Anti- activity of clerodane diterpenes and their methyl ester derivatives from (Alismataceae).

Journal: Natural product research
Published Date:

Abstract

The effect of the EtOAc extract of leaves against (trypomastigotes) was evaluated . As this extract caused 100% parasite reduction (at 300 µg/mL), it was subjected to chromatographic fractionation to obtain two related diterpenes, clerodermic () and patagonic () acids. Both compounds showed antiparasitic potential against with EC of 41.7 µM (trypo)/60.7 µM (ama) and 37.6 µM (trypo)/73.1 µM (ama), respectively. Considering that the antiparasitic activity of carboxylic acid diterpenoids may be enhanced after esterification, methylation of both compounds was performed. The EC values for methyl esters and were determined to be 19.7 µM (trypo)/7.5 µM (ama) and 21.8 µM (trypo)/9.3 µM (ama), respectively. Based on the potency of the methyl esters, they may be future candidates for optimisation studies to design new drugs for treatment of Chagas' disease.

Authors

  • Mariana Magalhães Borges
    School of Engineering, Mackenzie Presbyterian University, São Paulo, Brazil.
  • João Pedro Valdo Moriconi
    School of Engineering, Mackenzie Presbyterian University, São Paulo, Brazil.
  • Amanda Oliveira de Pinho
    School of Engineering, Mackenzie Presbyterian University, São Paulo, Brazil.
  • Vinicius Silva Londero
    Center for Natural and Human Sciences, Federal University of ABC, Santo Andre, Brazil.
  • Andre G Tempone
    Laboratory of Pathophysiology, Butantan Institute, São Paulo, Brazil.
  • João Henrique G Lago
    Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Diadema 09972-270, SP, Brazil. joao.lago@unifesp.br.
  • Edgard Antonio Ferreira
    School of Engineering, Mackenzie Presbyterian University, São Paulo, Brazil.

Keywords

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