GEX1 compounds, novel antitumor antibiotics related to herboxidiene, produced by Streptomyces sp -: 1.: Taxonomy, production, isolation, physicochemical properties and biological activities

被引:61
作者
Sakai, Y
Yoshida, T
Ochiai, K
Uosaki, Y
Saitoh, Y
Tanaka, F
Akiyama, T
Akinaga, S
Mizukami, T
机构
[1] Kyowa Hakko Kogyo Co Ltd, Tokyo Res Labs, Machida, Tokyo 1948533, Japan
[2] Kyowa Hakko Kogyo Co Ltd, Pharmaceut Res Inst, Nagaizumi, Shizuoka 4118731, Japan
关键词
D O I
10.7164/antibiotics.55.855
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
Six structurally related antitumor antibiotics named GEX1 compounds were isolated from a culture broth of Streptomyces sp. GEX1A was identified as a known herbicide, berboxidiene, structurally interested by the tetrahydropyran moiety and the side chain including a conjugated diene. GEX1Q1similar toQ5 were determined as novel compounds related to herboxidiene. All GEX1 compounds showed cytotoxicity with IC50 values of 0.0037similar to0.99 muM against human tumor cell lines in vitro, but were not active against both Gram-positive and -negative bacteria. Though GEX1A/herboxidiene exhibited antitumor activity in murine tumor-planted mouse models, both GEX1Q3 and GEX1Q5 did not.
引用
收藏
页码:855 / 862
页数:8
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