Isolation and structure elucidation of a novel androgen antagonist, arabilin, produced by Streptomyces sp MK756-CF1

被引:19
|
作者
Kawamura, Tatsuro
Fujimaki, Takahiro
Hamanaka, Natsuki
Torii, Kentaro
Kobayashi, Hiroki
Takahashi, Yoshikazu [2 ]
Igarashi, Masayuki [2 ]
Kinoshita, Naoko [2 ]
Nishimura, Yoshio [2 ]
Tashiro, Etsu
Imoto, Masaya [1 ]
机构
[1] Keio Univ, Dept Biosci & Informat, Fac Sci & Technol, Kohoku Ku, Yokohama, Kanagawa 2238522, Japan
[2] Inst Microbial Chem, Tokyo 141, Japan
来源
JOURNAL OF ANTIBIOTICS | 2010年 / 63卷 / 10期
关键词
androgen antagonist; prostate cancer PSA; PROSTATE-CANCER; SNF4435C; RECEPTOR; SPECTINABILIN; SPECTABILIS; STRAIN;
D O I
10.1038/ja.2010.98
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
In the course of screening for a new type of androgen receptor (AR) antagonist, we isolated a novel compound, arabilin, with two structural isomers, spectinabilin and SNF4435C, produced by Streptomyces sp MK756-CF1 Structure elucidation on the basis of the spectroscopic properties showed that arabilin is a novel polypropionate-derived metabolite with a p-nitrophenyl group and a substituted gamma pyrone ring Arabilin competitively blocked the binding of androgen to the ligand-binding domain of AR in vitro In addition, arabilin inhibited androgen induced prostate specific antigen mRNA expression in prostate cancer LNCaP cells The Journal of Antibiotics (2010) 63, 601-605, doi 10 1038/ja 2010 98, published online 25 August 2010
引用
收藏
页码:601 / 605
页数:5
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