氯代木脂素A和B，从全缘金粟兰中分离出的两种高效且具选择性的钾通道阻滞剂。

Chlorahololides A and B, two potent and selective blockers of the potassium channel isolated from Chloranthus holostegius.

作者信息

Yang Sheng-Ping, Gao Zhao-Bing, Wang Fang-Dao, Liao Shang-Gao, Chen Hua-Dong, Zhang Chuan-Rui, Hu Guo-Yuan, Yue Jian-Min

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, PRC.

出版信息

Org Lett. 2007 Mar 1;9(5):903-6. doi: 10.1021/ol0700759. Epub 2007 Jan 31.

DOI:10.1021/ol0700759

PMID:17263543

Abstract

[structure: see text] Chlorahololides A(1) and B(2), two highly complex sesquiterpenoid dimers, were isolated from Chloranthus holostegius. Their structures and absolute configurations were established by NMR spectroscopy, X-ray crystallography, and CD. Chlorahololides A (1) and B (2) exhibited potent and selective inhibition on the delayed rectifier (IK) K+ current, with an IC50 of 10.9 and 18.6 microM, respectively.

摘要

[结构：见正文] 氯代霍洛内酯A（1）和B（2）是从全缘金粟兰中分离得到的两种高度复杂的倍半萜二聚体。它们的结构和绝对构型通过核磁共振光谱、X射线晶体学和圆二色光谱确定。氯代霍洛内酯A（1）和B（2）对延迟整流钾电流（IK）表现出强效且选择性的抑制作用，IC50分别为10.9和18.6微摩尔。