Lidya Tumewu, Hilkatul Ilmi, Ratih Dewi Saputri, Defi Kartika Sari, Adita Ayu Permanasari, Hanifah Khairun Nisa, Saipul Maulana, Tjitjik Srie Tjahjandarie, Mulyadi Tanjung, Che Puteh Osman, Nor Hadiani Ismail, Aty Widyawaruyanti, Achmad Fuad Hafid
Aims: To investigate the potential antimalarial plant belonging to the Artocarpus genus, Artocarpus sericicarpus, and isolate the antimalarial active compound from leaves extract. Methods: The isolation of the antimalarial compound was based on bioassay-guided isolation. The compound isolation was conducted by chromatography and identified using spectroscopic techniques, including1H,13C, and 2D NMR. The compound was tested for its antimalarial activity against Plasmodium falciparum and evaluated for cytotoxicity using several cell lines, including Huh7, HepG2, BHK-21, and Vero cells. In silico investigation of the compound against falcipain-2 protein was conducted as well. Results: Fractionation and purification of dichloromethane leaves extract led to the isolation of a dihydrochalcone compound identified as 1-(2,4-dihydroxyphenyl)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]propan-1-one. The dihydrochalcone compound exhibited antimalarial activity with an IC50 value of 34.80 µM. Cytotoxicity test revealed CC50 values of the compound were more than 20 µg/mL, and the selectivity indexes (SI) were 4.50, 5.52, 3.02, and 6.68 on Huh7, HepG2, BHK-21, and Vero cells, respectively. The CC50 and SI indicated the nontoxic criteria of the compound. In silico investigation showed that the compound could bind to the falcipain-2 active sites. Conclusions: The dihydrochalcone compound identified as 1-(2,4-dihydroxyphenyl)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]propan-1-one was isolated from Artocarpus sericicarpus leaves extract showed antimalarial activity and the ability to bind to the falcipain-2 active sites on in silico investigation. © 2023 Journal of Pharmacy & Pharmacognosy Research, 11 (5), 797-809, 2023 ISSN 0719-4250 https://jppres.com.
Doctoral Program, Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia; Natural Product Medicine Research and Development, Institute of Tropical Disease, Universitas Airlangga, Surabaya, Indonesia; Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Negeri Surabaya, Surabaya, Indonesia; Master of Pharmaceutical Sciences, Faculty of Pharmacy, Airlangga University, Indonesia; Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Tadulako University, Central Sulawesi, Indonesia; Natural Product Chemistry Research Group, Organic Chemistry Division, Department of Chemistry, Faculty of Science and Technology, Universitas Airlangga, Surabaya, Indonesia; Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA, Cawangan Selangor, Kampus Puncak Alam, Selangor, Bandar Puncak Alam, 42300, Malaysia; Faculty of Applied Sciences, Universiti Teknologi MARA, Selangor, Shah Alam, 40450, Malaysia; Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Surabaya, Indonesia
