Lignans and diterpenes isolated from Tirpitzia ovoidea and their biological activities  

作　　者：YANG Xue-Yan ZHANG Yi-Fan LIU Li-Jia WANG Yi SHANG Ming-Ying XU Feng LIU Guang-Xue CAI Shao-Qing 

机构地区：[1]Department of Natural Medicine, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191,China

出　　处：《Chinese Journal of Natural Medicines》2017年第12期938-943,共6页中国天然药物（英文版）

基　　金：supported by the National Key Technology R&D Program“New Drug Innovation”of China(Nos.2013ZX09103002-006 and 2013ZX09508104)

摘　　要：A new lignan, tirpitzin A(17) together with 20 known compounds(1-16, and 18-21) were isolated from the ethyl acetate soluble fraction of ethanol extract of the aerial parts of Tirpitzia ovoidea. The structure of new compound was elucidated by means of spectroscopic analysis. Of the known compounds, 7-21 were isolated from Linaceae family for the first time. The pharmacological activity of the crude extracts was tested using a mouse inflammation model induced by dimethyl benzene. The results demonstrated that the ethyl acetate soluble fraction had anti-inflammatory activity. Moreover, the cytotoxic and anti-inflammatory activities of some compounds were studied. The new compound 17 showed moderate cytotoxic effect against Bx PC-3 cell line(IC_50 = 19.51μmol·L^(-1)) and Compound 10 showed significant cytotoxicity against Hep G2, HL-60, U87 and Bx PC-3 cell lines with IC_50 values in the range 4.2-8.3μmol·L^(-1). Additionally, Compounds 2, 10, 11, and 13 exhibited potent inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages at the concentration of 50μmol·L^(-1).A new lignan, tirpitzin A（17） together with 20 known compounds（1-16, and 18-21） were isolated from the ethyl acetate soluble fraction of ethanol extract of the aerial parts of Tirpitzia ovoidea. The structure of new compound was elucidated by means of spectroscopic analysis. Of the known compounds, 7-21 were isolated from Linaceae family for the first time. The pharmacological activity of the crude extracts was tested using a mouse inflammation model induced by dimethyl benzene. The results demonstrated that the ethyl acetate soluble fraction had anti-inflammatory activity. Moreover, the cytotoxic and anti-inflammatory activities of some compounds were studied. The new compound 17 showed moderate cytotoxic effect against Bx PC-3 cell line（IC_50 = 19.51μmol·L^-1） and Compound 10 showed significant cytotoxicity against Hep G2, HL-60, U87 and Bx PC-3 cell lines with IC_50 values in the range 4.2-8.3μmol·L^-1. Additionally, Compounds 2, 10, 11, and 13 exhibited potent inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages at the concentration of 50μmol·L^-1.

关 键 词：Tirpitzia ovoidea Linaceae Lignans DITERPENES CYTOTOXIC ACTIVITY ANTI-INFLAMMATORY ACTIVITY 

分 类 号：R284.1[医药卫生—中药学] R917[医药卫生—中医学]