天然抗HIV药物——第一部分：来自毛叶木姜子的（+）-去甲氧基表卓越木姜子素和轮叶木姜子醇

Natural anti-HIV agents-part I: (+)-demethoxyepiexcelsin and verticillatol from Litsea verticillata.

作者信息

Hoang Vu Dinh, Tan Ghee Teng, Zhang Hong-Jie, Tamez Pamela A, Hung Nguyen Van, Cuong Nguyen Manh, Soejarto D Doel, Fong Harry H S, Pezzuto John M

机构信息

Program for Collaborative Research in Pharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood St., Chicago, IL 60612, USA.

出版信息

Phytochemistry. 2002 Feb;59(3):325-9. doi: 10.1016/s0031-9422(01)00454-x.

DOI:10.1016/s0031-9422(01)00454-x

PMID:11830141

Abstract

The eudesmane sesquiterpenoid, verticillatol (1), as well as the lignan, (+)-5'-demethoxyepiexcelsin (2), and a known lignan, (+)-epiexcelsin (3), were isolated from Litsea verticillata Hance. Lignan 2 showed moderate anti-HIV activity with an IC(50) value of 16.4 microg/ml (42.7 microM), while the known lignan 3 was inactive up to a concentration of 20 microg/ml (48.3 microM). Compound 1 demonstrated weak activity with an IC(50) value of 34.5 microg/ml (144.7 microM) while being devoid of cytotoxicity at 20 microg/ml. The structures were elucidated by 1D and 2D NMR spectroscopy, and the absolute configuration of the new sesquiterpenoid was determined by the generation of Mosher esters.

摘要

从毛叶木姜子（Litsea verticillata Hance）中分离得到了桉叶烷倍半萜类化合物轮叶木姜醇（1）、木脂素（+）-5'-去甲氧基表滇南素（2）以及一种已知木脂素（+）-表滇南素（3）。木脂素2表现出中等强度的抗HIV活性，IC50值为16.4 μg/ml（42.7 μM），而已知木脂素3在浓度高达20 μg/ml（48.3 μM）时无活性。化合物1表现出较弱的活性，IC50值为34.5 μg/ml（144.7 μM），且在20 μg/ml时无细胞毒性。通过一维和二维核磁共振光谱对结构进行了阐明，并通过生成莫舍尔酯确定了新倍半萜类化合物的绝对构型。