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Abstract

Phenolic acids have recently gained substantial attention due to their various practical, biological and pharmacological effects. Chlorogenic Acid (CGA, 3-CQA) is a most abundant isomer among caffeoylquinic acid isomers (3-, 4-, and 5-CQA), that currently known as 5-CQA as per guidelines of IUPAC. It is one of the most available acids among phenolic acid compounds which can be naturally found in green coffee extracts and tea. CGA is an important and biologically active dietary polyphenol, playing several important and therapeutic roles such as antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension, free radicals scavenger and a central nervous system (CNS) stimulator. In addition, it has been found that CGA could modulate lipid metabolism and glucose in both genetically and healthy metabolic related disorders. It is speculated that CGA can perform crucial roles in lipid and glucose metabolism regulation and thus help to treat many disorders such as hepatic steatosis, cardiovascular disease, diabetes, and obesity as well. Furthermore, this phenolic acid (CGA) causes hepatoprotective effects by protecting animals from chemical or lipopolysaccharide-induced injuries. The hypocholesterolemic influence of CGA can result from the altered metabolism of nutrients, including amino acids, glucose and fatty acids (FA). The purpose of this review was to broaden the scope of knowledge of researchers to conduct more studies on this subject to both unveil and optimize its biological and pharmacological effects. As a result, CGA may be practically used as a natural safeguard food additive to replace the synthetic antibiotics and thereby reduce the medicinal cost.
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... CGAs have different subgroups that include caffeoylquinic, p-coumaroylquinic, and feruloyquinic acids [12]. Caffeoylquinic acids (CQAs), esters of caffeic acid and quinic acid, are among the important polyphenols found in plant families Asteraceae and Lamiaceae [13], and are ones of the main components of coffee [14]. 3-caffeoylquinic acid (3-CQA or neochlorogenic acid) are present in several plants, such as Coffea spp., tomato, artichoke, potato, apples, and fresh stone fruits (peaches and plums) [13,14]. ...
... Caffeoylquinic acids (CQAs), esters of caffeic acid and quinic acid, are among the important polyphenols found in plant families Asteraceae and Lamiaceae [13], and are ones of the main components of coffee [14]. 3-caffeoylquinic acid (3-CQA or neochlorogenic acid) are present in several plants, such as Coffea spp., tomato, artichoke, potato, apples, and fresh stone fruits (peaches and plums) [13,14]. 5-CQA, also called chlorogenic acid, is the most abundant isomer among CQA derivatives (3-, 4-, and 5-CQA) with many beneficial effects on human health [13,15]. ...
... 3-caffeoylquinic acid (3-CQA or neochlorogenic acid) are present in several plants, such as Coffea spp., tomato, artichoke, potato, apples, and fresh stone fruits (peaches and plums) [13,14]. 5-CQA, also called chlorogenic acid, is the most abundant isomer among CQA derivatives (3-, 4-, and 5-CQA) with many beneficial effects on human health [13,15]. CQAs possess a wide range of pharmacological activities, including antioxidant, antibacterial, antiviral, anti-Alzheimer, and neuroprotective activities [15]. ...
