产乙酸菌生物活性物质的基本结构特征：双四氢呋喃环相邻羟基的作用。

Essential structural features of acetogenins: role of hydroxy groups adjacent to the bis-THF rings.

作者信息

Abe Masato, Kenmochi Atsushi, Ichimaru Naoya, Hamada Takeshi, Nishioka Takaaki, Miyoshi Hideto

机构信息

Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University, Sakyo-ku, Kyoto 606-8502, Japan.

出版信息

Bioorg Med Chem Lett. 2004 Feb 9;14(3):779-82. doi: 10.1016/j.bmcl.2003.11.021.

DOI:10.1016/j.bmcl.2003.11.021

PMID:14741288

Abstract

The presence of two hydroxy groups adjacent to the THF ring(s) is a common structural feature of natural acetogenins. To elucidate the role of each hydroxy group in the inhibitory action of acetogenins, we synthesized three acetogenin analogues which lack either or both of the hydroxy groups, and investigated their inhibitory activities with bovine heart mitochondrial complex I. Our results indicate that the presence of either of the two hydroxy groups sufficiently sustains a potent inhibitory effect.

摘要

四氢呋喃环（THF环）相邻位置存在两个羟基是天然产乙酸细菌素的常见结构特征。为阐明每个羟基在产乙酸细菌素抑制作用中的作用，我们合成了三种分别缺失一个或两个羟基的产乙酸细菌素类似物，并研究了它们对牛心线粒体复合物I的抑制活性。我们的结果表明，两个羟基中的任何一个的存在都足以维持强效的抑制作用。