Isolation and identification of phase I metabolites of phillyrin in rats

被引：25

作者：

Li, Chang ^{[1
]}

Yao, Zhi-Hong ^{[2
,3
]}

Qin, Zi-Fei ^{[2
]}

Zhang, Jin-Bo ^{[2
]}

Cao, Rui-Yuan ^{[4
]}

Dai, Yi ^{[2
,3
]}

Yao, Xin-Sheng ^{[1
,2
,3
]}

机构：

[1] Shenyang Pharmaceut Univ, Coll Tradit Chinese Mat Med, Shenyang 110016, Peoples R China

[2] Jinan Univ, Inst Tradit Chinese Med & Nat Prod, Coll Pharm, Guangzhou 510632, Guangdong, Peoples R China

[3] Jinan Univ, Guangdong Prov Key Lab Pharmacodynam Constituents, Guangzhou 510632, Guangdong, Peoples R China

[4] Beijng Inst Pharmacol & Toxicol, Natl Engn Res Ctr Strateg Drugs, Beijing 100850, Peoples R China

来源：

FITOTERAPIA | 2014年 / 97卷

基金：

中国国家自然科学基金;

关键词：

Phillyrin; Forsythia suspensa; Phase I metabolites; Antivirus; PERFORMANCE LIQUID-CHROMATOGRAPHY; LIGNANS; STEREOCHEMISTRY; ANTIOXIDANT;

D O I：

10.1016/j.fitote.2014.05.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Phillyrin was one of the main chemical constituents of the fruit of Forsythia suspense (Thunb.) Vahl. It showed various bioactivities including antioxidant and anti-inflammatory activities. However, the metabolism of phillyrin remained unknown. This report described the isolation and identification of phase I metabolites of phillyrin in rats. Nine metabolites including six new ones were isolated by various column chromatographies and high-performance liquid chromatography. Their structures were elucidated by extensive spectroscopic analysis. The antiviral activities of phillyrin and the metabolites were evaluated against influenza A (H3N2) virus. Among them, one metabolite M8 showed moderate activity with the IC50 value of 26.39 mu M, and three metabolites (M2, M3, M9) showed weak antiviral activities at the concentration of 100 mu M. Based on the structures of the metabolites, possible metabolic pathways of phillyrin in rats were also proposed. (c) 2014 Elsevier B.V. All rights reserved.

引用

页码：92 / 97

页数：6

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