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

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Lopes-Rodrigues V, Sousa E, Vasconcelos MH

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

Pharmaceuticals (Basel). 2016 Nov 10;9(4). pii: ph9040071. doi: 10.3390/ph9040071.

PubMed ID

27834897 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drugs

Curcumin

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Curcumin	P-glycoprotein 1	Protein	Humans	Unknown	Inhibitor	Details