summaries were analysed and 29 articles were included in the study. Results. Energy drinks contain methylxanthines, carbohydrates, taurine, vitamins and/or guaraná (caffeine source from an Amazon region berry). Most stimulant effects happen at the expense of high concentrations of methylxanthines such as caffeine. Such high concentrations increase the risk of poisoning and caffeine dependence. Cases of arrhythmia, heart attack, exacerbation of psychiatric symtomatology and convulsions associated with their consumption have been reported. Furthermore, mixing them with alcohol increases alcohol poisoning-related damage. They are not recommended for sportspeople due to their diuretic and cardiovascular effects. Conclusions. It has been shown that energy drink components are not completely innocuous. Even though their chronic effects remain unknown, the literature does warn about the damage to health which could be caused by strong acute consumption or frequent consumption. Measures must thus be implemented which are aimed at broadcasting the consequences of these substances and restricting their consumption by at-risk populations.
... The proportion of caffeine in dry weight of guarana plant seeds is 2-6%, which corresponds to 2 fold of the caffeine present in the coffee beans (de Oliveira Campos et al., 2011;Lima et al., 2005;Haskell, Kennedy, Wesnes, Milne, & Scholey, 2007;EFSA, 2008;Pennay et al., 2011). Caffeine contents of leaves, seeds and crusts of the dry weight of guarana are different. ...
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Botanically known as Paullinia cupana (Sapindaceae), guarana is widely grown in Amazon region and naturally in Brazil, Ecuador, Venezuela, Colombia, Peru and the Cooperative Republic of Guyana. It is used in sugar and/or carbonated soft drinks, herbal teas and energy drinks in the form of guarana extract. Guarana has antioxidant, antibacterial, antifungal, antidepressant effects; improves cognitive performance; triggers weight loss and reduces lipid peroxidation. It has important effects on various methods and treatments from cardiovascular to neurological diseases, from memory and liveliness to cancer. It is also known that guarana enhances biological activities and psychological effects on the body. This compilation has been conducted to evaluate the chemical and physical properties of guarana, its metabolites, the mechanism of its effect on psychological activities and health. GUHES 2 (2020) 709067
... This increase in OVX animals' body weight is in accordance with the previous observations reported in the literature (15,37). Weight gain is the result of complex multifaceted processes, involving particularly the resistance to leptin, a decreased expression of adiponectin and excessive conversion of glucose into fat (41). It could be explained by deposits of fat subsequent to the alteration of the energetic metabolism of lipids and increased abdominal adipose tissue caused by estrogen deficiency engendered by ovariectomy (42). ...
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The present study aims to determine the estrogenicity of Millettia macrophylla , a Cameroonian medicinal plant, in ovariectomized rats and to investigate the underlying mecha -nisms, in order to justify scientifically its traditional use. To accomplish this objective, we used dichloromethane (DCM) and methanol (MeOH) extracts of the stem bark of M. macrophylla. In the cell culture based assay, the MeOH extract significantly transactivated estrogen receptor a (ER a) and estrogen receptor b (ER b); in addition, the estrogen-like effects of both, DCM and MeOH extracts, could be inhibited in vitro by the pure ER antagonist ICI 182,780, indicating that these effects were primarily mediated through ERs. In animal experiments, both DCM and MeOH extracts significantly increased the uterine and vaginal epithelial heights in the 3-day treatment assay, while only the MeOH extract exhibited such effects in the sub-chronic treatment regimen. Furthermore, the MeOH extract significantly decreased fasting serum triglycerides, total cholesterol levels and artherogenic risk in the sub-chronic treatment. These results indicate that M. macrophylla extracts have estrogen-like effects supporting their traditional use in Cameroon to alleviate some menopausal problems (See graphical abstract in Supplementary Fig. 1, available in the online version only).
... Teobromina i teofilina mogą powstawać w organizmie człowieka na skutek przemian kofeiny [11], ale mogą być także dostarczane jako składnik kakao, kawy czy herbaty [5,6]. W ekstrakcie herbaty zawartość teofiliny szacuje się na poziomie około 1,5 mg/l [5,15], a teobrominy na poziomie 7,5 -21 mg/l [7,13]. Zawartość tych alkaloidów w 100 g czekolady zwykle nie przekracza 3 mg w przypadku teofiliny i 1 g w przypadku teobrominy [7]. ...
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The effect was assessed of the N-methylxanthines: caffeine, theophylline, and theobromine, commonly consumed with the diet, on the emulsification of butter lipids and bioavailability thereof under the in vitro simulated conditions of human stomach and intestines. The research material was farmhouse butter containing a 40 μmol/1g addition of the tested compounds. Based on the results obtained, it was found that, in the dose analyzed, each of the alkaloids intensified the process of forming the emulsion by increasing the dispersion degree thereof. The power of the pro-emulsifying activity of alkaloids depended on the arrangement of methyl groups in a molecule and increased according to the order: 1,3-dimethylxanthine (theophylline) → 1,3,7-thrimethylxanthine (caffeine) → 3,7-dimethylxanthine (theobromine). At the same time, each of the alkaloids significantly reduced the bioavailability of lipids. In the case of theophylline, the amount of fatty acids and glycerol, released from the lipids, decreased by 9% on the average compared to the control sample; in the case of caffeine: by 16%, and as for the theobromine by as much as 27%. The results as indicated above suggest that under the conditions of simulated digestion of lipids in the alimentary canal, the alkaloids must have impacted not only the hydrophobic substrate that stimulated emulsification thereof, but, also, the pancreatic lipase. In the latter case, they partially displaced the pancreatic lipase from the micelle's surface, and, thereby, reduced its direct contact with the substrate, and effectively inhibited it.
... This increase in OVX animals' body weight is in accordance with the previous observations reported in the literature (15,37). Weight gain is the result of complex multifaceted processes, involving particularly the resistance to leptin, a decreased expression of adiponectin and excessive conversion of glucose into fat (41). It could be explained by deposits of fat subsequent to the alteration of the energetic metabolism of lipids and increased abdominal adipose tissue caused by estrogen deficiency engendered by ovariectomy (42). ...
Article
Full-text available
The present study aims to determine the estrogenicity of Millettia macrophylla, a Cameroonian medicinal plant, in ovariectomized rats and to investigate the underlying mechanisms, in order to justify scientifically its traditional use. To accomplish this objective, we used dichloromethane (DCM) and methanol (MeOH) extracts of the stem bark of M. macrophylla. In the cell culture based assay, the MeOH extract significantly transactivated estrogen receptor α (ERα) and estrogen receptor β (ERβ); in addition, the estrogen-like effects of both, DCM and MeOH extracts, could be inhibited in vitro by the pure ER antagonist ICI 182,780, indicating that these effects were primarily mediated through ERs. In animal experiments, both DCM and MeOH extracts significantly increased the uterine and vaginal epithelial heights in the 3-day treatment assay, while only the MeOH extract exhibited such effects in the sub-chronic treatment regimen. Furthermore, the MeOH extract significantly decreased fasting serum triglycerides, total cholesterol levels and artherogenic risk in the sub-chronic treatment. These results indicate that M. macrophylla extracts have estrogen-like effects supporting their traditional use in Cameroon to alleviate some menopausal problems (See graphical abstract in Supplementary Fig. 1, available in the online version only).
... Furthermore, ecto-adenosine deaminase activity (E-ADA) is another important enzyme that catalyzes the irreversible deamination of adenosine and 2′-deoxyadenosine to inosine and 2′-deoxyinosine, respectively , therefore contributing to the removal of adenosine from the extracellular compartment (Latini and Pedata, 2001). In addition, previous experimental investigations have suggested that guaraná (Paullinia cupana) has positive effects on lipid metabolism because increased metabolism of adipose tissue in rats was observed with increasing lipolysis because of the activation of adenosine A1 receptors (Lima et al., 2005) as well as body weight loss (Boozer et al., 2001). Guaraná is a rich source of caffeine, which stimulates the metabolism and may enhance thermogenesis , acting as an ergogenic agent and assisting in the degradation of lipids and atherosclerosis prevention (Shimada et al., 2004). ...
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Hypercholesterolemia is a metabolic disorder characterized by high levels of low-density lipoprotein and blood cholesterol, causing inflammatory lesion. Purinergic signaling modulates the inflammatory and immune responses through adenine nucleotides and nucleoside. Guaraná has hypocholesterolemic and antiinflammatory properties. Considering that there are few studies demonstrating the effects of guaraná powder on the metabolism of adenine nucleotides, we investigated its effects on the activity of ecto-nucleoside triphosphate diphosphohydrolase (E-NTPDase) and ecto-adenosine deaminase activity in lymphocytes of rats with diet-induced hypercholesterolemia. The rats were divided into hypercholesterolemic and normal diet groups. Each group was subdivided by treatment: saline, guaraná powder 12.5, 25, or 50 mg/kg/day and caffeine concentration equivalent to highest dose of guaraná, fed orally for 30 days. An increase in adenosine triphosphate hydrolysis was observed in the lymphocytes of rats with hypercholesterolemia and treated with 25 or 50 mg/kg/day when compared with the other groups. The hypercholesterolemic group treated with the highest concentration of guaraná powder showed decreased ecto-adenosine deaminase activity compared with the normal diet groups. Guaraná was able to reduce the total cholesterol and low-density lipoprotein cholesterol to basal levels in hypercholesterolemic rats. High concentrations of guaraná associated with a hypercholesterolemic diet are likely to have contributed to the reduction of the inflammatory process. Copyright © 2015 John Wiley & Sons, Ltd.
... Os autores também demonstraram que doses elevadas e o uso de cafeína isolada não foram capazes de produzir o mesmo efeito. Lima et al. (2005) evidenciaram que o extrato de P. cupana aumentou o metabolismo de lipídeos em ratos e que este efeito está associado à presença da cafeína. Quanto à efeitos psicológicos do uso, Silvestrini, Mariano e Cosentino (2013) demonstraram que 350 mg administradas três vezes por dia por cinco dias consecutivos não é capaz de alterar as escalas de ansiedade, bem estar e de humor, porém em um relato de caso de uma paciente de 38 anos indica a possibilidade de atrofia do lobo frontal direito do cérebro após uma superdosagem (PENDLETON et al., 2012). ...
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RESUMO Considerando-se a crescente demanda da utilização de fitoterápicos em academias de musculação, o presente estudo objetivou avaliar a forma de obtenção de informações sobre os fitoterápicos e os riscos causados por tais usos em academias de musculação. Aplicaram-se formulários estruturados à praticantes de atividades físicas de duas academias de ginástica de Juiz de Fora/MG. Realizou-se pesquisa em literatura científica sobre as espécies utilizadas. O principal objetivo para o uso de fitoterápicos ergogênicos foi o emagrecimento e a principal alegação para o uso foi melhoria no desempenho para a realização da atividade física praticada. Encontrou-se que Camellia sinensis, Baccharis trimera, Paullinia cupana, Phaseoulus vulgaris e Gymnema sylvestre vem sendo usados de maneira consonante com a literatura científica. Citrus aurantium apresentou atividade comprovada, porém vários artigos discutem sua toxicidade. Tribulus terrestris apresentou-se contraditório, uma vez que alguns artigos comprovam sua eficácia e outros comprovam sua incapacidade de exercer efeitos significativos. Não foram encontrados artigos que discutem a atividade citada para Oenothera biennis e Cynara scolymus. Nota-se que mesmo a legislação estando de acordo com a realidade dos profissionais de saúde, esta não é eficiente em garantir o uso respaldado por médicos, nutricionistas e farmacêuticos no âmbito de academias de musculação.
