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