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Ethanol Extracts of Eriobotrya japonica (Loquat) Seeds, Leaves, and Fruits Have Anti-obesity and Hypolipidemic Effects in Rats
Abstract
Background
Obesity is a serious public health problem contributing to development of several diseases, including hyperlipidemia, hyperglycemia, and hypertension. The plant Eriobotrya japonica (loquat) has been used in traditional Chinese medicine to treat many ailments and traditional healers used it to reduce weight.
Objective
To examine the potential anti-obesity and hypolipidemic effects of ethanol extract of loquat in rats.
Materials and Methods
Loquat leaves, fruits, or seeds were extracted with ethanol. About 96 Wistar male rats were fed either a normal rat diet (normal control group; group 1) or a high-fat diet (HFD) for 12 weeks (obese; groups 2−12). Obese rats were divided into11 groups as follows: (obese control: group 2) (obese positive control which received the hypolipidemic reference drug atorvastatin: group 3). Groups (4−6), (7−9), and (10−12) were given seed, leaf, or fruit extract, respectively, at 40,100, and 400 mg/kg. Body weight, serum glucose, lipid profile, creatinine, liver enzymes, albumin, and total protein were measured weekly.
Results
HFD consumption significantly increased body weight and serum total cholesterol (TC), triglycerides (TGs), low-density lipoprotein (LDL), very-low density lipoprotein (VLDL), and glucose and decreased HDL compared to rats fed the normal diet. HFD also increased serum glutamic-oxaloacetic transaminase (GOT), gamma-glutamyl transferase (GGT), alkaline phosphatase (ALP) and creatinine but decreased serum albumin and total protein. Administration of E. japonica seed, leaf, or fruit extract significantly decreased body weight, TC, TGs, LDL, VLDL, glucose, liver, and renal enzymes but increased HDL, albumin, and total protein levels.
Conclusion
E. japonica seed, leaf, and fruit ethanol extract regulates body weight gain, has hypolipidemic properties, and positively affects liver and kidney enzymes.
... 12 To date, several scientific studies have investigated the biological properties of various parts of the loquat plant, including its antidiabetic, antihyperlipidemic, anti-obesity, hepatoprotective and antioxidant effects in different animal models. 11,[13][14][15][16] However, the protective effect of fruit peel against tyloxapol-induced hyperlipidemia and liver and kidney toxicity has not yet been studied. ...
... 44 Our findings align with previous reports demonstrating that the ingestion of E. japonica seed, leaf, and fruit extracts resulted in a significant reduction in serum cholesterol levels. 13,15 On the other hand, the atherogenic index is now well regarded as a significant predictor of the development of atherosclerosis. 45 So, it was revealed that the peel extract suppressed the elevated values of the atherogenic index and LDL-C/HDL-C ratio, offering strong evidence for the anti-atherogenic properties of such an extract. ...
... [59][60][61] As previously hypothesized, the protective effect of the peel extract could be due to the presence of phenolic compounds, which are known especially for their hypolipidemic, anti-oxidant and hepatoprotective activities. 2,15,16 Thus, after HPLC analysis, we realized that the studied extract contained five major phenolic compounds, namely, ferulic acid, caffeic acid, neochlorogenic acid, chlorogenic acid and quercetin. Furthermore, it appears that neochlorogenic acid is the most prevalent phenolic component, which is known in the literature for its interesting pharmacological activities. ...
Hyperlipidemia is the most well-known cause of metabolic complications and tissue toxicity such as liver steatosis, atherosclerosis and obesity. This study aims to evaluate the preventive effect of loquat fruit peel extract (PE) against tyloxapol-induced hyperlipidemia and related tissue lipotoxicity in mice. The in vivo study was conducted on mice injected daily with tyloxapol at 100 mg per kg B.W. and treated simultaneously with the PE at concentrations of 100 and 200 mg kg-1 or fenofibrate for 28 days. Plasma and tissue lipid biochemical analyses were undertaken using enzymatic methods. The antioxidative stress was revealed by measuring the malondialdehyde content and activities of superoxide dismutase and catalase as well as the scavenging activity against lipoperoxyl radicals. The PE significantly prevented oxidative stress and restored lipid metabolism, plasma glucose, body weight, organ relative mass and biomarkers of hepato-nephrotoxicity as well as the histological structure of the liver and kidneys. It contains five major polyphenols, namely, ferulic acid, caffeic acid, neochlorogenic acid, chlorogenic acid and quercetin. According to molecular docking analysis, these compounds and their circulating metabolites could interact with major proteins implicated in lipid metabolism and oxidative stress. Overall, the study suggests that PE could prevent hyperlipidemia and related toxic tissue complications.
... Indeed, loquat is a plant with strong therapeutic potential since various parts have been used traditionally to treat cough, chronic bronchitis, inflammation, diabetes, and cancer as known in Chinese folk medicine (Zhou et al., 2019;Kumar and Pallavi, 2014). Until this point in time, numerous scientific studies focused on the biological properties of different parts of loquat plant such as antidiabetic, antihyperlipidemic, anti-obesity and antioxidant effects in different animal models (Shafi and Tabassum, 2013;Lin et al., 2018;Abdelrahman et al., 2022;Kim et al., 2011). ...
... In light of this, we hypothesize that the extract promotes the synthesis and expression of hepatic and extra-hepatic LDL-receptors, hence enhancing the absorption of plasma LDL-C, particularly by the liver and peripheral organs. Our results agree with the findings of Abdelrahman et al. (2022), who reported that the administration of E. japonicaseed, leaf, and fruit extracts significantly decreased serum cholesterol. ...
... On the other hand, the effect of the extract on cholesterol metabolism is accompanied by a significant increase in HDL-C fraction levels, which is in accordance with previous studies on different parts of E. Japonica extracts (Shafi and Tabassum, 2013;Abdelrahman et al., 2022;Khouya et al., 2022). So, at this experiment stage, we first suggested that the hepatobiliary reverse cholesterol transport (RCT) was activated under the effect of phenolic compounds of the studied extract or their circulating metabolites. ...
