Antiplasmodial activity of Hyptis pectinata extract and its analogue against 3D7 Plasmodium falciparum through caseinolytic protease proteolytic (ClpP) inhibition:(TJPS-2021-0001.R1)

Abstract

Hyptolide and epoxy hyptolide was successfully isolate and synthesize from Hyptis pectinata extract that potential to cure malaria diseases. The previous studies showed that these compounds contain lactone groups associated with antibacterial and anticancer activity. However, the antimalaria activity remains unclear. Therefore, in this study aims to investigate the antiplasmodial activity of Hyptis pectinata extract, hyptolide, and epoxy hyptolide. These compounds were tested in vitro for antiplasmodial activity against chloroquine‑sensitive 3D7 strain of Plasmodium falciparum. Thin blood smears were used to assess the levels of parasitemia and growth inhibition of the isolates and the ClpP inhibition was analyze under well diffusion assay using Plasmodium knowlesi. The results showed that hyptolide, epoxy hyptolide and Hyptis pectinata extracts potential inhibit proliferation of Plasmodium falciparum in doses-dependent manner with IC50 value of 2.06; 2.75; and 11.84 µg/ml, respectively. Further inhibition assay towards Pk-ClpP revealed that hyptolide (δ-lactone) more potent than β-lactone and PMSF demonstrated remarkable inhibition activity in doses-dependent manner. The results suggest that hyptolide have antiplasmodial activity thro