2005
DOI: 10.1007/s00280-005-0052-1 View full text |Buy / Rent full text
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Abstract: Multidrug resistance is a major cause of chemotherapy failure in cancer patients. One of the resistance mechanisms is the overexpression of drug efflux pumps such as P-glycoprotein and multidrug resistance protein 1 (MRP1, (ABCC1)). In this study, curcumin mixture and three major curcuminoids purified from turmeric (curcumin I, II, and III) were tested for their ability to modulate the function of MRP1 using HEK293 cells stably transfected with MRP1-pcDNA3.1 and pcDNA3.1 vector alone. The IC(50) of curcuminoid… Show more

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“…We have shown previously that curcuminoids are inhibitors of the ABC transporters, ABCB1 (25,26) and ABCC1 (27), which are known to play a major role in the development of MDR in cancer cells. In this study, purified curcuminoids were tested for their interaction with ABCG2.…”
Section: Discussionmentioning
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“…We have shown previously that curcuminoids are inhibitors of the ABC transporters, ABCB1 (25,26) and ABCC1 (27), which are known to play a major role in the development of MDR in cancer cells. In this study, purified curcuminoids were tested for their interaction with ABCG2.…”
Section: Discussionmentioning
“…NF-κB regulates the expression of genes involved in the suppression of the apoptotic response, and is responsible for tumor cell survival (6). Additionally, Cur is also known to downregulate the intracellular levels of three major ABC drug transporters, P-gp, MDR-associated protein 1 (MRP1) and ABCG2, which are important in MDR (7)(8)(9). In spite of these various promising therapeutic applications of Cur, its therapeutic efficacy is limited due to its markedly poor water solubility, and consequently, remarkably low systemic concentrations are achieved when Cur is consumed orally (4).…”
Section: Introductionmentioning
“…Curcuminoids, from the rhizomes of Curcuma longa, have been reported to reverse the drug resistance phenotype in cancer cells overexpressing ABC transporters, viz., ABCB1, ABCG2, and ABCC1 (2,4,5). Curcuminoids blocked the efflux of fluorescent substrates calcein AM, rhodamine 123, and bodipy-FL-vinblastine in MDR cervical carcinoma cell lines overexpressing ABCB1 and the efflux of mitoxantrone and pheophorbide A, mediated by ABCG2, in HEK293 cells (3,4).…”
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