Please use this identifier to cite or link to this item: https://hdl.handle.net/10216/120487
Author(s): Lopes-Rodrigues V.
Sousa E.
Vasconcelos M.H.
Title: Curcumin as a modulator of P-glycoprotein in cancer: Challenges and perspectives
Publisher: MDPI
Issue Date: 2016
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. © 2016 by the authors; licensee MDPI, Basel, Switzerland.
URI: https://hdl.handle.net/10216/120487
Source: Pharmaceuticals, vol. 9(4):71
Document Type: Artigo em Revista Científica Internacional
Rights: openAccess
Appears in Collections:CIIMAR - Artigo em Revista Científica Internacional

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