| Abstrak/Abstract |
)e previous study showed that xanthone had antiplasmodial activity. Xanthone, with additional hydroxyl groups, was syn-thesized to increase its antiplasmodial activity. One of the strategies to evaluate a compound that can be developed into anantimalarial drug is by testing its mechanism in inhibiting heme polymerization. In acidic condition, hematin can be polymerizedto?-hematinin vitro, which is analog with hemozoin inPlasmodium. )is study was conducted to evaluate the antiplasmodialactivity of hydroxyxanthone derivative compounds on two strains ofPlasmodium falciparum3D-7 and FCR-3, to assess inhibitionof heme polymerization activity and determine the selectivity of hydroxyxanthone derivative compounds. )e antiplasmodialactivity of each compound was tested onPlasmodium falciparum3D-7 and FCR-3 with 72 hours incubation period, triplicated inthree replications with the microscopic method. )e compound that showed the best antiplasmodial activity underwent flowcytometry assay. Heme polymerization inhibition test was performed using the in vitro heme polymerization inhibition activity(HPIA) assay. )e antiplasmodial activity and heme polymerization inhibition activity were expressed as the 50% inhibitoryconcentration (IC50). In vitro cytotoxicity was tested using the MTT assay method on Vero cell lines to determine its selectivityindex. )e results showed that among 5-hydroxyxanthone derivative compounds, the 1,6,8-trihydroxyxanthone had the bestinvitroantiplasmodial activity on both 3D-7 and FCR-3Plasmodium falciparumstrains with IC50values of 6.10±2.01 and6.76±2.38?M, respectively. )e 1,6,8-trihydroxyxanthone showed inhibition activity of heme polymerization with IC50value of2.854 mM and showed the high selectivity with selectivity index of 502.2–556.54. In conclusion, among 5-hydroxyxanthonederivatives tested, the 1,6,8-trihydroxyxantone showed the best antiplasmodial activity and has heme polymerization inhibitionactivity and high selectivity. |
