红果五味子中木脂素抗 HIV-1 活性的研究。

Anti-HIV-1 activity of lignans from the fruits of Schisandra rubriflora.

机构信息

Kunming Institute of Botany, Chinese Academy of Sciences, Yunnan, China.

出版信息

Arch Pharm Res. 2010 May;33(5):697-701. doi: 10.1007/s12272-010-0508-7. Epub 2010 May 29.

PMID:20512467

Abstract

This study investigated the 70% aqueous acetone extract of the fruits of Schisandra rubriflora which led to the isolation of eight lignans, including a new isolate, rubrisandrin C (1), and seven known lignans (2-8). The structure of 1 was established by extensive 1D and 2D NMR spectroscopy and its absolute stereochemistry was determined by CD spectrum. Compounds 1-5 and 7-8 were evaluated for their anti-HIV-1 activity that showed inhibitory activity on HIV-1(IIIB) induced syncytium formation with EC(50) values in the range of 2.26 approximately 20.4 microg/mL. Compounds 1 and 7 exerted their obvious protection of HIV-1(IIIB) inducted MT-4 host cells lytic effects with a selectivity index of 15.4 and 24.6, respectively.

摘要

本研究调查了五味子果实的 70%水性丙酮提取物，该提取物导致了八种木脂素的分离，包括一种新的分离物，红五味子素 C（1）和七种已知的木脂素（2-8）。通过广泛的 1D 和 2D NMR 光谱确定了 1 的结构，其绝对立体化学通过 CD 光谱确定。化合物 1-5 和 7-8 被评估其抗 HIV-1 活性，显示出对 HIV-1（IIIb）诱导的合胞体形成的抑制活性，EC（50）值在 2.26 至 20.4μg/mL 范围内。化合物 1 和 7 对 HIV-1（IIIb）诱导的 MT-4 宿主细胞裂解作用表现出明显的保护作用，选择性指数分别为 15.4 和 24.6。