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dc.contributor.CRUESPUNIVERSIDADE ESTADUAL DE CAMPINASpt_BR
dc.contributor.authorunicampBarata, Lauro Euclides Soares-
dc.typeArtigopt_BR
dc.titleEffects of the antimycobacterial compound 2-phenoxy-1-phenylethanone on rat hepatocytes and formation of metabolitespt_BR
dc.contributor.authorCoutinho, Ana Paula Rodrigues-
dc.contributor.authorMoraes, Luiz Alberto Beraldo de-
dc.contributor.authorBarata, Lauro Euclides Soares-
dc.contributor.authorSouza, Ana Olívia de-
dc.subjectCitotoxicidadept_BR
dc.subject.otherlanguageCytotoxicitypt_BR
dc.description.abstractNeolignans are usually dimers formed by oxidative coupling of allyl and propenyl phenols, and the neolignan analogue, 2-phenoxy-1-phenylethanone (LS-2) is a promising antimycobacterial compound showing very weak cytotoxicity in mammalian cells and lack of acute toxicity in murine models. Objectives: To investigate the mechanism of action of LS-2 in rat hepatocytes by evaluating the activity levels of enzymes related to oxidation status and drug-metabolizing activity. Materials and methods: Hepatocytes were treated with LS-2 from 0.05 up to 1 mM, for 24 and 48 h, and reduced glutathione (GSH), lipid peroxidation and cytochrome P450 enzyme (CYP450) activity were assayed. A homologous series of phenoxazone ethers were used as substrates to measure the enzymatic profile. The biotransformation of LS-2 was studied in hepatocytes by gas chromatography-mass spectrometry (GC-MS) for detection and analysis of possible metabolites. Results: Hepatocytes treated with LS-2 up to 1 mM for 24 or 48 h did not induce the formation of GSH and lipid peroxidation. O-Dealkylation activities of the isoenzymes CYP4501A1, CYP4501A2, CYP4502B1 and CYP4502B2 were also not detected in the hepatocytes treated with LS-2 for 24 or 48 h. Discussion and conclusion: The results indicate that LS-2 or its two detected metabolites, 2-phenoxy-1-phenylethanol and 2,4-(2-hydroxy-2-phenylethoxy)phenol, are not cytotoxic to rat hepatocytes. These compounds maintain a balance between the production of pro-oxidant agents and their respective antioxidant systems. The data show that enzymes related to oxidation status and drug-metabolizing activities are not involved in the mechanism of action of LS-2pt_BR
dc.relation.ispartofPharmaceutical biologypt_BR
dc.relation.ispartofabbreviationPharm biolpt_BR
dc.publisher.cityAbingdonpt_BR
dc.publisher.countryReino Unidopt_BR
dc.publisherTaylor & Francispt_BR
dc.date.issued2012-
dc.date.monthofcirculationAug.pt_BR
dc.language.isoengpt_BR
dc.description.volume50pt_BR
dc.description.issuenumber10pt_BR
dc.description.firstpage1317pt_BR
dc.description.lastpage1325pt_BR
dc.rightsAbertopt_BR
dc.sourceWOSpt_BR
dc.identifier.issn1388-0209pt_BR
dc.identifier.eissn1744-5116pt_BR
dc.identifier.doi10.3109/13880209.2012.674949pt_BR
dc.identifier.urlhttps://www.tandfonline.com/doi/full/10.3109/13880209.2012.674949pt_BR
dc.description.sponsorshipFUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULO - FAPESPpt_BR
dc.description.sponsordocumentnumberSem informaçãopt_BR
dc.date.available2020-09-09T14:51:41Z-
dc.date.accessioned2020-09-09T14:51:41Z-
dc.description.provenanceSubmitted by Thais de Brito Barroso (tbrito@unicamp.br) on 2020-09-09T14:51:41Z No. of bitstreams: 0. Added 1 bitstream(s) on 2021-01-04T15:13:03Z : No. of bitstreams: 1 000308526600017.pdf: 908697 bytes, checksum: 7a0d7af5ae0fee3c8591b9e0b0fc90aa (MD5)en
dc.description.provenanceMade available in DSpace on 2020-09-09T14:51:41Z (GMT). No. of bitstreams: 0 Previous issue date: 2012en
dc.identifier.urihttp://repositorio.unicamp.br/jspui/handle/REPOSIP/348939-
dc.contributor.departmentDepartamento de Química Organicapt_BR
dc.contributor.unidadeInstituto de Químicapt_BR
dc.subject.keywordBiotransformationpt_BR
dc.subject.keywordMetabolitespt_BR
dc.subject.keywordReduced glutathione (GSH)pt_BR
dc.subject.keywordLipid peroxidationpt_BR
dc.subject.keywordCytochrome P450 activity (CYP450)pt_BR
dc.identifier.source000308526600017pt_BR
dc.creator.orcid0000-0003-0909-769Xpt_BR
dc.type.formArtigo de pesquisapt_BR
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