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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| Format: | Article |
| Language: | English |
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MDPI AG
2016-11-01
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| Series: | Pharmaceuticals |
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| Online Access: | http://www.mdpi.com/1424-8247/9/4/71 |
| _version_ | 1818273694760304640 |
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| author | Vanessa Lopes-Rodrigues Emília Sousa M. Helena Vasconcelos |
| author_facet | Vanessa Lopes-Rodrigues Emília Sousa M. Helena Vasconcelos |
| author_sort | Vanessa Lopes-Rodrigues |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-12-12T22:02:02Z |
| format | Article |
| id | doaj.art-7820f7c4eb5c4eb1bec247a29a57d8d7 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-12-12T22:02:02Z |
| publishDate | 2016-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-7820f7c4eb5c4eb1bec247a29a57d8d72022-12-22T00:10:30ZengMDPI AGPharmaceuticals1424-82472016-11-01947110.3390/ph9040071ph9040071Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and PerspectivesVanessa Lopes-Rodrigues0Emília Sousa1M. Helena Vasconcelos2i3S, Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, PortugalLaboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugali3S, Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, PortugalMultidrug 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.http://www.mdpi.com/1424-8247/9/4/71P-glycoproteinmultidrug resistancecurcumincurcumin analogs |
| spellingShingle | Vanessa Lopes-Rodrigues Emília Sousa M. Helena Vasconcelos Curcumin as a Modulator of P-Glycoprotein in Cancer: Challenges and Perspectives Pharmaceuticals P-glycoprotein multidrug resistance curcumin curcumin analogs |
| 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 | P-glycoprotein multidrug resistance curcumin curcumin analogs |
| url | http://www.mdpi.com/1424-8247/9/4/71 |
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