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Capsaicin and Piperine Can Overcome Multidrug Resistance in Cancer Cells to Doxorubicin

1
Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, Im Neuenheimer Feld 364, D-69120 Heidelberg, Germany
2
Heidelberg University Biochemistry Centre (BZH), Heidelberg University, Im Neuenheimer Feld 328, 69120 Heidelberg, Germany
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(3), 557; https://doi.org/10.3390/molecules23030557
Received: 17 January 2018 / Revised: 13 February 2018 / Accepted: 28 February 2018 / Published: 2 March 2018
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Abstract

Background: Multidrug resistance (MDR) can develop in cancer cells after treatment with anticancer drugs, mainly due to the overexpression of the ATP-binding cassette (ABC) transporters. We analyzed the ability of two pungent-tasting alkaloids—capsaicin and piperine from Capsicum frutescens and Piper nigrum, respectively—to reverse multidrug resistance in the cancer cell lines Caco-2 and CEM/ADR 5000, which overexpress P-glycoprotein (P-gp) and other ABC transporters. Methods: The MTT assay was first used to determine the cytotoxicity of doxorubicin, the alkaloids, and digitonin alone, and then their combinations. Furthermore, rhodamine (Rho) 123 and calcein-AM were used to detect the effects of alkaloids on the activity of P-gp. Results: Capsaicin and piperine synergistically enhanced the cytotoxicity of doxorubicin in Caco-2 and CEM/ADR 5000 cells. Furthermore, capsaicin and piperine increased the intracellular accumulation of the fluorescent P-glycoprotein (P-gp) substrates rhodamine and calcein and inhibited their efflux from the MDR cell lines. Conclusion: Our study has demonstrated that capsaicin and piperine are P-gp substrates and have potential chemosensitizing activity, which might be interesting for the development of novel modulators of multidrug resistance. View Full-Text
Keywords: capsaicin; piperine; multidrug resistance; Caco-2; HCT 116; CEM/ADR 5000; CCRF-CEM capsaicin; piperine; multidrug resistance; Caco-2; HCT 116; CEM/ADR 5000; CCRF-CEM
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Li, H.; Krstin, S.; Wang, S.; Wink, M. Capsaicin and Piperine Can Overcome Multidrug Resistance in Cancer Cells to Doxorubicin. Molecules 2018, 23, 557.

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