Inhibition of P-glycoprotein transport function and reversion of MDR1 multidrug resistance by cnidiadin

Barthomeuf, Chantal; Grassi, Jérôme; Demeule, Michel; Fournier, Carole; Boivin, Dominique; Béliveau, Richard

doi:10.1007/s00280-004-0914-y

Cited by 55 publications

(25 citation statements)

References 25 publications

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“…Previous study shown that six natural coumarins (umbelliferone, esculin, esculetin, cnidiadin, angelicin and psoralen), only cnidiadin was capable of significantly accumulating rhodamin-123 and inhibit ABCB1 photolabeling in MDR1-transfected MadinDarby canine kidney (MDCK-MDR1) cells (Barthomeuf et al, 2005). This study indicate that the results of psoralen decrease ABCB1 expression and capability inhibit ABCB1 pumping activity may have cellular specific correlation.…”

Section: Discussionmentioning

confidence: 60%

Psoralen reverses docetaxel-induced multidrug resistance in A549/D16 human lung cancer cells lines

Hsieh

Chen

et al. 2014

Phytomedicine

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Section: Discussionmentioning

confidence: 60%

Psoralen reverses docetaxel-induced multidrug resistance in A549/D16 human lung cancer cells lines

Hsieh

Chen

et al. 2014

Phytomedicine

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“…cyclosporine [9], valspodar (PSC 833) [10], Pyronaridine [11], and natural and synthetic polymers [12]. Numerous plant-derived dietary compounds, for instance cnidiadin and schizandrins, could also modulate P-gp transport [13,14]. However, the results of clinical trials with these compounds have been disappointing because of side effects and/or weak potency.…”

Section: Introductionmentioning

confidence: 99%

Reversion of Multidrug Resistance in a Chemoresistant Human Breast Cancer Cell Line by β-Elemene

et al. 2012

Pharmacology

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Background: Multidrug resistance (MDR) presents a problem in cancer chemotherapy, and developing new agents to overcome MDR is important. This study intends to investigate the reversal effect of β-elemene on MDR in human breast carcinoma MCF-7 and doxorubicin-resistant MCF-7 cells. Methods: MTT cytotoxicity assays, flow cytometry, and Western blot analysis were performed to investigate the antiproliferative effects of the combination of anticancer drugs with β-elemene, to study the reversal of drug resistance, and to examine the inhibitory effects on protein expression. Results: The results showed that β-elemene (30 µmol/l) had a strong potency to increase the cytotoxicity of doxorubicin to MCF-7/DOX cells, with a reversal fold of 6.38. In addition, the mechanisms of β-elemene in reversing P-glycoprotein (P-gp)-mediated MDR demonstrated that β-elemene significantly increases the intracellular accumulations of doxorubicin and Rh123 via inhibition of the P-gp transport function in MCF-7/DOX cells. Flow cytometry and Western blot analyses revealed that β-elemene could inhibit the expression of P-gp, while it had little effect on the expression of MRP1 protein. In addition, β-elemene had little inhibitory effect on the intracellular GSH levels and GST activities in MCF-7/DOX cells. Conclusions: β-Elemene might represent a promising agent for overcoming MDR in cancer therapy.

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“…However, when co-treatment with cnidiadin (10 mM)/VCR on the KB/VCR cells, the cells resulted from long-term exposure of the parental sensitive KB human oral epidermis carcinoma cell line to VCR. No cell toxicity was detected after exposure to cnidiadin and cnidiadin sensitized KB/VCR cells 103 . In another study, bioguided fractionation from the roots of Citrus sinensis (Rutaceae) led to the isolation and identification of five coumarins, namely, clausarin, suberosin, poncitrin, xanthyletin and thamnosmonin 104 .…”

Section: Coumarinsmentioning

confidence: 90%

Advances in plant-based inhibitors of P-glycoprotein

Zhou

James

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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Multidrug resistance (MDR) has emerged as the main problem in anti-cancer therapy. Although MDR involves complex factors and processes, the main pivot is the expression of multidrug efflux pumps. P-glycoprotein (P-gp) belongs to the family of adenosine triphosphate (ATP)-binding cassette (ABC) transporters. It functions in cellular detoxification, pumping a wide range of xenobiotic compounds out of the cell. An attractive therapeutic strategy for overcoming MDR is to inhibit the transport function of P-gp and thus, increase intracellular concentration of drugs. Recently, various types of P-gp inhibitors have been found and used in experiments. However, none of them has passed clinical trials due to their high side-effects. Hence, the search for alternatives, such as plant-based P-gp inhibitors have gained attention recently. Therefore, we give an overview of the source, function, structure and mechanism of plant-based P-gp inhibitors and give more attention to cancer-related studies. These products could be the future potential drug candidates for further research as P-gp inhibitors.

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Inhibition of P-glycoprotein transport function and reversion of MDR1 multidrug resistance by cnidiadin

Cited by 55 publications

References 25 publications

Psoralen reverses docetaxel-induced multidrug resistance in A549/D16 human lung cancer cells lines

Psoralen reverses docetaxel-induced multidrug resistance in A549/D16 human lung cancer cells lines

Reversion of Multidrug Resistance in a Chemoresistant Human Breast Cancer Cell Line by β-Elemene

Advances in plant-based inhibitors of P-glycoprotein

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