This study elucidated the role of boeravinone B, a NorA multidrug efflux pump inhibitor, in biofilm inhibition. The effects of boeravinone B plus ciprofloxacin, a NorA substrate, were evaluated in NorA-overexpressing, wild-type, and knocked-out Staphylococcus aureus (SA-1199B, SA-1199, and SA-K1758, respectively). The mechanism of action was confirmed using the ethidium bromide accumulation and...

Darunavir is a second-generation protease inhibitor designed to have antiviral efficacy against HIV-1 with multiple resistance mutations to protease inhibitors. It is always coadministered with a subtherapeutic dose of ritonavir. It has been shown that darunavir and ritonavir are substrates of P-glycoprotein (P-gp). We explored the contribution of P-gp to the transport characteristics of daruna...

BACKGROUND In primary percutaneous coronary intervention (PCI), glycoprotein (GP) IIb/IIIa inhibitors are often given in order to attain and maintain better myocardial perfusion. We tested the hypothesis that intracoronary (IC) bolus of GP IIb/IIIa inhibitors might produce a greater improvement in left ventricular (LV) systolic and diastolic function than an intravenous(IV) bolus. METHODS AND...

From previous fits of drug transport kinetics across confluent Madin-Darby canine kidney II cell line overexpressing human multidrug resistance 1 cell monolayers, we found that a drug's binding constant to P-glycoprotein (P-gp) was significantly smaller than its IC(50) when that drug was used as an inhibitor against another P-gp substrate. We tested several IC(50) candidate functions, including...

BACKGROUND Edoxaban, an oral direct factor Xa inhibitor, is in development for thromboprophylaxis, including prevention of stroke and systemic embolism in patients with atrial fibrillation (AF). P-glycoprotein (P-gp), an efflux transporter, modulates absorption and excretion of xenobiotics. Edoxaban is a P-gp substrate, and several cardiovascular (CV) drugs have the potential to inhibit P-gp an...

The overexpression of P-glycoprotein (P-gp) on the surface of tumor cells causes multidrug resistance (MDR). This protein acts as an energy-dependent drug efflux pump reducing the intracellular concentration of structurally unrelated drugs. Modulators of P-gp function can restore the sensitivity of MDR cells to such drugs. XR9576 is a novel anthranilic acid derivative developed as a potent and ...

The overexpression of P-glycoprotein (P-gp) on the surface of tumor cells causes multidrug resistance (MDR). This protein acts as an energy-dependent drug efflux pump reducing the intracellular concentration of structurally unrelated drugs. Modulators of P-gp function can restore the sensitivity of MDR cells to such drugs. XR9576 is a novel anthranilic acid derivative developed as a potent and ...

OBJECTIVES The aim of this study was to observe the effects of bortezomib (PS341) on the expression of NF-κB (nuclear factor-kappa B), IκB (inhibitor kB) and P-gp (P-glycoprotein) of K562 cells induced by daunorubicin (K562/DNR). MATERIALS AND METHODS MTT method was used to determine the drug resistance of K562 cells and the cellular toxicity of bortezomib. Detect the expression of NF-κB, IκB...

The clinical pharmacokinetics and in vitro inhibition of digoxin were examined to predict the P-glycoprotein (P-gp) component of drug-drug interactions. Coadministered drugs (co-meds) in clinical trials (N = 123) resulted in a small, <or=100% increase in digoxin pharmacokinetics. Digoxin is likely to show the highest perturbation, via inhibition of P-gp, because of the absence of metabolic clea...

Darunavir is a second-generation protease inhibitor designed to have antiviral efficacy against HIV-1 with multiple resistance mutations to protease inhibitors. It is always coadministered with a subtherapeutic dose of ritonavir. It has been shown that darunavir and ritonavir are substrates of P-glycoprotein (P-gp). We explored the contribution of P-gp to the transport characteristics of daruna...