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

dc.contributor.authorBelchor, Mariana Novo [UNESP]
dc.contributor.authorGaeta, Henrique Hessel [UNESP]
dc.contributor.authorBittencourt Rodrigues, Caroline Fabri [UNESP]
dc.contributor.authorCruz Costa, Caroline Ramos da [UNESP]
dc.contributor.authorToyama, Daniela de Oliveira
dc.contributor.authorDomingues Passero, Luiz Felipe [UNESP]
dc.contributor.authorLaurenti, Marcia Dalastra
dc.contributor.authorToyama, Marcos Hikari [UNESP]
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionBrazil Univ
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.date.accessioned2018-11-28T21:36:46Z
dc.date.available2018-11-28T21:36:46Z
dc.date.issued2017-09-01
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 inflammation; therefore, 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 Sao Paulo, Postgrad Program Food Nutr & Hlth, BR-11015020 Sao Paulo, Brazil
dc.description.affiliationUniv Estadual Paulista, Biosci Inst, BR-11330900 Sao Paulo, Brazil
dc.description.affiliationBrazil Univ, Prorector Res, BR-08230030 Sao Paulo, Brazil
dc.description.affiliationUniv Sao Paulo, Pathol Lab Infect Dis LIM50, Dept Pathol, Sch Med, BR-01246903 Sao Paulo, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Biosci Inst, BR-11330900 Sao Paulo, Brazil
dc.description.sponsorshipUNESP
dc.description.sponsorshipUNIFESP
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.format.extent13
dc.identifierhttp://dx.doi.org/10.3390/molecules22091441
dc.identifier.citationMolecules. Basel: Mdpi Ag, v. 22, n. 9, 13 p., 2017.
dc.identifier.doi10.3390/molecules22091441
dc.identifier.fileWOS000411499400046.pdf
dc.identifier.issn1420-3049
dc.identifier.lattes8573195327542061
dc.identifier.urihttp://hdl.handle.net/11449/165804
dc.identifier.wosWOS:000411499400046
dc.language.isoeng
dc.publisherMdpi Ag
dc.relation.ispartofMolecules
dc.relation.ispartofsjr0,855
dc.rights.accessRightsAcesso aberto
dc.sourceWeb of Science
dc.subjectrhamnetin
dc.subjectmethylated quercetins
dc.subjectphospholipase A2
dc.subjectanti-inflammatory
dc.subjectBothrops jararacussu
dc.titleEvaluation of Rhamnetin as an Inhibitor of the Pharmacological Effect of Secretory Phospholipase A2en
dc.typeArtigo
dcterms.rightsHolderMdpi Ag
unesp.advisor.lattes8573195327542061
unesp.author.orcid0000-0001-6836-3084[8]

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