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This study investigated the effects and the mechanism of actions of neochlorogenic acid (3-caffeoylquinic acid; 3-CQA) on glucose and lipid metabolism in rats fed a high fat-high fructose diet (HFFD). Male rats were fed HFFD (40 % lard and 20 % fructose) for 16 weeks. At the 10th week, the HFFD rats were split into 3 groups: HFFD receiving distilled water (HFFD control group), HFFD receiving 3-CQA 50 mg/kg and HFFD receiving metformin 200 mg/kg once daily for a further 6 weeks. At the end of treatment, fasting blood glucose (FBG), oral glucose-tolerance test (OGTT), lipid profile, insulin, leptin, adiponectin, markers of oxidative stress, and hepatic triglyceride content were measured. Liver, adipose tissue, and skeletal muscle were collected for histological, gene and protein examinations. Compared to the HFFD control group, the 3-CQA group exhibited significantly reduced FBG, insulin and leptin levels, and improved OGTT. Serum adiponectin increased and lipid profiles were normalized. Hepatic triglyceride was reduced with a decrease in lipid droplets in liver histological sections. Levels of serum SOD and CAT activity, and MDA were reversed by 3-CQA treatment. Moreover, 3-CQA significantly reduced the expression of adipocyte pro-inflammatory cytokine genes (MCP-1, TNF-α, and IL-6), hepatic lipogenic genes (SREBP1c, FAS, and GPAT), and hepatic gluconeogenic genes (PEPCK and G6Pase). Additionally, 3-CQA increased expression of muscle GLUT4 gene, and of GLUT4 protein with increased p-AKT and p-AMPK in skeletal muscle. In conclusion, 3-CQA improves glucose and lipid metabolism plausibly by decreasing oxidative stress and inflammation-induced insulin resistance, downregulating the expression of lipogenic and gluconeogenic genes, and enhancing insulin signaling in HFFD-induced insulin-resistant rats. HIGHLIGHTS Neochlorogenic acid (3-CQA) improves glucose and lipid metabolism by decreasing insulin resistance Neochlorogenic acid (3-CQA) deceases insulin resistance due to its activities in ameliorating obesity, oxidative stress, and adipose tissue inflammation The beneficial effects of Neochlorogenic acid (3-CQA) to improve glucose and lipid homeostasis may be mediated via suppression of hepatic glucose production and lipogenesis, and activation of muscle glucose uptake and AKT and AMPK pathways GRAPHICAL ABSTRACT
... The amount of sinapoylquinic acid in the flower buds was 1.05-fold, 21.75fold and 5.61-fold higher than that in flowers, leaves and stems, respectively. Caffeoylquinic acid and its derivatives are the main active ingredients of LJT, which have many therapeutic effects, such as antioxidant activity, antibacterial, liver protection, heart protection, anti-inflammatory, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension [38]. The amount of phenolic acid-glucosides was higher in the flower buds than in other tissues such as caffeoylquinic acid-glucoside, feruloylquinic acid-glucoside, di-caffeoylquinic acid-glucoside. ...
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Lonicera japonica Thunb. (LJT) has been widely used as medicines or food additives in Asian countries for thousands of years. The flower buds are often medicinally used, and the other tissues are ignored. However, flowers, leaves and stems have also been reported to have antimicrobial, anti-inflammatory and antioxidant effects. In the current study, un-targeted metabolomics analysis was performed to investigate the metabolic difference among different tissues (flowers, flower buds, stems and leaves) of LJT based on liquid chromatography with mass spectrometry. A total of 171 metabolites were identified, including 28 flavonoids, 35 phenolic acids, 43 iridoids, 9 amino acids, 6 nucleotides, 16 fatty acids, 22 lipids and 12 others. Four new secondary metabolites were discovered. Some flavonoids and iridoids were not detected in leaves and stems. Principal component analysis showed significant differences among four different tissues. Some 27, 81, 113 differential metabolites were found between flowers/flower buds, leaves/flower buds, stems/flower buds, respectively. Primary metabolites showed a higher content in the flowers and flower buds. For the flavonoids, flavones were mainly accumulated in the leaves, flavonols were mainly accumulated in the flower buds, and acylated flavonol glucosides were mainly accumulated in the flowers. Most phenolic acids showed a higher content in the flowers or flower buds, while phenolic acid-glucosides showed significantly higher content in the flower buds. The most abundant iridoids in the LJT also showed a higher content in the flowers and flower buds. These results can provide new insights into the understanding of the metabolites changes in different tissues, and lay a theoretical foundation for the comprehensive utilization of LJT.
