delta-Lactam derivative from thermophilic soil fungus exhibits in vitro anti-allergic activity

dc.creatorAndrioli, W. J.
dc.creatorSantos, M. S.
dc.creatorSilva, V. B.
dc.creatorOliveira, R. B.
dc.creatorChagas-Paula, D. A.
dc.creatorJorge, J. A.
dc.creatorFurtado, N. A. J. C.
dc.creatorPupo, M. T.
dc.creatorSilva, C. H. T. P.
dc.creatorNaal, R. M. Z. G.
dc.creatorBastos, J. K.
dc.date2012
dc.date2013-09-19T18:06:09Z
dc.date2016-07-01T12:54:26Z
dc.date2013-09-19T18:06:09Z
dc.date2016-07-01T12:54:26Z
dc.date.accessioned2018-03-29T01:53:46Z
dc.date.available2018-03-29T01:53:46Z
dc.identifierNatural Product Research. Taylor & Francis, v.26, n.23, p.2168-2175, 2012
dc.identifier1478-6419
dc.identifierWOS:000310313100002
dc.identifier10.1080/14786419.2011.647020
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/1937
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/1937
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1308479
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.descriptionFrom cultures of thermophilic soil fungus Humicola grisea var thermoidea, a delta-lactam derivative (3-(2-(4-hydroxyphenyl)-2-oxoethyl)-5,6-dihydropyridin-2( 1H)-one) that displayed anti-allergic activity was isolated, which was predicted by in silico computational chemistry approaches. The in vitro anti-allergic activity was investigated by beta-hexosaminidase release assay in rat basophilic leukaemia RBL-2H3 cells. The delta-lactam derivative exhibited similar anti-allergic activity (IC50 = 18.7 +/- 6.7 mu M) in comparison with ketotifen fumarate (IC50 = 15.0 +/- 1.3 mu M) and stronger anti-allergic activity than azelastine (IC50 = 32.0 mu M). Also, the MTT cytotoxicity assay with RBL-2H3 cells showed that delta-lactam does not display cytotoxicity at concentrations lower than 50 mu M. This study suggests that the delta-lactam derivative has the potential to be used as a lead compound in the development of anti-allergic drugs for clinical use in humans.
dc.description26
dc.description23
dc.description2168
dc.description2175
dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.languageeng
dc.publisherTaylor & Francis
dc.publisherAbingdon
dc.relationNatural Product Research
dc.rightsfechado
dc.sourceWOS
dc.subjectHumicola grisea var thermoidea
dc.subjectthermophylic fungus
dc.subjectdelta-lactam derivative
dc.subjectin silico
dc.subjectanti-allergic activity
dc.subjectMAST-CELLS
dc.subjectHISTAMINE
dc.subjectRELEASE
dc.titledelta-Lactam derivative from thermophilic soil fungus exhibits in vitro anti-allergic activity
dc.typeArtículos de revistas


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