Ethnopharmacological relevance:
In Moroccan traditional medicine, fresh or dried loquat (Eriobotrya japonica (Thunb.) Lindl.) fruit peels infused in water and taken for 45 days are used as natural remedies against hypercholesterolemia, hyperglycemia and cardiovascular diseases. This is the first experimental study approving the folk medicinal use of loquat fruit peels originated from eastern Morocco.
Aim of the study:
The study aims to investigate the effect of loquat fruit peel extract on lipid metabolism and liver oxidative status in mice as well as to predict the possible mechanisms.
Materials and methods:
The study was carried out using high fat/fructose diet-induced hyperlipidemic mice model treated with the loquat peel extract for 45 days at two doses (100 and 200 mg/kg/day) in comparison to fenofibrate drug. The plasma, tissue, fecal and biliary lipids and blood glucose were analyzed using enzymatic methods. The liver oxidative status was evaluated and the polyphenol profiling was conducted using the HPLC-DAD method. Possible mechanisms involved in the observed pharmacological effects were predicted by in silico method.
Results:
The extract at a dose of 200 mg/kg possessed higher effect than at 100 mg/kg. It significantly reduced plasma total cholesterol (TC), triglycerides (TG), LDL-cholesterol, atherogenic index, LDL-C/HDL-C ratio and plasma glucose (-36%, -45%, -45%, -82%, -87%, 58%, respectively), while the HDL-cholesterol was increased (+172%). Moreover, the extract reduced TC and TG in the liver and adipose tissue by increasing their excretion in bile and fecal matter. It prevented the liver oxidative stress and decreased body weight and organ relative mass. The extract appears to be nontoxic (LD50 > 5000 mg/kg) and contains five polyphenols including ferulic acid (32.74 ± 0.71 mg/g), caffeic acid (21.48 ± 0.32 mg/g), 5-O-Caffeoylquinic acid (112.15 ± 1.86 mg/g), chlorogenic acid (42.05 ± 0.92 mg/g) and quercetin (32.69 ± 0.68 mg/g). These phenolics and/or their circulating metabolites presented differential interaction capacities with the potential enzymes and transcription factors implicated in lipid homeostasis such as HMG-CoA reductase, lipoprotein lipase, fatty acid synthase, Cyp7a1, ABCG, PPARs, RXR, FXR and RAR.
Conclusion:
Our findings justify the traditional use of loquat fruit peels and suggest that their aqueous extract could be used as substrate to produce phytotherapeutic drugs or dietary supplements to prevent hyperlipidemia, hyperglycemia and related cardiovascular diseases.
... Numerous studies using varying experimental models found beneficial effects on each part of the plant, including fruit, leaf, and seed (79)(80)(81). Pre-clinical studies reported the antifatigue potential of loquat leaf extract (LLE) in vitro and in vivo (82). Additionally, LLE improved muscle contraction-induced activation of p70S6K phosphorylation in rat skeletal muscles, preventing atrophy (83). ...
The review specifically assesses the impact of herbal supplements on muscle mass, strength, and performance in adults. Given their potential anti-inflammatory and antioxidant properties, herbal supplements such as Curcuma longa and Panax ginseng are hypothesized to counteract muscle degradation and enhance muscle function, which are key factors in managing sarcopenia among the elderly. Of 3,332 records found after a comprehensive database search, 13 trials were analyzed. Importantly, high-dose Viscum album coloratum and formulated Curcuma longa increased muscle mass and TUG, and handgrip strength and endurance, respectively, supporting their inclusion in preventive strategies against sarcopenia. Schisandra chinensis, Glycine max, and Arctium lappa also proved beneficial in improving handgrip strength and performance. Most trials reported minimal adverse events. This review underscores the benefits of herbal supplements in enhancing muscle health and calls for further studies on the long-term effects of Asparagus racemosus, Cistanche tubulosa, and Anacardium occidentale to better understand their mechanisms.
... The elevated levels of these enzymes observed in the HFD group suggest changes in liver metabolic function. This result is consistent with the study conducted by [63], which showed that the EJ ethanolic extract had inhibitory effects on the elevation of liver enzyme levels. Different extracts of EJ leaves, including the aqueous extract, were also found to have hepatotoxicity activity by decreasing serum levels of liver enzymes such as ALP, ALT, AST [64]. ...
This study deals with the in vitro and in vivo evaluation of the antioxidant, anti-obesity and anti-inflammatory activities of Eriobotrya japonica (EJ) aqueous leaf extract. The obtained results showed that the EJ extract exhibited an important antioxidant capacity based on performing the DPPH assay. HPLC analysis revealed the presence of major phenolic compounds such as gallic acid, chlorogenic acid and quercetin. A six-week treatment with 100 mg EJ extract/kg bw or 30 mg orlistat/kg bw reduced fat cell size and significantly decreased body weight of obese rats by 10.73% and 15.42%, respectively. The EJ extract also reduced serum lipid and liver enzyme levels, as well as oxidative stress parameters. Histopathological examination of liver sections supported the biochemical tests. Oral administration of EJ extract was also effective in reducing oedema formation in rats against carrageenan-induced inflammation. These results therefore suggest that EJ aqueous extract may have promising effects in the treatment of obesity and inflammation. Rezumat Acest studiu evaluează activitățile antiinflamatorii, antioxidante și anti-obezitate ale extractului apos obținut din frunzele speciei de Eriobotrya japonica (EJ), in vitro și in vivo. Rezultatele obţinute au arătat că extractul de EJ a prezentat o capacitate antioxidantă importantă pe baza testului DPPH. Analiza HPLC a relevat prezența compușilor fenolici majori, cum ar fi acidul galic, acidul clorogenic și quercetina. Un tratament de șase săptămâni cu 100 mg extract de EJ/kgc sau 30 mg orlistat/kgc a redus dimensiunea celulelor adipoase și a scăzut semnificativ greutatea corporală a șobolanilor obezi cu 10,73% și, respectiv, 15,42%. Extractul de EJ a redus, de asemenea, nivelurile serice de lipide și enzime hepatice, precum și parametrii de stres oxidativ. Examenul histopatologic al secțiunilor hepatice a susținut rezultatele testelor biochimice. Administrarea orală a extractului de EJ a fost, de asemenea, eficientă în reducerea formării edemului la șobolani într-un model de inflamație indusă de caragenan. Prin urmare, aceste rezultate sugerează că extractul apos de EJ poate avea efecte promițătoare în tratamentul obezității și inflamației.
... Notably, mice receiving the juice had lower hepatic cholesterol and higher biliary cholesterol levels than controls, indicating adequate peripheral cholesterol clearance through the RCT pathway. These findings align with and extend previous research on loquat's benefits against lipid metabolism disorders [19,34]. ...
Background: Loquat fruit is consumed for its flavorful taste and a rich array of health-promoting compounds like phenolics, flavonoids, and carotenoids. This study aimed at the biochemical characterization of fresh juice from the Moroccan Mkarkeb variety of loquat and evaluating its effects on lipid homeostasis and liver steatosis in hyperlipidemic mice. Methods: The biochemical characterization followed AOAC methods. In vivo study involved hyperlipidemic mice fed a high-fat, high-fructose diet for 6 weeks and treated with loquat juice at 3.5 and 7 mL kg⁻¹ or fenofibrate at 4 mg·kg⁻¹. The concentrations of lipids in plasma, liver, adipose tissue, feces, and bile and blood glucose levels were quantified. Liver steatosis was visually examined and confirmed histologically, and liver injury markers (AST, ALT, ALP, LDH, and TB) were measured. Liver oxidative stress was assessed by measuring MDA content and antioxidative enzyme activities. Results: Our findings indicate that fresh loquat juice is poor in fat and protein and contains moderate sugars with a low energy value (40.82 ± 0.25 kcal/100 g). It is also rich in minerals, vitamin C, phenolic acids, flavonoids, and carotenoids. The juice effectively restored lipid metabolism by enhancing reverse cholesterol transport and lowering LDL-cholesterol, triglycerides, and the atherogenic index. The studied juice decreases blood glucose and prevents weight gain and lipid accumulation in the liver and adipose tissue. The juice prevents lipotoxicity-induced liver injury, corrects toxicity markers, and improves the liver’s morphological and histological structures. It also reduces oxidative stress by lowering MDA and activating SOD and catalase. Conclusions: The juice holds high nutritional and medicinal value, potentially preventing lipid disorders and cardiovascular issues.
... This finding indicates that the excess peripheral cholesterol was efficiently transported back to the liver via the RCT pathway and ultimately excreted into the bile. These findings align with and complement previous studies highlighting the positive effects of loquat on lipid metabolism (Abdelrahman et al., 2023;Mokhtari et al., 2023b). Conversely, the atherogenic indices are currently regarded as more meaningful indicators for atherosclerotic risk evaluation. ...
Loquat (Eriobotrya japonica L.) is a popular fruit known for its sweet and slightly tangy flavor, which is widely consumed both fresh and in various processed forms. This study aimed to analyze the biochemical composition of loquat juice and investigate its metabolic benefits in mice fed a high-fat/high-sucrose diet (HFSD). Mice were fed either a standard diet or an HFSD and received or not the loquat juice at 4 or 8 mL/kg body weight for 8 weeks. Body weight, food efficiency ratio, plasma lipoprotein profile, plasma glucose, and lipid indices were monitored throughout the experiment. At the end of the experiment, additional assessments were performed, including lipid content measurements in liver, adipose tissue, bile, and feces; hepatic antioxidant enzyme activities (superoxide dismutase and catalase); hepatic malondialdehyde content; plasma biomarkers of liver injury; liver histology; and organ relative weight. Feeding mice with the HFSD resulted in a significant perturbation in lipid and glucose metabolism, obesity, liver steatosis, and oxidative stress-related enzymes. However, the concomitant administration of loquat juice significantly corrected this imbalance. Fresh loquat juice is low in fat and protein, moderately sugary, and energetically light; however, it is rich in minerals, vitamin C, and various phytochemicals compounds, such as phenolic acids, flavonoids, and carotenoids. The loquat juice could be considered a functional food and could be valorized through the extraction of active substances and their use as food supplements to prevent lipid metabolism disorders and the resulting health complications.
Plants are sources of many therapeutics used for the treatments of many complex diseases since ancient times. Plants can synthesize a plethora of natural compounds with diverse chemical structures. Despite many advances in the world, a large population of the world is still relying on the herbal system. Therefore, a holistic effort must be made for the conservation of herbal hot spots as well as also for the scientific documentation of active herbal ingredients present in a plant. A paradigm shift has taken from the herbal medicine system to modern approaches of drug design and therapy with the advancement of scientific research in the field of structural biology, genomics, proteomics, therapeutic biology, biochemistry, systems biology, and computer science. Rational approaches of drug development have made it possible to model the target, design various analogs, and dock them with the target, screen, analyze, and predict the pharmacokinetic and pharmacodynamic properties. Rational approaches have significantly reduced the cost, labor, and risk of failure in the process of drug discovery.
Graphical Abstract
Improvements in the yield and solubility of chestnut wood extractives, by using different extraction methods and molybdenum catalysts as support, have rarely been reported in literature. Many studies focus on the different parts of trees, except for the chemical characteristics of the remaining extractives achieved from thermally modified (THM) chestnut (Castanea sativa Mill) wood. This research seeks to better understand the effects of extraction techniques and catalysts on the yield and solubility of extractives. GC-MS analysis of the chloroform soluble and insoluble fractions was also used. Accelerated Solvent Extraction (ASE) 110 °C, Soxhlet, and autoclave extraction techniques were used to obtain extractives from untreated and thermally modified (THM) chestnut wood (170 °C for 3 h). Ethanol/H2O, ethanol/toluene, and water were the solvents used for each technique. A polyoxometalate compound (H3PMo12O40) and MoO3 supported on silica were used as catalysts. The THM induced a change in the wood’s surface color (ΔE = 21.5) and an increase in mass loss (5.9%), while the equilibrium moisture content (EMC) was reduced by 17.4% compared to the control wood. The yields of the extractives and their solubility were always higher in THM and mainly used ASE as the technique. GC-MS analysis of the extractives, without catalyst support, showed different results for each extraction technique and type of wood (untreated and THM). Ultimately, the amount of extractive compound dissolved in each solvent will differ, and the choice of extraction technique will depend on the intended final application of the extracted chemical product.
