Cantrell C L, Franzblau S G, Fischer N H
U.S. Department of Agriculture, Agricultural Research Service, National Center for Agricultural Utilization Research, Peoria, Illinois 61604, USA.
Planta Med. 2001 Nov;67(8):685-94. doi: 10.1055/s-2001-18365.
Abstract. Tuberculosis (TB), mainly caused by Mycobacterium tuberculosis, is the leading killer among all infectious diseases worldwide and is responsible for more than two million deaths annually. For over thirty years no antitubercular agents with new mechanisms of action have been developed. The recent increase in the number of multi-drug resistant clinical isolates of M. tuberculosis has created an urgent need for the discovery and development of new antituberculosis leads. This review covers recent reports on plant-derived terpenoids that have demonstrated moderate to high activity in in vitro bioassays against M. tuberculosis. In this review, mono-, sesqui-, di- and triterpenes, and sterols, their structural analogs and semisynthetic derivatives will be discussed, with particular emphasis on the structural features essential for antimycobacterial activity.
摘要。结核病(TB)主要由结核分枝杆菌引起,是全球所有传染病中的主要杀手,每年导致超过200万人死亡。三十多年来,尚未开发出具有新作用机制的抗结核药物。最近,耐多药结核分枝杆菌临床分离株数量的增加,迫切需要发现和开发新的抗结核先导化合物。本综述涵盖了关于植物来源萜类化合物的最新报道,这些萜类化合物在体外生物测定中对结核分枝杆菌表现出中度至高活性。在本综述中,将讨论单萜、倍半萜、二萜和三萜以及甾醇、它们的结构类似物和半合成衍生物,特别强调抗分枝杆菌活性所必需的结构特征。