In Vivo Comparison of the Bioavailability of (+)-Catechin, (−)-Epicatechin and Their Mixture in Orally Administered Rats

Baba, Seigo; Osakabe, Naomi; Natsume, Mitsutaka; Muto, Yuko; Takizawa, Toshio; Terao, Junji

doi:10.1093/jn/131.11.2885

Cited by 197 publications

(163 citation statements)

References 26 publications

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“…50) Monomers are easily absorbed; in this respect, epicatechin is more efficient than catechin. 51) While only small amounts of procyanidin dimer are absorbed directly by humans, 52,53) it can be digested into the monomer form before being absorbed. 54) As compared with the other dietary procyanidins, such as those from grape, apple, and cocoa, our results show that the procyanidins present in Chinese hawthorn fruits have lower mDP values and are composed mainly of epicatechin.…”

Section: Protease Inhibitory Activitiesmentioning

confidence: 99%

Polyphenolic Content and Physiological Activities of Chinese Hawthorn Extracts

Cui

Nakamura

Tian

et al. 2006

Bioscience, Biotechnology, and Biochemistry

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Hawthorn polyphenol (HP) was prepared by ethyl acetate treatment of the ethanol extract (HE) of Chinese hawthorn fruit. The concentrations of 15 polyphenols in the HP, HE, extraction residue (HJ), and a hawthorn leaf extract (HF) were determined by HPLC. For HP, the total content of the 15 polyphenols was 21.4%, comprised of 19.7% of procyanidins, 1.21% of chlorogenic acid, and 0.48% of flavonoids, compared to 2.55% for the HE. The yields of procyanidin monomer, dimer, trimer, tetramer, and pentamer were 50.5%, 30.3%, 23.0%, 14.6%, and 12.5% respectively, and the mean degree of polymerization was reduced to 1.39 (HP) from 1.65 (HE). Seven different physiological actions of the four extracts were investigated. The HP showed strong O 2 À and OH scavenging capacities (IC 50 values of 6.3 g/ml and 1.1 g/ml respectively), as well as selective prolyl endopeptidase inhibition (IC 50 of 60 g/ml). The active constituents appeared to be procyanidins.Key words: Crataegus pinnatifida; HPLC; procyanidin; antioxidant; free radicalsIn Europe, standardized extracts of the leaves and flowers of Crataegus oxyacantha and Crataegus monogyna are used in the therapy for moderate (NYHA II) congestive heart failure. 1,2) These extracts exert several pharmacological and clinical effects, such as antiischemia/reperfusion-injury, anti-arrhythmic, hypolipidemic, and hypotensive effects. 1,2) Flavonoids and procyanidins are considered to be the two main active constituents. 2) Species of Chinese hawthorn, particularly Crataegus pinnatifida and Crataegus pinnatifida Bge. var. major NE Br., have also been used as herbal medicines. 2,3) Studies indicate that Chinese hawthorn extracts have beneficial effects, such as antioxidant, 4,5) anti-inflammatory, 6) and hypolipidemic effects, 7) as well as protective effects on the brain and vascular endothelium 8,9) and endothelium-dependent relaxation. 10) Recently, we analyzed 37 major cultivars of Chinese hawthorn using high performance liquid chromatography (HPLC), and found that procyanidins, which were present in high concentrations, were the main phenolic active constituents in these fruits. 11) In general, the hawthorn found in China is an edible fruit that is popular for its special acidic taste. It is bigger than its European counterpart. Since the content of organic acid in Chinese hawthorn fruits can be up to 5% (fresh weight), they are used to produce various foods, such as jams, jellies, juices, tinned foods, wines, and various sweet foods. However, the high sugar content of these fruits counteracts the benefits of polyphenols for consumers of advanced age or for those who suffer from hypertension, cardiovascular disease, or diabetes. Hence, it is desirable to separate the polyphenol and sugar components. Previously, hawthorn extract (HE) for medical applications were ethanol-extracted from the dried fruit of the Chinese hawthorn. 12) These crude extracts contain many undesirable substances, such as carbohydrates, organic acids, and moisture, which not only reduce the concentration of acti...

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Section: Protease Inhibitory Activitiesmentioning

confidence: 99%

Polyphenolic Content and Physiological Activities of Chinese Hawthorn Extracts

Cui

Nakamura

Tian

et al. 2006

Bioscience, Biotechnology, and Biochemistry

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Section: Resultsmentioning

confidence: 99%

“…Anthocyanins comprise the -3-galactoside and -3-arabinoside derivatives of cyaniding (Cooper et al, 2007). The cocoa nib was ground after roasting known as the cocoa liquor (Baba et al, 2001).The total flavonoid content of cocoa beans during convection roasting and superheated steam roasting at different temperatures for 10 − 50 min is shown in Fig. 2.…”

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confidence: 99%

Comparison between Superheated Steam and Convectional Roasting on Changes in the Phenolic Compound and Antioxidant Activity of Cocoa Beans

