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

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

Volume: 9 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Li Qingyong, He Wuna, Zhang Li, Zu Yuangang, Zhu Qiaochu, Deng Xiaoqiu, Zhao Tengfei, Gao Wenqing and Zhang Baoyou, Synthesis, Anticancer Activities, Antimicrobial Activities and Bioavailability of Berberine-Bile Acid Analogues, Letters in Drug Design & Discovery 2012; 9 (6) . https://dx.doi.org/10.2174/157018012800673010