Present research explored the anti-obesity effect of Moringa olifera oil extract and lycopene (LYC). Forty eight male Sprauge Dawely rats were divided equally into 6 groups. Group Ι (C) served as control, Group ΙΙ (MC) was given Moringa olifera (800 mg/kg b.wt) for 8 weeks, Group ΙΙΙ (LC) was given (20 mg/kg b.wt) LYC for 8 weeks, Group ΙV (O) received high fat diet (HFD) for 20 weeks, Group Ѵ (MO), was given HFD for 20 weeks and received (800 mg/kg b.wt) Moringa olifera oil extract for last 8 weeks and Group ѴΙ (LO), received HFD for 20 weeks and was given (20 mg/kg b.wt) LYC for last 8 weeks. Hematology, lipid peroxidation and antioxidants, non-esterified fatty acids (NEFA), glucose, lipid profile, serum liver and kidney biomarkers, inflammatory markers, leptin, resistin and heart fatty acid binding protein (HFABP) were determined. Also histopathology for liver, kidney and aorta were performed besides immunohistochemistry (IHC) for aortic inducible nitric oxide synthase (iNOS). Administration of Moringa olifera and LYC significantly ameliorated the HFD induced hematological and metabolic perturbations as well as increased leptin and resistin. Both treatments exerted these effects through promotion of antioxidant enzymes and reducing lipid peroxidation as well as inflammatory cytokines along with reduced iNOS protein expression. Administration of Moringa olifera oil extract and LYC have anti-obesity potential in HFD induced obesity in male Sprauge Dawely rats.
Eugenol, a component of essential oils of medicinal and food plants, has a hypolipidemic effect in experimental animals although its mechanism of action is still unclear. This study aims to explore the mechanism of the hypolipidemic effect of eugenol in rats fed a high cholesterol and fat diet (HCFD). Eugenol significantly reduced total cholesterol (TC), low-density lipoproteins (LDL), atherogenic index (AI) but not high-density lipoproteins (HDL) or triglycerides (TG). Eugenol also decreased steatosis and hepatic inflammation in liver sections, decreased hepatomegaly, and the hepatic marker enzymes alanine aminotransferase (ALT) and alkaline phosphatase (ALP) activity and increased the antioxidant enzymes superoxide dismutase (SOD) and catalase (CAT) activity in hypercholesterolemic rats. Eugenol did not inhibit hepatic 3-hydroxy-3-methyl-glutaryl-CoA (HMG-CoA) reductase but caused down-regulation of transient receptor potential vanilloid (TRPV1) channels in the liver. Docking simulation using fast, rigid exhaustive docking (FRED) software indicated a tail-up/head-down interaction of eugenol with TRPV1 channel. Data indicate that eugenol does not inhibit HMG-CoA reductase but rather induces its action by interaction with TRPV1 channels.
With the improvement of living standards, obesity has become a serious health problem all over the word. Currently, the methods and drugs for obesity treatment have some limitations and side effects. Flavonoids are active constituents with various biological activities, widely found in plants, and numerous studies have shown that flavonoids can inhibit obesity and related metabolism disorders effectively. This perspective reviews the recent progress in understanding the anti‐obesity effects of flavonoids through modulating food intake, enzyme activities, nutrition absorption, adipogenesis and adipocyte lifecycle, thermogenesis, energy consumption, and intestinal microbiota.
Practical applications
Natural bioactive substance flavonoids have anti‐obesity property, which may play a role in anti‐obesity drugs or functional food without any side effects. Flavonoids can inhibit weight gain directly or through their biologically active metabolites by various potential pathways. A better understanding of the modulatory effect and the mechanism of flavonoids on obesity will allow us to better utilize flavonoids in plants to treat obesity and related metabolic syndrome.
Eriobotrya japonica is traditionally used as an antipyretic, digestive, and diuretic agent. Its flowers possess free radical–scavenging, antioxidative, and hepatoprotective effects. We investigated the hepatoprotective potential of E. japonica leaf extract and its various fractions against hepatotoxicity in rats. Liver injury was stimulated by the oral administration of carbon tetrachloride (CCl 4 ; 2.5 mL/kg b.wt.). Male albino rats (n = 55) were distributed arbitrarily into 11 groups: Group I, normal control group; Group II, CCl 4 (positive control group); Group III, CCl 4 + silymarin; Groups IV and V, CCl 4 + two doses of 250 and 500 mg/kg of the 80% methanolic extract of E. japonica leaves, respectively; Groups VI and VII, CCl 4 + 250 mg/kg and 500 mg/kg of the ethyl acetate fraction, respectively; Groups VIII and IX, CCl 4 + 250 and 500 mg/kg of the butanol fraction, respectively; and Groups X and XI, CCl 4 + 250 and 500 mg/kg of the aqueous fraction of E. Japonica leaves, respectively. CCl 4 -treated rats that were given 250 or 500 mg/kg of the methanol extract of E. Japonica leaves, or its ethyl acetate, butanol, or aqueous fractions, had significantly lower levels of biochemical parameters such as alanine aminotransferase, aspartate transaminase, alkaline phosphate, total protein, gamma-glutamyl transferase, and bilirubin levels than those of the CCl 4 positive group. However, the extract and fractions did not significantly affect lipid profiles. Thus, we conclude that Eriobotrya leaf extract and its fractions have a hepatoprotective effect against CCl 4 -induced hepatotoxicity in rats.
