The multidrug transporter ABCG2 (BCRP) is inhibited by plant-derived cannabinoids.

ABSTRACT:

Background and purpose

Cannabinoids are used therapeutically for the palliation of the adverse side effects associated with cancer chemotherapy. However, cannabinoids also inhibit both the activity and expression of the multidrug transporter, P-glycoprotein in vitro. Here we address the interaction of cannabinol (CBN), cannabidiol (CBD) and delta 9-tetrahydrocannabinol (THC) with the related multidrug transporter, ABCG2.

Experimental approach

Cannabinoid inhibition of Abcg2/ABCG2 was assessed using flow cytometric analysis of substrate accumulation and ATPase activity assays. The cytotoxicity and chemosensitization by cannabinoids was determined with cell viability assays. Expression of cannabinoid and vanilloid receptors was assessed using reverse transcriptase polymerase c

SUBMITTER: Holland ML 

PROVIDER: S-EPMC2190019 | biostudies-literature | 2007 Nov

REPOSITORIES: biostudies-literature