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

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Arquivos
art_BELCHOR_Evaluation_of_Rhamnetin_as_an_Inhibitor_of_the_2017.PDF (1.15 MB)
Citações na Scopus
27
Tipo de produção
article
Data de publicação
2017
DOI
Scopus
Web of Science
PubMed
Título da Revista
ISSN da Revista
Título do Volume
Editora
MDPI AG
Autores
BELCHOR, Mariana Novo
GAETA, Henrique Hessel
RODRIGUES, Caroline Fabri Bittencourt
COSTA, Caroline Ramos da Cruz
TOYAMA, Daniela de Oliveira
PASSERO, Luiz Felipe Domingues
TOYAMA, Marcos Hikari
Citação
MOLECULES, v.22, n.9, article ID 1441, 13p, 2017
Projetos de Pesquisa
Unidades Organizacionais
Fascículo
Resumo
Rhamnetin (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.
Palavras-chave
rhamnetin, methylated quercetins, phospholipase A2, anti-inflammatory, Bothrops jararacussu
URI
https://observatorio.fm.usp.br/handle/OPI/22024
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Coleções
Artigos e Materiais de Revistas Científicas - FM/MPT
Artigos e Materiais de Revistas Científicas - LIM/50