Patients with diabetes type 2 have an increased risk for cardiovascular disease and commonly use combination therapy consisting of the anti-diabetic drug metformin and a cholesterol-lowering statin. However, both drugs act on glucose and lipid metabolism which could lead to adverse effects when used in combination as compared to monotherapy. In this review, the proposed molecular mechanisms of action of statin and metformin therapy in patients with diabetes and dyslipidemia are critically assessed, and a hypothesis for mechanisms underlying interactions between these drugs in combination therapy is developed.
The objective of this work is to put forth the optimization and kinetics of total phenolic compound extraction from A.indica leaves in a stirred batch extraction. Various experiential extraction parameters have been studied for maximum extraction of the total phenolic compounds. The maximum yield of total phenolic compounds was found to be 10.80 mg/g of dried neem powder at the optimized conditions. The extraction kinetics behavior followed first-order kinetics with diffusion coefficient ranged from 1.8 × 10⁻¹² to 3.2 × 10⁻¹² m²/s for all sets. Activation energy (Ea) value for the extraction of the total phenolic compounds was found to be 22.87 kJ/mol. The kinetic expression model developed by Spiro and Siddique showed a good agreement with the experimental outcomes. The obtained results can be used to scale up the operations for industrial purposes.
The occurrence of atherosclerosis and diabetes is expanding rapidly worldwide. These two metabolic disorders often co-occur, and are part of what is often referred to as the metabolic syndrome. In order to determine future therapies, we propose that molecular mechanisms should be investigated. Once the aetiology of the metabolic syndrome is clear, a nutritional intervention should be assessed. Here we focus on the protective effects of some dietary flavonoids, and their metabolites. Further studies may also pave the way for development of novel drug candidates.
The present study is to evaluate the anti-obesity effects of Eriobotrya japonica (EJ), Nelumbo nucifera (NN), and their mixture (MIX, 1:1 ratio) in 3T3-L1 adipocytes and high-fat diet-induced obese mice. The treatment of EJ, NN, and MIX in 3T3-L1 adipocytes effectively inhibited lipid accumulation, significantly decreased expression of peroxisome proliferator-activated receptor gamma (PPARγ), sterol regulatory element binding protein (SREBP1c), and adipocyte lipid-binding protein (aP2), and significantly increased phosphorylation of AMP-activated protein kinase (AMPK). Moreover, oral treatment of MIX showed stronger effects than individual treatment. C57BL/6J mice (6 week old) were divided into two groups; low fat diet (LFD) containing 10% calories from fat and high fat diet (HFD) containing 60% calories from fat. The HFD groups were further divided into five subgroups; treated with distilled water (HFD), treated with 400 mg/kg EJ (EJ400), treated with 400 mg/kg NN (NN400), treated with 200 mg/kg MIX (MIX200), and treated with 400 mg/kg MIX (MIX400) during 13 weeks. In our results, the administration of EJ, NN, and MIX significantly decreased body weight (BW), fat weight, liver weight, hepatic triglyceride (TG) and total cholesterol (TC), lipid droplets in the liver, food efficacy ratio, and the plasma TG, TC, glucose, insulin, alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in a dose-dependent manner, and MIX treatment showed stronger effect than their individual treatments. Similarly, MIX treatment decreased the expression of PPARγ, SREBP-1c, FAS, and ACC more strongly in the adipose tissue than single treatments. In conclusion, the MIX of EJ and NN extract may strongly regulate BW gain than EJ or NN alone, and its anti-obesity effect is associated with the control of lipid metabolism, including adipogenesis and lipogenesis.
The characteristics, phenolic compound contants, and antioxidant capacities of 6 cultivars of loquat fruit grown in China were evaluated. HPLC was used to identify and quantify phenolics. Chlorogenic acid, neochlorogenic acid, 4-O-caffeoylquinic acid, protocatechuic acid, 4-hydroxybenzoic acid, caffeic acid, ferulic acid, ellagic acid, and o-coumaric acid were the main phenolic compounds of mature loquat fruits. Contents of chlorogenic acid, neochlorogenic acid, 4-hydroxybenzoic acid, protocatechuic acid, and o-coumaric acid were all significantly correlated with antioxidant capacities determined using DPPH, ABTS radical scavenging activity, and ferric reducing/antioxidant power assays. The ‘Taxiahong’ cultivar contained the highest amounts of total phenolics and flavonoids and the highest antioxidant capacity, while ‘Taipingbai’ showed the lowest. The high level of phenolic compounds and antioxidant capacities of some cultivars indicates that these cultivars can be sources of bioactive compounds that are relevant to human health.
Obesity became major health problem in the world, the objective of this work was to examine the effect of high sucrose and high fat diet to induce obesity on antioxidant defense system, biochemical changes in blood and tissue of control, non treated and treated groups by administration of Garcinia cambogia, and explore the mechanisms that link obesity with altered renal function.
Rats were fed a standard control diet for 12 week (wk) or a diet containing 65% high sucrose (HSD) or 35% fat (HFD) for 8 wk and then HFD group divided into two groups for the following 4 wks. One group was given Garcinia+HFD, the second only high fat, Also the HSD divided into two groups, 1st HSD+Garcinia and 2nd HSD. Blood and renal, mesenteric, Perirenal and epididymal adipose tissues were collected for biochemical assays.
HFD and HSD groups of rats showed a significant increase in feed intake, Body weight (BW) and body mass index (BMI). Also there were significant increases in weights of mesenteric, Perirenal and epididymal adipose tissues in HFD and HSD groups.HFD and HSD affect the kidney by increasing serum urea and creatinine levels and decreased level of nitric oxide (NO) and increased blood glucose, low density lipoproteins (LDL), triacylglycerol (TG), total cholesterol (TC) and malondialdehyde (MDA). Glucose 6-phosphate dehydrogenase (G6PD) activities were significantly decreased in HFD while there were significant increases in HSD and HSD+G groups p ≤ 0.05 compared with control. Moreover, renal catalase activities and MDA levels were significantly increased while NO level was lowered. These changes improved by Garcinia that decreased the oxidative stress biomarkers and increased NO level.There were significant positive correlations among BMI, kidney functions (Creatinine and urea), TG and Oxidative markers (renal MDA and catalase).
