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学科主题: Biochemistry & Molecular Biology; Chemistry, Physical
题名: Microbial biotransformation of water-insoluble herbimycin A to 11-hydroxy-(11-demethoxy)-herbimycin C by Eupenicillium sp SD017
作者: Xie, LW ; Wang, GH ; Zhang, H ; Ouyang, YC ; Sun, W ; Li, X
通讯作者: xiecsu@126.com
关键词: Herbimycin A ; Biotransformation ; Water-insoluble anti-tumor drug ; O-Demethylase
刊名: JOURNAL OF MOLECULAR CATALYSIS B-ENZYMATIC
发表日期: 2010
卷: 62, 期:1, 页:76-80
收录类别: sci
部门归属: [Xie, Lianwu] Cent S Univ Forestry & Technol, Sch Sci, Changsha 410004, Hunan, Peoples R China; [Xie, Lianwu; Wang, Guanghua; Ouyang, Yongchang; Sun, Wei; Li, Xiang] Chinese Acad Sci, LMB, LMM GD, S China Sea Inst Oceanol, Guangzhou 510301, Guangdong, Peoples R China; [Zhang, Hua] N China Pharmaceut Grp Corp, New Drug Res & Dev Ctr, Natl Microbial Med Engn & Res Ctr, Shijiazhuang 050015, Peoples R China
项目归属: LMB
摘要: Herbimycin A, a typically water-insoluble anti-tumor drug and an analog of geldanamycin, was transformed by fungus Eupenicillium sp. SD017. The water solubility and anti-tumor activity of converted products were evaluated after separation, purification, and structure elucidation. The results showed that herbimycin A can be converted into herbimycin C 1 and 11-hydroxy-(11-demethoxy)-herbimycin C 2 with water solubility increased. The latter is a novel compound, and its IC50 to A549, MCF-7, Ehrlich and HeLa cells is 152.9, 0.46, 10.7 and 109.3 mu g/ml, respectively, which are nearly in the range of those between herbimycin A and herbimycin C. It is suggested that an O-demethylase or/and methyltransferase may play an important role on biotransformation in this case. This study will firstly serve as a fundamental methodology for further structural alteration and functional improvement of the water-insoluble anti-tumor drugs using microbial resources. (C) 2009 Elsevier B.V. All rights reserved.
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WOS记录号: WOS:000272316800012
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内容类型: 期刊论文
URI标识: http://ir.scsio.ac.cn/handle/344004/3918
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Xie, LW; Wang, GH; Zhang, H; Ouyang, YC; Sun, W; Li, X.Microbial biotransformation of water-insoluble herbimycin A to 11-hydroxy-(11-demethoxy)-herbimycin C by Eupenicillium sp SD017,JOURNAL OF MOLECULAR CATALYSIS B-ENZYMATIC,2010,62(1):76-80
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