Human MDR1 and MRP1 recognize berberine as their transport substrate.
To examine whether human ATP-binding cassette (ABC) transporters play a role in the detoxification of plant alkaloid berberine, we investigated berberine transport using multidrug resistance protein1 (MDR1) and multidrug resistance-associated protein1 (MRP1). Cells expressing MDR1 or MRP1 accumulated less berberine. Berberine accumulation depended on the cellular ATP level, and was reversed by typical inhibitors of MDR1, suggesting that human MDR1 and MRP1 directly efflux berberine as their substrate.
Shitan
Nobukazu
N
Laboratory of Plant Gene Expression, Research Institute for Sustainable Humanosphere, Kyoto University, Japan.
Tanaka
Miyako
M
Terai
Koichiro
K
Ueda
Kazumitsu
K
Yazaki
Kazufumi
K
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000255:Adenosine Triphosphate / Q000494:pharmacology; D001599:Berberine; D001692:Biological Transport / Q000187:drug effects; D002460:Cell Line; D006801:Humans; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000378:metabolism*; D013379:Substrate Specificity
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000255:Adenosine Triphosphate; D001599:Berberine; D027425:ATP-Binding Cassette, Sub-Family C Proteins; C421109:multidrug resistance-associated protein 1