Evaluation of Rhamnetin as an Inhibitor of the Pharmacological Effect of Secretory Phospholipase A2

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dc.contributor.authorBelchor, Mariana Novo [UNIFESP]
dc.contributor.authorGaeta, Henrique Hessel
dc.contributor.authorBittencourt Rodrigues, Caroline Fabri
dc.contributor.authorda Cruz Costa, Caroline Ramos
dc.contributor.authorToyama, Daniela de Oliveira
dc.contributor.authorDomingues Passero, Luiz Felipe
dc.contributor.authorLaurenti, Marcia Dalastra
dc.contributor.authorToyama, Marcos Hikari
dc.date.accessioned2019-08-19T11:48:34Z
dc.date.available2019-08-19T11:48:34Z
dc.date.issued2017
dc.description.abstractRhamnetin (Rhm), 3-O-methylquercetin (3MQ), and Rhamnazin (Rhz) are methylated derivatives of quercetin commonly found in fruits and vegetables that possess antioxidant and anti-inflammatory properties. Phospholipase A2 (PLA2) displays several important roles during acute inflammationen
dc.description.abstracttherefore, this study aimed at investigating new compounds able to inhibit this enzyme, besides evaluating creatine kinase (CK) levels and citotoxicity. Methylated quercetins were compared with quercetin (Q) and were incubated with secretory PLA2 (sPLA2) from Bothrops jararacussu to determine their inhibitory activity. Cytotoxic studies were performed by using the J774 cell lineage incubated with quercertins. In vivo tests were performed with Swiss female mice to evaluate decreasing paw edema potential and compounds' CK levels. Structural modifications on sPLA2 were made with circular dichroism (CD). Despite Q and Rhz showing greater enzymatic inhibitory potential, high CK was observed. Rhm exhibited sPLA2 inhibitory potential, no toxicity and, remarkably, it decreased CK levels. The presence of 3OH on the C-ring of Rhm may contribute to both its anti-inflammatory and enzymatic inhibition of sPLA2, and the methylation of ring A may provide the increase in cell viability and low CK level induced by sPLA2. These results showed that Rhm can be a candidate as a natural compound for the development of new anti-inflammatory drugs.en
dc.description.affiliationUniv Fed São Paulo, Postgrad Program Food Nutr & Hlth, BR-11015020 São Paulo, Brazil
dc.description.affiliationUniv Estadual Paulista, Biosci Inst, BR-11330900 São Paulo, Brazil
dc.description.affiliationBrazil Univ, Prorector Res, BR-08230030 São Paulo, Brazil
dc.description.affiliationUniv São Paulo, Pathol Lab Infect Dis LIM50, Dept Pathol, Sch Med, BR-01246903 São Paulo, Brazil
dc.description.affiliationUnifespUniv Fed São Paulo, Postgrad Program Food Nutr & Hlth, BR-11015020 São Paulo, Brazil
dc.description.sourceWeb of Science
dc.description.sponsorshipUniversidade Estadual Paulista (UNESP)
dc.description.sponsorshipUniversidade Federal de São Paulo (UNIFESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.format.extent-
dc.identifierhttp://dx.doi.org/10.3390/molecules22091441
dc.identifier.citationMolecules. Basel, v. 22, n. 9, p. -, 2017.
dc.identifier.doi10.3390/molecules22091441
dc.identifier.fileWOS000411499400046.pdf
dc.identifier.issn1420-3049
dc.identifier.urihttp://repositorio.unifesp.br/handle/11600/51284
dc.identifier.wosWOS:000411499400046
dc.language.isoeng
dc.publisherMdpi Ag
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectrhamnetinen
dc.subjectmethylated quercetinsen
dc.subjectphospholipase A2en
dc.subjectanti-inflammatoryen
dc.subjectBothrops jararacussuen
dc.titleEvaluation of Rhamnetin as an Inhibitor of the Pharmacological Effect of Secretory Phospholipase A2en
dc.typeinfo:eu-repo/semantics/article
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