Zzaman

Bhat

Abedin

et al. 2013

FSTR

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Cocoa beans (Theobroma cacao) are rich in phenolic compounds which show antioxidant properties. Roasting is one of the most important unit operations in the cocoa base industries which reduces the antioxidant activity. Cocoa beans were subjected to roast at 150, 200 and 250℃ for 10 − 50 min using conventional and superheated steam methods on changes in the total phenol content (TPC), total flavonoid content (TFC), free radical scavenging activity and antioxidant properties. The total phenols and total flavonoid were significantly (p < 0.05) higher using superheated steam than conventional roasting method. The cocoa beans treated by conventional method showed significantly (p < 0.05) lower the free radical scavenging activity and antioxidant properties than superheated steam roasting method.Keywords: cocoa bean, superheated steam roasting, conventional roasting, phenolic compound, antioxidant properties *To whom correspondence should be addressed. E-mail: taris@usm.my IntroductionThe phenolic compounds present in the food that can prevent or delay lipid oxidation through the inhibiting of oxidizing reactions in our body. It has been reported that food such as fruit, vegetable and seeds contain a significant amount of natural antioxidant components including phenolics (Mandic et al., 2008;Katalinic et al., 2004). Studies reported that there is a negative correlation found between dietary intake phenolics and coronary heart diseases, stroke and cancer (Sun et al., 2002).Cocoa beans are the seed from the fruit Theobroma cacao tree which is the essential ingredient of chocolate and chocolate base products. The cocoa beans are rich in phenolic and other antioxidant properties. Approximately 12 − 18% of phenolic compounds are reported in unfermented cocoa beans (dry weight). Almost 60% of the total phenolic compounds are procyanidin (oligomers), epicatechin and catechin (flavanol monomers) in raw cocoa beans (Dreosti, 2002). The study described that the cocoa beans contain higher amount of flavan-3-ol. The flavan-3-ol (catechin and epicatechin) are the main monomeric compound of polyphenol found in cocoa (Lamuela-Raventós et al., 2005). These compound have the highest bioavailability among cocoa phenolic compound because the absorption is depends on the molecular size. The monomeric compounds are biologically more active than oligomers and polymers and found in high concentration that can interact with the target compound easily especially free radicals (Cooper et al., 2009). These compounds have a potential contestant to inhibit or delay the oxidative damages in our body (Adamson et al., 1999). The studies revealed that these compounds are capability to reduce lipid peroxidation, inhibit peroxyl radicals and scavenge superoxide radicals and hydroxyl radicals (Salah et al., 1995;Vinson and Hontz, 1995;Kanner et al., 1994). Furthermore, the study demonstrated that the antihyperglycaemic effects on streptozotocin induced diabetic rats were found using the extracts prepared from cocoa (Ruzaidi et al., 2005). Antioxidant p...

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“…When piperine and EGCG were orally administered concurrently to rats, piperine enhanced the plasma C max and area under the curve (AUC) values of EGCG by 1.3-fold [24] . Additionally, Baba et al suggested that (+)-C and (-)-epicatechin (another type of catechin) might be competitively absorbed in the gastrointestinal tract when coadministered [25] , and Jiang et al reported that when Pue and gastrodin (one of the main components of Tian-ma in TCM) were concurrently administered, the oral bioavailability of Pue was 10.7-fold higher than that in the Pue-only group [26] . However, no studies regarding the oral absorptive interactions of (+)-C and Pue following concurrent administration to rats have been reported, and the absorption mechanism of these two compounds when co-administered in vitro remains to be elucidated.…”

Section: Introductionmentioning

confidence: 99%

Absorptive interactions of concurrent oral administration of (+)-catechin and puerarin in rats and the underlying mechanisms

Lin

Wang

et al. 2016

Acta Pharmacol Sin

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Aim: (+)-Catechin and puerarin are polyphenol and flavonoid, respectively, in green tea and foodstuffs. They exhibit potent antioxidant activity and are widely used for treating cardiocerebrovascular diseases. The aim of this work was to investigate the potential interactions between (+)-catechin and puerarin following concurrent oral administration in rats, and their absorption mechanisms in Caco-2 cell monolayers. Methods: Pharmacokinetic studies were conducted in male rats received (+)-catechin (140 mg/kg, po) and/or puerarin (200 mg/kg, po). The cell uptake and transport behavior in Caco-2 cell monolayers and the interactions of the two compounds were analyzed. Results: When (+)-catechin and puerarin were administered concurrently, the AUC 0-12 h and C max values of puerarin were 2.48-fold and 3.91-fold, respectively, as large as those of puerarin alone; the AUC 0-12 h and C max values of (+)-catechin were decreased to 57.62% and 77.55%, respectively, compared with those of (+)-catechin alone. In Caco-2 cell monolayers, (+)-catechin (300 and 600 μmol/L) significantly increased the cell uptake and transport of puerarin, whereas puerarin (300 and 600 μmol/L) significantly decreased the cellular uptake and transport of (+)-catechin. Furthermore, both cyclosporine A (P-glycoprotein inhibitor) and MK-571 (MRP-2 inhibitor) significantly increased the cellular uptake and transport of (+)-catechin and puerarin. Conclusion: Concurrent oral administration of (+)-catechin and puerarin significantly increased the absolute oral bioavailability of puerarin, but decreasing that of (+)-catechin. The competitive efflux of (+)-catechin and puerarin by P-glycoprotein and MRP-2 might lead to this interaction during their absorption process in the small intestine.

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In Vivo Comparison of the Bioavailability of (+)-Catechin, (−)-Epicatechin and Their Mixture in Orally Administered Rats

Cited by 197 publications

References 26 publications

Polyphenolic Content and Physiological Activities of Chinese Hawthorn Extracts

Polyphenolic Content and Physiological Activities of Chinese Hawthorn Extracts

Comparison between Superheated Steam and Convectional Roasting on Changes in the Phenolic Compound and Antioxidant Activity of Cocoa Beans

Absorptive interactions of concurrent oral administration of (+)-catechin and puerarin in rats and the underlying mechanisms

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