Rats fed a diet with HFD or HSD showed, hypertriglyceridemia, increased LDL production, increased oxidative stress and renal alteration. Moreover, suggesting association between lipid peroxidation, obesity and nephropathy, while Garcinia ameliorated the damaging effects of the HFD or HSD and decreased feed intake, MDA level and decreased oxidative stress in renal tissues.
Epidemiological studies have shown a positive relationship between dietary fat intake and obesity. Since rats and mice show a similar relationship, they are considered an appropriate model for studying dietary obesity. The present paper describes the history of using high-fat diets to induce obesity in animals, aims to clarify the consequences of changing the amount and type of dietary fats on weight gain, body composition and adipose tissue cellularity, and explores the contribution of genetics and sex, as well as the biochemical basis and the roles of hormones such as leptin, insulin and ghrelin in animal models of dietary obesity. The major factors that contribute to dietary obesity - hyperphagia, energy density and post-ingestive effects of the dietary fat - are discussed. Other factors that affect dietary obesity including feeding rhythmicity, social factors and stress are highlighted. Finally, we comment on the reversibility of high-fat diet-induced obesity.
The hypoglycemic effects of Eriobotrya japonica seeds were investigated in type 2 diabetic Otsuka Long-Evans Tokushima fatty (OLETF) rats and KK-A(y) mice. The rats and mice were fed on a diet containing 10% powdered Eriobotrya japonica seeds with the coat intact for 4 months. Although the blood glucose concentration in the OLETF rats fed on the control diet without Eriobotrya japonica seeds was increased with time, the concentration in the OLETF rats fed on the diet with Eriobotrya japonica seeds was consistently low throughout the experimental period and was comparable to the level in Long-Evans Tokushima Otsuka (LETO) rats which are normal non-diabetic rats. Serum insulin was significantly lower in the OLETF rats fed on the Eriobotrya japonica seed diet than in those fed on the control diet at the termination of the experimental period. Eriobotrya japonica seeds suppressed the increment of blood glucose for 4 months and also effectively improved the glucose tolerance in the KK-A(y) mice, these actions being mainly exerted by the ethanol extract of the seeds. These results suggest that Eriobotrya japonica seeds had a hypoglycemic property and the effect is attributable to the components extracted by ethanol.
Rationale: The loquat (Eriobotrya japonica Lindl.) is a fruit tree used in Chinese medicine for thousands of years for the treatment of various diseases. The loquat leaves extracts contain several bioactive compounds with antioxidant and antimicrobial properties, and identification of these substances by quick and simple methods has been an analytical trend.
Methods: The influence of dehydration of loquat leaves (without drying, at 40 °C, and at 60 °C), the type of solvent (ethanol and methanol), and the method of extraction (shaking and ultrasound) on obtaining extracts containing phenolic compounds and substances with antioxidant and antimicrobial activities were evaluated. The chemical constituents of an extract were identified by paper spray‐mass spectrometry (PS‐MS).
Results: The extract obtained with the dehydrated leaves at 40 °C presented the best results. The extracts obtained these leaves and with ethanol had the highest values of total phenolics and antioxidant activities, but the methanolic extract submitted to ultrasound had the highest levels of chlorogenic, caffeic and ellagic acids. All extracts evaluated inhibited the growth of Staphylococcus aureus . By use of PS‐MS technique, it was possible to suggest the presence of 49 substances such as organic acids, phenolic acids, flavonoids, sugars, quinones, and terpenes.
Conclusions: In general, extracts of dehydrated leaves at 40 °C and extracted with ethanol by ultrasound can be considered a good source of bioactive compounds with potential applications as functional ingredients or additives in food and pharmaceutical industry. PS‐MS was demonstrated to be a simple and ultrafast technique to obtain the chemical profile of loquat leaves extract.
Atherosclerosis is plaque formation in the arteries which will further develop into plaque, narrowing and shocking the artery. Continuous plaque formation leads to acute and chronic inflammation and soon develop into atherosclerosis. A combination of herbs in form of drink, consist of tanjung leaves (Mimusops elengi L.), starfruit leaves (Averrhoa carambola L.), and temulawak (Curcuma xanthorrhiza R.) is empirically believed to be anti-atherosclerotic; because it contains quercetin that initiate anti-inflammatory activity. Quercetin concentration test was conducted using an aluminum chloride colorimetric assay with variations in particle size (simplicia, 60<D<16 mesh powder, and D≤60 mesh powder) and herb mass, which further extracted in reflux and infusion method. Herbs with 60<D<16 mesh size and D≤60 mesh powder were extracted by infusion in 200 mL water, and leaf herbs were extracted by reflux in 600 mL water. The results show that increases in extracted herb mass related to the increasing in quercetin concentration. For future product commercialization purpose, quercetin concentration in leaves needs to be equal to its concentration within the range of particle size variation. Quercetin concentration in the leaves (459.91 ppm) was almost equal to that for 2.4 gram herbs in 60<D<16 mesh powder (489.09 ppm). The highest total flavonoid content was achieved in 2.4 gram 60<D<16 mesh herb powder with 41.508 mg QE (Quercetin Equivalent)/g. Therefore, it can be concluded that the anti-atherosclerotic herbs contain quercetin.
Nonalcoholic fatty liver disease (NAFLD) and metabolic syndrome (MS) are highly prevalent, affecting approximately one-third of the US population. The relationship between NAFLD and MS is complex and may be bidirectionally associated. NAFLD is strongly associated with MS, the components of which include abdominal obesity, hyperglycemia, hypertension, and dyslipidemia. NAFLD associated with certain genetic factors such as the PNPLA3 G allele variant is not accompanied by insulin resistance and MS. Lifestyle modification, including diet and physical activity targeting visceral adiposity, remains the standard of care for patients with NAFLD and MS.
