截短侧耳素及其衍生物的研究进展  

Progress in research of pleuromutilin and its derivatives

作　　者：邹懿[1] 黄宇琪[1] 胡昌华[1] 

机构地区：[1]西南大学药学院,重庆400716

出　　处：《中国抗生素杂志》2009年第2期65-68,73,共5页Chinese Journal of Antibiotics

摘　　要：截短侧耳素是重要的二萜类兽用抗生素。发现至今,针对其衍生物进行了深入研究,发现了抗菌活性更强、应用范围更广的泰妙菌素、沃尼妙林、retapamulin和一系列水溶性衍生物等。其中retapamulin是2007年4月FDA批准的近二十年来第一个新的局部应用的抗菌药物,同时作为第一个人用截短侧耳素衍生物,标志着此类抗生素实现了从兽用到人用的飞跃。本文就截短侧耳素的作用机制、生物合成及其衍生物应用等方面的最新进展做简要概述。Pleuromutilin is an important diterpene veterinary antibiotic. Recently, a number of derivatives which possessed stronger antimicrobial activities and broader applications, e.g. tiamulin , valnemulin, and a series of water-soluble derivatives have been discovered. In April, 2007, retapamulin, a pleuromutilin derivatives, has been approved as a topical antibacterial agent in two decades, firstly to be used in the human body by FDA. In this article, an overview of the recent advances in the pleuromutilin family, mode of action, biosynthesis and the therapeutic usage were briefly discussed.

关 键 词：截短侧耳素 衍生物 抗生素 生物合成 作用机制 

分 类 号：R978.1[医药卫生—药品]