... The GC-MS is composed of two major building blocks; the gas chromatograph and the mass spectrometer. The gas chromatograph utilizes a capillary column whose properties regarding molecule separation depends on the column's dimension (length, diameter, and film thickness) as well as the phase properties (e.g. 5% phenyl polysiloxane) [7]. The difference in the chemical properties between different molecules in a mixture and their relative affinity for the stationary phase of the column will promote separation of the molecules as the sample travels the length of the column. ...
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The use of herbal medicine has achieved global success as an ethno-medicine, yet there are lots of drawbacks in their commercial value and wide acceptance due to poor regulation and standardization. Present study aims to chemo-metrically characterize the phyto-chemical principles present in the n-hexane seed extracts of Xylopia aethiopica using chromatographic and spectroscopic methods. The crude n-hexane extracts were analyzed using Fourier Transform Infrared Spectroscopy (FTIR) model 8400S and GC-MS (Model-QP 2010 plus Spec). The identification of compounds was done using NIST ver.2.0-year 2005 Library. The biological activity are based on Dr. Duke's phytochemical and ethno-botanical databases. The FTIR revealed functional groups such as alkenes, alkanes, alcohols, aromatic rings as well as fatty acids. The GC-MS revealed phyto-compounds such as alpha-Terpineol, alpha-cubabene, pinocarvone, copaene and alpha-muurolene. The presence of these vital phytochemicals with excellent pharmacological activity may explain their usage in traditional medicine.
... 41 It has been discerned that hydroxyl groups (OH) on phenolic acids act as positive moieties for their antioxidant properties which is associated with the number of hydroxyl groups as follows: Tri-hydroxy phenolic acids > di-hydroxy (catechol) > monohydroxy. 15,42 These morphological, hormonal and biochemical findings showed developmental ability and functional potential of CGA in PCOS. ...
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Polycystic ovarian syndrome (PCOS) is a complex endocrine and metabolic disorder. Chlorogenic acid (CGA) bears antioxidant properties with protective effects on different tissues. This study was conducted to evaluate the effect of CGA on follicular development, hormonal status and biomarkers of oxidative stress in a rat model of PCOS. In this experimental study, 18 rats were divided into three equal groups including: control, non-treated PCOS [(estradiol valerate (EV): 40.00 mg kg-1 intramuscularly)], and PCOS-CGA (EV: 40.00 mg kg-1 intramuscularly and CGA: 100 mg kg-1 intraperitoneally once a week for eight consecutive weeks). At the end of treatment period, all rats were anesthetized. Then 5.00 mL blood samples of rats in the three groups were taken and prepared for hormonal analyses and their ovaries were isolated and dissected mechanically free of fat and mesentery. The ovaries underwent the following analyses: Morphological study with Hematoxylin and Eosin staining and biochemical study using the malondialdehyde (MDA) level and total antioxidant activity. Data were analyzed using one-way ANOVA and post hoc Tukey's test. The serum level of luteinizing hormone, estrogen, testosterone, antioxidant capacity, glutathione and the number of cystic follicles in the PCOS group treated with 100 mg kg-1 Chlorogenic acid compared to the non-treated PCOS group were significantly decreased, however, the serum level of follicle stimulating hormone, progesterone, MDA and the number of secondary, graafian follicles and corpus luteum were significantly increased. Chlorogenic acid could be effective in ameliorating follicular development as well as hormonal and biochemical disorders in rats with PCOS.
... These phenolic acids were found in extracts of both A. eupatoria and O. vulgare, but the highest amounts were found in the extracts of O. vulgare roots, where the highest inhibition of PA-Lux growth was determined ( Figure 5, Table 2). Chlorogenic acid is present in many plant families such as Lamiaceae, Asteraceae, Solanaceae, Rosaceae and others, and is responsible for antioxidant, anti-inflammatory, anti-diabetic and antimicrobial effects [36]. Extracts from shoots of some conifers containing chlorogenic and caffeic acids showed significant antimicrobial activity [37]. ...
