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Pharmaceuticals (Basel). 2016 Nov 10;9(4). pii: E71.

Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives.

Author information

1
i3S, Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal. vrodrigues@ipatimup.pt.
2
Cancer Drug Resistance Group, IPATIMUP-Institute of Molecular Pathology and Immunology of the University of Porto, IPATIMUP, 4200-465 Porto, Portugal. vrodrigues@ipatimup.pt.
3
ICBAS-UP-Institute of Biomedical Sciences Abel Salazar, University of Porto, ICBAS-UP, 4099-003 Porto, Portugal. vrodrigues@ipatimup.pt.
4
Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal. esousa@ff.up.pt.
5
CIIMAR/CIMAR-Interdisciplinary Centre of Marine and Environmental Research, University of Porto, 4050-123 Porto, Portugal. esousa@ff.up.pt.
6
i3S, Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal. hvasconcelos@ipatimup.pt.
7
Cancer Drug Resistance Group, IPATIMUP-Institute of Molecular Pathology and Immunology of the University of Porto, IPATIMUP, 4200-465 Porto, Portugal. hvasconcelos@ipatimup.pt.
8
Laboratory of Microbiology, Department of Biological Sciences, FFUP-Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal. hvasconcelos@ipatimup.pt.

Abstract

Multidrug resistance (MDR) presents a serious challenge to the efficiency of cancer treatment, and may be associated with the overexpression of drug efflux pumps. P-glycoprotein (P-gp) is a drug efflux pump often found overexpressed in cases of acquired MDR. Nevertheless, there are no P-gp inhibitors being used in the current clinical practice, due to toxicity problems, drug interactions, or pharmacokinetic issues. Therefore, it is important to identify novel inhibitors of P-gp activity or expression. Curcumin is a secondary metabolite isolated from the turmeric of Curcuma longa L. which has been associated with several biological activities, particularly P-gp modulatory activity (by inhibiting both P-gp function and expression). However, curcumin shows extensive metabolism and instability, which has justified the recent and intensive search for analogs of curcumin that maintain the P-gp modulatory activity but have enhanced stability. This review summarizes and compares the effects of curcumin and several curcumin analogs on P-glycoprotein function and expression, emphasizing the potential of these molecules for the possible development of safe and effective inhibitors of P-gp to overcome MDR in human cancer.

KEYWORDS:

P-glycoprotein; curcumin; curcumin analogs; multidrug resistance

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