Oxidative stress is one of the major mechanisms implicated in inorganic arsenic poisoning. Punica granatum is known by its free radical scavenging properties. The aim of this study was to evaluate the protective role of combined selenium and P. granatum against arsenic-induced liver injury. Seventy-five female albino rats were divided into five groups (of 15 rats each). Toxicity was induced by oral sodium arsenite (5.5 mg/kg body weight (bw) daily) (group ІІ). Treatment of arsenic-intoxicated rats was induced by daily oral administration of sodium selenite (3 mg/kg bw) (group ІІІ), 100 mg of P. granatum ethanol extract per kilogram body weight dissolved in 300 mL distilled water in three divided doses (100 mL of this suspension every 8 h) (group IV), and combined daily oral treatment with both selenite and P. granatum ethanol extract (group V). After 3 weeks, serum and liver tissues were obtained from the decapitated rats for different estimations. Hepatotoxicity was demonstrated by significant elevation in liver weights and activities of liver enzymes, alanine aminotransferase (ALT) and aspartate aminotransferase (AST), and decrease in serum total proteins and albumin (p < 0.05) which were confirmed by histopathological examination. Additionally, arsenic hepatotoxicity led to an increased values of malondialdehyde, advanced oxidation protein products, nitric oxide, and interleukin-6 (IL-6) (p < 0.05) and decreased activity of thioredoxin reductase, values of total anti-oxidant capacity, and nuclear factor erythroid 2-related factor 2 (Nrf2) gene expression. Significant improvement in all assessed parameters was observed in rat group treated with both P. granatum and selenium. It was concluded that combined P. granatum and selenium treatment had a synergistic hepatoprotective effect against arsenic toxicity through activation of Nrf2 anti-oxidant pathway.
Leaves and fruits (peel and flesh) of six improved cultivars (‘Mizuho’, ‘Néctar de Cristal’, ‘Mizauto’, ‘Mizumo’, ‘Centenária’ and ‘NE-3’) of loquat (Eriobotrya japonica Lindl.) were studied for their phenolic composition and antioxidant capacity. The analysis by HPLC-DAD-ESI-MS/MS allowed the identification of 18 compounds (8 hydroxycinnamic acid derivatives and 10 flavonoid glycosides). The quantification of the identified compounds revealed distinct profiles amongst the three analysed materials. Loquat leaves exhibited the lowest amounts of phenolics. 3- And 5-caffeoylquinic, and 5-feruloylquinic acids were the major compounds. Generally, ‘Mizauto’ cultivar presented the highest phenolic content. All loquat materials exhibited DDPH scavenging capacity, in a concentration-dependent manner, the leaves being the most active one. This effect seems to be related to the flavonoid content.
The antioxidative activity of the extracts of loquat fruits, Eriobotrya japonica Lindley was examined. Loquat fruit was separated into three parts (peel, flesh and seed), and each part was extracted with either water or ethanol. The extracts were then assessed for their free radical scavenging ability and effects on the oxidation of human low density lipoprotein (LDL) in vitro. Results in this study show that the ethanol extracts of all three loquat parts and the water extract of the peels exhibited a strong ability to scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. Among extracts of different loquat parts, the ethanol extract of loquat seeds was the most potent one. The ethanol extract of the seed was also effective in suppressing the oxidation of linoleic acid which was demonstrated by a slow discoloration of β-carotene/linoleic acid conjugation system. The ethanol extract of loquat seeds as compared to other extracts could also suppress significantly the 2,2′-azobis(4-methoxy-2,4-dimethylvaleronitrile) (MeO-AMVN)-induced LDL oxidation. When the content of total polyphenolic compounds in different loquat parts (peel, flesh and seed) was examined, a significantly higher level of total polyphenols was found in the seed than the peels and flesh. Using reverse-phase HPLC-ESI EM analysis, significant levels of polyphenolic compounds such as chlorogenic acid, cyanidine glucoside, epicatechin, epigalocatechin gallate and procyanidin B2 in the ethanol extract of different loquat parts were identified and quantified. The latter two compounds were found mainly in the ethanol extract of loquat seeds, but not in peels and flesh. Therefore, it is suggested that the high ability to scavenge free radicals and suppress the LDL oxidation exerted by the ethanol extract of loquat seeds was at least in part due to the high content of polyphenolic compounds in the seeds.
Experimental studies have proven that melatonin has many beneficial pleiotropic actions. The aim of this study was to assess melatonin efficacy in patients with metabolic syndrome (MS). The study included 33 healthy volunteers (who were not treated with melatonin) and 30 patients with MS, who did not respond to 3-month lifestyle modification. Patients with MS were treated with melatonin (5 mg/day, 2 hr before bedtime) for 2 months. The following parameters were studied: systolic and diastolic blood pressure (SBP, DBP), levels of glucose, serum lipids, C-reactive protein, fibrinogen, activities of antioxidative enzymes: catalase (CAT), glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), thiobarbituric acid reactive substrates (TBARS). After 2-month therapy in comparison with baseline, the following significant changes were measured: systolic blood pressure (132.8±9.8 versus 120.5±11.0 mmHg, P<0.001), DBP (81.7±8.8 versus 75±7.4 mmHg, P<0.01), low-density lipoprotein cholesterol (LDL-C) (149.7±26.4 versus 139.9±30.2 mg/dL, P<0.05), TBARS (0.5±0.2 versus 0.4±0.1 μm/gHb, P<0.01), and CAT (245.9±46.9 versus 276.8±39.4 U/gHb). Melatonin administered for 2 months significantly improved antioxidative defense (increase in CAT activity, decrease in TBARS level) and lipid profile (decrease in LDL-C), and lowered blood pressure. We conclude that melatonin therapy may be of benefit for patients with MS, particularly with arterial hypertension. Further studies with higher doses of melatonin or prolonged supplementation are awaited.
The potent antioxidant activity of Eriobotrya japonica seed extract (ESE) and its usefulness in the prevention and treatment of various disorders has been reported previously. Its antioxidant activity associated with beta-sitosterol and polyphenols contained in the extract was also validated. In this study, anti-allergic activity of Eriobotrya japonica seed extract was investigated.