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Pseudomonas aeruginosa is one of the most antibiotic multi-resistant bacteria, causing chronic pulmonary disease and leading to respiratory failure and even mortality. Thus, there has been an ever-increasing search for novel and preferably natural antimicrobial compounds. Agrimonia eupatoria L. and Origanum vulgare L. shoots are commonly used as teas or alcoholic tinctures for their human health-promoting and antibacterial properties. Here, we explored the antimicrobial effects of all plant parts, i.e., leaf, flower, stem, and root extracts, prepared in water or in 60% ethanol, against P. aeruginosa. The impact of these extracts on bacterial survival was determined using a luminescent strain of P. aeruginosa, which emits light when alive. In addition, the antimicrobial effects were compared with the antioxidant properties and content of phenolic compounds of plant extracts. Ethanolic extracts of O. vulgare roots and flowers showed the highest antimicrobial activity, followed by A. eupatoria roots. In particular, chlorogenic acid, the ethanolic extract of O. vulgare roots contained high levels of protocatechuic acid, hesperidin, shikimic acid, rutin, quercetin, and morin. The synergistic effects of these phenolic compounds and flavonoids may play a key role in the antibacterial activity of teas and tinctures.
... Chlorogenic acid is the most abundant among the caffeoyl quinic acid isomers in nature [60]. It is widely recognized to have antioxidant activities and a wide range of differing biological effects; it has been proven to be an efficient defense molecule against a broad range of insect herbivores in different plant species. ...
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Mediterranean pasture and forage legumes are important components of sustainable production systems. Subterranean clover and sulla represent key species having proven high agro-nomic value and traits for production and multiple services. Our research investigated the potential of the abovementioned species as a source of phenolic compounds and antioxidants for contributing to support their full exploitation in the fodder, animal welfare, and nutraceutical sectors. Antioxi-dant capacity, as well as the content of total phenolic compounds and individual phenolic compounds , was determined in subterranean clover and sulla shoots at the vegetative, flower bud, flowering , and seed ripening phenological stages. The antioxidant capacity and the phenolic content were affected significantly by harvest time. In subterranean clover, 10 individual phenolic compounds were detected, and isoflavones were the most abundant (3.19-18.27 mg·g −1 DM). Eleven phenolic compounds were identified in sulla shoots, and chlorogenic acid (0.76-3.43 mg·g −1 DM) and diosmin (3.64-4.94 mg·g −1 DM) were the most represented compounds at the vegetative and flower bud stage. On the basis of our findings, a complementary utilization of both legume species is suggested; this might ensure the exploitation of all phenolic compounds in view of the potential benefits for animal production and health.
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The aim of this study was to determine the possible therapeutic effect of chlorogenic acid (CGA) on cisplatin (CDDP)-induced ovarian damage in rats. Rats were first exposed to CDDP (5 mg/kg) and then treated CGA (1.5 and 3 mg/kg) for three days. Oxidative stress (OS), inflammation and apoptosis markers were determined using spectrophotometric methods. Ovarian tissues were also evaluated histologically. The levels of OS, inflammation and apoptosis biomarkers increased by CDDP administration (p < 0.05). Treatments with CGA significantly alleviated these markers dose-dependently (p < 0.05). These data reveal that CGA may exert an ovoprotective effect by reducing pro-inflammatory mediators and enhancing antioxidant status in ovarian tissue.
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Introduction: Coffee silver skin (CSS) is a thin covering over green coffee seeds inside coffee cherry. It is a good source of bioactive compounds like chlorogenic acid and caffeine. It is produced as a by-product of the roasting process. Objective: The goal of this study is to apply spray drying method to encapsulate 5-O-caffeoylquinic acid (chlorogenic acid) and caffeine extracted from CSS. Methods: The main-plots for optimisation were feed solid concentration (2.5, 5, 10°Bx), and the sub-plots of the whole-plot were carrier material type (maltodextrin, modified starch, arabic gum) and inlet air temperature (130, 160, 190°C). Responses included were drying yield, chlorogenic acid concentration, caffeine content, Carr index, and solubility values. Results: Suitable conditions were spray drying inlet temperature of 190°C, extract concentration of 10°Bx, and wall material composition [modified starch/arabic gum (MS:AG)] 10.5:9.5. As the feeding CSS extract concentration increased, the amount of chlorogenic acid and caffeine in the final powder increased, while the powder's flow characteristics improved. Conclusions: The concentration stage might be used to produce free-flowing powdered particles with good bioactive retention for use in the food processing industry.
