Bioassay-Guided Isolation of Antiplasmodial Compounds from Hypericum lanceolatum Lam. (Hypericaceae) and Their Cytotoxicity and Molecular Docking.

Autor: Happi GM; Department of Chemistry, Higher Teacher Training College, The University of Bamenda, P.O. Box 39, Bambili, Cameroon., Ahmed SA; Department of Chemistry and Industrial Chemistry, Kwara State University, Malete, P.M.B 1530, Ilorin 23431, Nigeria., Kemayou GPM; Department of Organic Chemistry, Faculty of Sciences, University of Yaounde I, P.O. Box 812, Yaounde, Cameroon., Salau S; Department of Chemistry and Industrial Chemistry, Kwara State University, Malete, P.M.B 1530, Ilorin 23431, Nigeria., Dzouemo LC; Department of Chemistry, Faculty of Sciences, University of Douala, P.O. Box 24157, Douala, Cameroon., Sikam KG; Department of Chemistry, Faculty of Sciences, University of Douala, P.O. Box 24157, Douala, Cameroon., Yimtchui MT; Department of Chemistry, Faculty of Sciences, University of Douala, P.O. Box 24157, Douala, Cameroon., Wansi JD; Department of Chemistry, Faculty of Sciences, University of Douala, P.O. Box 24157, Douala, Cameroon.
Jazyk: angličtina
Zdroj: BioMed research international [Biomed Res Int] 2023 May 29; Vol. 2023, pp. 4693765. Date of Electronic Publication: 2023 May 29 (Print Publication: 2023).
DOI: 10.1155/2023/4693765
Abstrakt: 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 IC 50 values of 2.8 ± 0.8  μ g/mL and 11.8 ± 3.2  μ g/mL, respectively. Furthermore, both compounds were also the most cytotoxic against P388 cell lines with IC 50 values of 6.8 ± 2.2  μ g/mL and 2.5 ± 0.6  μ g/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.
Competing Interests: The authors declare that they have no conflicts of interest.
(Copyright © 2023 Gervais Mouthé Happi et al.)
Databáze: MEDLINE
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