Bioassay-Guided Isolation of Antiplasmodial Compounds from Hypericum lanceolatum Lam. (Hypericaceae) and Their Cytotoxicity and Molecular Docking
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Date
2023
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Abstract
In Cameroon, malaria is still the cause of several deaths yearly and leading to the continued search for new potent leads to fight
against Plasmodium falciparum. Medicinal plants like Hypericum lanceolatum Lam. are introduced in local preparations for the
treatment of affected people. The bioassay-guided fractionation of the crude extract of the twigs and stem bark of H.
lanceolatum Lam. led to the identification of the dichloromethane-soluble fraction as the most active (with 32.6% of the
parasite P. falciparum 3D7 survival) which was further purified by successive column chromatography to obtain four
compounds identified by their spectrometric data as two xanthones 1,6-dihydroxyxanthone (1) and norathyriol (2) and two
triterpenes betulinic acid (3) and ursolic acid (4). In the antiplasmodial assay against P. falciparum 3D7, the triterpenoids 3
and 4 displayed the most significant potencies with IC50 values of 2:8 ± 0:8 μg/mL and 11:8 ± 3:2 μg/mL, respectively.
Furthermore, both compounds were also the most cytotoxic against P388 cell lines with IC50 values of 6:8 ± 2:2 μg/mL and 2:5
± 0:6 μg/mL, respectively. Further insights on the inhibition method of the bioactive compounds and their drug-likeness were
obtained from their molecular docking and ADMET studies. The results obtained help in identifying additional antiplasmodial
agents from H. lanceolatum and support its use in folk medicine for the treatment of malaria. The plant might be considered
as a promising source of new antiplasmodial candidates in new drug discovery.