Status of Flavonols as P-Glycoprotein Inhibitors in Cancer Chemotherapy

2009 ◽  
Vol 5 (2) ◽  
pp. 89-99 ◽  
Author(s):  
Tripta Bansal ◽  
Manu Jaggi ◽  
Roop Khar ◽  
Sushama Talegaonkar
Keyword(s):  
Cancer Chemotherapy ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

scholarly journals Overcoming multidrug-resistance in vitro and in vivo using the novel P-glycoprotein inhibitor 1416

2012 ◽  
Vol 32 (6) ◽  
pp. 559-566 ◽  
Author(s):  
Yan Xu ◽  
Feng Zhi ◽  
Guangming Xu ◽  
Xiaolei Tang ◽  
Sheng Lu ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cancer Chemotherapy ◽  
Antitumour Activity ◽  
Multidrug Resistant ◽  
The Novel ◽  
Mice Model ◽  
P Glycoprotein ◽  
Channel Currents

MDR (multidrug-resistance) represents a major obstacle to successful cancer chemotherapy and is usually accomplished by overexpression of P-gp (P-glycoprotein). Much effort has been devoted to developing P-gp inhibitors to modulate MDR. However, none of the inhibitors on the market have been successful. 1416 [1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (phenoprolamine hydrochloride)] is a new VER (verapamil) analogue with a higher IC50 for blocking calcium channel currents than VER. In the present paper, we examined the inhibition effect of 1416 on P-gp both in vitro and in vivo. 1416 significantly enhanced cytotoxicity of VBL (vinblastine) in P-gp-overexpressed human multidrug-resistant K562/ADM (adriamycin) and KBV cells, but had no such effect on the parent K562 and KB cells. The MDR-modulating function of 1416 was further confirmed by increasing intracellular Rh123 (rhodanmine123) content in MDR cells. Human K562/ADM xenograft-nude mice model verified that 1416 potentiates the antitumour activity of VBL in vivo. RT-PCR (reverse transcriptase-PCR) and FACS analysis demonstrated that the expression of MDR1/P-gp was not affected by 1416 treatment. All these observations suggest that 1416 could be a promising agent for overcoming MDR in cancer chemotherapy.

Chemosensitization potential of P-glycoprotein inhibitors in malaria parasites

2013 ◽  
Vol 134 (2) ◽  
pp. 235-243 ◽  
Author(s):  
Laura M. Alcantara ◽  
Junwon Kim ◽  
Carolina B. Moraes ◽  
Caio H. Franco ◽  
Kathrin D. Franzoi ◽  
...  
Keyword(s):  
Malaria Parasites ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

NEW 4-ARYL-1,4-DIHYDROPYRIDINES AND 4-ARYLPYRIDINES AS P-GLYCOPROTEIN INHIBITORS

2004 ◽  
Vol 33 (3) ◽  
pp. 321-328 ◽  
Author(s):  
Xiao-fei Zhou ◽  
Linping Zhang ◽  
Elaine Tseng ◽  
Elizabeth Scott-Ramsay ◽  
Jerome J. Schentag ◽  
...  
Keyword(s):  
P Glycoprotein ◽  
Glycoprotein Inhibitors

Discovery of New 4-Indolyl Quinazoline Derivatives as Highly Potent and Orally Bioavailable P-Glycoprotein Inhibitors

2021 ◽  
Vol 64 (19) ◽  
pp. 14895-14911
Author(s):  
Shuo Yuan ◽  
Bo Wang ◽  
Qing-Qing Dai ◽  
Xiao-Nan Zhang ◽  
Jing-Ya Zhang ◽  
...  
Keyword(s):  
P Glycoprotein ◽  
Quinazoline Derivatives ◽  
Orally Bioavailable ◽  
Glycoprotein Inhibitors

Effect of Clarithromycin on Steady-State Digoxin Concentrations

2003 ◽  
Vol 37 (2) ◽  
pp. 178-181 ◽  
Author(s):  
Hideko Tanaka ◽  
Kana Matsumoto ◽  
Kazuyuki Ueno ◽  
Mayumi Kodama ◽  
Kohji Yoneda ◽  
...  
Keyword(s):  
Heart Failure ◽  
Congestive Heart Failure ◽  
Digoxin Concentration ◽  
Concomitant Administration ◽  
Percentage Increase ◽  
P Glycoprotein ◽  
Before And After ◽  
Glycoprotein Inhibitors ◽  
Dose Dependent ◽  
Digoxin Therapy

OBJECTIVE: To evaluate the magnitude and dose-relatedness of the effect of clarithromycin on the pharmacokinetics of digoxin, and to compare the effects of clarithromycin with those of P-glycoprotein inhibitors. METHODS: Eight Japanese inpatients with congestive heart failure participated in this study. Each patient received oral digoxin therapy for at least 7 days and were coadministered oral clarithromycin to prevent or treat pneumonia. To evaluate the effects of clarithromycin on the pharmacokinetics of digoxin, digoxin concentrations were compared before and after coadministration of clarithromycin. RESULTS: Digoxin concentrations were higher after coadministration of clarithromycin in all patients (before, 0.838 ± 0.329 ng/mL; after, 1.36 ± 0.619 ng/mL); (p < 0.005). A significant correlation was observed between the dose of clarithromycin and the percentage of increase in the digoxin concentration. CONCLUSIONS: Digoxin concentrations increased during concomitant administration of clarithromycin, and this effect was dose-dependent on clarithromycin. The percentage increase in digoxin concentrations after the usual oral dose of clarithromycin (400 mg/d) is approximately 70%. Therefore, digoxin concentrations must be monitored carefully after coadministration of clarithromycin, and the doses of digoxin may need readjustment in patients who are concomitantly receiving clarithromycin.

scholarly journals P-glycoprotein inhibitors of natural origin as potential tumor chemo-sensitizers: A review

2015 ◽  
Vol 6 (1) ◽  
pp. 45-62 ◽  
Author(s):  
Hossam M. Abdallah ◽  
Ahmed M. Al-Abd ◽  
Riham Salah El-Dine ◽  
Ali M. El-Halawany
Keyword(s):  
Natural Origin ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

Jatrophane Diterpenes as P-Glycoprotein Inhibitors. First Insights of Structure−Activity Relationships and Discovery of a New, Powerful Lead

2003 ◽  
Vol 46 (15) ◽  
pp. 3395-3402 ◽  
Author(s):  
Gabriella Corea ◽  
Ernesto Fattorusso ◽  
Virginia Lanzotti ◽  
Orazio Taglialatela-Scafati ◽  
Giovanni Appendino ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors
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