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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...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2016
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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. |
format | Online Article Text |
id | pubmed-5198046 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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