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

• Published in: British journal of pharmacology Vol. 152; no. 5; pp. 815 - 824
• Main Authors: Holland, M L, Lau, D T T, Allen, J D, Arnold, J C
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.11.2007; Nature Publishing Group
• Subjects: ABCG2; Adenosine Triphosphatases - metabolism; Animals; ATP Binding Cassette Transporter, Sub-Family G, Member 2; ATP-Binding Cassette Transporters - antagonists & inhibitors; ATP-Binding Cassette Transporters - genetics; ATP-Binding Cassette Transporters - metabolism; BCRP; breast cancer resistance protein; cannabidiol; cannabinoids; Cannabinoids - chemistry; Cannabinoids - isolation & purification; Cannabinoids - pharmacology; cannabis; Cell Line; Cell Line, Tumor; Cell Survival - drug effects; chemotherapy; Dose-Response Relationship, Drug; Dronabinol - analogs & derivatives; Dronabinol - pharmacology; Flow Cytometry; Humans; Immunoblotting; Inhibitory Concentration 50; Mice; Mitoxantrone - pharmacology; multidrug resistance; multidrug transporters; Neoplasm Proteins - antagonists & inhibitors; Neoplasm Proteins - genetics; Neoplasm Proteins - metabolism; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Receptor, Cannabinoid, CB1 - genetics; Receptor, Cannabinoid, CB1 - metabolism; Research Papers; Reverse Transcriptase Polymerase Chain Reaction; Sulfasalazine - pharmacology; Topotecan - pharmacology; TRPV Cation Channels - genetics; TRPV Cation Channels - metabolism; Δ9‐tetrahydrocannabinol

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...