... Single therapies -NSAID application: A dose of 1 g diclofenac sodium gel generic 10 mg/g (EMS®, Santo André, São Paulo, Brazil) was used on the knee joint previously subjected to OA induction. -Physical exercise protocol: The physical exercise protocol used was adapted from the study by Lima et al. [16]. A 100 × 50 × 75-cm glass tank with water at a temperature of 31°C was used for this purpose. ...
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Osteoarthritis (OA) triggers increased levels of inflammatory markers, including prostaglandin (PG) E2 and proinflammatory cytokines. The elevation of cytokine levels is closely associated with increased articular tissue degeneration. Thus, the use of combination therapies may presumably be able to enhance the effects on the modulation of inflammatory markers. The present study aimed to evaluate and compare the effects of photobiomodulation therapy (PBMT), physical exercise, and topical nonsteroidal anti-inflammatory drug (NSAID) use on the inflammatory process after they were applied either alone or in different combinations. OA was induced by intra-articular papain injection in the knee of rats. After 21 days, the animals began treatment with a topical NSAID and/or with physical exercise and/or PBMT. Treatments were performed three times a week for eight consecutive weeks, totaling 24 therapy sessions. Analysis of real-time polymerase chain reaction (RT-PCR) gene expression; interleukin (IL)-1β, IL-6, and tumor necrosis factor alpha (TNF-α) protein expression; and PGE2 levels by enzyme-linked immunosorbent assay (ELISA) was conducted. Our results showed that PBMT alone and Exerc + PBMT significantly reduced IL-1β gene expression (p < 0.05) while no treatment changed both IL-6 and TNF-α gene expression. Treatment with NSAID alone, PBMT alone, Exerc + PBMT, and NSAID + PBMT reduced IL-1β protein expression (p < 0.05). All therapies significantly reduced IL-6 and TNF-α protein expression (p < 0.05) compared with the OA group. Similarly, all therapies, except Exerc, reduced the levels of PGE2 (p < 0.05) compared with the OA group. The results from the present study indicate that treatment with PBMT is more effective in modulating the inflammatory process underlying OA when compared with the other therapies tested.
... Previous experimental investigations have suggested that guarana (Paullinia cupana) may increase metabolism of adipose tissue in rats thereby increasing lipolysis as a result of the activation of adenosine A1 receptors [32] and reduction of body weight [33]. Guarana is a rich source of caffeine, which may stimulate the metabolism and enhance thermogenesis by acting as an ergogenic agent, assisting in the degradation of lipids and prevention of atherosclerosis [34]. ...
Article
Hyperlipidemia is a risk factor for the development of cognitive dysfunction and atherosclerosis. Currently, the natural compounds have received special attention in relation to the treatment of diseases due to their low cost and wide margin of safety. Thus, the aim of this study was to determine the possible preventive effect of guarana powder (Paullinia cupana) on memory impairment and acetylcholinesterase (AChE) activity in brain structures of poloxamer407 induced hyperlipidemic rat. Adult male Wistar rats were pretreated with guarana 12.5, 25 and 50mg/kg/day and caffeine (0.2mg/kg/day) by gavage for a period of 30days. Simvastatin (0.04mg/kg) was administered as a comparative standard in this study. Hyperlipidemia was acutely induced with intraperitoneally injection of 500mg/kg of poloxamer407. Memory test and evaluation of anxiety were performed. The cortex, cerebellum, hippocampus, hypothalamus and striatum were separated for the assessment of acetylcholinesterase activity. Our results revealed that guarana powder was able to reduce the levels of TC and LDL-C in a manner similar to simvastatin and partially reduced the liver damage caused by hyperlipidemia. Guarana was able to prevent changes in the activity of AChE and improve memory impairment caused by hyperlipidemia. Guarana powder may therefore be a source of promising phytochemicals that can be used as an adjuvant therapy in the management of hyperlipidemia and cognitive disorders.
... • Physical exercise protocol: The exercise protocol used was adapted from the study of Lima et al. 18 For the swimming training, we used a glass tank 100 × 50 × 75 cm 3 , filled with water with a temperature of 31°C. The animals were submitted to a physical exercise protocol of swimming, with the first 2 weeks designed to adapt the animals to physical activity, while the other 6 weeks were assigned to the training itself. ...
Article
Osteoarthritis (OA) is a chronic inflammatory disease and is characterized as a degenerative process. This study aimed to evaluate and compare the effects of a topical nonsteroidal anti-inflammatory drug (NSAID), physical activity, and photobiomodulation therapy (PBMT) applied alone and/or in combination between them in an experimental model of knee OA. OA was induced by injection of papain in the knees of rats. After 21 days, the animals started to be treated with the above treatment. Histological analysis shows that the experimental model of OA induction causes morphological changes consistent with the disease, and among treatments, the PBMT is the most effective for reducing these changes. Moreover, the results demonstrate that PBMT and NSAID reduce the total number of cells in the inflammatory infiltrate (p<0.05) and PBMT was the most effective for reducing the activity of myeloperoxidase (p<0.05). Finally, we observed that both NSAID and PBMT were effective for reducing the gene expression of MMP-3 (p<0.05), but in relation to the gene expression of MMP-13, PBMT was the most effective treatment (p<0.05). The results of this study indicate that PBMT is the most effective therapy in stopping disease progression, and improving inflammatory conditions observed in OA. © 2016 Society of Photo-Optical Instrumentation Engineers (SPIE).
... The functional properties of guaraná that are potentially the most similar to those of green tea are those properties related to metabolic disorders. Investigations have shown that guaraná positively affects lipid metabolism (Lima et al., 2005), enhances weight loss (Boozer et al., 2001;Opala et al., 2006), and increases basal energy expenditure (Bérubé-Parent et al., 2005). Therefore, these data suggest that guaraná potentially conveys an antiobesity effect. ...
Article
The aim of the present study was to evaluate the associations of metabolic disorders and anthropometric and biochemical biomarkers of lipid, glucose and oxidative metabolism and the habitual ingestion of guaraná (Paullinia cupana, Mart. Var. sorbilis) by an elderly population residing in the Amazon Riverine region of the Maués municipality (Brazil). A case-controlled study was performed that included 637 elderly (≥60 years of age) patients classified as either those who habitually drank guaraná (GI, n = 421) or those who never drank guaraná (NG, n = 239) based upon their self-reported intake of guaraná. Indeed, the prevalence of various metabolic disorders was associated with guaraná ingestion. The prevalence of hypertension, obesity and metabolic syndrome in the GI group was lower than the prevalence found in the NG group. The NG group exhibited lower systolic and diastolic blood pressure values. The males in the GI group exhibited a lower waist circumference, on average, than the circumference found in the NG group, whereas the females in the GI group had lower cholesterol (total and LDL-c) levels than the control cohort. Additionally, a significant association was found between lower levels of advanced oxidative protein product (AOPP) and habitual guaraná consumption. The results constitute the first epidemiological study to suggest a potentially protective effect of habitual guaraná ingestion against metabolic disorders in elderly subjects. Copyright © 2011 John Wiley & Sons, Ltd.
... The Paullinia cupana is a plant that exhibits various biological properties, such as antioxidant (Basile et al., 2005;Jimoh, Sofidiya & Afolayan, 2007;Mattei, Dias, Espínola, Carlini, & Barros, 1998), antimicrobial (da Fonseca, Leal, Costa, & Leitão, 1994, anti-allergic (Jippo et al., 2009), antiplatelet (Haller, Jacob & Benowitz, 2005), antitumor (Fukumasu et al., 2008), anti-fatigue (Haskell, Kennedy, Wesnes, Milne, & Scholey, 2007;Kennedy, Haskell, Wesnes, & Scholey, 2004), and antiobesogenic activities (Lima et al., 2005). ...
Article
The effects of guarana (Paullinia cupana) supplementation in capsules, for 30 days, were evaluated for the following dosages: placebo, 200 mg/day, and 400 mg/day. Clinical symptomatology, hematological, biochemical, and renal function parameters were evaluated in chronic kidney disease patients undergoing hemodialytic treatment. Most patients in the groups of 200 mg/day and 400 mg/day of guarana reported increased mood/energy, decreased fatigue, and increased appetite. The rate of patients reporting increased headache, insomnia, gastric discomfort, and nausea/vomiting was higher in the 400 mg/day group, while most patients in the placebo group and 200 mg/day of guarana group did not report any changes. The 200 mg/day and 400 mg/day groups had higher hemoglobin and hematocrit values after 30 days of supplementation when compared to the placebo group. Additionally, a reduction in hematological parameters and increase in glucose were seen in the placebo group. Guarana, especially at a dosage of 200 mg/day, is safe and effective in improving clinical symptoms and maintaining hemoglobin and hematocrit values.
... The proportion of caffeine in dry weight of guarana plant seeds is 2-6%, which corresponds to 2 fold of the caffeine present in the coffee beans (de Oliveira Campos et al., 2011;Lima et al., 2005;Haskell, Kennedy, Wesnes, Milne, & Scholey, 2007;EFSA, 2008;Pennay et al., 2011). Caffeine contents of leaves, seeds and crusts of the dry weight of guarana are different. ...
Article
Botanically known as Paullinia cupana (Sapindaceae), guarana is widely grown in Amazon region and naturally in Brazil, Ecuador, Venezuela, Colombia, Peru and the Cooperative Republic of Guyana. It is used in sugar and/or carbonated soft drinks, herbal teas and energy drinks in the form of guarana extract. Guarana has antioxidant, antibacterial, antifungal, antidepressant effects; improves cognitive performance; triggers weight loss and reduces lipid peroxidation. It has important effects on various methods and treatments from cardiovascular to neurological diseases, from memory and liveliness to cancer. It is also known that guarana enhances biological activities and psychological effects on the body. This compilation has been conducted to evaluate the chemical and physical properties of guarana, its metabolites, the mechanism of its effect on psychological activities and health. GUHES 2 (2020) 709067
... The proportion of caffeine in dry weight of guarana plant seeds is 2-6%, which corresponds to 2 fold of the caffeine present in the coffee beans (de Oliveira Campos et al., 2011;Lima et al., 2005;Haskell, Kennedy, Wesnes, Milne, & Scholey, 2007;EFSA, 2008;Pennay et al., 2011). Caffeine contents of leaves, seeds and crusts of the dry weight of guarana are different. ...
... The proportion of caffeine in dry weight of guarana plant seeds is 2-6%, which corresponds to 2 fold of the caffeine present in the coffee beans (de Oliveira Campos et al., 2011;Lima et al., 2005;Haskell, Kennedy, Wesnes, Milne, & Scholey, 2007;EFSA, 2008;Pennay et al., 2011). Caffeine contents of leaves, seeds and crusts of the dry weight of guarana are different. ...
Article
Botanically known as Paullinia cupana (Sapindaceae), guarana is widely grown in Amazon region and naturally in Brazil, Ecuador, Venezuela, Colombia, Peru and the Cooperative Republic of Guyana. It is used in sugar and/or carbonated soft drinks, herbal teas and energy drinks in the form of guarana extract. Guarana has antioxidant, antibacterial, antifungal, antidepressant effects; improves cognitive performance; triggers weight loss and reduces lipid peroxidation. It has important effects on various methods and treatments from cardiovascular to neurological diseases, from memory and liveliness to cancer. It is also known that guarana enhances biological activities and psychological effects on the body. This compilation has been conducted to evaluate the chemical and physical properties of guarana, its metabolites, the mechanism of its effect on psychological activities and health.