Thesis
Polyphenols are known for their antioxidant properties and as modulators of redox signalling pathways, which have a positive effect on human health. Given their superiority in terms of presence in systemic circulation and their often higher bioactivity than parent polyphenols, there is now more interest in the gut microbiota`s pivotal role in the production of low molecular weight metabolites. Thus, we have focused our study on 5-O-caffeoylquinic acid (5-CQA), a dietary polyphenol, subjected to a resting cell biotransformation study using Lactobacillus reuteri, Bacteroides fragilis and Bifidobacterium longum. Our study highlighted the ability of only L. reuteri to bioconverse 5-CQA into several metabolites, including a known natural compound esculetin. This biotransformation capacity was also evaluated in co-culture. This study put in the spotlight, for the first time, an interesting oxidative pathway carried out by gut bacteria. Electrochemical and enzymatic studies led to identify, after LC-MS/MS analysis, the oxidized compounds of 5-CQA and caffeic acid. In addition, esculetin has shown a beneficial effect on the integrity of the epithelial barrier using an original in vitro quadruple intestinal model.
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Chlorogenic acid (CGA), an important biologically active dietary polyphenol, is produced by certain plant species and is a major component of coffee. Reduction in the risk of a variety of diseases following CGA consumption has been mentioned in recent basic and clinical research studies. This systematic review discusses in vivo animal and human studies of the physiological and biochemical effects of chlorogenic acids (CGAs) on biomarkers of chronic disease. We searched PubMed, Embase, Amed and Scopus using the following search terms: ("chlorogenic acid" OR "green coffee bean extract") AND (human OR animal) (last performed on April 1st, 2015) for relevant literature on the in vivo effects of CGAs in animal and human models, including clinical trials on cardiovascular, metabolic, cancerogenic, neurological and other functions. After exclusion of editorials and letters, uncontrolled observations, duplicate and not relevant publications the remaining 94 studies have been reviewed. The biological properties of CGA in addition to its antioxidant and anti-inflammatory effects have recently been reported. It is postulated that CGA is able to exert pivotal roles on glucose and lipid metabolism regulation and on the related disorders, e.g. diabetes, cardiovascular disease (CVD), obesity, cancer, and hepatic steatosis. The wide range of potential health benefits of CGA, including its anti-diabetic, anti-carcinogenic, anti-inflammatory and anti-obesity impacts, may provide a non-pharmacological and non-invasive approach for treatment or prevention of some chronic diseases. In this study, the effects of CGAs on different aspects of health by reviewing the related literatures have been discussed.
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Chlorogenic acid (5-O-caffeoylquinic acid) is a phenolic compound fromthe hydroxycinnamic acid family. This polyphenol possesses many health-promoting properties, most of them related to the treatment of metabolic syndrome, including anti-oxidant, anti-inflammatory, antilipidemic, antidiabetic, and antihypertensive activities. The first part of this review will discuss the role of chlorogenic acid as a nutraceutical for the prevention and treatment of metabolic syndrome and associated disorders, including in vivo studies, clinical trials, and mechanisms of action. The second part of the review will be dealing with the role of chlorogenic acid as a food additive. Chlorogenic acid has shown antimicrobial activity against a wide range of organisms, including bacteria, yeasts, molds, viruses, and amoebas. These antimicrobial properties can be useful for the food industry in its constant search for new and natural molecules for the preservation of food products. In addition, chlorogenic acid has antioxidant activity, particularly against lipid oxidation; protective properties against degradation of other bioactive compounds present in food, and prebiotic activity. The combination of these properties makes chlorogenic acid an excellent candidate for the formulation of dietary supplements and functional foods.
