TY - JOUR KW - Diterpenes KW - Trypanosoma cruzi KW - Clerodane KW - NCTC cells KW - Echinodorus grandiflorus AU - Borges MM AU - Moriconi JPV AU - de Pinho AO AU - Londero VS AU - Tempone AG AU - Lago JHG AU - Ferreira EA AB -

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.

BT - Natural Product Research DO - 10.1080/14786419.2025.2500732 LA - eng M3 - Research Article N2 -

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.

PB - Informa UK Limited PY - 2025 SP - 1 EP - 6 T2 - Natural Product Research TI - Anti-Trypanosoma cruzi activity of clerodane diterpenes and their methyl ester derivatives from Aquarius grandiflorus (Alismataceae) UR - https://www.tandfonline.com/doi/full/10.1080/14786419.2025.2500732 SN - 1478-6419, 1478-6427 ER -