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Obesity is a major health concern of modern times and should be considered a global epidemic. Conventional or allopathic medicines used to treat obesity have high abuse potential and frequently exhibit side effects. Few botanicals included in natural weight loss products have been thoroughly researched on a basic and clinical level and it is imperative that this be done to validate their widespread consumption for weight management. Many natural weight loss products are sold and used globally with no (or very little) proof of efficacy or quality, and concerns regarding safety have surfaced with good reason. The continued search for new therapies has revealed multiple targets to combat obesity and highly complex plant extracts are ideally suited to fulfil a multi-targeted approach. This review explores targets for anti-obesity treatment and contains a comprehensive, yet succinct, overview of the phytochemistry and scientific evidence collated for 50 commercially important plants that have been investigated in vivo and/or clinically for their anti-obesity effects.
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There has been increased interest in recent years in very low carbohydrate ketogenic diets (VLCKD) that, even though they are much discussed and often opposed, have undoubtedly been shown to be effective, at least in the short to medium term, as a tool to tackle obesity, hyperlipidemia and some cardiovascular risk factors. For this reason the ketogenic diet represents an interesting option but unfortunately suffers from a low compliance. The aim of this pilot study is to ascertain the safety and effects of a modified ketogenic diet that utilizes ingredients which are low in carbohydrates but are formulated to simulate its aspect and taste and also contain phytoextracts to add beneficial effects of important vegetable components. The study group consisted of 106 Rome council employees with a body mass index of ≥ 25, age between 18 and 65 years (19 male and 87 female; mean age 48.49 ± 10.3). We investigated the effects of a modified ketogenic diet based on green vegetables, olive oil, fish and meat plus dishes composed of high quality protein and virtually zero carbohydrate but which mimic their taste, with the addition of some herbal extracts (KEMEPHY ketogenic Mediterranean with phytoextracts). Calories in the diet were unlimited. Measurements were taken before and after 6 weeks of diet. There were no significant changes in BUN, ALT, AST, GGT and blood creatinine. We detected a significant (p < 0.0001) reduction in BMI (31.45 Kg/m2 to 29.01 Kg/m2), body weight (86.15 kg to 79.43 Kg), percentage of fat mass (41.24% to 34.99%), waist circumference (106.56 cm to 97.10 cm), total cholesterol (204 mg/dl to 181 mg/dl), LDLc (150 mg/dl to 136 mg/dl), triglycerides (119 mg/dl to 93 mg/dl) and blood glucose (96 mg/dl to 91 mg/dl). There was a significant (p < 0.0001) increase in HDLc (46 mg/dl to 52 mg/dl). The KEMEPHY diet lead to weight reduction, improvements in cardiovascular risk markers, reduction in waist circumference and showed good compliance.
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The management of overweight may include the use of dietary supplements targeted to counter the feeling of hunger. A randomized, double-blind, placebo-controlled trial has been performed in 20 overweight females. These subjects were randomly assigned to supplement their diet with either an extract from Griffonia Simplicifolia (10 subjects) or a placebo (10 matched subjects) for 4-weeks, in conjunction with a personalised reduced calorie diet. The main aim of this study was to evaluate the efficacy, by the assessment of 24-h urinary 5-hydroxyindoleacetic acid levels (5-HIAA), of 1-month administration of a dietary supplement containing 5-hydroxytryptophan (5-HTP) from botanical extracts in healthy, overweight females. Secondary endpoints were the assessment of sensation of appetite (by Haber score), body composition, and severity of binge eating. The supplemented group had a significant increase of 24-h urinary 5-HIAA levels (p<0.001), and a decrease in Haber score (p<0.001) while the placebo group did not show significant changes. With regard to changes in body composition, statistically significant differences between the treatment groups were found for the mean change in BMI, suprailiac skinfold thicknesses, arm circumference and hip circumference. Other parameters were found to be similar in the treated and in the placebo groups. In conclusion, this study shows that the 5-hydroxytryptophan present in the Griffonia extract, administered via spray to the oral cavity, is adequately absorbed, as confirmed by the increase in 24-h urinary 5-HIAA, and that the supplementation of the diet of overweight women with 5-hydroxytryptophan increases the feeling of satiety associated with a decrease in BMI.
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In addition to its stimulatory effect, caffeine has been also associated with suppressing lipid accumulation and weight gain, making the well established energy drink market an ideal avenue to expand product health functionality. The objective of this study was to evaluate the effect of caffeine extracted from Yerba mate (Ilex paraguariensis) (matein, MT) and green coffee (Coffea arabica) byproducts (fractions GC1, GC2, GC3 and GC4) on inhibition of lipid accumulation in 3T3-L1 adipocytes compared to synthetic caffeine (SC). The antioxidant capacity (AC) and total polyphenol content (TPC) of these novel caffeine sources were also investigated and compared to SC using the Oxygen Radical Absorbance (ORAC) assay and the Folin-Ciocalteu method, respectively. Lipid quantification was done by the Oil Red O staining and real time polymerase chain reaction (RT-PCR) was performed to determine expression of two genes involved in lipid metabolism, lipoprotein lipase (LPL) and fatty acid synthase (FAS). Inhibition of lipid accumulation (%) was highly correlated to caffeine concentration of the samples (R2 = 0.88). MT and GC1 had the highest caffeine concentrations (90.8 and 93.8%, respectively), and exhibited the highest lipid reduction (18.3 and 17.1%, respectively) compared to untreated cells (p<0.05). MT and GC1 had similar inhibition of lipid accumulation compared to SC (16.3%), epigallocatechin gallate (EGCG) (17.5%), and Orlistat (17.9%). Adipocytes treated throughout differentiation resulted in an elevated inhibitory effect, with MT (22.8 ± 2.2%) and GC1 (26.8 ± 1.8%) having similar inhibitory capacity to SC (29.3 ± 0.5%). RT-PCR showed MT and GC1 may play a role in lipid metabolism by suppressing LPL and FAS. The GC byproducts and MT at 1000 µM had an AC range of 19.4 ± 0.2 to 1550.2 ± 19.2 with a mean of 446.5 Trolox µM equivalents (eq.), whereas SC had none. The TPC of the GC byproducts, MT, and SC ranged from 5.7 ± 0.3 to 153.5 ± 1.1 gallic acid (GA) µg eq., with SC resulting in the lowest. In conclusion, these results suggest that the incorporation of MT and GC1 into beverage formulations would provide a natural source of caffeine and potentially aid in long-term weight maintenance, and give in contrast to SC, antioxidant benefits.
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To test the effect on satiety of a formulation comprising plant extracts naturally containing 5-hydroxytryptophan, delivered as sublingual spray (5HTP-Nat Exts), administered five times a day for 2 months. Two-month, randomized, double-blind, placebo-controlled trial. A total of 27 healthy, adult overweight women were randomly assigned to the treatment (14) or the placebo group (13). Visual analog scales were used to assess appetite sensations every day. Moreover, the study evaluated the bioavailability of 5-hydroxytryptophan following sublingual delivery over 8 weeks, by comparing 24-h urinary excretion of 5-hydroxy-3-indoleacetic acid (5-HIAA), determined at baseline and after 2 months. Other secondary end points of the study were to compare body composition, depressive symptoms, severity of binge eating and quality of life. Finally, the study tested whether a single administration of 5HTP-Nat Exts in fasting state has an effect on amino-acid profile and on appetite ratings and whether 5HTP-Nat Exts administered before a fixed test meal has any effect on satiety. The group using the 5HTP-Nat Exts experienced a significantly greater increase in their sensation of satiety over an 8-week timeframe and in fasting state following administration of 5HTP-Nat Exts than the placebo group did (AUC=305.2 (52.8) vs 236.6 (59.4), mean difference -68.7 (95% confidence interval (CI) -116.2 to -21.2), P=0.007; mean difference in Haber score change 2.5 (95% CI 0.62-3.12, P=0.007)). A difference was observed between the groups for the mean change in 5-HIAA. All the amino acids evaluated after a single administration of 5HTP-Nat Exts were found to be similar. Differences were found for the mean change in body mass index, skinfold thicknesses and hip circumference. The other parameters were found to be similar. All these findings suggest that 5HTP-Nat Exts may be safely used to treat the problem of appetite control in overweight women during a weight loss program.
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Brazil possesses great biological and cultural diversity, above all, in view of the great number of indigenous ethnic groups - 218 in all - that inhabit the five main biomas in Brazil. The purpose of this review is to analyze the relationship between chemical constituents of species utilized by several groups of Brazilian Indians and the uses/indications made of the species by these same groups using ethnopharmacological surveys by different researchers, as from the seventies. The 34 publications selected, involving 26 indigenous ethnic groups, showed a total of 307 species utilized for 67 different diseases or effects possibly related to the Central Nervous System (CNS). These plants belong to 85 taxonomic families, mostly Fabaceae, Asteraceae, Rubiaceae, Poaceae, Apocynaceae, Bignoniaceae, Euphorbiaceae, and Solanaceae. The chemical constitution of these plants was researched as from the Pubmed and Web of Science and the information obtained was crossed with different indigenous uses, grouped in 12 categories according to similarities between their expected effects on the CNS: analgesics, to counteract fever, tonics and/or adaptogens, hallucinogens, anxiolytics, anticonvulsants, head illnesses, hypnotics, stimulants, weight control, memory enhancers, and others. Some phytochemical classes were observed to be more common among plants utilized for certain purposes: flavonoids (analgesia, fever, anxiety, hypnotic, weight control, and as a stimulant), alkaloids (hallucinogens, head illnesses, and as a stimulant), essential oils (fever and anxiety), lignans (hallucinogen), tannins (anxiety), triterpenes and saponins (hypnotic). These data suggest that these phytochemical classes possibly possess a greater number of chemical constituents that perform the effects described or that, in some way, assist in determining the use of the plant by the Indians.
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Guarana (Paullinia cupana) is a plant from the Amazon region with cultural importance. Despite its early ancestral use by indigenous tribes, the first reports regarding the benefits of guarana consumption for human health were published in the 19th century. Since then, the use of guarana seed in powder and extract forms has been studied for its diverse effects on human health, such as stimulating, anti-inflammatory, antioxidant, anticancer, hypocholesterolemic, and anti-obesity effects. These effects are attributed to the high content of bioactive compounds found in guarana seeds, especially methylxanthines and flavonoids. In fact, the Brazilian Food Supplement Law has officially acknowledged guarana as a source of bioactive compounds. The number and diversity of studies focused on guarana and human health are increasing; thus, organizing and describing the available evidence on guarana and its applications is necessary to provide a framework for future studies. In this narrative review, we have organized the available information regarding guarana and its potential effects on human health. Guarana produces unique fruits with great potential for human health applications. However, the available evidence lacks human studies and mechanistic investigations. Future studies should be designed considering its applicability to human health, including intake levels and toxicity studies.
