Pesquisa | SciELO

Poincianella pluviosa is a tree whose stem bark is reputed to have antidiarrheal, wound healing, antitumoral and antimalarial properties. Considering that the leaves of the tree are a more abundant and renewable source than the stem bark, we chose to study the antimalarial potential of this organ part. The aqueous leaf extract exhibited a rich phenolic profile. It was active (IC50= 6.88 ± 1.64 µg mL-1) against chloroquine resistant Plasmodium falciparum (W2) without toxicity to HepG2 A16 cells. The organic fraction was more active (IC50= 1.83 µg mL-1) than the aqueous leaf extract itself. Ten phenolic compounds were obtained from the latter. This is the first report on the phenolic composition of P. pluviosa leaves. Ellagic acid (IC50= 0.215 ± 0.007 µg mL-1) proved to be 32 fold more active than the aqueous leaf extract itself. Considering their renewable aspect, leaves of P. pluviosa appear to be a more interesting source of antimalarial compounds than stem bark.

We herein report the synthesis of hybrid kauranoid molecules of type 1,2,3-triazole-1,4-disubstituted aiming to improve the antimalarial activity of kaurenoic and xylopic acids. The CuI-catalyzed cycloaddition of azides and kauranoid terminal alkynes was explored as a hybridization strategy. Kauranoid terminal alkynes were prepared from kaurenoic and xylopic acids that were isolated from Wedelia paludosa D. C. (Asteraceae) and Xylopia frutescens Aubl. (Annonaceae). A total of 15 kauranoid derivatives, including nine new triazoles, were obtained and five out of these were more active than the original diterpenes. Interestingly, an increased activity was observed for a kauranoid propargyl ether. Interaction between ent-kaurane diterpene derivatives and Ca2+-ATPase (PfATP6) was investigated. Synthesis of diterpene derivatives emerges as a possible route to be explored in the quest of potentially new inhibitors of PfATP6.

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