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

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

Author Belchor, Mariana Novo Autor UNIFESP Google Scholar
Gaeta, Henrique Hessel Google Scholar
Bittencourt Rodrigues, Caroline Fabri Google Scholar
da Cruz Costa, Caroline Ramos Google Scholar
Toyama, Daniela de Oliveira Google Scholar
Domingues Passero, Luiz Felipe Google Scholar
Laurenti, Marcia Dalastra Google Scholar
Toyama, Marcos Hikari Google Scholar
Abstract 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.
Keywords rhamnetin
methylated quercetins
phospholipase A2
Bothrops jararacussu
Language English
Sponsor Universidade Estadual Paulista (UNESP)
Universidade Federal de São Paulo (UNIFESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Date 2017
Published in Molecules. Basel, v. 22, n. 9, p. -, 2017.
ISSN 1420-3049 (Sherpa/Romeo, impact factor)
Publisher Mdpi Ag
Extent -
Origin http://dx.doi.org/10.3390/molecules22091441
Access rights Open access Open Access
Type Article
Web of Science ID WOS:000411499400046
URI http://repositorio.unifesp.br/handle/11600/51284

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