The inhibition of histamine release-mediated type 1 allergy by Eriobotrya japonica seed extract was used as an index.
The administration of this extract inhibited histamine release from rat mast cells, suggesting its usefulness in allergic disease treatment. In an experiment using a guinea-pig allergic rhinitis model, this extract reduced the frequency of sneezing and nose-scratching.
These results suggest that Eriobotrya japonica seed extract may contribute to the relief of allergic disease-related symptoms.
The aim of this review was to bring together results obtained from studies on different aspects of HDL as related to CHD and atherosclerosis. As atherosclerosis is a multistep process, the various components of HDL can intervene at different stages, such as induction of monocyte adhesion molecules, prevention of LDL modification and removal of excess cholesterol by reverse cholesterol transport. Transgenic technology has provided a model for atherosclerosis, and permitted evaluation of the contributions of different HDL components towards the global effect. The availability of apo AIV transgenic mice amplified the results obtained from apo AI overexpressors with respect to prevention of atherosclerosis. Prevention of atherosclerosis in apo E deficient mice by relatively small amounts of macrophage derived apo E may open new possibilities for therapeutic intervention. Contrary to early notions, increased plasma levels of CETP, even in the presence of low but functionally normal HDL, were atheroprotective. The extent to which paraoxonase and apo J participate in prevention of human atherosclerosis needs further evaluation. The findings that LCAT overexpression in rabbits was atheroprotective in contrast to increase in atherosclerosis in h LCAT tg mice, which was only partially corrected by CETP expression, call for some caution in the extrapolation of results from transgenic animals to humans. The important discovery of SR-BI as the receptor for selective uptake of CE from HDL revived interest in the clearance of CE from plasma. This pathway supplies also the vital precursor for steroidogenesis in adrenals and gonads and was shown to be dependent on apo AI.
Eriobotrya japonica is considered a medicinal plant, and its leaves (Eriobotrya folia) have been used to treat skin diseases, as well as to relieve inflammation, pain, coughing, and sputa. In our evaluation of the pharmacological efficacy of the seed extracts, constituents of the seeds were found to contain the unsaturated fatty acids linolenic and linoleic acids and the sterol beta-sitosterol in the 70% EtOH and the MeOH extracts. The seed extracts were orally administered to rats with dimethylnitrosamine-induced hepatopathy, and blood L-asparate aminotransferase (AST) and L-alanine aminotransferase (ALT) levels, liver retinoid level, and hydroxyproline level were measured. Liver fibrosis rates calculated after Azan-Mallory staining and evaluation of the liver function-improving effects of extracts were showed that AST, ALT, and hydroxyproline levels and liver fibrosis rates were significantly lower, and retinoid levels were significantly higher in hepatopathic rats treated with 70% EtOH and MeOH extracts of the seed than in water-treated control rats. This suggests that the positive effect on liver function of the extracts varies depending on the extracting solvent used. 70% EtOH and MeOH extract of the seeds inhibited the development of liver fibrosis in hepatopathic rats, thus exhibiting potent improvement. The unsaturated linolenic and linoleic acids and the sterol beta-sitosterol contained in these extracts may also contribute to the improvement of liver function.
There is a large body of evidence demonstrating an inverse correlation between circulating levels of high-density lipoprotein (HDL) cholesterol and cardiovascular disease risk. For every 1-mg/dL increase in HDL, it is estimated that the risk of cardiovascular events decreases by 2% to 3%. HDL is one of many factors that contribute to the regulation of the atherosclerotic process. HDL mediates reverse cholesterol transport and exhibits numerous beneficial properties, including antioxidant, antiinflammatory, and antithrombotic effects on the vasculature. Recent studies have expanded our understanding of the vasoprotective mechanisms of HDL to include enhanced nitric oxide production and improved endothelium-dependent relaxation. Progress has also been made in determining the molecular mechanisms that mediate reverse cholesterol transport. Recently published National Cholesterol Education Program Adult Treatment Panel guidelines have broadened the definition of low levels of HDL and encourage more aggressive screening and treatment of lipid abnormalities. Several therapeutic interventions can augment HDL concentrations, and there is increasing evidence that these interventions improve cardiovascular outcomes. Research focusing on defining the molecular roles of HDL will likely identify potential therapeutic targets for decreasing the incidence and progression of coronary heart disease. This review highlights the role of HDL in coronary heart disease, from basic mechanisms of action to recent clinical trial results.
The effect of Eriobotrya japonica seed extract (ESE) prepared with 70% ethanol on gastric mucosal injury was investigated. Six experimental models with different action mechanisms were used for the evaluation. Three concentrations of ESE were prepared for each model. ESE administration was initiated 14 days before induction of gastric mucosal injury, and its effect was investigated. ESE inhibited formation of gastric mucosal injury.
The hypoglycemic and hypolipidemic effects of flavonoid rich extract obtained from seeds of Eugenia jambolana (EJ) was analyzed in streptozotocin induced diabetic rats. Hypoglycemic activity was assessed by reduction in fasting blood glucose (FBG) and peak blood glucose level within 60 min of glucose tolerance test (GTT) in mild and severe diabetic (MD and SD respectively) rats. Different biochemical parameters like glycogen biosynthesis, glucose homeostatic enzyme (glucose-6-phosphatase, hexokinase) activities demonstrated significant (p<0.05) improvement as compared to diabetic counter parts. Further, the flavonoids also stimulated 16% increase in insulin release in vitro from pancreatic islets. The hypolipidemic action after this extract supplementation was confirmed by significant (p<0.05) decrease in the levels of LDL (27% MD, 29% SD), triglycerides (about 35% MD, 37% SD) and increase in HDL (21% MD, 34% SD) over untreated diabetic rats. The above mentioned action of this plant extract was found to be through dual up regulation of both the peroxisome proliferators-activated receptors (PPARalpha and PPARgamma) up to about 3-4 folds (over control) and their capacity to differentiate 3T3-L1 preadipocytes. The present data suggests that the flavonoid rich extract from EJ plant has both hypoglycemic and hypolipidemic effects which can help the cure and management of diabetes.