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Resveratrol as a Bioenhancer to Improve Anti-Inflammatory Activities of Apigenin.

Lee JA, Ha SK, Cho E, Choi I - Nutrients (2015)

Bottom Line: Co-administration of apigenin (50 mg/kg) and resveratrol (25 mg/kg) also showed a significant reduction of carrageenan-induced paw edema in mice (61.20% to 23.81%).Co-administration of apigenin and resveratrol led to a 2.39 fold increase in plasma apigenin levels compared to administration of apigenin alone, suggesting that co-administration of resveratrol could increase bioavailability of apigenin.These results suggested that resveratrol helps apigenin to bypass hepatic metabolism and maintain apigenin's anti-inflammatory activities in the body.

View Article: PubMed Central - PubMed

Affiliation: Research Group of Nutraceuticals for Metabolic Syndrome, Korea Food Research Institute, 1201-62, Anyangpangyoro, Seongnam, Gyeonggi 463-746, Korea. 07636@kfri.re.kr.

ABSTRACT
The aim of this study was to improve the anti-inflammatory activities of apigenin through co-treatment with resveratrol as a bioenhancer of apigenin. RAW 264.7 cells pretreated with hepatic metabolites formed by the co-metabolism of apigenin and resveratrol (ARMs) in HepG2 cells were stimulated with lipopolysaccharide (LPS). ARMs prominently inhibited (p < 0.05) the production of nitric oxide (NO), prostaglandin E₂ (PGE₂), interleukin (IL)-1β, IL-6 and TNF-α. Otherwise no such activity was observed by hepatic metabolites of apigenin alone (AMs). ARMs also effectively suppressed protein expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Co-administration of apigenin (50 mg/kg) and resveratrol (25 mg/kg) also showed a significant reduction of carrageenan-induced paw edema in mice (61.20% to 23.81%). Co-administration of apigenin and resveratrol led to a 2.39 fold increase in plasma apigenin levels compared to administration of apigenin alone, suggesting that co-administration of resveratrol could increase bioavailability of apigenin. When the action of resveratrol on the main apigenin metabolizing enzymes, UDP-glucuronosyltransferases (UGTs), was investigated, resveratrol mainly inhibited the formation of apigenin glucuronides by UGT1A9 in a non-competitive manner with a Ki value of 7.782 μM. These results suggested that resveratrol helps apigenin to bypass hepatic metabolism and maintain apigenin's anti-inflammatory activities in the body.

No MeSH data available.


Related in: MedlinePlus

Structures of apigenin (A) and resveratrol (B).
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nutrients-07-05485-f001: Structures of apigenin (A) and resveratrol (B).

Mentions: Apigenin (for chemical structure see Figure 1), a common bioactive flavonoid, is found in high amounts in several herbs including parsley, thyme, and peppermint. It has been reported as an important dietary flavonoid with strong anti-inflammatory activities [1]. It is extensively metabolized and mainly eliminated in humans by first-pass metabolism via glucuronidation and sulfation [2,3]. Rapid metabolism results in large amount of conjugates in the systemic circulation and cause low bioavailability [4]. Bioavailability is the rate and extent to which a therapeutically active substance enters systemic circulation and becomes available at the required site of action. Therefore, enhancement of bioavailability would be of utmost importance in order to exert health effects of flavonoids in a body.


Resveratrol as a Bioenhancer to Improve Anti-Inflammatory Activities of Apigenin.

Lee JA, Ha SK, Cho E, Choi I - Nutrients (2015)

Structures of apigenin (A) and resveratrol (B).
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4663613&req=5

nutrients-07-05485-f001: Structures of apigenin (A) and resveratrol (B).
Mentions: Apigenin (for chemical structure see Figure 1), a common bioactive flavonoid, is found in high amounts in several herbs including parsley, thyme, and peppermint. It has been reported as an important dietary flavonoid with strong anti-inflammatory activities [1]. It is extensively metabolized and mainly eliminated in humans by first-pass metabolism via glucuronidation and sulfation [2,3]. Rapid metabolism results in large amount of conjugates in the systemic circulation and cause low bioavailability [4]. Bioavailability is the rate and extent to which a therapeutically active substance enters systemic circulation and becomes available at the required site of action. Therefore, enhancement of bioavailability would be of utmost importance in order to exert health effects of flavonoids in a body.

Bottom Line: Co-administration of apigenin (50 mg/kg) and resveratrol (25 mg/kg) also showed a significant reduction of carrageenan-induced paw edema in mice (61.20% to 23.81%).Co-administration of apigenin and resveratrol led to a 2.39 fold increase in plasma apigenin levels compared to administration of apigenin alone, suggesting that co-administration of resveratrol could increase bioavailability of apigenin.These results suggested that resveratrol helps apigenin to bypass hepatic metabolism and maintain apigenin's anti-inflammatory activities in the body.

View Article: PubMed Central - PubMed

Affiliation: Research Group of Nutraceuticals for Metabolic Syndrome, Korea Food Research Institute, 1201-62, Anyangpangyoro, Seongnam, Gyeonggi 463-746, Korea. 07636@kfri.re.kr.

ABSTRACT
The aim of this study was to improve the anti-inflammatory activities of apigenin through co-treatment with resveratrol as a bioenhancer of apigenin. RAW 264.7 cells pretreated with hepatic metabolites formed by the co-metabolism of apigenin and resveratrol (ARMs) in HepG2 cells were stimulated with lipopolysaccharide (LPS). ARMs prominently inhibited (p < 0.05) the production of nitric oxide (NO), prostaglandin E₂ (PGE₂), interleukin (IL)-1β, IL-6 and TNF-α. Otherwise no such activity was observed by hepatic metabolites of apigenin alone (AMs). ARMs also effectively suppressed protein expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Co-administration of apigenin (50 mg/kg) and resveratrol (25 mg/kg) also showed a significant reduction of carrageenan-induced paw edema in mice (61.20% to 23.81%). Co-administration of apigenin and resveratrol led to a 2.39 fold increase in plasma apigenin levels compared to administration of apigenin alone, suggesting that co-administration of resveratrol could increase bioavailability of apigenin. When the action of resveratrol on the main apigenin metabolizing enzymes, UDP-glucuronosyltransferases (UGTs), was investigated, resveratrol mainly inhibited the formation of apigenin glucuronides by UGT1A9 in a non-competitive manner with a Ki value of 7.782 μM. These results suggested that resveratrol helps apigenin to bypass hepatic metabolism and maintain apigenin's anti-inflammatory activities in the body.

No MeSH data available.


Related in: MedlinePlus