Isolation and identification of β-hematin inhibitors from Flacourtia indica as promising antiplasmodial agents

Abstract

An ethanolic extract (A001) of the leaves and twigs of Flacourtia indica (Burm.f.) Merr., was purified to give a new phenolic glycoside, 2-(2-benzoyl-β-glucopyranosyloxy)-7-(1α, 2α, 6α -trihydroxy-3-oxocyclo-hex-4-enoyl)-5-hydroxybenzyl alcohol (1 ) together with poliothrysoside (2), catechin-[5,6-e]-4β-(3,4-dihydroxyphenyl)-dihydro-2(3H)-pyranone (3), 2-(6-benzoyl-β-glucopyranosyloxy)-7-(1α, 2α, 6α-trihydroxy-3-oxocyclo-hex-4-enoyl)-5-hydroxybenzyl alcohol (4), chrysoeriol-7-O-β-D-glucopyranoside (5) and mururin A (6). Compound 6 significantly inhibited the in vitro growth of both a chloroquine-sensitive (3D7) and a chloroquine-resistant (K1) strain of Plasmodium falciparum. It forms a complex with hematin and inhibits the β-hematin formation, suggesting that this compound act on a heme polymerization target.