贯叶连翘心材中的木脂素及其对乙型肝炎病毒的抑制活性。
Lignans from the heartwood of Streblus asper and their inhibiting activities to hepatitis B virus.
机构信息
Key Laboratory of Ecology of Rare and Endangered Species and Environmental Protection (Ministry of Education of China), School of Environment and Resource of Guangxi Normal University, Guilin, PR China.
出版信息
Fitoterapia. 2012 Mar;83(2):303-9. doi: 10.1016/j.fitote.2011.11.008. Epub 2011 Nov 17.
Three new lignans, erythro-strebluslignanol (1), threo-7'-methoxyl strebluslignanol (2) and erythro-7'-methoxyl strebluslignanol (3), together with twelve known compounds were isolated from the n-butanol and chloroform fractions of the heartwood of Streblus asper. Their structures were elucidated through extensive spectroscopic methods, including MS and 2D NMR experiments (HMQC and HMBC). The stereochemistry at the chiral center was determined using CD spectra, as well as analysis of coupling constants and optical rotation data, respectively. Primary bioassays showed that 6-hydroxyl-7-methoxyl-coumarin (5) and ursolic acid (10) showed anti-HBV activities, with IC(50) values of 29.60 μM and 89.91 μM for HBsAg at no cytotoxicity, and IC(50) values of 46.41 μM and 97.61 μM for HBeAg at no cytotoxicity, respectively.
从 Asper 心材的正丁醇和氯仿部分分离得到三种新的木脂素，分别为赤式-strebluslignanol（1）、苏式-7'-甲氧基 strebluslignanol（2）和赤式-7'-甲氧基 strebluslignanol（3），以及 12 种已知化合物。通过广泛的光谱方法，包括 MS 和 2D NMR 实验（HMQC 和 HMBC），阐明了它们的结构。通过 CD 光谱、偶合常数和旋光数据的分析，分别确定了手性中心的立体化学。初步生物测定表明，6-羟基-7-甲氧基香豆素（5）和熊果酸（10）具有抗乙肝病毒活性，HBsAg 的 IC50 值分别为 29.60 μM 和 89.91 μM，无细胞毒性，HBeAg 的 IC50 值分别为 46.41 μM 和 97.61 μM，无细胞毒性。
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