Cyclothialidine, a novel DNA gyrase inhibitor. II. Isolation, charactenzation and structure elucidation

Abstract

Cyclothialidine is a novel DNA gyrase inhibitor produced by Streptomyces filipinensis NR 0484. It was isolated from the culture broth by charcoal adsorption, Diaion HP-21, Amberlite CG-50, DEAE Toyopearl, and Toyopearl HW-40 SF column chromatography. The structure of cyclothialidine was determined to be a unique twelve membered lactone by amino acid analysis and various 2D-NMR experiments. Cyclothialidine inhibited Escherichia coli DNA gyrase with an IC50 of 30 ng/ml. © 1994, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.