蜡蚧轮枝菌素，来自陆生真菌蜡蚧轮枝菌6144的非甾体类孕激素。

The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.

作者信息

Roll Deborah M, Barbieri Laurel R, Bigelis Ramunas, McDonald Leonard A, Arias Daniel A, Chang Li-Ping, Singh Maya P, Luckman Scott W, Berrodin Thomas J, Yudt Matthew R

机构信息

Chemical Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, New York 10965, USA.

出版信息

J Nat Prod. 2009 Nov;72(11):1944-8. doi: 10.1021/np9004882.

DOI:10.1021/np9004882

PMID:19863083

Abstract

Four new indolosesquiterpenes, lecanindoles A-D (1-4), were isolated from fermentations of the terrestrial fungus Verticillium lecanii 6144. The structures of compounds 1-4 were elucidated from analysis of spectroscopic data. Compound 2 was reduced to give 4 and its isomer 5. Compound 4 was found to be a potent and selective progesterone receptor agonist with an EC50 of 1.1 +/- 0.4 nM in a cell-based luciferase reporter assay.

摘要

从陆地真菌蜡蚧轮枝菌6144的发酵产物中分离出四种新的吲哚倍半萜，即蜡蚧吲哚A-D（1-4）。通过光谱数据分析阐明了化合物1-4的结构。化合物2经还原得到4及其异构体5。在基于细胞的荧光素酶报告基因检测中，发现化合物4是一种强效且选择性的孕酮受体激动剂，其半数有效浓度（EC50）为1.1±0.4 nM。