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Novel cytotoxic bufadienolides derived from bufalin by microbial hydroxylation and their structure-activity relationships
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
2004-06-01
DOI10.1016/j.jsbmb.2004.01.010
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
引用统计
被引频次:68[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/60190
专题北京大学药学院
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
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GB/T 7714
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.
APA Ye, M,Qu, GQ,Guo, HZ,&Guo, D.(2004).Novel cytotoxic bufadienolides derived from bufalin by microbial hydroxylation and their structure-activity relationships.JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,91(1-2),87-98.
MLA Ye, M,et al."Novel cytotoxic bufadienolides derived from bufalin by microbial hydroxylation and their structure-activity relationships".JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY 91.1-2(2004):87-98.
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