Dietary polyphenols are thought to be beneficial for human health as antioxidants. Coffee beans contain a common polyphenol, chlorogenic acid. Chlorogenic acid is the ester of caffeic acid and quinic ...acid. Although these polyphenols have received much attention, there is little evidence indicating a relationship between the effect and the rate of absorption. In this study, we focused on the beneficial effects of chlorogenic acid and caffeic acid, a major metabolite of chlorogenic acid. We carried out in vitro and in vivo experiments. In the in vitro study, caffeic acid had stronger antioxidant activity than that of chlorogenic acid. The uptake of chlorogenic acid by Caco-2 cells was much less than that of caffeic acid. The physiological importance of an orally administered compound depends on its availability for intestinal absorption and subsequent interaction with target tissues. We then used an intestinal ischemia–reperfusion model to evaluate antioxidant activities in vivo. We found that both chlorogenic acid and caffeic acid had effects on intestinal ischemia–reperfusion injury. Since caffeic acid has a stronger antioxidant activity than that of chlorogenic acid and chlorogenic acid is hydrolyzed into caffeic acid in the intestine, it is possible that caffeic acid plays a major role in the protective effect of chlorogenic acid against ischemia–reperfusion injury.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
Chlorogenic acid (5-O-caffeoylquinic acid) is a phenolic compound from thehydroxycinnamic acid family. This polyphenol possesses many health-promoting properties, mostof 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 discussthe role of chlorogenic acid as a nutraceutical for the prevention and treatment of metabolicsyndrome and associated disorders, including in vivo studies, clinical trials, and mechanisms ofaction. The second part of the review will be dealing with the role of chlorogenic acid as a foodadditive. Chlorogenic acid has shown antimicrobial activity against a wide range of organisms,including bacteria, yeasts, molds, viruses, and amoebas. These antimicrobial properties can beuseful for the food industry in its constant search for new and natural molecules for thepreservation of food products. In addition, chlorogenic acid has antioxidant activity, particularlyagainst lipid oxidation; protective properties against degradation of other bioactive compoundspresent in food, and prebiotic activity. The combination of these properties makes chlorogenic acidan excellent candidate for the formulation of dietary supplements and functional foods.
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IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
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In the present study, a formulation system consisting of cholesterol and phosphatidyl choline was used to prepare an effective chlorogenic acid-loaded liposome (CAL) with an improved ...oral bioavailability and an increased antioxidant activity. The developed liposomal formulation produced regular, spherical and multilamellar-shaped distribution nanoparticles. The pharmacokinetic analysis of CAL compared with chlorogenic acid (CA), showed a higher value of Cmax(6.42±1.49min versus 3.97±0.39min) and a delayed Tmax(15min versus 10min), with 1.29-fold increase in relative oral bioavailability. The tissue distribution in mice also demonstrated that CAL predominantly accumulated in the liver which indicated hepatic targeting potential of the drug. The increased activities of antioxidant enzymes (Total Superoxide Dismutase (T-SOD) and Glutathione Peroxidase (GSH-Px)) and total antioxidant capacity (T-AOC), in addition to decreased level of malondialdehyde (MDA) in CCl4-induced hepatotoxicity study further revealed that CAL exhibited significant hepatoprotective and antioxidant effects. Collectively, these findings present a liposomal formulation with significantly improved oral bioavailability and an increased in vivo antioxidant activity of CA.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
Phenolics are widespread dietary antioxidants. Among these, chlorogenic acids (CGAs) received considerable attention for their wide distribution and part of human diet with potential biological ...effects. CGAs (71 compounds), being esters of derivatives of cinnamic acids with quinic acid are widely distributed in plant materials. Coffee is among the highest found in plants, ranging from 4 to 14%. Besides, these are reported in plant foods such as apples, pears, carrot, tomato, sweet potato, Phyllostachys edulis, oilseeds, Prunus domestica L, cherries, and eggplant. The traditional Chinese medicinal plants such as flowers and buds of Lonicera japonica Thunb and the leaves of Eucommia ulmodies contained CGAs as bioactive compound. These play an important role in the formation of roasted coffee flavor and have a marked influence on coffee cup quality. CGAs are considered as main precursors of coffee flavor and pigments. Recent technological advancements in the separation and purification of CGAs such as molecular-imprinted polymer technique; microwave-assisted extraction; pH gradient counter current chromatography has also been described. The consumption of coffee correlated to several health benefits such as reducing the risk of human chronic diseases such as inflammation, diabetes, and cardiovascular disease owing to its antioxidant potential.
