Different structures of berberine and five other protoberberine alkaloids that affect P-glycoprotein-mediated efflux capacity.

ABSTRACT: Berberine, berberrubine, thalifendine, demethyleneberberine, jatrorrhizine, and columbamine are six natural protoberberine alkaloid (PA) compounds that display extensive pharmacological properties and share the same protoberberine molecular skeleton with only slight substitution differences. The oral delivery of most PAs is hindered by their poor bioavailability, which is largely caused by P-glycoprotein (P-gp)-mediated drug efflux. Meanwhile, P-gp undergoes large-scale conformational changes (from an inward-facing to an outward-facing state) when transporting substrates, and these changes might strongly affect the P-gp-binding specificity. To confirm whether these six compounds are substrates of P-gp, to investigate the differences in efflux capacity caused by their trivial structural dif

SUBMITTER: Zhang YT 

PROVIDER: S-EPMC6318324 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature