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

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Date
2017
Author
Belchor, Mariana Novo [UNIFESP]
Gaeta, Henrique Hessel
Bittencourt Rodrigues, Caroline Fabri
da Cruz Costa, Caroline Ramos
Toyama, Daniela de Oliveira
Domingues Passero, Luiz Felipe
Laurenti, Marcia Dalastra
Toyama, Marcos Hikari
Type
Artigo
ISSN
1420-3049
DOI
10.3390/molecules22091441
Metadata
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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.
 
Citation
Molecules. Basel, v. 22, n. 9, p. -, 2017.
Keywords
rhamnetin
methylated quercetins
phospholipase A2
anti-inflammatory
Bothrops jararacussu
Sponsorship
Universidade Estadual Paulista (UNESP)
Universidade Federal de São Paulo (UNIFESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
URI
http://repositorio.unifesp.br/handle/11600/51284
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  • EPM - Artigos [17701]

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