The beta-carboline alkaloid harmine inhibits BCRP and can reverse resistance to the anticancer drugs mitoxantrone and camptothecin in breast cancer cells.

Yonggang Ma, Michael Wink

University of Heidelberg, Institute of Pharmacy and Molecular Biotechnology, INF 364, 69120 Heidelberg, Germany.

Phytotherapy research : PTR 2010 Jan

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Multidrug resistance (MDR), mediated by highly expressed ABC transporters, is one of the most important mechanisms in tumor cells. Breast cancer resistance protein (BCRP) is a member of the ABC transporter family. This transporter expels different kinds of lipophilic anticancer drugs, which have diffused into the cells. In this study, 96-well plate based assays and flow cytometry analysis were employed to screen natural products for BCRP inhibition. The beta-carboline alkaloid harmine inhibited BCRP in a BCRP overexpressing breast cancer cell line (MDA-MB-231). Harmine reduced resistance to the anticancer drugs mitoxantrone and camptothecin mediated by BCRP and might be an interesting new reversal agent. Harmine did not inhibit P-glycoprotein (P-gp) mediated drug efflux. (c) 2009 John Wiley & Sons, Ltd.

Citation

Yonggang Ma, Michael Wink. The beta-carboline alkaloid harmine inhibits BCRP and can reverse resistance to the anticancer drugs mitoxantrone and camptothecin in breast cancer cells. Phytotherapy research : PTR. 2010 Jan;24(1):146-9