Antimalarial activity of flavonoid compound isolated from leaves of artocarpus altilis

Introduction: Artocarpus altilis leaves extract has previously been reported as a potential antimalarial drug. Inhibition concentration (IC₅₀) against P. falciparum and effective dose values (ED₅₀) against P. berghei have been reported at 1.32 µg/ml and 0.82 mg/kg, respectively. The aim of this study is to identify the active compound from the ethanol extract of A. Altilis leaves against P. falciparum. Materials and Methods: The isolation of the active compound from the ethanol extract of A. altilis were conducted using chromatography methods, and the chemical structure of the isolated compounds was determined based on NMR and MS spectra data. Antimalarial assay was determined using microscopic method against P. falciparum 3D7 and molecular docking studies was performed using Molegro Virtual Docker version 5.5 program. Results: A flavonoid compound, class of dihydrochalcone was finally isolated from A. altilis and identified as 1-(2,4-dihydroxy phenyl)-3-[8-hydroxy-2-methyl-2-(4-methyl-3-pentenyl)-2H-1-benzopyran-5-yl]-1-propanone (Compound-1). Antimalarial activity test revealed that the compound strongly inhibited P. falciparum growth, with IC₅₀ value of 1.05 μM. An in silico study to determine the mechanism of action of the compound revealed the existence a 3.BPF receptor that possesses a cysteine protease inhibitor of falcipain-2. Conclusion: Compound-1 were isolated from the leaves of A. Altilis is a good candidate of new source in the development of antimalarial drugs. An animal study using this compound is recommended before a clinical trial.