连翘苷在大鼠体内Ⅰ相代谢产物的分离与鉴定
Isolation and identification of phase I metabolites of phillyrin in rats.
作者信息
Li Chang, Yao Zhi-Hong, Qin Zi-Fei, Zhang Jin-Bo, Cao Rui-Yuan, Dai Yi, Yao Xin-Sheng
机构信息
College of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, People's Republic of China; Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou 510632,People's Republic of China.
出版信息
Fitoterapia. 2014 Sep;97:92-7. doi: 10.1016/j.fitote.2014.05.011. Epub 2014 May 29.
Phillyrin was one of the main chemical constituents of the fruit of Forsythia suspensa (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 μM, and three metabolites (M2, M3, M9) showed weak antiviral activities at the concentration of 100 μM. Based on the structures of the metabolites, possible metabolic pathways of phillyrin in rats were also proposed.
连翘苷是连翘果实的主要化学成分之一。它具有多种生物活性，包括抗氧化和抗炎活性。然而，连翘苷的代谢情况仍不清楚。本报告描述了大鼠体内连翘苷Ⅰ相代谢产物的分离与鉴定。通过各种柱色谱法和高效液相色谱法分离出9种代谢产物，其中包括6种新的代谢产物。通过广泛的光谱分析阐明了它们的结构。评估了连翘苷及其代谢产物对甲型流感病毒（H3N2）的抗病毒活性。其中，一种代谢产物M8表现出中等活性，IC50值为26.39 μM，三种代谢产物（M2、M3、M9）在100 μM浓度下表现出较弱的抗病毒活性。基于代谢产物的结构，还提出了大鼠体内连翘苷可能的代谢途径。
Zotero 插件