新型人拓扑异构酶I选择性抑制剂，源自喜树碱的BM2419 - 1和-2 。

Novel selective inhibitors for human topoisomerase I, BM2419-1 and -2 derived from saintopin.

作者信息

Ishiyama D, Futamata K, Futamata M, Kasuya O, Kamo S, Yamashita F, Kanazawa S

机构信息

Drug Discovery Research Laboratories, Kaken Pharmaceutical CO., LTD., Shizuoka, Japan.

出版信息

J Antibiot (Tokyo). 1998 Dec;51(12):1069-74. doi: 10.7164/antibiotics.51.1069.

DOI:10.7164/antibiotics.51.1069

PMID:10048564

Abstract

Compounds BM2419-1 and -2 were isolated from a culture broth of a fungus Paecilomyces sp. BM2419. It was shown that these novel compounds were artifacts derived from saintopin, a dual inhibitor of topoisomerase I and II by independent processes. In the human topoisomerase I inhibition assay using the recombinant Saccharomyces cerevisiae, BM2419-1 and -2 inhibited selectively the yeast growth dependent on human topoisomerase I induction with IC50 values of 0.3 ng/ml and 6.0 ng/ml, respectively.

摘要

化合物BM2419 - 1和 - 2是从真菌拟青霉属菌株BM2419的培养液中分离得到的。结果表明，这些新型化合物是圣多平通过独立过程衍生而来的人工制品，圣多平是一种拓扑异构酶I和II的双重抑制剂。在使用重组酿酒酵母的人拓扑异构酶I抑制试验中，BM2419 - 1和 - 2分别以0.3 ng/ml和6.0 ng/ml的IC50值选择性抑制依赖于人拓扑异构酶I诱导的酵母生长。