Marmesin isolated from Celtis durandii Engl. root bioactive fraction inhibits β-hematin formation and contributes to antiplasmodial activity
Loading...
Date
2023
Journal Title
Journal ISSN
Volume Title
Publisher
Journal of Ethnopharmacology
Abstract
Ethnopharmacological relevance: Malaria is a leading cause of death in many developing countries, especially in
sub-Saharan Africa. Nigeria is endowed with an abundance of medicinal plants, many of which are used to treat
malaria. Celtis durandii Engl. is one such plant used as a traditional antimalarial remedy in southeast Nigeria.
However, its antiplasmodial potential is poorly explored.
Aim of the study: The study aimed at identifying the antiplasmodial components of C. durandii root extract
through antiplasmodial activity-guided fractionation.
Materials and methods: Dichloromethane/methanol mixture extract (1:1 v/v) of C. durandii root was prepared and
partitioned against water to obtain the organic phase, which was further separated by column chromatography
into nine (C1 – C9) fractions. The antiplasmodial activity was evaluated by in vitro screening of the different
fractions against drug-sensitive and drug-resistant Plasmodium falciparum strains. Further purification of the
active column fractions resulted in a potent anti-Plasmodial compound that was subsequently investigated for its
effect on β-hematin formation. Additionally, the isolated compound was characterized and identified as marmesin using mass spectrometry and nuclear magnetic resonance spectroscopy.
Results: Celtis durandii root extract exhibited promising antiplasmodial activity {IC50 (μg/ml) 5.92, 6.04, and
6.92} against PfW2mef, PfINDO, and Pf3D7 respectively. Pooled fractions with good antiplasmodial activity
{IC50 (μg/ml) Pf3D7: 3.99; PfINDO: 2.24} and selectivity for the parasites (SI: 21) yielded a compound that was
fourteen-fold potent in antiplasmodial activity against Pf3D7(IC50: 0.28 μg/ml). It also inhibited β-hematin
formation with an IC50 = 150 μM. Further studies using spectral data, literature, and chemical databases
identified the purified compound as marmesin.
Conclusion: This work has demonstrated that Celtis durandii root extract has good antiplasmodial activity against
drug-sensitive and drug-resistant P. falciparum. The inhibition of β-hematin formation by marmesin accounts in
part for this activity.
Description
Research Article
Keywords
Antiplasmodial, Celtis durandii, Malaria, Marmesin