BACKGROUND Supernatants from epithelial cell cultures enhance eosinophil survival in vitro, this effect being abrogated by previous incubation of eosinophils with glucocorticosteroids. This property has resulted in the development of an in vitro test to compare the potency of these drugs. A comparative study was performed with dexamethasone, methylprednisolone, deflazacort, and budesonide. ME...

Irreversible CYP3A inhibition by drugs constitutes one of the major causes of inhibition-based drug interactions. We evaluated time-dependent inactivation of CYP3A in cryopreserved human hepatocytes for six structurally diverse compounds known to exhibit this property. Inactivation kinetic parameters were also determined using human liver microsomes. Except for diclofenac, which did not cause C...

Atpenin B, a new antifungal antibiotic produced by Penicillium sp. FO-125, inhibited the growth of Raji cells (IC50, 30 microM). The incorporation of [14C]leucine and [3H]thymidine into Raji cells was inhibited by atpenin B with IC50 values of 0.10 and 0.12 microM, respectively. The incorporation of [14C]palmitate into the cells was not inhibited but its incorporation into lipid fractions was i...

Supplementary Figure S1: (A) IC50 of proliferation after treatment with Olaparib: 72 hours versus 6 days. (B) Grafic representation of IC50 of ES cell lines after treatment with Olaparib with regard to ES cell lines1q status. (C) Grafic representation of IC50 of ES cell lines with regard to their p53 status.

Background: Wild edible fruits are good source of phenolic compounds such as anthocyanins. Those known for their anti-inflammatory potential. They interact with many mediators the physiopathological pathway NF-kB which is at a central position in inflammatory response macrophages. This study aimed to determine and antioxidant potential ten wild aqueous extracts. Methods: The was evaluate throug...

The purpose of this study was to determine the impact of CYP3A5 expression on inhibitory potency (Ki or IC50 values) of CYP3A inhibitors, using recombinant CYP3A4 and CYP3A5 (rCYP3A4 and rCYP3A5) and CYP3A5 genotyped human liver microsomes (HLMs). IC50 ratios between rCYP3A4 and rCYP3A5 (rCYP3A5/rCYP3A4) of ketoconazole (KTZ) and itraconazole (ITZ) were 8.5 and 8.8 for midazolam (MDZ), 4.7 and ...

In the present study, the mechanism(s) of synergistic interaction of various platelet mediators such as arachidonic acid (AA) when combined with 5-hydroxytryptamine (5-HT) or adenosine diphosphate (ADP) on human platelet aggregation were examined. The results demonstrated that 5-HT had no or negligible effect on aggregation but it did potentiate the aggregation response of AA. Similarly, the co...

1. Fully automated inhibition screens for the major human hepatic cytochrome P450s have been developed and validated. Probe assays were the fluorometric-based ethoxyresorufin O-deethylation for CYP1A2 and radiometric analysis of erythromycin N-demethylation for CYP3A4, dextromethorphan O-demethylation for CYP2D6, naproxen O-demethylation for CYP2C9 and diazepam N-demethylation for CYP2C19. For ...

Sulfation of ethinyl estradiol (EE) is a major pathway of first pass metabolism in both the intestine and liver. Consequently, we sought to identify the human sulfotransferases (SULTs) involved in the 3-O-sulfation of EE (EE-SULT). Based on the results described herein, cDNA-expressed human cytosolic SULT1A3 and SULT1E1 were identified as low Km isoforms (18.9 and 6.7 nM, respectively) mediatin...

Purpose: To investigate the inhibitory effects of various ratios of polysaccharides/ alkaloids from the rhizome of Coptis chinensis Franch (RCC) on α-glucosidase. Methods: The polysaccharides (PSD) and alkaloids (ALK) from RCC were prepared using the water extraction and alcohol precipitation method and Reinecke’s salt precipitation method, respectively. Subsequently, the α-glucosidase inhibito...