Anti-Trypanosoma cruzi activity of clerodane diterpenes and their methyl ester derivatives from Aquarius grandiflorus (Alismataceae)
Tipo
Artigo
Data de publicação
2025
Periódico
Natural Product Research
Citações (Scopus)
0
Autores
Borges M.M.
Moriconi J.P.V.
de Pinho A.O.
Londero V.S.
Tempone A.G.
Lago J.H.G.
Ferreira E.A.
Moriconi J.P.V.
de Pinho A.O.
Londero V.S.
Tempone A.G.
Lago J.H.G.
Ferreira E.A.
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Resumo
© 2025 Informa UK Limited, trading as Taylor & Francis Group.The effect of the EtOAc extract of Aquarius grandiflorus leaves against Trypanosoma cruzi (trypomastigotes) was evaluated in vitro. As this extract caused 100% parasite reduction (at 300 µg/mL), it was subjected to chromatographic fractionation to obtain two related diterpenes, clerodermic (1) and patagonic (2) acids. Both compounds showed antiparasitic potential against T. cruzi with EC50 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 EC50 values for methyl esters 1a and 2a 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.