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dc.contributor.CRUESPUNIVERSIDADE ESTADUAL DE CAMPINASpt_BR
dc.contributor.authorunicampMelo, Patricia da Silva-
dc.contributor.authorunicampBarata, Lauro Euclides Soares-
dc.typeArtigopt_BR
dc.titleStructure activity relationship, acute toxicity and cytotoxicity of antimycobacterial neolignan analoguespt_BR
dc.contributor.authorde Souza, Ana Olivia-
dc.contributor.authorBernabe Alderete, Joel-
dc.contributor.authorRegazi Minarini, Paulo Roberto-
dc.contributor.authorMelo, Patricia da Silva-
dc.contributor.authorFerreira, Iasmin-
dc.contributor.authorSoares Barata, Lauro Euclides-
dc.contributor.authorSilva, Celio Lopes-
dc.subjectTuberculosept_BR
dc.subject.otherlanguageTuberculosispt_BR
dc.description.abstractObjectives The study's aims were to evaluate the antimycobacterial activity of 13 synthetic neolignan analogues and to perform structure activity relationship analysis (SAR). The cytotoxicity of the compound 2-phenoxy-1-phenylethanone (LS-2, 1) in mammalian cells, such as the acute toxicity in mice, was also evaluated. Methods The extra and intracellular antimycobacterial activity was evaluated on Mycobacterium tuberculosis H37Rv. Cytotoxicity studies were performed using V79 cells, J774 macrophages and rat hepatocytes. Additionally, the in-vivo acute toxicity was tested in mice. The SAR analysis was performed by Principal Component Analysis (PCA). Key findings Among the 13 analogues tested, LS-2 (1) was the most effective, showing promising antimycobacterial activity and very low cytotoxicity in V79 cells and in J774 macrophages, while no toxicity was observed in rat hepatocytes. The selectivity index (SI) of LS-2 (1) was 91 and the calculated LD50 was 1870 mg/kg, highlighting the very low toxicity in mice. SAR analysis showed that the highest electrophilicity and the lowest molar volume are physical-chemical characteristics important for the antimycobacterial activity of the LS-2 (1). Conclusions LS-2 (1) showed promising antimycobacterial activity and very weak cytotoxicity in cell culture, as well as an absence of toxicity in primary culture of hepatocytes. In the acute toxicity study there was an indication of absence of toxicity on murine models, in vivopt_BR
dc.relation.ispartofJournal of pharmacy and pharmacologypt_BR
dc.relation.ispartofabbreviationJ. pharm. pharmacol.pt_BR
dc.publisher.cityOxfordpt_BR
dc.publisher.countryReino Unidopt_BR
dc.publisherJohn Wiley & Sonspt_BR
dc.date.issued2011-
dc.date.monthofcirculationJulypt_BR
dc.language.isoengpt_BR
dc.description.volume63pt_BR
dc.description.issuenumber7pt_BR
dc.description.firstpage936pt_BR
dc.description.lastpage942pt_BR
dc.rightsFechadopt_BR
dc.sourceWOSpt_BR
dc.identifier.issn0022-3573pt_BR
dc.identifier.eissn2042-7158pt_BR
dc.identifier.doi10.1111/j.2042-7158.2011.01290.xpt_BR
dc.identifier.urlhttps://onlinelibrary.wiley.com/doi/full/10.1111/j.2042-7158.2011.01290.xpt_BR
dc.description.sponsorshipCONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQpt_BR
dc.description.sponsorshipFUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULO - FAPESPpt_BR
dc.description.sponsordocumentnumbersem informaçãopt_BR
dc.date.available2020-09-09T21:07:16Z-
dc.date.accessioned2020-09-09T21:07:16Z-
dc.description.provenanceSubmitted by Sanches Olivia (olivias@unicamp.br) on 2020-09-09T21:07:16Z No. of bitstreams: 0. Added 1 bitstream(s) on 2021-01-04T15:13:08Z : No. of bitstreams: 1 000291225800007.pdf: 570323 bytes, checksum: cc7bddea02b1b22fdaca074ca2ea8191 (MD5)en
dc.description.provenanceMade available in DSpace on 2020-09-09T21:07:16Z (GMT). No. of bitstreams: 0 Previous issue date: 2011en
dc.identifier.urihttp://repositorio.unicamp.br/jspui/handle/REPOSIP/348990-
dc.contributor.departmentsem informaçãopt_BR
dc.contributor.departmentDepartamento de Química Organicapt_BR
dc.contributor.unidadeInstituto de Biologiapt_BR
dc.contributor.unidadeInstituto de Químicapt_BR
dc.subject.keywordAcute toxicitypt_BR
dc.subject.keywordCytotoxicitypt_BR
dc.subject.keywordStructure activity relationshippt_BR
dc.identifier.source000291225800007pt_BR
dc.creator.orcidsem informaçãopt_BR
dc.creator.orcid0000-0003-0909-769Xpt_BR
dc.type.formArtigopt_BR
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