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

• Published in: Fitoterapia Vol. 151; p. 104869
• Main Authors: Ma'mag, Larissa Kom, Zintchem, Auguste Abouem A, Théodora, Kopa Kowa, Atchadé, Alex de Théodore, Lauve, Tchokouaha Yamthe, Frédérich, Michel, Bikobo, Dominique Serge Ngono, Pegnyemb, Dieudonné Emmanuel
• Format: Journal Article Web Resource
• Language: English
• Published: Netherlands Elsevier B.V 01.06.2021; Elsevier Science Ltd; Elsevier
• Subjects: Alkaloids; Antileishmanial activity; Antimalarial agents; Antiparasitic agents; Antiplasmodial activity; Antiprotozoal agents; Apocynaceae; Elastica; Funtumia elastica; Human health sciences; NMR; Nuclear magnetic resonance; Pharmacie, pharmacologie & toxicologie; Pharmacy, pharmacology & toxicology; Promastigotes; Sciences de la santé humaine; Steroidal alkaloids; Triterpenes; Ursane triterpenes; Apocynaceae; Antiplasmodial activity; Ursane triterpenes; Steroidal alkaloids; Funtumia elastica; Antileishmanial activity
• ISSN: 0367-326X; 1873-6971
• DOI: 10.1016/j.fitote.2021.104869

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. [Display omitted] •Isolation of four undescribed compounds from the leaves of Funtumia elastica.•They possess ursane type triterpenoid and dihydroconessine derivative type alkaloid.•Their structures were elucidated using IR, MS, 1H and 13C NMR, 1D and 2D.•In vitro evaluation of these compounds for antiplasmodial and antileishmanial activities.•Compounds 1 and 2 were the most potent antitplasmodial and antileishmanial agents.