Reversal of P-Glycoprotein-Mediated Drug Efflux by Eudesmin from Haplophyllum perforatum and Cytotoxicity Pattern versus Diphyllin, Podophyllotoxin and Etoposide

Planta Medica ◽  
2007 ◽  
Vol 73 (15) ◽  
pp. 1563-1567 ◽  
Author(s):  
Suzanne Lim ◽  
Jérôme Grassi ◽  
Valentina Akhmedjanova ◽  
Eric Debiton ◽  
Guy Balansard ◽  
...  
Keyword(s):  
Drug Efflux ◽  
P Glycoprotein ◽  
Haplophyllum Perforatum ◽  
Pattern Versus

scholarly journals THE MODULATION OF DRUG EFFLUX TRANSPORTER BY CURCUMIN IN MCF7 BREAST CANCER CELLS AFTER REPEATED EXPOSURE OF ENDOXIFEN AND ESTRADIOL

2018 ◽  
Vol 10 (1) ◽  
pp. 102
Author(s):  
Robby Hertanto ◽  
Wilson Bastian ◽  
Paramita . ◽  
Melva Louisa
Keyword(s):  
Breast Cancer ◽  
Cell Viability ◽  
Mrna Expression ◽  
Rna Extraction ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Mcf7 Cells ◽  
Total Rna ◽  
P Glycoprotein ◽  
Drug Efflux Transporters

Objective: The aim of the present study was to determine whether curcumin (CM) can prevent drug sensitivity of breast cancer (BC) cells when E andβ-E2 are administered together and whether the underlying mechanism involves modulation of drug efflux transporters.Methods: MCF7 BC cells were treated with the vehicle only, E+β-E2, or E+β-E2+CM repeatedly for 8 weeks. Afterward, the cells were harvested,counted, and isolated for total RNA extraction. Total RNA was then processed into cDNA and further processed for the determination of mRNAexpression patterns of drug efflux transporters (P-glycoprotein, BCRP, and MRP1).Results: Decreased sensitivity of BC cells was shown by the increased cell viability of MCF7 cells after 8 weeks. This condition was accompanied withincreased mRNA expression of P-glycoprotein, BCRP, and MRP1 in cells treated with E+β-E2, as compared with the vehicle only. CM, administered incombination with E+β-E2, resulted in decreased cell viability versus E and β-E2 and also decreased in mRNA expression of P-glycoprotein, BCRP, andMRP1.Conclusion: CM partially reversed the sensitivity loss of BC cells to E in the presence of β-E2 by modulating drug efflux transporters.

Evaluation of the Impact of P-Glycoprotein (P-gp) Drug Efflux Transporter Blockade on the Systemic and Ocular Disposition of P-gp Substrate

2008 ◽  
Vol 24 (3) ◽  
pp. 290-300 ◽  
Author(s):  
Srinivasan Senthilkumari ◽  
Thirumurthy Velpandian ◽  
Nihar R. Biswas ◽  
Narayanan Sonali ◽  
Supriyo Ghose
Keyword(s):  
Drug Efflux ◽  
Efflux Transporter ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
The Impact

scholarly journals Multidrug resistant P-glycoprotein positive L1210/VCR cells are also cross-resistant to cisplatin via a mechanism distinct from P-glycoprotein-mediated drug efflux activity

2009 ◽  
Vol 28 (4) ◽  
pp. 391-403 ◽  
Author(s):  
L. Gibalová ◽  
J. Sedlák ◽  
M. Labudová ◽  
M. Barančík ◽  
A. Reháková ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Drug Efflux ◽  
P Glycoprotein

Effects of Schisandra Lignans on P-Glycoprotein-Mediated Drug Efflux in Human Intestinal Caco-2 Cells

Planta Medica ◽  
2007 ◽  
Vol 73 (5) ◽  
pp. 444-450 ◽  
Author(s):  
Hye Yoo ◽  
Mijin Lee ◽  
Min Lee ◽  
Sun Lim ◽  
Jongheon Shin ◽  
...  
Keyword(s):  
Drug Efflux ◽  
P Glycoprotein

P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells

Life Sciences ◽  
1992 ◽  
Vol 51 (18) ◽  
pp. 1427-1437 ◽  
Author(s):  
Akira Tsuji ◽  
Tetsuya Terasaki ◽  
Yasushi Takabatake ◽  
Yoshiyuki Tenda ◽  
Ikumi Tamai ◽  
...  
Keyword(s):  
Endothelial Cells ◽  
Efflux Pump ◽  
Bovine Brain ◽  
Drug Efflux ◽  
Brain Capillary ◽  
Brain Capillary Endothelial Cells ◽  
P Glycoprotein ◽  
Capillary Endothelial Cells ◽  
Drug Efflux Pump

Drug efflux mediated by the human multidrug resistance P-glycoprotein is inhibited by cell swelling

1994 ◽  
Vol 107 (12) ◽  
pp. 3281-3290
Author(s):  
A. Sardini ◽  
G.M. Mintenig ◽  
M.A. Valverde ◽  
F.V. Sepulveda ◽  
D.R. Gill ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Chloride Channels ◽  
Drug Transport ◽  
Atp Hydrolysis ◽  
Cell Swelling ◽  
Drug Efflux ◽  
Fluorescent Substrate ◽  
Membrane Stretch ◽  
P Glycoprotein ◽  
In Cells

P-glycoprotein (P-gp), the product of the human multidrug resistance (MDR1) gene, confers multidrug resistance on cells by acting as an ATP-dependent drug transporter. A method using confocal microscopy was developed to measure the transport activity of P-gp from the rate of movement of doxorubicin, a fluorescent substrate of P-gp, across the membrane of a single cell. Recent work has shown that expression of P-gp enhances the activation of chloride channels in response to cell swelling, suggesting that membrane stretch might switch P-gp from a drug-transporting mode to a mode in which it activates chloride channels. In agreement with this idea, we find that cell swelling inhibits drug efflux in cells expressing P-gp but is without effect on the slower background efflux in cells not expressing P-gp and in cells transiently transfected with a mutated MDR1 in which the ATP hydrolysis sites had been inactivated. The identification of a novel means for inhibiting P-gp-mediated drug transport may have implications for the reversal of multidrug resistance during chemotherapy.

Citrus auraptene induces drug efflux transporter P-glycoprotein expression in human intestinal cells

2020 ◽  
Vol 11 (6) ◽  
pp. 5017-5023 ◽  
Author(s):  
Tomohiro Nabekura ◽  
Tatsuya Kawasaki ◽  
Yu Kato ◽  
Kazuyoshi Kawai ◽  
Serena Fiorito ◽  
...  
Keyword(s):  
Protein Expression ◽  
Drug Interactions ◽  
Intestinal Cells ◽  
Drug Efflux ◽  
Efflux Transporter ◽  
Glycoprotein Gene ◽  
P Glycoprotein ◽  
Human Intestinal Cells

Citrus phytochemical auraptene activates the drug efflux transporter P-glycoprotein gene (MDR1) promoter in human intestinal LS174T cells. Auraptene increases protein expression of P-glycoprotein. Auraptene can cause food–drug interactions.

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