Abstract

The persistent increase of resistance to existing antimalarials underscores the needs for new drugs. Historically, most of the successful antimalarial are derived from plants. The leaves of the S. cymosum is one of the plant materials used by traditional healers in malaria-endemic areas in Bangladesh for treatment of malaria. Here, we investigated the crude extract and its fractions against chloroquine (CQ)-sensitive 3D7, CQ-resistant Dd2, and artemisinin (ART)-resistant IPC 4912 Mondulkiri strains of Plasmodium falciparum. The antimalarial activities were tested using HRP II based in-vitro antimalarial drug sensitivity ELISA described by WWARN and half inhibitory concentrations (IC50) were calculated by non-linear regression analysis using GraphaPad Prism. The cytotoxicity of the crude methanolic extract was assessed using the MTT assay on Vero cell line. The methanolic crude extract revealed promising activity against 3D7 (IC50 6.28 µg/mL), Dd2 (IC50 13.42 µg/mL), and moderate activity against IPC 4912 Mondulkiri (IC50 17.47 µg/mL). Among the fractionated portions, the chloroform fraction revealed highest activity against IPC 4912 Mondulkiri (IC50 1.65 µg/mL) followed by Dd2 (1.73 µg/mL) and 3D7 (2.39 µg/mL). The crude methanolic extract also demonstrated good selectivity with the selectivity indices of > 15.92, > 7.45, and > 6.91 against 3D7, Dd2, and IPC 4912, respectively when tested against Vero cell line. This is the first report on S. cymosum for its putative antimalarial activity, and is imperative to go for further phytochemical analyses in order to investigate possible novel antimalarial drug compound(s).

Highlights

  • The persistent increase of resistance to existing antimalarials underscores the needs for new drugs

  • 6.28 μg/mL against 3D7 strain, 13.42 μg/mL against Dd2, and 17.47 μg/mL against IPC 4912 Mondulkiri, the crude extract was undertaken for further solvent-solvent fractionation which yielded three different fractions of n-hexane, chloroform, and the left over aqueous methanol

  • These fractions were applied to 3D7 strain and gave the IC50s of 3.47, 2.39, and 7.60 respectively at the μg/mL level (Table 1)

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Summary

Introduction

The persistent increase of resistance to existing antimalarials underscores the needs for new drugs. The leaves of the S. cymosum is one of the plant materials used by traditional healers in malariaendemic areas in Bangladesh for treatment of malaria. We investigated the crude extract and its fractions against chloroquine (CQ)sensitive 3D7, CQ-resistant Dd2, and artemisinin (ART)-resistant IPC 4912 Mondulkiri strains of Plasmodium falciparum. The crude methanolic extract demonstrated good selectivity with the selectivity indices of > 15.92, > 7.45, and > 6.91 against 3D7, Dd2, and IPC 4912, respectively when tested against Vero cell line. Consistent high prevalence of CQ resistance in Chittagong Hill Tracts of Bangladesh [3], accentuate the needs for new antimalarial in the near future as an alternative to ACTs failure. We attempted to investigate the antimalarial properties of a Bangladeshi plant, Syzygium cymosum, locally known as Khudijam

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