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Chlorogenic acid (CHA) and caffeic acid (CA) are phenolic compounds found in coffee, which inhibit oxidative stress-induced interleukin (IL)-8 production in intestinal epithelial cells, thereby suppressing serious cellular injury and inflammatory intestinal diseases. Therefore, we investigated the anti-inflammatory mechanism of CHA and CA, both of which inhibited hydrogen peroxide (H2O2)-induced IL-8 transcriptional activity. They also significantly suppressed nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) transcriptional activity, nuclear translocation of the p65 subunit, and phosphorylation of IκB kinase (IKK). Additionally, upstream of IKK, protein kinase D (PKD) was also suppressed. Finally, we found that they scavenged H2O2-induced reactive oxygen species (ROS) and the functional moiety responsible for the anti-inflammatory effects of CHA and CA was the catechol group. Therefore, we conclude that the presence of catechol groups in CHA and CA allows scavenging of intracellular ROS, thereby inhibiting H2O2-induced IL-8 production via suppression of PKD-NF-κB signaling in human intestinal epithelial cells.
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Flavonoids, a group of natural substances with variable phenolic structures, are found in fruits, vegetables, grains, bark, roots, stems, flowers, tea and wine. These natural products are well known for their beneficial effects on health and efforts are being made to isolate the ingredients so called flavonoids. Flavonoids are now considered as an indispensable component in a variety of nutraceutical, pharmaceutical, medicinal and cosmetic applications. This is attributed to their anti-oxidative, anti-inflammatory, anti-mutagenic and anti-carcinogenic properties coupled with their capacity to modulate key cellular enzyme function. Research on flavonoids received an added impulse with the discovery of the low cardiovascular mortality rate and also prevention of CHD. Information on the working mechanisms of flavonoids is still not understood properly. However, it has widely been known for centuries that derivatives of plant origin possess a broad spectrum of biological activity. Current trends of research and development activities on flavonoids relate to isolation, identification, characterisation and functions of flavonoids and finally their applications on health benefits. Molecular docking and knowledge of bioinformatics are also being used to predict potential applications and manufacturing by industry. In the present review, attempts have been made to discuss the current trends of research and development on flavonoids, working mechanisms of flavonoids, flavonoid functions and applications, prediction of flavonoids as potential drugs in preventing chronic diseases and future research directions.
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Helichrysum stoechas (L.) Moench is one of the scientific names of everlasting flower, which has traditionally been used as an ornamental, medicinal and food plant. The aim of this study was to identify the main phytochemical constituents as well as to evaluate the potential of this plant in terms of antioxidant, antidiabetic and neuroprotective activities. The phytochemical analysis of the methanolic extract allowed for the identification of ten constituents mainly of phenolic nature and with chemosystematic relevance: two heterodimeric phloroglucinols, arzanol (1) and compound (3), one homodimeric α-pyrone, helipyrone (2), three phenolic acids, p-hydroxybenzoic (4), caffeic (5) and neochlorogenic (6) acids, one polymethoxylated and two glycosidic flavonoids, 5,7-dihydroxy-3,6,8-trimethoxyflavone (7), isoquercitrin (8) and quercetagetin-7-O-glucopyranoside (9) together with santinol B (10). Bioassays showed significant antioxidant and antiproliferative effects and for the first time the potential of Helichrysum stoechas to inhibit the MAO-A, AChE and TYR enzymes, as well as to exert anti-α-glucosidase and anti-dipeptidyl peptidase-4 activities.
