De-glycosylation could be an important process for enhancing the biological activities of flavonoids. In this study we investigated de-glycosylation of rutin by acid treatment by comparing hydrolysis of rutin to quercetin with two different solvents and acid concentrations. Antioxidant activity was measured using chemical methods and biological activities were examined in cell-based systems. Rutin hydrolysis occurred more rapidly when 80% ethanol was used as the reaction solvent (as compared to water), and the rate of hydrolysis accelerated as acid concentrations increased. In reactions of rutin with 0.5 M HCl in 80% ethanol for 3 h, almost all the rutin was converted into quercetin. 2,2-Diphenyl-1-picrylhydrazyl, 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging activities, and reducing powers were correlated with conversion rate. Protective activity in HepG2 cells, anti-inflammatory activity in RAW264.7 cells, and antiadipogenic activity were increased with increased conversion of rutin to quercetin. This study suggests that de-glycosylation of glycoside flavonoids may increase physiological activity and, therefore, enhance its use in various fields.

Phenolic acids, found in cereals, legumes, vegetables, and fruits, have various biological functions. We aimed to compare the antihypertensive potential of different phenolic acids by evaluating their ACE inhibitory activity and cytoprotective capacity in EA.hy 926 endothelial cells. In addition, we explored the mechanism underlying the antihypertensive activity of sinapic acid. Of all the phenolic acids studied, sinapic acid, caffeic acid, coumaric acid, and ferulic acid significantly inhibited ACE activity. Moreover, gallic acid, sinapic acid, and ferulic acid significantly enhanced intracellular NO production. Based on the results of GSH depletion, ROS production, and MDA level analyses, sinapic acid was selected to study the mechanism underlying the antihypertensive effect. Sinapic acid decreases endothelial dysfunction by enhancing the expression of antioxidant-related proteins. Sinapic acid increased phosphorylation of eNOS and Akt in a dose-dependent manner. These findings indicate the potential of sinapic acid as a treatment for hypertension.

We aimed to investigate the effects of nobiletin on hepatic lipogenesis in high glucose‐induced lipid accumulation in HepG2 cells. Nobiletin, a citrus polymethoxyflavonoid with six methoxy groups, is present abundantly in the peels of citrus fruits. HepG2 cells were incubated in Dulbecco’s modified Eagle’s medium containing high glucose (25 mM) and subsequently treated with nobiletin at different concentrations (5, 25, and 50 μM). Results showed that nobiletin markedly inhibited high glucose‐induced hepatic lipid accumulation in HepG2 cells. In addition, it reduced the protein expression of lipogenic factors, including sterol regulatory element‐binding protein 1c (SREBP‐1c) and fatty acid synthase (FAS). Nobiletin significantly increased the phosphorylation of AMP‐activated protein kinase (AMPK) and acetyl‐CoA carboxylase. Pretreatment with compound C, an AMPK inhibitor, abolished the inhibitory effects of nobiletin on SREBP‐1c and FAS expression. These results suggested that nobiletin might attenuate high glucose‐induced lipid accumulation in HepG2 hepatocytes via modulation of AMPK signaling pathway. Therefore, nobiletin might be useful for the prevention and treatment of nonalcoholic fatty liver diseases.