2070-DTI，一种由链霉菌属2070号菌株产生的拓扑异构酶抑制剂。

2070-DTI, a topoisomerase inhibitor produced by Streptomyces sp. strain No. 2070.

作者信息

Suzuki Keitarou, Doi Satoru, Yahara Shoji, Uyeda Masaru

机构信息

Department of Pharmaceutical Microbiology, Faculty of Medical and Pharmaceutical Sciences, Kumamoto University, Kumamoto 862-0973, Japan.

出版信息

J Enzyme Inhib Med Chem. 2003 Dec;18(6):497-503. doi: 10.1080/14756360310001613076.

DOI:10.1080/14756360310001613076

PMID:15008514

Abstract

A novel inhibitor of topoisomerase II designated as 2070-DTI was isolated from the culture filtrate of Streptomyces sp. strain No. 2070. The structure was determined to be that of the known soyasaponin I on the basis of spectroscopic methods (NMR and MS). 2070-DTI strongly inhibited the decatenation activity of human placenta topoisomerase II in a noncompetitive manner, and weakly inhibited or was inert towards the relaxation activities of various topoisomerase I's and DNA-related enzymes. 2070-DTI is an inhibitor belonging to the cleavable complex-nonforming type without DNA intercalation.

摘要

从链霉菌属2070号菌株的培养滤液中分离出一种新型的拓扑异构酶II抑制剂，命名为2070-DTI。基于光谱方法（核磁共振和质谱）确定其结构为已知的大豆皂苷I。2070-DTI以非竞争性方式强烈抑制人胎盘拓扑异构酶II的解连环活性，对各种拓扑异构酶I和DNA相关酶的松弛活性有微弱抑制作用或无活性。2070-DTI是一种属于可裂解复合物非形成型且无DNA嵌入的抑制剂。