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Background: Inula viscosa L. (Asteraceae) is a medicinal plant widely used as a folk medicine in oriental Morocco, to treat hypertension. The antihypertensive effect of the methanolic extract obtained from I. viscosa leaves was evaluated in hypertensive L-NAME rats. Systolic blood pressure (SBP) was measured using a non-invasive indirect tail-cuff plethysmographic method. Four groups of rats were used: a control group; a hypertensive group treated with L-NAME (32mg/kg/day); a positive control group treated with L-NAME plus enalapril (15mg/kg/day) as a reference antihypertensive agent; and a group treated with L-NAME plus MeOH-extract (40mg/kg/day). Methods: Treatment with L-NAME alone caused a progressive increase in SBP. After 4 weeks, the value of SBP reached 160±2mmHg which shows the installation of hypertension. Enalapril prevented the increase in SBP, which remained normal at 123±1mmHg after 4 weeks of treatment. The administration of MeOH-extract along with L-NAME prevented the increase in SBP as well, which remained constant at 115±1mmHg after 4 weeks of treatment. In ex-vivo models, MeOH-extract produced a relaxation of pre-contracted ring aorta (54 ± 2% of relaxation at 3g/L). But, when the rings were denuded, MeOH-extract failed to relax pre-contracted rings of aorta. Phytochemical study of I. viscosa MeOH-extract revealed the presence of phenolic compounds, such as cynarin and chlorogenic acid. Results: The present results suggest that I. viscosa MeOH-extract has an antihypertensive, predominantly mediated by an endothelium-dependent vasodilatory effect. Cynarin and chlorogenic acid, which have a strong vasorelaxant effect may be involved in the antihypertensive effect of the plant extract. The bioinformatic POM analysis confirms the therapeutic potential of cynarin and chlorogenic acids as inhibitors of various biotargets. Based on the results, the coordination of these phytochemicals with calcium and transition metals should be studied, for better scope at antihypertensive drug development.
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Chlorogenic acid (CGA), one of the most abundant dietary polyphenolic compounds, has been reported to exhibit anti-inflammatory ability. However, the hepatoprotective effects and molecular mechanisms of CGA on concanavalin A (Con A)-induced hepatitis have not been explored. In the present study, we found that pretreatment with CGA dose-dependently inhibited the elevation of plasma aminotransferases and alleviated hepatic pathological damage as well as hepatocyte apoptosis in Con A-exposed mice. Additionally, CGA markedly suppressed the production of serum tumor necrosis factor (TNF)-α and interferon (IFN)-γ, alleviated the infiltration of hepatic macrophages, neutrophils, and activated CD4(+) T lymphocytes in Con A-primed mice. Moreover, CGA downregulated Con A-induced hepatic expression of adhesion molecules (ICAM-1, VCAM-1 and ELAM-1) mRNA and protein, and inhibited Con A-activated Toll-like receptor (TLR) 4 signal molecules including TLR4, p-IRAK1, p-IκB, and p-p38. Finally, our results also showed that CGA exhibited a therapeutic effect, which CGA posttreatment improved hepatic damage at 1, 3, and 6h after Con A. Taken together, these data suggested that CGA could effectively prevent mice from Con A-induced hepatitis, which might be through suppressing the activation of TLR4 signaling, downregulating the expression of adhesion molecules, and alleviating the infiltration and activation of hepatic leukocytes and the production of pro-inflammatory cytokines.
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Stachys palustris, well-known as marsh woundwort, is a perennial herb growing in wet environments of Europe. Its tubers, leaves and seeds are eaten raw or cooked. Alike other Stachys species, the plant is also used as a traditional remedy. Despite S. palustris has been consumed for centuries, little is known about its chemical constituents. In this work the main secondary metabolites of S. palustris from Hungary and France have been analysed. From the plant ethanolic extracts, ethanoid glucosides, isoscutellarein derivatives, caffeoyl-quinic acids and iridoids have been isolated and structurally characterized by NMR. The essential oils were analysed by GC-MS and showed (E)-phytol, fatty acids and carbonylic compounds as the most abundant compounds. The radical scavenger capacity of plant ethanolic extracts, as evaluated by the DPPH assay, was noteworthy, with IC50 values of 92.08-105.42 μg/ml. This article is protected by copyright. All rights reserved.