Synthesis, Anticancer Activities, Antimicrobial Activities and Bioavailability of Berberine-Bile Acid Analogues
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: Anticancer; Antimicrobial; Berberine; Bile acids; Oral bioavailability; Synthesis; lipophilicity; steroid skeleton
Document Type: Research Article
Affiliations: Key Laboratory of Forest Plant Ecology (Northeast Forestry University), Ministry of Education, 332 No. 26 Hexing Road, Harbin city, Heilongjiang Province, 150040, China.
Publication date: 01 July 2012
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