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The impact of two commercially available products, a patented herb extract Yerbe Maté, Guarana and Damiana (YGD) formulation and an inulin-based soluble fermentable fibre (SFF), alone or in combination, on appetite and food intake were studied for the first time in a double blind, placebo-controlled, cross-over design. 58 normal to slightly overweight women consumed a fixed-load breakfast followed 4 hours later by an ad libitum lunch. They were administered YGD (3 tablets) and SFF (5g in 100ml water), YGD and water (100ml), SFF and placebo (3 tablets) or water and placebo 15 minutes before meals. Appetite was assessed using visual analogue scales, and energy intake was measured at lunch. Significant reductions in food intake and energy intake were observed when YGD was present (59.5g, 16.3%; 112.4kcal, 17.3%) and when SFF was present (31.9g, 9.1%; 80kcal, 11.7%) compared with conditions were products were absent. The lowest intake (gram and kcal) was in the YGD+SFF condition. Significant reductions in AUC hunger and AUC desire to eat were also observed after YGD+SFF combination. The data demonstrate that YGD produces a robust short-term effect on caloric intake, an effect augmented by SFF. Caloric compensation for SFF indicates independent effects on appetite regulation.
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Although chewing gum has been considered a potential method for reducing energy intake, little empirical data exist to support this idea. The purpose of this study was to test the hypothesis that chewing gum before eating reduces motivation to eat, hunger, and energy intake. In order to test this hypothesis, we conducted two experiments in which participants chewed gum prior to completing a food reinforcement task or before all eating occasions for two of three weeks. In Experiment 1, we found that chewing gum had no influence on the reinforcing value of food, but chewing mint gum reduced liking of and energy intake from fruit. In addition, chewing gum reduced self-reported hunger immediately after gum chewing and after eating compared with the no gum condition. In Experiment 2, gum chewing had no significant effect on total energy intake, but participants consumed fewer meals, consumed more energy per meal, and had a lower nutrient adequacy ratio during the gum chewing weeks. These studies provide no evidence that acute or chronic gum chewing reduces hunger or energy intake. In fact, chewing mint-flavored gum may deter consumption of fruit and reduce diet quality.
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Understanding the behavioral effects of herbal extracts presents a number of challenges to behavioral pharmacology. This review briefly summarizes these issues using guaraná (Paullinia cupana) as an example to illustrate certain key elements of this field. Guaraná has a long history of use as a stimulant in South America. Its purported stimulant effects have often been attributed to the presence of caffeine. However, guaraná's. behavioral profile can, be differentiated from that of caffeine. Receat evidence in humans and rodents suggests that other components of the plant (for example flavonoids) may contribute to its modulation of cognitive performance. This research is still in its infancy and further work is necessary in order to delineate whether guaraná has robust and replicable behavioral effects in humans. The contribution of different fractions of guaraná to its neurocognitive effects is unknown. Furthermore, whether acute advantages can be translated to chronic effects in cognitively vulnerable populations remains to be elucidated. Copyright 2008 Prous Science, S.A.U. or its licensors. All rights reserved.
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Background: The aim of this study was to assess cognitive performance and heart rate variability (HRV) following the ingestion of either a multi-vitamin-mineral preparation supplemented with 300 mg guaraná (Ac); a caffeine supplement (C) or a placebo supplement (Pl). Methods: Fifty six subjects took part in a randomized, double-blind crossover design, consisting in three experimental sessions ran on a different day. Cognitive performance was assessed using a go/no-go task and a simple reaction time (SRT) task. HRV was assessed in the time domain (RMSSD) and in the frequency domain (HF) and cognitive tasks were performed before ingestion, 15 minutes after ingestion and then every 15 minutes over the course of 3 h. Results: Responses were faster (without change in accuracy) when the go/no-go task was performed between 30 and 90 minutes after ingestion of Ac (+ 4.6 + 0.8%, p<.05). No effect was observed on SRT task. A significant decrease in HRV was observed during the first hour under C and Pl, whereas HRV remained stable under Ac. The results suggest that the ingestion of a multi-vitamin-mineral with added guaraná improves decision making performance and is accompanied by a stable autonomic nervous system regulation during the first hour.
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O câncer é a segunda maior causa de morte no Brasil, atrás apenas de doenças cardíacas. Por isto, é evidente que grandes recursos sejam direcionados para a pesquisa no descobrimento de novas opções com a finalidade de erradicar esta doença. Dentre estas opções, a quimioprevenção do câncer tem chamado a atenção já que, mesmo com os imensos avanços no conhecimento sobre os mecanismos da carcinogênese e conseqüente desenvolvimento de novas drogas, os dados estatísticos de mortalidade não se tornaram menores. Somando-se a estes fatos, deve ser considerado que no Brasil o tratamento padrão do câncer não chega a todas as pessoas por ser extremamente caro. Desta forma, a quimioprevenção do câncer com fatores presentes na dieta ou oriundos de fontes consideradas baratas como fitoterápicos, deve ser apreciada. Assim, este trabalho teve como objetivo avaliar os efeitos quimiopreventivos e antineoplásicos de uma planta brasileira, o guaraná (Paullinia cupana Mart var. sorbilis). Foram utilizados alguns experimentos em camundongos como indução genotóxica em fígado pela Dietilnitrosamina (DEN); carcinogênese pulmonar induzida pela 4-(metilnitrosamino)-1-(3-piridil)-1-butanona (NNK), uma nitrosamina presente no tabaco; tumor ascítico de Ehrlich; disseminação hematógena de melanoma B16/f10; e cultivo de células tumorais e não tumorais. Além disso, caracterizou-se o papel da Conexin43 na carcinogênese pulmonar induzida pelo NNK e os efeitos do guaraná sobre o receptor CAR e sua ação quando da administração do ligante do CAR, 1,4-bis[2-(3,5-dichloropiridiloxi)]benzeno (TCPOBOP). Pudemos observar efeitos quimiopreventivos e antineoplásicos do guaraná dependendo do modelo utilizado, demonstrando que seu modo de ação principal é a redução da proliferação celular. Além disso, observamos que os tumores de pulmão dos animais tratados com a planta apresentavam menor tamanho, menor grau maligno, menor índice de proliferação celular e menor ativação do fator de transcrição CREB. Observamos também que a Conexina43 (Cx43) tem importante papel na carcinogênese pulmonar induzida pelo NNK, atuando como supressor tumoral e em fases tardias possivelmente tendo papel inverso, ou seja, como um oncogene. Caracterizamos os efeitos do guaraná sobre a ativação do receptor CAR e demonstramos que, por si só, o guaraná induz a expressão do CAR, além de alterar a expressão de alguns de seus transcritos como a CYP2B10 e CYP3A11. Ao analisarmos os efeitos de extratos de guaraná sobre células de tumor de pulmão (E9) in vitro, verificamos o mesmo efeito antiproliferativo, diminuindo a expressão do PCNA e da Conexina43 de maneira dose-dependente, além de verificar um aumento da expressão do receptor CAR. Ao fim propomos uma hipótese de mecanismo de ação baseando-se nas alterações encontradas oriundas da administração do guaraná. Concluímos que o guaraná apresenta componentes com ação antitumoral em camundongos, tendo efeito quimiopreventivo ou antineoplásico dependendo do modelo utilizado.
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Hyperlipidemia causes lipotoxicity which prompts an inflammatory response linked to the development of cardiovascular diseases. Natural compounds have been receiving special attention for its potential to treat diseases, inexpensiveness, and safety. Guarana (Paullinia cupana) has demonstrated notable anti-inflammatory and antioxidant effects, which may prevent chronic diseases caused by changes in lipid profile. Thus, this study aims to evaluate the effect of guarana powder (Paullinia cupana) in the purine metabolism and inflammatory profile in lymphocytes and serum of rats with Poloxamer-407-induced hyperlipidemia. Pretreatment with guarana 12.5, 25, and 50 mg/kg/day or caffeine (0.2 mg/kg/day) by gavage was applied to adult male Wistar rats for a period of 30 days. As a comparative standard, we used simvastatin (0.04 mg/kg) post-induction. Hyperlipidemia was acutely induced with intraperitoneally injection of Poloxamer-407 (500 mg/kg). Guarana powder and caffeine increased the activity of the E-NTPDase (ecto-apyrase), and all pretreatments decreased the E-ADA (ecto-adenosine deaminase) activity, reducing the inflammatory process caused by lipotoxicity. In hyperlipidemic rats, ATP levels were increased while adenosine levels were decreased, guarana and caffeine reverted these changes. Guarana powder, caffeine, and simvastatin also prevented the increase in INF-γ and potentiated the increase in IL-4 levels, promoting an anti-inflammatory profile. Guarana promoted a more robust effect than caffeine. Our results show that guarana powder and caffeine have an anti-inflammatory as seen by the shift from a proinflammatory to an anti-inflammatory profile. The effects of guarana were more pronounced, suggesting that guarana powder may be used as a complementary therapy to improve the lipotoxicity-associated inflammation.
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Introdução: A diabete é uma epidemia mundial. Objetivo: O objetivo desse estudo foi identificar os efeitos do treinamento de força no metabolismo de lipídeos, na saúde, em pacientes com diabetes tipo II discutindo e modificando conceitos. Materiais e Métodos: Foi feita uma revisão de literatura narrativa e sistemática para a construção deste artigo. As bases de dados consultadas foram Scielo, Google Acadêmico e Pub Med. Resultados: Foram analisados 56 artigos e 10 selecionados para avaliação. Dos selecionados 70% são estudos recentes, dos anos de 2011 e 2012. Houve uma prevalência dos estudos crônicos sobre os agudos, sendo 80% dos estudos analisados de caráter crônico. Dos 10 artigos analisados obteve-se como resultado que 90% dos estudos foram realizados utilizando o exercício de alta intensidade. Todos estudos analisados proporcionaram maior controle glicêmico. Discussão: Existe uma maior preocupação atual com a elaboração de estudos originais que possam comprovar a eficácia do exercício resistido do que no passado. O exercício resistido agudo ou crônico proporcionam melhorias na saúde. Os estudos demonstraram maior eficácia do treino de alta intensidade. O mecanismo da hipertensão arterial está diretamente ligado ao controle da glicemia. O exercício resistido agudo ou crônico demonstrou ser uma ferramenta importante para controle da glicemia. Conclusão: O exercício resistido seja de cunho agudo ou crônico, de alta intensidade é considerado um melhor modelador do metabolismo lipídico do que o exercício moderado ou leve e oferece maiores benefícios aos portadores de diabete mellitus tipo 2.
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This study investigated the effect of vitamin B6 deficiency on the utilization and recuperation of stored fuel in physically trained rats. 48 rats were given either vitamin B6-deficient (B6-) diet or control (B6) diet for 4 weeks and were trained on treadmill for 30 minutes daily. All animals were then subdivided into 3 groups: before-exercise (BE); during-exercise (DE); after-exercise (AE). The DE group was exercised on treadmill for 1 hour just before being sacrificed. Animals in the AE group were allowed to take a rest for 2 hours after being exercised like the DE group. Glucose and free fatty acids were compared in plasma. Glycogen and triglyceride were compared in liver and skeletal muscle. Protein levels were compared in plasma, liver, and skeletal muscle. Compared with the B6+ group, plasma glucose levels of the B6- group were significantly lower before and after exercise. Muscle glycogen levels of the B6- group were significantly lower than those of the B6+ group regardless of exercise. The liver glycogen level of the B6- group was also significantly lower than that of B6+ group during and after exercise. Before exercise, plasma free fatty acid levels were not significantly different between the B6+ and B6- groups, and plasma free fatty acid levels of the B6- group were significantly lower during and after exercise. The muscle triglyceride level of the B6- group was significantly lower than that of the B6+ group before exercise, and there were no differences between B6+ and B6- groups during and after exercise. Liver triglyceride levels were not significantly different between B6+ and B6- groups. Plasma protein levels of the B6- group were lower than those of B6+ before and after exercise. Muscle protein levels of the B6- group were not significantly different from those of the B6 group. Liver protein levels of the B6- group were significantly lower than that of the B6+ group after exercise. Liver protein levels of both B6+ and B6- groups were not significantly changed, regardless of exercise. Thus, it is suggested that vitamin B6 deficiency may reduce fuel storage and utilization with exercise in physically trained rats.
