In vivo and in vitro antimalarial activity of bergenin

Malaria is a potentially life-threatening protozoal parasitic disease transmitted by female Anopheles mosquitoes. Drug therapy is currently the most widely used method for the control and treatment of this disease. Several plants were found to contain substances possessing antimalarial properties. In this study, we investigated the antimalarial activity of bergenin, a sesquiterpene lactone compound derived from Rodgersia aesculifolia Batal. The results indicated that bergenin effectively inhibited Plasmodium falciparum growth in vitro (IC₅₀, 14.1 μg/ml, with ~100% inhibition at 50 μg/ml), without apparent cytotoxicity to erythrocytes or to mammalian HeLa and HepG2 cells. Bergenin exhibited less cytotoxic activity and the selectivity index (SI) was 887 and 1,355 for HeLa and HepG2 cells, respectively. The administration of bergenin to Plasmodium berghei-infected mice for 6 days significantly inhibited the growth of the parasites. Taken together, these findings provide evidence that bergenin may be a promising novel drug for antimalarial treatment.