Curcumin as a modulator of P-glycoprotein in cancer: Challenges and perspectives

Detalhes bibliográficos
Autor(a) principal: Lopes-Rodrigues V.
Data de Publicação: 2016
Outros Autores: Sousa E., Vasconcelos M.H.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: https://hdl.handle.net/10216/120487
Resumo: 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. © 2016 by the authors; licensee MDPI, Basel, Switzerland.
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spelling Curcumin as a modulator of P-glycoprotein in cancer: Challenges and perspectivesMultidrug 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. © 2016 by the authors; licensee MDPI, Basel, Switzerland.MDPI20162016-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/10216/120487eng1424824710.3390/ph9040071Lopes-Rodrigues V.Sousa E.Vasconcelos M.H.info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-09-27T08:17:08Zoai:repositorio-aberto.up.pt:10216/120487Portal AgregadorONGhttps://www.rcaap.pt/oai/openairemluisa.alvim@gmail.comopendoar:71602024-09-27T08:17:08Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv 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
spellingShingle Curcumin as a modulator of P-glycoprotein in cancer: Challenges and perspectives
Lopes-Rodrigues V.
title_short 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_sort Curcumin as a modulator of P-glycoprotein in cancer: Challenges and perspectives
author Lopes-Rodrigues V.
author_facet Lopes-Rodrigues V.
Sousa E.
Vasconcelos M.H.
author_role author
author2 Sousa E.
Vasconcelos M.H.
author2_role author
author
dc.contributor.author.fl_str_mv Lopes-Rodrigues V.
Sousa E.
Vasconcelos M.H.
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. © 2016 by the authors; licensee MDPI, Basel, Switzerland.
publishDate 2016
dc.date.none.fl_str_mv 2016
2016-01-01T00:00:00Z
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