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The BLAST programs are widely used tools for searching protein and DNA databases for sequence similarities. For protein comparisons, a variety of definitional, algorithmic, and statistical refinements permits the execution time of the BLAST programs to be decreased substantially while enhancing their sensitivity to weak similarities. A new criterion for triggering the extension of word hits, combined with a new heuristic for generating gapped alignments, yields a gapped BLAST program that runs at approximately three times the speed of the original. In addition, a method is described for automatically combining statistically significant alignments produced by BLAST into a position-specific score matrix, and searching the database using this matrix. The resulting Position Specific Iterated BLAST (PSLBLAST) program runs at approximately the same speed per iteration as gapped BLAST, but in many cases is much more sensitive to weak but biologically relevant sequence similarities.
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The syndrome of cancer cachexia is accompanied by several alterations of lipid metabolism, especially that in the liver. In this study we have investigated a possible mechanism whereby the presence of the Walker 256 carcinosarcoma affects hepatic fatty acid oxidative capacity in tumour-bearing rats. Hepatic mitochondrial outer membrane carnitine palmitoyltransferase I (CPT I), generally accepted as the main site of regulation of fatty acid oxidation, was unaffected by the presence of the extra-hepatic tumour. However, mitochondrial inner-membrane carnitine palmitoyltransferase II (CPT II) activity was markedly decreased in mitochondria isolated from the liver of tumour-bearing rats. Immuno-detection by Western blotting using a CPT II-specific antibody identified two bands (corresponding to M(r) 69,000 and 54,000) in tumour-bearing rats whereas only the normal-sized CPT II was present (at the expected M(r) 69,000) in mitochondria from control rats. It is suggested that the emergence of the second, smaller protein may represent a catalytically less active protein that arises in vivo, since its appearance was not affected by the inclusion of proteolysis inhibitors in the mitochondrial preparation buffers. Treatment of the tumour-bearing rats with indomethacin, a prostaglandin (including PGE2) synthesis inhibitor, increased CPT II activity to levels even higher than those found in the control animals. It is suggested that PGE2 may play a role in the control of CPT II expression in the liver of tumour-bearing rats. Indomethacin treatment did not affect either of the two CPT activities of the mitochondria isolated from tumour tissue.
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The effects of an aqueous extract of guaraná (Paullinia cupana) on rabbit platelet aggregation and thromboxane synthesis were examined. The guaraná extract (100 mg/ml) and fractions separated by TLC (origin and xanthines) decreased platelet aggregation (37, 27 and 31% of control values, respectively) and platelet thromboxane formation from [14C]-arachidonic acid (78, 70 and 50% of control values, respectively). The decreased thromboxane synthesis could be responsible, at least in part, for the antiaggregatory action of guaraná.
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Properties of the carnitine palmitoyltransferase (EC 2.3.1.21) (CPT) enzyme system were compared in isolated mitochondria from a range of tissues in rodents, monkey, and man. Common features were as follows: (a) while membrane-bound, CPT I, but not CPT II, was inhibited reversibly by malonyl-coenzyme A (CoA) and irreversibly by CoA esters of certain oxirane carboxylic acids; (b) the detergent, Tween-20, readily solubilized CPT II in active form while leaving CPT I membrane associated and catalytically functional; (c) octyl glucoside and Triton X-100 released active CPT II but caused essentially complete loss of CPT I activity. Use of [3H]tetradecylglycidyl-CoA, a covalent ligand for CPT I, yielded estimates of the enzyme's monomeric molecular size: approximately 86 kDa in non-hepatic tissues and approximately 90-94 kDa in liver, depending upon species. A polyclonal antibody to purified rat liver CPT II recognized a single protein in each tissue; its apparent molecular mass was approximately 70 kDa in all rat tissues and approximately 68 kDa in all mouse tissues as well as monkey and human liver. On Northern blot analysis a rat liver CPT II cDNA probe detected a single approximately 2.5-kilobase mRNA in all rat and mouse tissues examined. The following points are emphasized. First, CPT I and II are different proteins. Second, within a species CPT II, but not CPT I, is probably conserved across tissue lines. Third, slight variations in size of both enzymes were found in different species, although, at least in the case of CPT II, significant amino acid identity exists among the various isoforms. Fourth, CPT I, unlike CPT II, requires membrane integrity for catalytic function. Finally, the strategic use of detergents provides a simple means of discriminating between the two enzyme activities.
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A new method of total RNA isolation by a single extraction with an acid guanidinium thiocyanate-phenol-chloroform mixture is described. The method provides a pure preparation of undegraded RNA in high yield and can be completed within 4 h. It is particularly useful for processing large numbers of samples and for isolation of RNA from minute quantities of cells or tissue samples.
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1. The activities of pyruvate dehydrogenase in rat lymphocytes and mouse macrophages are much lower than those of the key enzymes of glycolysis and glutaminolysis. However, the rates of utilization of pyruvate (at 2 mM), from the incubation medium, are not markedly lower than the rate of utilization of glucose by incubated lymphocytes or that of glutamine by incubated macrophages. This suggests that the low rate of oxidation of pyruvate produced from either glucose or glutamine in these cells is due to the high capacity of lactate dehydrogenase, which competes with pyruvate dehydrogenase for pyruvate. 2. Incubation of either macrophages or lymphocytes with dichloroacetate had no effect on the activity of subsequently isolated pyruvate dehydrogenase; incubation of mitochondria isolated from lymphocytes with dichloroacetate had no effect on the rate of conversion of [1-14C]pyruvate into 14CO2, and the double-reciprocal plot of [1-14C]pyruvate concentration against rate of 14CO2 production was linear. In contrast, ADP or an uncoupling agent increased the rate of 14CO2 production from [1-14C]pyruvate by isolated lymphocyte mitochondria. These data suggest either that pyruvate dehydrogenase is primarily in the a form or that pyruvate dehydrogenase in these cells is not controlled by an interconversion cycle, but by end-product inhibition by NADH and/or acetyl-CoA. 3. The rate of conversion of [3-14C]pyruvate into CO2 was about 15% of that from [1-14C]pyruvate in isolated lymphocytes, but was only 1% in isolated lymphocyte mitochondria. The inhibitor of mitochondrial pyruvate transport, alpha-cyano-4-hydroxycinnamate, inhibited both [1-14C]- and [3-14C]-pyruvate conversion into 14CO2 to the same extent, and by more than 80%. 4. Incubations of rat lymphocytes with concanavalin A had no effect on the rate of conversion of [1-14C]pyruvate into 14CO2, but increased the rate of conversion of [3-14C]pyruvate into 14CO2 by about 50%. This suggests that this mitogen causes a stimulation of the activity of pyruvate carboxylase.
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Exposure of rat liver mitochondrial membranes to octyl glucoside, Triton X-100, or Tween 20 solubilized an active and tetradecylglycidyl-CoA (TG-CoA)-insensitive carnitine palmitoyltransferase (presumed to be carnitine palmitoyltransferase II). The residual membranes after octyl glucoside or Triton X-100 treatment were devoid of all transferase activity. By contrast, Tween 20-extracted membranes were still rich in transferase; this was completely blocked by TG-CoA and thus was presumed to be carnitine palmitoyltransferase I. The residual carnitine palmitoyltransferase activity disappeared from the membranes upon subsequent addition of octyl glucoside or Triton X-100 and could not be recovered in the supernatant fraction. Antibody raised against purified rat liver transferase II (Mr 80,000) recognized only this protein in immunoblots from untreated liver mitochondrial membranes containing both transferases I and II. Tween 20-extracted membranes, which contained only transferase I, did not react with the antibody. Purified transferase II from skeletal muscle (also of Mr 80,000) was readily recognized by the antiserum, suggesting antigenic similarity with the liver enzyme. These and other studies on the effects of detergents on the mitochondrial [3H]TG-CoA binding protein provide further support for the model of carnitine palmitoyltransferase proposed in the preceding paper. They suggest that: 1) carnitine palmitoyltransferases I and II in rat liver are immunologically distinct proteins; 2) transferase I is more firmly anchored into its membrane environment than transferase II; 3) association of carnitine palmitoyltransferase I with a membrane component(s) is necessary for catalytic activity. While carnitine palmitoyltransferase I is a different protein in liver and muscle, it seems likely that both tissues share the same transferase II.
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This two-part investigation compared the ergogenic and metabolic effects of theophylline and caffeine. Initially (part A), the ergogenic potential of theophylline on endurance exercise was investigated. Eight men cycled at 80% maximum O(2) consumption to exhaustion 90 min after ingesting either placebo (dextrose), caffeine (6 mg/kg; Caff), or theophylline (4.5 mg/kg Theolair; Theo). There was a significant increase in time to exhaustion in both the Caff (41.2+/-4.8 min) and Theo (37.4+/-5.0 min) trials compared with placebo (32.6+/-3.4 min) (P<0.05). In part B, the effects of Theo on muscle metabolism were investigated and compared with Caff. Seven men cycled for 45 min at 70% maximum O(2) consumption (identical treatment protocol as in part A). Neither methylxanthines (MX) affected muscle glycogen utilization (P>0.05). Only Caff increased plasma epinephrine (P<0.05), but both MX increased blood glycerol levels (P<0.05). Muscle cAMP was increased (P<0.05) by both MX at 15 min and remained elevated at 45 min with Theo. This demonstrates that both MX are ergogenic and that this can be independent of muscle glycogen.
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To examine in overweight humans the short-term safety and efficacy for weight loss of an herbal supplement containing Ma Huang, Guarana and other ingredients. An 8 week randomized, double-blind placebo controlled study of a herbal dietary supplement (72 mg/day ephedrine alkaloids and 240 mg/day caffeine). Overweight men and women (body mass index, > or =29 and < or =35 kg/m2). The primary outcome variable was body weight change. Secondary variables included anthropometric, metabolic and cardiovascular changes. Sixty-seven subjects were randomized to either placebo (n=32) or active Ma Huang/Guarana (n=35). Twenty-four subjects in each group completed the study. Active treatment produced significantly (P<0.006) greater loss of weight (X+/-s.d.,-4.0+/-3.4 kg) and fat (-2.1+/-3.0% fat) over the 8-week treatment period than did placebo (-0.8+/-2.4 kg and 0.2+/-2.3% fat). Active treatment also produced greater reductions in hip circumference and serum triglyceride levels. Eight of the 35 actively treated subjects (23%) and none of the 32 placebo-treated control subjects withdrew from the protocol because of potential treatment-related effects. Dry mouth, insomnia and headache were the adverse symptoms reported most frequently by the herbal vs placebo group at the final evaluation visit. This herbal mixture of Ma Huang and Guarana effectively promoted short-term weight and fat loss. Safety with long-term use requires further investigation.
