1. Antiplasmodial and antileishmanial flavonoids from Mundulea sericea.
- Author
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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, and Yenesew A
- Subjects
- Antimalarials isolation & purification, Antineoplastic Agents, Phytogenic isolation & purification, Antiprotozoal Agents isolation & purification, Cell Line, Tumor, Flavonoids, Humans, Kenya, Molecular Structure, Nitric Oxide metabolism, Phytochemicals isolation & purification, Phytochemicals pharmacology, Plant Leaves chemistry, Plant Roots chemistry, Plasmodium falciparum drug effects, Antimalarials pharmacology, Antineoplastic Agents, Phytogenic pharmacology, Antiprotozoal Agents pharmacology, Fabaceae chemistry
- 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
50 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 IC50 values of 9.0 and 5.0 μM, respectively. In a cytotoxicity assay, lupinifolin (3) showed significant activity on BEAS-2B (IC50 4.9 μM) and HePG2 (IC50 10.8 μM) human cell lines. All the other compounds showed low cytotoxicity (IC50 > 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)., (Copyright © 2020 The Authors. Published by Elsevier B.V. All rights reserved.)- Published
- 2021
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