吉马烷型倍半萜内酯的抗分枝杆菌评估

Antimycobacterial evaluation of germacranolides.

作者信息

Fischer N H, Lu T, Cantrell C L, Castañeda-Acosta J, Quijano L, Franzblau S G

机构信息

Department of Chemistry, Louisiana State University, Baton Rouge 70803-1804, USA.

出版信息

Phytochemistry. 1998 Sep;49(2):559-64. doi: 10.1016/s0031-9422(98)00253-2.

DOI:10.1016/s0031-9422(98)00253-2

PMID:9747541

Abstract

The minimum inhibitory concentrations (MIC) against Mycobacterium tuberculosis and M. avium of parthenolide, costunolide, 1 (10)-epoxycostunolide and other germacranolide-type sesquiterpene lactones and derivatives were determined by use of a radiorespirometric bioassay. Structure-activity relationship studies with natural and semisynthetic sesquiterpene lactones suggested that the alpha-methylene-gamma-lactone moiety is an essential, but not sufficient, structural requirement for significant in vitro activity against M. tuberculosis and M. avium.

摘要

通过放射性呼吸测定生物测定法测定了小白菊内酯、木香烯内酯、1（10）-环氧木香烯内酯及其他吉马烷型倍半萜内酯及其衍生物对结核分枝杆菌和鸟分枝杆菌的最低抑菌浓度（MIC）。对天然和半合成倍半萜内酯的构效关系研究表明，α-亚甲基-γ-内酯部分是对结核分枝杆菌和鸟分枝杆菌具有显著体外活性的必要但不充分的结构要求。