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Antiplasmodial and antileishmanial flavonoids from Mundulea sericea.

Authors :: Chepkirui C
Ochieng PJ
Sarkar B
Hussain A
Pal C
Yang LJ
Coghi P
Akala HM
Derese S
Ndakala A
Heydenreich M
Wong VKW
Erdélyi M
Yenesew A
Source :: Fitoterapia [Fitoterapia] 2021 Mar; Vol. 149, pp. 104796. Date of Electronic Publication: 2020 Nov 30.
Publication Year :: 2021
Abstract: Five known compounds (1-5) were isolated from the extract of Mundulea sericea leaves. Similar investigation of the roots of this plant afforded an additional three known compounds (6-8). The structures were elucidated using NMR spectroscopic and mass spectrometric analyses. The absolute configuration of 1 was established using ECD spectroscopy. In an antiplasmodial activity assay, compound 1 showed good activity with an IC <subscript>50</subscript> of 2.0 μM against chloroquine-resistant W2, and 6.6 μM against the chloroquine-sensitive 3D7 strains of Plasmodium falciparum. Some of the compounds were also tested for antileishmanial activity. Dehydrolupinifolinol (2) and sericetin (5) were active against drug-sensitive Leishmania donovani (MHOM/IN/83/AG83) with IC <subscript>50</subscript> values of 9.0 and 5.0 μM, respectively. In a cytotoxicity assay, lupinifolin (3) showed significant activity on BEAS-2B (IC <subscript>50</subscript> 4.9 μM) and HePG2 (IC <subscript>50</subscript> 10.8 μM) human cell lines. All the other compounds showed low cytotoxicity (IC <subscript>50</subscript>  > 30 μM) against human lung adenocarcinoma cells (A549), human liver cancer cells (HepG2), lung/bronchus cells (epithelial virus transformed) (BEAS-2B) and immortal human hepatocytes (LO2).<br /> (Copyright © 2020 The Authors. Published by Elsevier B.V. All rights reserved.)