01935nas a2200265 4500000000100000008004100001260002300042653001500065653002200080653001400102653001500116653002900131100001400160700001700174700001600191700001500207700001500222700001300237700001600250245013700266856007100403300000800474520116200482022002501644 2025 d bInforma UK Limited10aDiterpenes10aTrypanosoma cruzi10aClerodane10aNCTC cells10aEchinodorus grandiflorus1 aBorges MM1 aMoriconi JPV1 ade Pinho AO1 aLondero VS1 aTempone AG1 aLago JHG1 aFerreira EA00aAnti-Trypanosoma cruzi activity of clerodane diterpenes and their methyl ester derivatives from Aquarius grandiflorus (Alismataceae) uhttps://www.tandfonline.com/doi/full/10.1080/14786419.2025.2500732 a1-63 a
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.
a1478-6419, 1478-6427