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There is controversy as to the use of intramuscular triacylglycerol (IMTAG) during exercise and to whether endurance training increases its utilization, despite the various methodologies used to address these questions. We used a histological-morphometrical approach to study the relative contribution of the two compartments of IMTAG storage, intramyocellular, and perimysial adipocytes, during exercise in sedentary and endurance-trained rats. After osmium impregnation, the soleus (SOL) and gastrocnemius (GAS) were studied under light and electron microscopy. IMTAG content (after Triton WR1339 treatment or not) and 14C-oleate incorporation into the muscles were studied. In GAS, training, but not exercise alone, decreased extramyocellular lipid (P < 0.001 vs sedentary), an effect not found for SOL. Both muscles presented reduced lipid inclusion number (P < 0.001) and area (P < 0.05), immediately after exercise in sedentary and trained rats. For SOL, a greater number (P < 0.001 vs sedentary) of inclusions was found 24 h after exercise in trained rats. Triton WR1339 treatment decreased IMTAG content 12 h after exercise in SOL (but not in GAS), in sedentary (33%), and trained rats (52%). The multi-analytical approach adopted allowed the discernment between the IMTAG compartments and provided evidence for an effect of training upon storage of lipid in perimysial adipocytes in rat gastrocnemius, as well as clearly showed that the IMTAG mobilized during submaximal exercise in sedentary and trained rats derives from intramyocellular lipid, both in SOL and GAS. Moreover, the reposition of these stores 12 h after exercise was shown to be different in GAS and SOL, as plasma triacylglycerol clearly contributed to the process only in the latter, possibly reflecting the differences in lipoprotein lipase activity in the muscles reported by others.
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Dietary supplements that contain Ma Huang (ephedra alkaloids) and guarana (caffeine) are widely marketed and used in the U.S. for weight loss and athletic performance enhancement, despite a lack of adequate research on the pharmacology of these botanical stimulants. We developed and applied a novel liquid chromatography-tandem mass spectrometry (LC-MS-MS) method to quantitate the various ephedra alkaloids found in dietary supplements that contain Ephedra species. The quantities of ephedrine, pseudoephedrine, norephedrine, norpseudoephedrine, methylephedine, methylpseudoephedrine, and caffeine were determined for 35 commercial dietary supplements and compared with the amounts listed on the product labels. The total ephedra alkaloid content ranged from 5.97 mg to 29.3 mg per serving. Two supplement brands did not list the quantity of ephedra alkaloids on the label, and four did not list the amount of caffeine per serving. Of the products tested, 31% contained > 110% of the total ephedra alkaloids listed on the label, and 6% of the supplements contained < 90% of the listed amount. For caffeine, 86% of the product lots that listed the caffeine amount contained less than 90% of the labeled quantity. No products contained > 110% of the declared caffeine content. The total ephedra alkaloid content varied significantly from lot to lot in 5 of 9 products. Three product brands contained proportions of alkaloids that exceeded amounts reported for E. sinica, including one that was 98% ephedrine, one that had 10% norpseudoephedrine, and one that contained an average of 13% methylephedrine. We conclude that product inconsistency is common among some commercially available dietary supplements that contain ephedra alkaloids and caffeine.
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This review article draws the attention to the many species of plants possessing activity on the central nervous system (CNS) In fact, they cover the whole spectrum of central activity such as psychoanaleptic, psycholeptic and psychodysleptic effects, and several of these plants are currently used in therapeutics to treat human ailments. Among the psychoanaleptic (stimulant) plants, those utilized by human beings to reduce body weight [Ephedra spp (Ma Huang), Paullinia spp (guarana), Catha edulis Forssk (khat)] and plants used to improve general health conditions (plant adaptogens) were scrutinized. Many species of hallucinogenic (psychodysleptic) plants are used by humans throughout the world to achieve states of mind distortions; among those, a few have been used for therapeutic purposes, such as Cannabis sativa L., Tabernanthe iboga Baill and the mixture of Psychotria viridis Ruiz and Pav and Banisteriopsis caapi (Spruce ex Griseb.) C.V Morton Plants showing central psycholeptic activities, such as analgesic or anxiolytic actions (Passiflora incarnata L., Valeriana spp and Piper methysticum G Forst.), were also analysed. Finally, the use of crude or semipurified extracts of such plants instead of the active substances seemingly responsible for their therapeutic effect is discussed. (C) 2003 Published by Elsevier Science Inc.
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This review article draws the attention to the many species of plants possessing activity on the central nervous system (CNS). In fact, they cover the whole spectrum of central activity such as psychoanaleptic, psycholeptic and psychodysleptic effects, and several of these plants are currently used in therapeutics to treat human ailments. Among the psychoanaleptic (stimulant) plants, those utilized by human beings to reduce body weight [Ephedra spp. (Ma Huang), Paullinia spp. (guaraná), Catha edulis Forssk. (khat)] and plants used to improve general health conditions (plant adaptogens) were scrutinized. Many species of hallucinogenic (psychodysleptic) plants are used by humans throughout the world to achieve states of mind distortions; among those, a few have been used for therapeutic purposes, such as Cannabis sativa L., Tabernanthe iboga Baill. and the mixture of Psychotria viridis Ruiz and Pav. and Banisteriopsis caapi (Spruce ex Griseb.) C.V. Morton. Plants showing central psycholeptic activities, such as analgesic or anxiolytic actions (Passiflora incarnata L., Valeriana spp. and Piper methysticum G. Forst.), were also analysed.Finally, the use of crude or semipurified extracts of such plants instead of the active substances seemingly responsible for their therapeutic effect is discussed.
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Plasma insulin concentrations in fed rats were altered acutely by administration of glucose or anti-insulin serum. Rates of fatty acid synthesis in adipose tissue and liver were estimated from the incorporation of 3H from 3H2O. In the adipose tissue dehydrogenase and acetyl-CoA carboxylase were evident. In liver, although changes in rates of fatty acid synthesis were found, the initial activity of pyruvate dehydrogenase did not alter, but small parallel changes in acetyl-CoA carboxylase activity were observed.
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Pretreatment of rats with caffeine potentiated the actions of the p-chloro- and p-methyl analogues of amphetamine and benzphetamine as depressants of deprivation-induced food consumption, although no such effects were seen with the unsubstituted compounds. Similar caffeine pretreatment completely antagonized the stimulant effect of amphetamine and p-chloroamphetamine on continuous avoidance responding. In contrast, combined dosage of caffeine potentiated the actions of p-methyl-amphetamine, or benzphetamine, drugs normally showing decreased avoidance responding. Caffeine, in combination with benzphetamine, caused a slight decrease in avoidance responding.
Article
We investigated the hypothesis that the increase in lipolysis that occurs in short-term (86-h) fasting is due to a decreased inhibitory influence of adenosine. In normal volunteers who fasted for 14 and 86 h, the response to adenosine receptor blockade was assessed by the infusion of theophylline at a rate sufficient to produce plasma concentrations (30 microM) that blocked adenosine receptors but that were well below the threshold for inhibition of phosphodiesterase. Lipolysis was assessed by determining the rate of appearance of glycerol using D-5-glycerol infusion. Fatty acid flux was also determined by means of [1-13C]palmitate infusion, and total fatty acid oxidation was determined by indirect calorimetry. There was a mild stimulatory effect of theophylline on lipolysis at 14 h. After the subjects fasted for 86 h, theophylline infusion caused a much greater increase in both lipolysis and fatty acid oxidation. These results suggest that the inhibitory effect of adenosine on lipolysis is increased during short-term fasting.
Article
Production of 14CO2 from an oral load of [1-14C]triolein was greatly decreased (70%) in lactating rats or immediately after (24-48 h) removal of the litter, compared with virgin rats. This decreased oxidation of dietary lipid was accompanied by accumulation of 14C-labelled lipid in lactating mammary gland or adipose tissue (after litter removal). No difference in 14CO2 production between lactating and virgin rats was observed when [1-14C]octanoate was administered. It is concluded that a major factor in this conservation of dietary triacylglycerol is the relative activity of lipoprotein lipase in the tissues.
Article
Aqueous extracts of guaraná were studied in terms of effects on the aggregation of human and rabbit platelets. Guaraná extracts have anti-aggregatory and de-aggregatory actions on platelet aggregation induced by ADP or arachidonate but not by collagen. The active material was shown to be water soluble and heat resistant and appeared to be different from salicylates, nicotinic acid or known xanthines. Guaraná extracts inhibited platelet aggregation in rabbits following either intravenous or oral administration.
Article
Rats were trained by daily swimming sessions (up to 3 h per day) for at least 6 weeks in water at 30, 36 and 38 degrees C. After this training, the adaptive changes obtained were compared with those typical of cold-acclimated (cold-specific changes) and running-trained (training-specific changes) rats. The most typical training-specific change, an increased activity of oxidative muscle enzymes was negligible for swimming-trained rats, while the lowered activity of muscle lactate dehydrogenase was evident for all trained groups. Cold-specific changes, such as increased food intake, increased calorigenic response to injected noradrenaline, an increase both in mass and metabolic capacity of brown adipose tissue, and maintenance of the stores of ascorbic acid and muscle glycogen during cold exposure, were observed for rats trained at 36 and 30 degrees C. The cold tolerance test in cold air did not make any distinct difference between the rats trained at different water temperatures, while in cool water the 30 degrees C -swimmers were clearly superior to other groups, that is, their cooling rate was slowest. Other adaptive changes were found, to a variable extent, for all trained groups. These included loss of body fat, cardiac hypertrophy, reduced urinary catecholamine excretion after test swimmings either in cold or warm water, increased tail-skin temperature response to isoprenaline, and a higher tail-skin temperature in response to cold. Generally, however, the adaptive changes observed for 30- and 36 degrees C-swimmers were similar, while the changes observed for 38 degrees C-swimmers were different. The latter group neither displayed any cardiac enlargement nor any cold-specific changes.(ABSTRACT TRUNCATED AT 250 WORDS)
Article
1The kinetics of the carnitine palmityltransferase and of the carnitine-stimulated oxidation of palmityl-CoA to acetoacetate in isolated rat liver mitochondria have been studied.2The particle-bound enzyme shows the same kinetic properties as the solubilized enzyme.3The rate of respiration is found to depend on the concentration of palmitylcarnitine formed in the reaction mixture, as long as this concentration is less than 2 × 10−6 M.4The capacity of isolated mitochondria for palmitylcarnitine formation exceeds severalfold their capacity for oxidation of palmitylcarnitine to acetoacetate. It is likely therefore that the long-chain acylcarnitine/carnitine substrate pair is nearly in equilibrium with the extramito-chondrial palmityl-CoA/CoA in the intact cell.5Relatively high concentrations of CoA and carnitine inhibit the oxidation of palmityl-CoA when the concentration of this substrate is low. These effects are in accordance with the kinetic properties of the carnitine palmityltransferase and may contribute to the slow rate of fatty acid oxidation when the concentration of long-chain acyl-CoA in the cell is low.6High concentrations of palmityl-CoA are oxidized by isolated mitochondria even in the absence of carnitine, possibly because of a detergent effect. Albumin inhibits this carnitine-independent oxidation, presumably because palmityl-CoA is bound to the protein.7The regulation of fatty acid oxidation is discussed. It is suggested that both the cellular concentration of long-chain acylcarnitines and the availability of mitochondrial free CoA are of importance. The existence of such a system permits regulation of fatty acid oxidation without interference with extramitochondrial CoA-dependent processes.
