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学科主题: 药学
题名:
Novel cytotoxic bufadienolides derived from bufalin by microbial hydroxylation and their structure-activity relationships
作者: Ye, M; Qu, GQ; Guo, HZ; Guo, D
关键词: bufalin ; bufadienolide ; microbial transformation ; Mucor spinosus ; cytotoxicity ; structure-activity relationship
刊名: JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
发表日期: 2004-06-01
DOI: 10.1016/j.jsbmb.2004.01.010
卷: 91, 期:1-2, 页:87-98
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Endocrinology & Metabolism
研究领域[WOS]: Biochemistry & Molecular Biology ; Endocrinology & Metabolism
关键词[WOS]: HUMAN LEUKEMIA-CELLS ; COMBINATORIAL BIOCATALYSIS ; SUSPENSION CULTURES ; CATHARANTHUS-ROSEUS ; NATURAL-PRODUCTS ; BUFO-MARINUS ; CHAN-SU ; TOAD ; BIOTRANSFORMATION ; CINOBUFAGIN
英文摘要:

Microbial transformation was used to prepare novel cytotoxic bufadienolides. Twelve products (3-14) were obtained from bufalin (1) by the fungus Mucor spinosus. Their structures were elucidated by high-resolution mass spectroscopy (HR-MS) and extensive NMR techniques, including H-1 NMR, C-13 NMR, DEPT, H-1-H-1 correlation spectroscopy (COSY), two dimensional nuclear Overhauser effect correlation spectroscopy (NOESY), heteronuclear multiple quantum coherence (HMQC), and heteronuclear multiple bond coherence (HMBC). Compounds 3, 4, 9 and 11-14 are new mono- or dihydroxylated derivatives of bufalin with novel oxyfunctionalities at C-1beta, C-7beta, C-11beta, C-12beta and C-16alpha positions. The in vitro cytotoxic activities against human cancer cell lines of 3-14, together with 16 biotransformed products derived from cinobufagin (15-30) were determined by the MTT method, and their structure-activity relationships (SAR) were discussed. (C) 2004 Elsevier Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000223088500010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60190
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Ye, M,Qu, GQ,Guo, HZ,et al. Novel cytotoxic bufadienolides derived from bufalin by microbial hydroxylation and their structure-activity relationships[J]. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,2004,91(1-2):87-98.
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