Cilostazol (OPC-13013; 6-[4-(1-cyclohexl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone) is widely used as an antiplatelet vasodilator agent. In vitro, the hydroxylation of the quinone moiety of cilostazol to OPC-13326 [6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-4-hydroxy-2(1H)-quinolinone], is the predominant route, and the hydroxylation of the hexane moiety to OPC-13217 i...

Cytochrome P450 enzymes (P450s, CYPs) are a superfamily of heme–thiolate proteins involved in the metabolism endogenous and exogenous substances insects. In this study, identification putative was done elimination repeated sequences resulted 57 from Gastropacha populifolia , 63 Dendrolimus punctatus 53 tabulaeformis . The were aligned together with seven other insect species based on five conse...

The model white rot fungus Phanerochaete chrysosporium has the extraordinary ability to degrade (to CO(2)) lignin and detoxify a variety of chemical pollutants. Whole genome sequencing of this fungus has revealed the presence of the largest P450ome in fungi comprising approx. 150 P450 genes, most of which have unknown function. On the basis of our genome-wide structural and evolutionary analysi...

OBJECTIVE To explore the possible significance of aromatase P450 in endometrial hyperplasia with a background of polycystic ovary syndrome (PCOS). METHODS Immunohistochemistry was used to determine the expression of aromatase P450 in endometrium of PCOS patients. Semiquantitative analysis of aromatase P450 expression of mRNA and protein level wasalso carried out by real-time quantitative RT-P...

Cytochrome P450 enzymes, which catalyze oxygenation reactions of both exogenous and endogenous chemicals, are membrane bound proteins that require interaction with their redox partners in order to function. Those responsible for drug and foreign compound metabolism are localized primarily in the endoplasmic reticulum of liver, lung, intestine, and other tissues. More recently, the potential for...

Rifampin causes drug interactions by altering hepatic drug metabolism. Because microRNAs (miRNAs) have been shown to regulate genes involved in drug metabolism, we determined the effect of rifampin on the expression of hepatic miRNAs. Primary human hepatocytes from seven subjects were treated with rifampin, and the expression of miRNA and cytochrome P450 (P450) mRNAs was measured by TaqMan assa...

The cytochrome P450, epoxide hydrolase, and glutathione S-transferase enzyme families play an important part in the metabolism of many carcinogens and anti-cancer drugs. The expression of two forms of cytochrome P450 (P450 1A and P450 3A), epoxide hydrolase and of the alpha, mu, and pi forms of glutathione S-transferase in normal colon, colonic adenomas, and adenocarcinoma of the colon were stu...

Multiple assays are available to measure P450 activity in insects, including mosquitoes; however, each of these assays has drawbacks in terms of the number of mosquitoes required, specificity, sensitivity, cost, and/or time required to prepare active enzyme homogenates. In this study, a commercially available luminescent assay, P450-Glo, was modified and evaluated to measure P450 activity from ...

[Ru(bpy)2(PVP)10] (RuPVP (bpy = 2,2-bipyridyl; PVP = poly(4-vinylpyridine)) was synthesized and characterized as described previously. Styrene (MW= 104.15), 2Acetylaminofluorene (2-AAF, MW= 223.27), 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK, MW= 207.23), poly(diallyldimethylammonium chloride) (PDDA, average Mw= 100,000200,000), poly(sodium 4-styrenesulfonate) (PSS, average MW= 70000),...

The genes for gibberellin (GA) biosynthesis are clustered in the fungus Gibberella fujikuroi. In addition to genes encoding a GA-specific geranylgeranyl diphosphate synthase and a bifunctional ent-copalyl diphosphate/ent-kaurene synthase, the cluster contains four cytochrome P450 monooxygenase genes (P450-1, -2, -3, -4). Recently it was shown that P450-4 and P450-1 encode multifunctional enzyme...