Article
Guaraná is considered an ideal crop for supplementing the incomes of small peasant farmers in the Amazon basin. A fast-growing perennial, guaraná can be planted in the midst of manioc crops, allowing the formation of extensive orchards in the place of regenerating scrub once the manioc has been harvested. Traditional forms of guaraná agriculture practised by the Saterê-Mawé Indians compare favourably with the plantation system favoured by government agronomists. Indigenous techniques of hand-processing guaraná are also shown to produce better quality in the finished product than those practices adopted by industrial concerns. A detailed comparison of two systems of production show the Indians' implicit concern to avoid oxidization of the phenolic compounds in the seed, since this leads to the guaraná becoming dark in colour, bitter in taste, and irritating to the gastrointestinal tract. The short-term medicinal effects of guaraná are commonly thought to result from a high content of caffeine and associated alkaloids, as well as from considerable amounts of tannin. Future research may well show that various saponins also play an important part in the drug's pharmacology, particularly with regard to its long-term influence as a general tonic and prophylactic.
Article
The effect of fasting on palmitoyl-CoA: carnitine palmitoyltransferase (EC 2.3.1.21) in rat liver mitochondria and its inhibition by malonyl-CoA has been investigated. The activity of the outer carnitine palmitoyltransferase (transferase I) is nearly doubled after 24 h fasting, while the activity of total carnitine palmitoyltransferase (transferase I + II) increases only about 25%. The inhibition of the increased outer transferase by malonyl-CoA is decreased in fasting rats. The results suggest that carnitine palmitoyltransferase less sensitive to malonyl-CoA is exposed on the outer surface of the inner mitochondrial membrane in fasting, thus reducing the latency of the enzyme.
Article
The intron-containing genes encoding rat and human ribosomal protein L19 (RPL19) have been cloned. The DNA sequences of the entire rat RPL19 gene and the 5' end of the human RPL19 gene have been determined. Sequence comparison of corresponding regions of the two genes reveals a striking interspecies homology in the 5' upstream region, outside the transcribed and coding regions. The transcriptional start sites of the two genes have been determined and are identical. Both rat and human RPL19 genes have 5' ends associated with CpG islands. A promoter deletion analysis of the rat RPL19 gene suggests that this promoter may differ from those of all previously characterized ribosomal protein genes in requiring far upstream sequences for efficient gene expression. By fluorescence in situ hybridization analysis, the position of the human RPL19 gene has been sublocalized to 17q11 and may be coamplified with the erbB-2 gene in human breast cancer cells. The similarities and differences between RPL19 and other previously characterized ribosomal protein genes are discussed.
Article
The seeds of Guaraná are rich in xanthines and are used for the preparation of guaraná powder which is very commonly given to horses as a 'tonic' in Brazil. In this paper, the xanthine content of guaraná powder was determined, in addition to its clearance time in horses. Thin-layer chromatography was used as a screening procedure and high-performance liquid chromatography was performed to quantify the drugs in both the powder and urine samples. The guaraná powder was found to contain 2.16, 1.10 and 36.78 mg g-1 of theobromine (TB), theophylline (TP) and caffeine (CF), respectively, and in urine it was possible to detect TB and TP up to 13 d and CF up to 9 d after the administration of guaraná powder.
Article
The involvement of CRH and the sympatho-adrenal system in the effects of caffeine on food intake and body weight gain has been investigated in rats. Food intake and body weight gain were measured in male rats after the treatment with caffeine in combination with either an injection of the CRH antagonist alpha-helical CRH(9-41), a surgical adrenal demedullation (medullectomy), or a ganglionic blockade. Alpha-helical CRH(9-41) was injected in the lateral ventricle of the brain and hexamethonium was used to chemically block the ganglionic transmission. From 4 to 24 h following a caffeine injection, spontaneous food intake, which was cumulated from the time caffeine was injected, was significantly (p < 0.01) lower in caffeine- than in saline-treated rats. In food-deprived rats, the anorectic effect of caffeine was biphasic, being significant at 0.5 and 1 h after the caffeine administration, then vanishing for 3 h, and becoming significant again 6 h after the caffeine administration. In both the spontaneously fed and food-deprived rats, caffeine reduced the rate of weight gain, which was measured at the end of a 12- or a 24-h period following the caffeine injection. A significant (p < 0.05) interaction effect of caffeine and alpha-helical-CRH(9-41) was found on the cumulative food intake at 1, 6, and 8 h, and on the amount of food eaten between the 4-6-h interval following the injection of caffeine; the effects of caffeine on food intake and body weight gain seem largely prevented by the use of a CRH antagonist.(ABSTRACT TRUNCATED AT 250 WORDS)
Article
We tested the hypothesis that adenosine is involved in regulating substrate metabolism during exercise. Seven trained cyclists were studied during 30 minutes of exercise at approximately 75% maximal oxygen uptake (VO2max). Lipid metabolism was evaluated by infusing [2H5]glycerol and [1-13C]palmitate, and glucose kinetics were evaluated by infusing [6,6-2H]glucose. Fat and carbohydrate oxidation were also measured by indirect calorimetry. The same subjects performed two identical exercise tests, but in one trial theophylline, a potent adenosine receptor antagonist, was infused for 1 hour before and throughout exercise. Theophylline did not increase whole-body lipolysis (glycerol rate of appearance [Ra]) or free fatty acid (FFA) release during exercise, but fat oxidation was lower than control values (9.5 +/- 3.0 v 18.0 +/- 4.2 micromol x min(-1) x kg(-1), P < .01). Glucose Ra was not affected by theophylline infusion, but glucose uptake was lower (31.6 +/- 4.1 v 40.4 +/- 5.0 micromol x min(-1) x kg(-1), P < .05) and glucose concentration was higher (6.4 +/- 0.6 v 5.8 +/- 0.4 mmol/L, P < .05) than in the control trial. Total carbohydrate oxidation (302.3 +/- 26.2 v 265.5 +/- 11.7 micromol x min(-1) x kg(-1), P < .06), estimated muscle glycogenolysis (270.7 +/- 23.1 v 225.1 +/- 9.7 micromol x min(-1) x kg(-1), P < .05), and plasma lactate concentration (7.9 +/- 1.6 v 5.9 +/- 1.1 mmol/L, P < .001) were also higher during the theophylline trial. These data suggest that adenosine may play a role in stimulating glucose uptake and restraining glycogenolysis but not in limiting lipolysis during exercise.
Article
Mice that ingested a suspension of guarana (Paullinia cupana, Sapindaceae) in a dose of 0.3 mg/ml showed a significant increase in physical capacity when subjected to a stressful situation such as forced swimming after 100 and 200 days of treatment. Such an effect, however, was not obtained with a concentration of 3.0 mg/ml, nor with the ingestion of a suspension of ginseng 5.0 mg/ml, nor of a solution of caffeine 0.1 mg/ml. Guarana, both after a single (3.0 and 30 mg/kg) or chronic administrations (0.3 mg/ml), was able to partially reverse the amnesic effect of scopolamine as measured through a passive avoidance test in mice and rats, indicating a positive effect on memory acquisition. However, no effect was observed when an active avoidance task was used in rats, even after 20 days of guarana administration. There was also a tendency of rats treated with 0.3 mg/ml of guarana to better maintain the memory of a Lashley III maze path. The animals had the same average lifespan, indicating a low toxicity of guarana, even after 23 months of treatment.
Article
The effects on toxic and behavioral levels of guarana (Paullinia cupana) were assessed in rats and mice subsequent to acute and chronic administrations and were compared to those produced by Ginseng (Panax ginseng). Experimental parameters included tests for antioxidant capacity in vitro and measured in vivo, toxicological screening, progress in weight, motor activity, death rate, and histopathological examination of the viscera. Guarana showed an antioxidant effect because, even at low concentrations (1.2 microg/ml), it inhibited the process of lipid peroxidation. In high doses of 1000-2000 mg/kg (i.p. and p.o.) it did not induce significant alterations in parameters for toxicological screening. No effects on motor activity were observed, neither did guarana alter the hypnotic effect of pentobarbital. Ginseng (250-1000 mg/kg i.p.), however, elicited reductions in motor activity, eyelid ptosis and bristling fur. Consumption of liquids containing guarana or ginseng and progress in weight of the animals remained at levels similar to the controls, even after prolonged administration. The percentage mortality was equivalent in control and in treated groups. The absence of toxicity of guarana was also demonstrated by histopathological examination, with no alteration being detected in heart, lungs, stomach, small and large intestine, liver, pancreas, kidneys, bladder and spleen.
Article
This study is conducted to investigate the influence of oral theophylline administration (100 mg/kg bw per day) on the activity of carnitine palmitoyltransferase (CPT) in cardiac tissues of rats for 5-week interval treatments. Results showed significant increase in the activity of CPT was observed in cardiac tissues of theophylline-treated groups as compared to either control or placebo groups. Moreover, the results showed positive correlations between the cardiac concentrations of long-chain acylcarnitine (LC) and the activity of CPT and between plasma concentrations of LC and the cardiac concentrations of LC (P<0.01), respectively. The observed changes in activity of cardiac CPT might be due to the result from theophylline- enhanced decrease the sensitivity of CPT to inhibition by malonyl-CoA and/or from theophylline-enhanced mobilization of lipid from adipose tissues which consequently stimulated an increased carnitine transport into the tissues to form palmitoylcarnitine groups for subsequent beta-oxidation inside the mitochondria. Thus, these accumulations of acylcarnitine groups in mitochondria may increase the catalytic action of CPT.
Article
Fasting elicits a progressive increase in lipid metabolism within skeletal muscle. To determine the effects of fasting on the transcriptional regulation of genes important for metabolic control in skeletal muscle composed of different fiber types, nuclei from control and fasted (24 and 72 h) rats were subjected to nuclear run-on analysis using an RT-PCR-based technique. Fasting increased (P < 0.05) transcription rate of the muscle-specific uncoupling protein-3 gene (UCP3) 14.3- to 21.1-fold in white gastrocnemius (WG; fast-twitch glycolytic) and 5.5- to 7.5-fold in red gastrocnemius (RG; fast-twitch oxidative) and plantaris (PL; mixed) muscles. No change occurred in soleus (slow-twitch oxidative) muscle. Fasting also increased transcription rate of the lipoprotein lipase (LPL), muscle carnitine palmitoyltransferase I (CPT I), and long-chain acyl-CoA dehydrogenase (LCAD) genes 1.7- to 3.7-fold in WG, RG, and PL muscles. Transcription rate responses were similar after 24 and 72 h of fasting. Surprisingly, increasing metabolic demand during the initial 8 h of starvation (two 2-h bouts of treadmill running) attenuated the 24-h fasting-induced transcriptional activation of UCP3, LPL, CPT I, and LCAD in RG and PL muscles, suggesting the presence of opposing regulatory mechanisms. These data demonstrate that fasting elicits a fiber type-specific coordinate increase in the transcription rate of several genes involved in and/or required for lipid metabolism and indicate that exercise may attenuate the fasting-induced transcriptional activation of specific metabolic genes.
Article
The mitochondrial carnitine system plays an obligatory role in beta-oxidation of long-chain fatty acids by catalyzing their transport into the mitochondrial matrix. This transport system consists of the malonyl-CoA sensitive carnitine palmitoyltransferase I (CPT-I) localized in the mitochondrial outer membrane, the carnitine:acylcarnitine translocase, an integral inner membrane protein, and carnitine palmitoyltransferase II localized on the matrix side of the inner membrane. Carnitine palmitoyltransferase I is subject to regulation at the transcriptional level and to acute control by malonyl-CoA. The N-terminal domain of CPT-I is essential for malonyl-CoA inhibition. In liver CPT-I activity is also regulated by changes in the enzyme's sensitivity to malonyl-CoA. As fluctuations in tissue malonyl-CoA content are parallel with changes in acetyl-CoA carboxylase activity, which in turn is under the control of 5'-AMP-activated protein kinase, the CPT-I/malonyl-CoA system is part of a fuel sensing gauge, turning off and on fatty acid oxidation depending on the tissue's energy demand. Additional mechanism(s) of short-term control of CPT-I activity are emerging. One proposed mechanism involves phosphorylation/dephosphorylation dependent direct interaction of cytoskeletal components with the mitochondrial outer membrane or CPT-I. We have proposed that contact sites between the outer and inner mitochondrial membranes form a microenvironment which facilitates the carnitine transport system. In addition, this system includes the long-chain acyl-CoA synthetase and porin as components.
