The antiplasmodial activity of chalcone derivative through the inhibition of haemozoin formation and the induction of stomatocytes formation

Background: One of methoxy aminochalcone derivatives, (E)-1-(4-aminophenyl)-3-(2,3-dimethoxyphenyl)prop-2-en-1-one has been synthesized and proven it’s in vitro antiplasmodial activity. In this study, we reported in vivo antiplasmodial activity of this compound against Plasmodium berghei infected mice. Its effect on the haemozoin and erythrocytes stomatocytes formations was also evaluated. Methods: The in vivo antiplasmodial activity was evaluated on P. berghei infected mice by the classical 4-day suppressive test. The effect of the tested compound on the haemozoin formation inhibition was evaluated by flowcytometry, whereas its effect on the stomatocytes formation was evaluated by microscopic examination of the thin blood smear. Doxucycline was used as positive control. The median effective dose (ED₅₀ ), which is the dose leading to 50% parasite growth inhibition or haemozoin formation inhibition or stomatocytes formation of tested compound and doxycycline were determined using probit analysis and compared using t test. Results: The ED₅₀ of tested compound to parasite growth inhibition were 17.36 ± 4.59 mg/kg BW. Furthermore, this compound exhibited on inhibition of haemozoin formation with the ED₅₀ of 18.56±5.19 mg/kg BW and induction of stomatoytes formation with the ED₅₀ more than > 160 mg/kg BW. Conclusion: The (E)-1-(4-aminophenyl)-3-(2,3-dimethoxyphenyl) prop-2-en-1-one exhibits potent antimalarial activity via inhibition of haemozoin formation and i nduction of stomatocytes formation. This compound might be developed into a new antimalarial drug.