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

被引:8
作者
Ishiyama, D [1 ]
Futamata, K [1 ]
Futamata, M [1 ]
Kasuya, O [1 ]
Kamo, S [1 ]
Yamashita, F [1 ]
Kanazawa, S [1 ]
机构
[1] Kaken Pharmaceut Co LTD, Drug Discovery Res Labs, Fujieda, Shizuoka 4268646, Japan
关键词
D O I
10.7164/antibiotics.51.1069
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
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.
引用
收藏
页码:1069 / 1074
页数:6
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