Article
This study investigated whether methylxanthines (caffeine and theophylline) would restore food and water intake in rats made aphagic and adipsic by bilateral 6-hydroxydopamine lesions of the nigrostriatal bundle, and these results were compared with the effects of d-amphetamine, the dopamine D(1) agonist SKF 38393, and the D(2/3) agonist quinpirole. In a separate experiment, we investigated whether the selective D(1) antagonist, SCH 23390, or the selective D(2) antagonist, sulpiride, would prevent the caffeine-induced restoration of food and water intake in bilaterally 6-hydroxydopamine denervated rats. The results showed that caffeine, theophylline, and quinpirole significantly reversed the aphagia and adipsia observed in lesioned animals. SKF 38393 had no significant effects on water intake, while it significantly restored food intake at the highest dose used. In contrast, d-amphetamine had no significant effects on food or water intake. Results from the second experiment showed that sulpiride attenuated the caffeine-induced restoration of food and water intake in lesioned rats to a greater extent than did SCH 23390. These data suggest that methylxanthines may mediate their effects on food and water intake in bilateral 6-hydroxydopamine-lesioned rats through an action at the dopaminergic system.
Article
Background: Obesity and overweight may soon affect more than half of the population in some regions of the world and are associated with diabetes, hypertension and other diseases that cause morbidity, mortality and high health-care expenditure. No one approach, whether dietetic management, medication, or commercial weight loss programme, can alone solve the problem--all potential treatments need to be investigated and exploited. Among the herbal preparations known to non-western cultures are materials which may have applications in modulating physiological processes which influence gut motility, food intake and energy balance. One such mixed herbal preparation is 'YGD' containing Yerbe Maté (leaves of Ilex paraguayenis), Guarana (seeds of Paullinia cupana) and Damiana (leaves of Turnera diffusa var. aphrodisiaca). Aims: This study had two distinct aims: to determine the effect of a herbal preparation 'YGD' containing Yerbe Maté, Guarana and Damiana on gastric emptying; to determine the effect of the same preparation on weight loss over 10 days and 45 days and weight maintenance over 12 months. Methods: Gastric emptying was observed using ultrasound scanning in seven healthy volunteers following YGD and placebo capsules taken with 420 mL apple juice. Body weight was observed before and after 10 days of treatment with three YGD capsules or three placebo capsules before each meal for 10 days in 44 healthy overweight patients attending a primary health care centre. Forty-seven healthy overweight patients entered a double-blind placebo-controlled parallel trial of three capsules of YGD capsules before each main meal for 45 days compared with three placebo capsules on body weight. Body weight was monitored in 22 patients who continued active (YGD capsules) treatment for 12 months. Results: The herb preparation YGD was followed by a prolonged gastric emptying time of 58 +/- 15 min compared to 38 +/- 7.6 min after placebo (P = 0.025). Body weight reductions were 0.8 +/- 0.05 kg after YGD capsules compared to 0.3 +/- 0.03 kg after placebo capsules over 10 days, and 5.1 +/- 0.5 kg after PGD capsules compared to 0.3 +/- 0.08 kg after placebo over 45 days. Active treatment with YGD capsules resulted in weight maintenance of the group (73 kg at the beginning and 72.5 kg at the end of 12 months). Conclusions: The herbal preparation, YGD capsules, significantly delayed gastric emptying, reduced the time to perceived gastric fullness and induced significant weight loss over 45 days in overweight patients treated in a primary health care context. Maintenance treatment given in an uncontrolled context resulted in no further weight loss, nor weight regain in the group as a whole. The herbal preparation is thus shown to be one that significantly modulates gastric emptying. Further clinical studies with dietetic monitoring of energy intake, dietary quality, satiety ratings, body weight and body composition are now indicated, and examination of the active principles contained in the three herbal components may prove rewarding.
Article
The higher concentration during exercise at which lactate entry in blood equals its removal is known as 'maximal lactate steady state' (MLSS) and is considered an important indicator of endurance exercise capacity. The aim of the present study was to determine MLSS in rats during swimming exercise. Adult male Wistar rats, which were adapted to water for 3 weeks, were used. After this, the animals were separated at random into groups and submitted once a week to swimming sessions of 20 min, supporting loads of 5, 6, 7, 8, 9 or 10% of body wt. for 6 consecutive weeks. Blood lactate was determined every 5 min to find the MLSS. Sedentary animals presented MLSS with overloads of 5 and 6% at 5.5 mmol/l blood lactate. There was a significant (P<0.05) increase in blood lactate with the other loads. In another set of experiments, rats of the same strain, sex and age were submitted daily to 60 min of swimming with an 8% body wt. overload, 5 days/week, for 9 weeks. The rats were then submitted to a swimming session of 20 min with an 8% body wt. overload and blood lactate was determined before the beginning of the session and after 10 and 20 min of exercise. Sedentary rats submitted to the same acute exercise protocol were used as a control. Physical training did not alter the MLSS value (P<0.05) but shifted it to a higher exercise intensity (8% body wt. overload). Taken together these results indicate that MLSS measured in rats in the conditions of the present study was reproducible and seemed to be independent of the physical condition of the animals.
Article
Since passage of the Dietary Supplement Health and Education Act of 1994, the sale of herbal dietary supplements containing caffeine and ephedrine for weight loss has become widespread in the United States. Reports of adverse events associated with the use of these non-prescription supplements have raised concerns in the United States regulatory community. Restricting the use of these products is now being considered. Such restriction should be based upon controlled clinical trials. This review of the literature in Medline relative to the use of caffeine and ephedrine in the treatment of obesity concludes that caffeine and ephedrine are effective in causing weight loss. Caffeine and ephedrine give equivalent weight loss to Diethylpropion and superior weight loss compared to dexfenfluramine. Caffeine and ephedrine have a long history of safe, non-prescription use. The adverse events accompanying acute dosing are mild and transient. Adverse events with caffeine and ephedrine reach and remain at placebo levels after 4-12 weeks of continuous treatment, but data from randomized trials up to 6 months only are available. Obesity is chronic, requires chronic treatment, its incidence is increasing and it has few effective treatments. The benefits of caffeine and ephedrine in treating obesity appear to outweigh the small associated risks. Restriction of dietary herbal supplements containing caffeine and ephedrine, often with other ingredients, should be based on controlled clinical trials of these products.
Article
The use of dietary botanicals is receiving considerable interest in the protection of skin from the adverse biological effects of solar ultraviolet (UV) radiation. Dietary feeding of proanthocyanidins extracted from grape seeds (GSP) (0.2 and 0.5%, w/w) in AIN76 control diet to SKH-1 hairless mice resulted in prevention of photocarcinogenesis in terms of tumor incidence (20-95%), tumor multiplicity (46-95%) and tumor size (29-94%) against UVB-induced complete (both initiation + promotion), initiation and promotion stages of photocarcinogenesis. Feeding of GSP (0.5%, w/w) also resulted in prevention of malignant transformation of UVB-induced papillomas to carcinomas in terms of carcinoma incidence (45%), carcinoma multiplicity (61%) and carcinoma size (75%) compared with non-GSP treated mice following UVB-induced complete carcinogenesis protocol at the end of 30 weeks. Biochemical analysis revealed that treatment of GSP in vivo and in vitro systems significantly inhibited UVB- or Fe3+-induced lipid peroxidation by 57-66% (P<0.01) and 41-77% (P< 0.05-0.001), respectively, thus suggesting the antioxidant mechanism of photoprotection by GSP. Long-term feeding of GSP did not show apparent signs of toxicity in mice when determined in terms of body weight, diet consumption and physical characteristics of internal body organs like spleen, liver and kidney. Feeding of GSP also did not show apparent signs of toxicity when determined in terms of total body mass (mass of lean + fat), total bone mineral density and total bone mineral content by employing dual-energy X-ray absorptiometry (DXA). DXA analysis also revealed that feeding of GSP significantly decreased tissue fat level (24-27%, P<0.05) without changing the total body mass of the animals compared with non-GSP-fed animals. This can be attributed to increased lipolysis or decreased synthesis of fat due to administration of GSP. Together, it can be suggested that inhibition of photocarcinogenesis by GSP treatment may be associated with the reduction in UVB-induced oxidative damage and tissue fat content.
Article
The effects of guarana (Paullinia cupana) extract were analyzed in rats on acute gastric lesions induced by ethanol and indomethacin and were compared to those produced by caffeine, a methylxanthine. Guarana (50 and 100 mg/kg p.o.) pretreated animals showed a significant reduction in the severity of gastric lesions induced by absolute ethanol in a manner similar to caffeine (20 and 30 mg/kg p.o.). Against indomethacin-induced gastric ulceration, guarana at a higher dose offered significant protection but caffeine was ineffective at the doses tested. In 4 h pylorus-ligated rats, both guarana and caffeine caused significant diminution in the gastric secretory volume as well as the total acidity. Gastrointestinal transit in mice was not significantly affected by either of these agents. These findings indicate that guarana has a gastroprotective property that needs further elucidation as regards to its mechanism.
Article
Since 1922 when Wu proposed the use of the Folin phenol reagent for the measurement of proteins (l), a number of modified analytical pro- cedures ut.ilizing this reagent have been reported for the determination of proteins in serum (2-G), in antigen-antibody precipitates (7-9), and in insulin (10). Although the reagent would seem to be recommended by its great sen- sitivity and the simplicity of procedure possible with its use, it has not found great favor for general biochemical purposes. In the belief that this reagent, nevertheless, has considerable merit for certain application, but that its peculiarities and limitations need to be understood for its fullest exploitation, it has been studied with regard t.o effects of variations in pH, time of reaction, and concentration of react- ants, permissible levels of reagents commonly used in handling proteins, and interfering subst.ances. Procedures are described for measuring pro- tein in solution or after precipitation wit,h acids or other agents, and for the determination of as little as 0.2 y of protein.
Article
Sorghum is a rich source of various phytochemicals including tannins, phenolic acids, anthocyanins, phytosterols and policosanols. These phytochemicals have potential to significantly impact human health. Sorghum fractions possess high antioxidant activity in vitro relative to other cereals or fruits. These fractions may offer similar health benefits commonly associated with fruits. Available epidemiological evidence suggests that sorghum consumption reduces the risk of certain types of cancer in humans compared to other cereals. The high concentration of phytochemicals in sorghum may be partly responsible. Sorghums containing tannins are widely reported to reduce caloric availability and hence weight gain in animals. This property is potentially useful in helping reduce obesity in humans. Sorghum phytochemicals also promote cardiovascular health in animals. Such properties have not been reported in humans and require investigation, since cardiovascular disease is currently the leading killer in the developed world. This paper reviews available information on sorghum phytochemicals, how the information relates to current phytonutrient research and how it has potential to combat common nutrition-related diseases including cancer, cardiovascular disease and obesity.