来自链霉菌属517 - 02的新型抗真菌抗生素UK - 2A的构效关系研究。第5部分：九元双内酯环部分在呼吸抑制中的作用。

Structure-activity relationship studies on UK-2A, a novel antifungal antibiotic from Streptomyces sp. 517-02. Part 5: Roles of the 9-membered dilactone-ring moiety in respiratory inhibition.

作者信息

Usuki Yoshinosuke, Adachi Noriko, Fujita Ken-ichi, Ichimura Akio, Iio Hideo, Taniguchi Makoto

机构信息

Department of Material Science, Graduate School of Science, Osaka City University, 3-3-138 Sugimoto, Sumiyoshi, Osaka 558-8585, Japan.

出版信息

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3319-22. doi: 10.1016/j.bmcl.2006.03.023. Epub 2006 Mar 27.

DOI:10.1016/j.bmcl.2006.03.023

PMID:16564168

Abstract

Several open-chained analogues of UK-2A, a novel antifungal antibiotic isolated from Streptomyces sp. 517-02, were prepared for structure-activity studies. The in vitro antifungal activities of these compounds against Rhodotorula mucilaginosa IFO 0001 and the inhibition of uncoupler-stimulated respiration in bovine heart submitochondrial particles (SMP) were evaluated. Oxidative potentials were measured by cyclic voltammetry. An analogue prepared from dihexyl L-glutamate showed comparable inhibitory activity as UK-2A.

摘要

从链霉菌属517-02中分离得到的新型抗真菌抗生素UK-2A的几种开链类似物被制备用于构效关系研究。评估了这些化合物对粘红酵母IFO 0001的体外抗真菌活性以及对牛心亚线粒体颗粒（SMP）中解偶联剂刺激呼吸的抑制作用。通过循环伏安法测量氧化电位。由L-谷氨酸二己酯制备的一种类似物表现出与UK-2A相当的抑制活性。