2. Academic Validation
  3. 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

  • Molecules. 2017 Aug 31;22(9):1441. doi: 10.3390/molecules22091441.
Mariana Novo Belchor 1 2,  Henrique Hessel Gaeta 3,  Caroline Fabri Bittencourt Rodrigues 4,  Caroline Ramos da Cruz Costa 5,  Daniela de Oliveira Toyama 6,  Luiz Felipe Domingues Passero 7,  Marcia Dalastra Laurenti 8,  Marcos Hikari Toyama 9
Affiliations

Affiliations

  • 1 Postgraduate Program in Food, Nutrition and Health, Federal University of São Paulo, Santos 11015-020, São Paulo, Brazil. [email protected].
  • 2 Bioscience Institute, Paulista State University, São Vicente 11330-900, São Paulo, Brazil. [email protected].
  • 3 Bioscience Institute, Paulista State University, São Vicente 11330-900, São Paulo, Brazil. [email protected].
  • 4 Bioscience Institute, Paulista State University, São Vicente 11330-900, São Paulo, Brazil. [email protected].
  • 5 Bioscience Institute, Paulista State University, São Vicente 11330-900, São Paulo, Brazil. [email protected].
  • 6 Pro-rector of Research, Brazil University, Itaquera 08230-030, São Paulo, Brazil. [email protected].
  • 7 Bioscience Institute, Paulista State University, São Vicente 11330-900, São Paulo, Brazil. [email protected].
  • 8 Pathology Laboratory of Infectious Diseases (LIM50), Department of Pathology, Medical School of the University of São Paulo, São Paulo 01246-903, Brazil. [email protected].
  • 9 Bioscience Institute, Paulista State University, São Vicente 11330-900, São Paulo, Brazil. [email protected].
PMID: 28858248 DOI: 10.3390/molecules22091441
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

Bothrops jararacussu; anti-inflammatory; methylated quercetins; phospholipase A2; rhamnetin.

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