来自长瓣瑞香 Daphniphyllum longeracemosum 的具有新型碳骨架的抗 HIV 瑞香烷二聚体 Logeracemin A。

Logeracemin A, an anti-HIV Daphniphyllum alkaloid dimer with a new carbon skeleton from Daphniphyllum longeracemosum.

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai, 201203, People's Republic of China.

出版信息

J Am Chem Soc. 2014 May 28;136(21):7631-3. doi: 10.1021/ja503995b. Epub 2014 May 16.

DOI:10.1021/ja503995b

PMID:24828017

Abstract

Logeracemin A (1), the first Daphniphyllum alkaloid dimer featuring an unprecedented carbon skeleton with a unique conjugated trispiro[4,5] decane backbone, was isolated from Daphniphyllum longeracemosum. Its structure and absolute configuration were established on the basis of spectroscopic data and X-ray crystallography. Logeracemin A showed significant anti-HIV activity with an EC50 of 4.5 ± 0.1 μM and a selectivity index of 6.2. The structure-activity relationship of the tested compounds was briefly discussed.

摘要

洛革拉敏 A（1），是首次从长叶木莲中分离得到的具有独特共轭三螺[4,5]癸烷骨架的罕见碳骨架的重楼生物碱二聚体，其结构和绝对构型是基于光谱数据和 X 射线晶体学确定的。洛革拉敏 A 表现出显著的抗 HIV 活性，EC50 为 4.5±0.1 μM，选择性指数为 6.2。简要讨论了测试化合物的构效关系。