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

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 inhibitor...

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Autores principales: Lopes-Rodrigues, Vanessa, Sousa, Emília, Vasconcelos, M. Helena
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5198046/
https://www.ncbi.nlm.nih.gov/pubmed/27834897
http://dx.doi.org/10.3390/ph9040071
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author Lopes-Rodrigues, Vanessa
Sousa, Emília
Vasconcelos, M. Helena
author_facet Lopes-Rodrigues, Vanessa
Sousa, Emília
Vasconcelos, M. Helena
author_sort Lopes-Rodrigues, Vanessa
collection PubMed
description 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.
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spelling pubmed-51980462017-01-04 Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives Lopes-Rodrigues, Vanessa Sousa, Emília Vasconcelos, M. Helena Pharmaceuticals (Basel) Review 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. MDPI 2016-11-10 /pmc/articles/PMC5198046/ /pubmed/27834897 http://dx.doi.org/10.3390/ph9040071 Text en © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Lopes-Rodrigues, Vanessa
Sousa, Emília
Vasconcelos, M. Helena
Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives
title Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives
title_full Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives
title_fullStr Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives
title_full_unstemmed Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives
title_short Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives
title_sort curcumin as a modulator of p-glycoprotein in cancer: challenges and perspectives
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5198046/
https://www.ncbi.nlm.nih.gov/pubmed/27834897
http://dx.doi.org/10.3390/ph9040071
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