“Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies”
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Date
2024-10
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Elsevier
Abstract
Malaria claims over 600,000 deaths annually with a disproportionately high burden in the WHO
African Region. The development of parasite resistance has warranted the search for novel anti plasmodial drug candidates. This research aimed at validating the efficacy of Senegalia atax acantha and tracking down its bioactive constituents. In vivo antiplasmodial activity of the extract
was assessed using suppressive and curative protocols. Yeast-induced pyrexia was employed to evaluate the antipyretic activity of the extract. In vitro anti-plasmodial activity of isolated compounds was done using SYBR green I fluorescence assay on chloroquine sensitive (3D7) and
resistant (Dd2) strains of P falciparum. In silico pharmacokinetic and interactions with parasites lactate dehydrogenase predictions of isolated compounds was conducted through molecular docking studies. Ethanol (70 %) extract of the plant showed in vitro and in vivo anti-plasmodial
effect. The extract demonstrated significant (p < 0.05) dose-dependent suppression of 63.39 % and 63.32 % respectively at the highest dose (300 mg kg-1). Artesunate (4 mg kg-1/day) had considerably better curative potential (85.25%). The compounds showed in vitro anti-plasmodial
activity in the order lupeol> friedelin/ friedelinol mixture>friedelin>β-sitosterol based on IC50 measurement. Friedelinol and lupeol exhibited higher binding affinities with pfLDH compared to Chloroquine. The extract and acetaminophen (positve control) showed significant (p < 0.05)
reduction in rectal temperature compared to the control group. In silico studies of the compounds revealed moderate interactions with some cytochrome P450 metabolizing enzymes.
Description
This article is published by Elsevier, 2024 and is also available at https://doi.org/10.1016/j.sciaf.2024.e02455
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Citation
Scientiϧc African 26 (2024) e02455