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Azole Antimycotics Differentially Affect Rifampicin-Induced Pregnane X Receptor-Mediated CYP3A4 Gene Expression
It is suggested that the ability of some azoles to affect recruitment of SRC-1 to PXR modulates their net effects in transactivation of CYP3A4 both in the absence or presence of rifampicin. Expand
Iron reduction potentiates hydroxyl radical formation only in flavonols.
A substantial ferric ions reduction was achieved under acidic conditions, particularly by flavonols and flavanols with the catecholic ring B, while 7-hydroxyflavone and hesperetin were the only flavonoids with dose-dependent inhibition of hydroxyl radical production. Expand
Interactions with selected drug renal transporters and transporter-mediated cytotoxicity in antiviral agents from the group of acyclic nucleoside phosphonates.
It is documented that among the studied transporters hOAT1 seems to be the decisive determinant for renal handling in most of the tested ANPs, and this transporter may also play an important role in the mechanism of their potential cytotoxic effects. Expand
Entecavir Interacts with Influx Transporters hOAT1, hCNT2, hCNT3, but Not with hOCT2: The Potential for Renal Transporter-Mediated Cytotoxicity and Drug–Drug Interactions
It is shown that the potency of ETV to cause nephrotoxicity and/or clinically significant drug-drug interactions related to the tested transporters is considerably lower than that of adefovir, tenofovir and cid ofovir. Expand
Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold.
A series of novel sulfonamides containing 5-chloro-2-hydroxybenzoic acid scaffolds and derivatives have shown the best activity against M. kansasii at the concentrations of 1-4 μmol/L, and the efficacy against other strains was weaker and the studied derivatives exhibited almost none antifungal potency. Expand
Analysis of renal handling of radiopharmaceuticals.
For the analysis of elimination mechanisms of radiopharmaceuticals in the kidney, different approaches at various experimental levels (the kidney perfusion technique, isolated, functionally intact renal tubules, and isolated membranes) could be successfully employed. Expand
The pregnane X receptor down‐regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for (“squelching”) SRC‐1 coactivator
Pregnane X receptor mediates induction of the principal xenobiotic metabolizing enzymes and transporters in the liver and down‐regulation of OCT1 expression by PXR activation is assessed. Expand
Trans-resveratrol, but not other natural stilbenes occurring in food, carries the risk of drug-food interaction via inhibition of cytochrome P450 enzymes or interaction with xenosensor receptors.
It is found that only polymethoxylated stilbenes are prone to significantly induce CYP2B6 or CYP3A4 in primary human hepatocytes via pregnane X receptor (PXR) interaction. Expand
Possible use of excretion of tubular epithelial cells for the study of the nephrotoxic effect of xenobiotics.
The method of determination of the minute excretion of tubular epithelial cells renders it possible to investigate the course of the nephrotoxic effect of the toxin by the influence of whichExpand
The involvement of selected membrane transport mechanisms in the cellular uptake of (177)Lu-labeled bombesin, somatostatin and gastrin analogues.
The study showed that active transport mechanisms are decisive for the cellular accumulation in all tested (177)Lu-labeled somatostatin, gastrin and bombesin analogues. Expand