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Molecules 2017, 22(9), 1441; doi:10.3390/molecules22091441

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

1
Postgraduate Program in Food, Nutrition and Health, Federal University of São Paulo, Santos 11015-020, São Paulo, Brazil
2
Bioscience Institute, Paulista State University, São Vicente 11330-900, São Paulo, Brazil
3
Pro-rector of Research, Brazil University, Itaquera 08230-030, São Paulo, Brazil
4
Pathology Laboratory of Infectious Diseases (LIM50), Department of Pathology, Medical School of the University of São Paulo, São Paulo 01246-903, Brazil
*
Author to whom correspondence should be addressed.
Received: 25 July 2017 / Revised: 28 August 2017 / Accepted: 29 August 2017 / Published: 31 August 2017
(This article belongs to the Special Issue Phospholipases and Lipases: Targets for Drug Development)
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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. View Full-Text
Keywords: rhamnetin; methylated quercetins; phospholipase A2; anti-inflammatory; Bothrops jararacussu rhamnetin; methylated quercetins; phospholipase A2; anti-inflammatory; Bothrops jararacussu
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Novo Belchor, M.; Hessel Gaeta, H.; Fabri Bittencourt Rodrigues, C.; Ramos da Cruz Costa, C.; de Oliveira Toyama, D.; Domingues Passero, L.F.; Dalastra Laurenti, M.; Hikari Toyama, M. Evaluation of Rhamnetin as an Inhibitor of the Pharmacological Effect of Secretory Phospholipase A2. Molecules 2017, 22, 1441.

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