Synthesis, Anticancer Activities, Antimicrobial Activities and Bioavailability of Berberine-Bile Acid Analogues

Author(s): Qingyong Li, Wuna He, Li Zhang, Yuangang Zu, Qiaochu Zhu, Xiaoqiu Deng, Tengfei Zhao, Wenqing Gao, Baoyou Zhang

Journal Name: Letters in Drug Design & Discovery

Volume 9 , Issue 6 , 2012


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Abstract:

Fifteen berberine–bile acid analogues were synthesized. Anticancer activities of these analogues compared with berberine (BBR) were evaluated in vitro; among the analogues, A4, B4, and B5 had higher cytotoxicity than that of BBR. Most of the analogues showed higher antimicrobial activity against Staphylococcus aureus ATCC 25923 and Staphylococcus albus ATCC 8799 than that of BBR, but Bacillus subtilis AS 1.398 and Escherichia coli ATCC 31343 were not sensitive to all of the analogues. A4 and B4 were stable in the serum stability assay. B4 showed promising oral bioavailability in mice.

Keywords: Berberine, Bile acids, Synthesis, Anticancer, Antimicrobial, Oral bioavailability

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Article Details

VOLUME: 9
ISSUE: 6
Year: 2012
Published on: 17 May, 2012
Page: [573 - 580]
Pages: 8
DOI: 10.2174/157018012800673010
Price: $65

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