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BFBNIB, GIS, IJS, KISLJ, NUK, PNG, UL, UM, UPUK
Chlorogenic acids (CGA) are cinnamic acid derivatives with biological effects mostly related to their antioxidant and antiinflammatory activities. Caffeoylquinic acids (CQA) and dicaffeoylquinic ...acids (diCQA) are the main CGA found in nature. Because green coffee is a major source of CGA, it has been used for production of nutraceuticals. However, data on the bioavailability of CGA from green coffee in humans are inexistent. The present study evaluated the pharmacokinetic profile and apparent bioavailability of CGA in plasma and urine of 10 healthy adults for 8 h after the consumption of a decaffeinated green coffee extract containing 170 mg of CGA. Three CQA, 3 diCQA, and caffeic, ferulic, isoferulic, and p-coumaric acids were identified in plasma by HPLC-Diode Array Detector-MS after treatment. Over 30% (33.1 ± 23.1%) of the ingested cinnamic acid moieties were recovered in plasma, including metabolites, with peak levels from 0.5 to 8 h after treatment. CGA and metabolites identified in urine after treatment were 4-CQA, 5-CQA, and sinapic, p-hydroxybenzoic, gallic, vanillic, dihydrocaffeic, caffeic, ferulic, isoferulic, and p-coumaric acids, totaling 5.5 ± 10.6% urinary recovery of the ingested cinnamic and quinic acid moiteties. This study shows that the major CGA compounds present in green coffee are highly absorbed and metabolized in humans.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Ulcerative colitis (UC) is a multifactorial disorder of the large intestine, especially the colon, and has become a challenge globally. Allopathic medicines are primarily available for the treatment ...and prevention of UC. However, their uses are limited due to several side effects. Hence, an alternative therapy is of utmost importance in this regard. Herbal medicines are considered safe and effective for managing human health problems. Chlorogenic acid (CGA), the herbal-derived bioactive, has been reported for pharmacological effects like antiinflammatory, immunomodulatory, antimicrobial, hepatoprotective, antioxidant, anticancer, etc. This review aims to understand the antiinflammatory and chemopreventive potential of CGA against UC. Apart from its excellent therapeutic potential, it has been associated with low absorption and poor oral bioavailability. In this context, colon-specific novel drug delivery systems (NDDS)are pioneering to overcome these problems. The pertinent literature was compiled from a thorough search on various databases such as ScienceDirect, PubMed, Google Scholar, etc., utilizing numerous keywords, including ulcerative colitis, herbal drugs, CGA, pharmacological activities, mechanism of actions, nanoformulations, clinical updates, and many others. Relevant publications accessed till now were chosen, whereas non-relevant papers, unpublished data, and non-original articles were excluded. The present review comprises recent studies on pharmacological activities and novel drug delivery systems of CGA for managing UC. In addition, the clinical trials of CGA against UC have been discussed.
Chlorogenic acids (CGAs) have gained considerable attention as pervasive human dietary constituents with potential cardiovascular-preserving effects. The main sources include coffee, yerba mate,
...leaves, and Lonicerae Japonicae Flos. CGA consumption can reduce the risks of hypertension, atherosclerosis, heart failure, myocardial infarction, and other factors associated with cardiovascular risk, such as obesity and type 2 diabetes. This review recapitulates recent advances of CGAs in the cardiovascular-preserving effects, pharmacokinetics, sources, and safety. Emerging evidence indicates that CGAs exhibit circulatory guarding properties through the suppression of oxidative stress, leukocyte infiltration, platelet aggregation, platelet-leukocyte interactions, vascular remodeling, and apoptosis as well as the regulation of glucose and lipid metabolism and vasodilatory action in the cardiovascular system. CGAs exert these effects by acting on complex signaling networks, but the global mechanisms are still not clear. The oral bioavailability of CGA is poor, and there is a potential sensitization concern about CGA. The bioactive metabolites, systematic toxicity, and optimized structure are needed for further identification.
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IJS, KILJ, NUK, PNG, UL, UM, UPUK
Abstract Chlorogenic acids (CQAs), a large family of naturally occurring esters of quinic acid with one, two or even three cinnamic acids moieties and/or moieties of cinnamic acids derivatives, ...supplied to human organisms mainly with coffee, tea, fruit and vegetables, have been among the most frequently studied polyphenols. Of these, caffeic acid esters predominate, and 5-O-caffeoylquinic acid (5-CQA) is their main and most widespread representative. Recently performed studies have shown that after removing water from the aqueous solution of 5-CQA, its dry residue contains two hydrates of this compound, each consisting of two 5-CQA molecules and two molecules of H 2 O (2 × 5-CQA*2xH 2 O). The results presented in the paper not only define the characteristic features of 5-CQA but, more importantly, offer solid evidence that 5-CQA hydrates begin to form already in the aqueous solution of 5-CQA immediately after the dissolution of this compound and that the analogous process can occur in food products containing 5-CQA during their storage. Moreover, the performed experiments indicate the validity of the hypothesis that 5-CQA hydrates are formed by active collisions of 5-CQA molecules with monomeric/dimeric water molecules existing in trace amount in strongly associated aqueous systems. The presence of 5-CQA hydrates in liquid food products may have a significant impact on the assessment of some of their physicochemical properties as well as their biochemical activity.
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EMUNI, FIS, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, MFDPS, NLZOH, NUK, OBVAL, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, SBNM, UKNU, UL, UM, UPUK, VKSCE, ZAGLJ
The purpose of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of Chlorogenic acid (CA), an important bioactive compound from ...Lonicerae Japonicae Flos with poor permeability. SMEDDS was prepared and characterized by self-emulsifying rate, morphological observation, droplet size determination, stability, in vitro release, in vivo bioavailability and tissue distribution experiments. Results shown that the SMEDDS of CA has a high self-emulsifying rate (>98%) in the dissolution media, and its microemulsion exhibits small droplet size (16.37nm) and good stability. In vitro release test showed a complete release of CA from SMEDDS in 480min. After oral administration in mice, significantly enhanced bioavailability of CA was achieved through SMEDDS (249.4% relative to the CA suspension). Interestingly, SMEDDS significantly changed the tissue distribution of CA and showed a better targeting property to the kidney (2.79 of the relative intake efficiency). It is suggested that SMEDDS improves the oral bioavailability of CA may mainly through increasing its absorption and slowing the metabolism of absorbed CA via changing its distribution from the liver to the kidney. In conclusion, it is indicated that SMEDDS is a promising carrier for the oral delivery of CA.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK, ZRSKP
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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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK, ZRSKP
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