Antiplasmodial procyanidins derivatives from Chinese Hawthorn.

The methanolic extract of the leaves of Chinese Hawthorn was investigated for its activity against chloroquine-sensitive strains of Plasmodium falciparum using the method of parasite lactate dehydrogenase assay. Four oligomeric procyanidins, such as epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin ( 1), epicatechin-(4β→8)-epicatechin-(4β→6)-epicatechin ( 2), epicatechin-(4β→6)-epicatechin-(4β→8)-epicatechin ( 3), and epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin-(4β→8) ( 4), were isolated and evaluated for in vitro antiplasmodial activity, as well as for their cytotoxic potential on SK-OV-3 cancer cell lines. Three procyanidins showed notable growth inhibitory activity against chloroquine-sensitive strains of P. falciparum with IC50 values of 2.7 μM (SI values of >55.5). The compounds showed no significant cytotoxicity (IC50 > 150 μM) toward the SK-OV-3 cancer cell line. This is the first report on the antiplasmodial activity of these oligomeric procyanidins from Chinese Hawthorn. [ABSTRACT FROM AUTHOR]