Abstract

Phillygenin is a bioactive intergradient in Osmanthus fragrans, a well-known food additive and Chinese traditional medicine. This study was to investigate the hepatoprotective effects and pharmacokinetics of phillygenin. The hepatoprotective effect of phillygenin was assessed in carbon tetrachloride- (CCl4-) intoxicated mice by monitoring levels of serum and tissue biomarkers. The pharmacokinetics of phillygenin was evaluated in the mouse after oral (po, 24 mg / kg) or intravenous (iv, 12 mg/kg) administration. Results showed that phillygenin has a great hepatoprotective effect on CCl4-induced liver injury in mice owing to its antioxidant activity and inhibition on cytochrome P450 2E1(CYP2E1). After oral administration, phillygenin was efficiently absorbed with the oral bioavailability of 56.4%. Two metabolites, hydroxylated and dimethylated phillygenin, were identified in mouse urine. These results suggested that phillygenin could be explored as new and potential natural antioxidants and hepatoprotective agents.

Highlights

  • Osmanthus fragrans is a plant belonging to the Oleaceae family [1], which has been cultivated and distributed in East Asia, spanning a large geographic region through China to Japan [2]

  • Our lab has found that Osmanthus fragrans flower extract (OFE) showed a great hepatoprotective effect on carbon tetrachloride- (CCl4-)induced hepatic injury mice [2]

  • The results demonstrated that both of phillygenin and ascorbic acid could eliminate DPPH and ABTS radicals in a dose-dependent manner

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Summary

Introduction

Osmanthus fragrans is a plant belonging to the Oleaceae family [1], which has been cultivated and distributed in East Asia, spanning a large geographic region through China to Japan [2]. Osmanthus fragrans flower is valued as an additive for tea and various foods and used as cosmetics for hair and skin and aromatic therapy [1]. Osmanthus fragrans flower has a wide range of pharmacological properties including antioxidation [3], neuroprotection [4], and antimicrobial effects [5]. Our lab has found that Osmanthus fragrans flower extract (OFE) showed a great hepatoprotective effect on CCl4-induced hepatic injury mice [2]. Phillygenin, extracted from Osmanthus fragrans flower for the first time by our group [6], has many medicinal properties. It can reduce blood lipid levels [7] and low density lipoprotein [8]. Phillygenin has many pharmacological activities, there is limited hepatoprotective information on phillygenin

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