0000000000385780

AUTHOR

Hélène Pelczar

showing 4 related works from this author

Rat olfactory bulb and epithelium UDP-glucuronosyltransferase 2A1 (UGT2A1) expression: in situ mRNA localization and quantitative analysis.

2001

UDP-glucuronosyltransferases (UGTs) form a multigenic family of enzymes involved in the biotransformation and elimination of numerous endo- and xenobiotic compounds. Beside the diverse UGT isoforms present in the liver as well as in other tissues, the UGT2A1 isoform, also called olfactory UGT, was initially thought to be expressed in the nasal epithelium only. In this work, we demonstrate the UGT2A1 mRNA expression in the olfactory bulb, using in situ hybridization and quantitative reverse transcription-polymerase chain reaction (RT-PCR) techniques. Within the epithelium, UGT2A1 mRNA is mainly found in the sustentacular cells and to a lesser extent in Bowman's gland cells. Moreover, in situ…

Olfactory systemMaleCentral nervous systemNerve Tissue ProteinsIn situ hybridizationBiologyCellular and Molecular NeuroscienceMiceRapid amplification of cDNA endsOlfactory MucosaGene expressionmedicineAnimalsNeurons AfferentRNA MessengerGlucuronosyltransferaseRats WistarMolecular BiologyIn Situ HybridizationAir PollutantsMice Inbred BALB CSequence Homology Amino AcidReverse Transcriptase Polymerase Chain ReactionEpithelial CellsMolecular biologyOlfactory BulbEpitheliumOlfactory bulbRatsIsoenzymesmedicine.anatomical_structureInactivation MetabolicOlfactory epitheliumBrain research. Molecular brain research
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Metabolism of nilutamide in rat lung.

2005

Nilutamide is a non-steroidal anti-androgen drug proposed in the treatment of metastatic prostatic carcinoma. Its therapeutic effects are overshadowed by the occurrence of adverse reactions, mediated by mechanisms that remain elusive. To elucidate possible mechanisms for nilutamide toxicity, we investigated the metabolism of nilutamide in rat lung homogenates, in subcellular fractions and in freshly isolated cells. In whole lung homogenates, the nitro group of nilutamide was reduced to the amine and hydroxylamine moieties. These conversions occurred exclusively in the absence of dioxygen, were increased by the addition of FMN, FAD, or NADPH. Reductive metabolism of nilutamide to the amine a…

MaleIn Vitro TechniquesImidazolidinesBiochemistryCofactorMass SpectrometryRats Sprague-Dawleychemistry.chemical_compoundHydroxylamineCytosolMacrophages AlveolarmedicineAnimalsEnzyme InhibitorsLungChromatography High Pressure LiquidPharmacologychemistry.chemical_classificationbiologyAndrogen AntagonistsEpithelial CellsMetabolismRatsNitric oxide synthaseCytosolKineticsEnzymeBiochemistrychemistryNilutamidebiology.proteinOxidation-ReductionDrug metabolismmedicine.drugChromatography LiquidBiochemical pharmacology
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CHARACTERIZATION OF MICROSOMAL CYTOCHROME P450-DEPENDENT MONOOXYGENASES IN THE RAT OLFACTORY MUCOSA

2005

Nasal administration of a drug ensures therapeutic action by rapid systemic absorption and/or the entry of some molecules into the brain through different routes. Many recent studies have pointed out the presence of xenobiotic-metabolizing enzymes in rat olfactory mucosa (OM). Nevertheless, very little is known about the precise identity of isoforms of cytochrome P450 (P450)-dependent monooxygenases (P450) and their metabolic function in this tissue. Therefore, we evaluated mRNA expression of 19 P450 isoforms by semiquantitative reverse transcriptase-polymerase chain reaction and measured their microsomal activity toward six model substrates. For purposes of comparison, studies were conduct…

MaleGene isoformPharmaceutical ScienceOlfactionSubstrate SpecificityOlfactory mucosaOlfactory MucosaMicrosomesmedicineAnimalsRNA MessengerEnzyme InhibitorsRats WistarPharmacologychemistry.chemical_classificationbiologyReverse Transcriptase Polymerase Chain ReactionCYP1A2Cytochrome P450MonooxygenaseRatsIsoenzymesKineticsEnzymemedicine.anatomical_structureBiochemistrychemistryMicrosomes Liverbiology.proteinMicrosomeAryl Hydrocarbon HydroxylasesDrug Metabolism and Disposition
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Distribution of nitroreductive activity toward nilutamide in rat.

2004

Abstract Nilutamide is a pneumotoxic and hepatotoxic nitroaromatic (R-NO 2 ) antiandrogen used in the treatment of prostate carcinoma in man. Previously, we established that in the rat lung, the drug is metabolized into the corresponding hydroxylamine (R-NHOH) and amine (R-NH 2 ) derivatives. These results evidenced a cytosolic oxygen-sensitive (type II) nitroreductase activity in lung. In the present studies, we extended the characterization of nilutamide metabolism in liver, brain, kidney, heart, blood, intestine (small, cecum, and large, and their respective luminal contents) of male Sprague–Dawley rats. Subcellular fractions for all tissues (except blood) examined (postmitochondrial, cy…

MaleBiologyToxicologyImidazolidinesKidneyRats Sprague-DawleyNitroreductaseCecumCytosolmedicineAnimalsIntestinal MucosaCells CulturedChromatography High Pressure LiquidPharmacologyKidneyBrainAndrogen AntagonistsMetabolismNitroreductasesSmall intestineRatsCytosolmedicine.anatomical_structureBiochemistryLiverNilutamideMicrosomemedicine.drugToxicology and applied pharmacology
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