Antiplasmodial and antileishmanial inhibitory activity of triterpenes and steroidal alkaloid from the leaves of Funtumia elastica (Preuss) Stapf (Apocynaceae)

Abstract

The phytochemical study of leaves of Funtumia elastica led to the isolation of three undescribed ursane derivatives, funtumic acids A, B and C (1-3), as well as one steroidal alkaloid, elasticine (4) and five other known compounds (5-9). Their structures were elucidated on the basis of NMR, MS, IR, UV spectroscopic data as well as by comparison with the literature. The compound 5-hydroxypyridine-3-carboxamide (9) was isolated for the first time from the Apocynaceae family. All the isolated compounds were evaluated for their antiparasitic effects against 3D7 and Dd2 strains of Plasmodium falciparum and promastigotes of Leishmania donovani (MHOM/SD/62/1S). Compounds 1-4 possessed good in vitro antimalarial activities against CQR Dd2 with IC₅₀ values ranging from 4.68 to 5.36 μg/mL and moderate on CQS 3D7. Only compounds 1 and 2 showed leishmanicidal activities with IC₅₀ values ranging between 10.49 and 13.21 μg/mL. In addition, crude extract exhibited potent antiplasmodial (IC₅₀ 0.91 and 3.12 μg/mL) and antileishmanial (IC₅₀ 3.32 μg/mL) activities, thus demonstrating their potential synergistic action.

Keywords: Antileishmanial activity; Antiplasmodial activity; Apocynaceae; Funtumia elastica; Steroidal alkaloids; Ursane triterpenes.