ORIGINAL ARTICLE

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

Lilik Wijayanti, Kristanto Yuli Yarso, Bambang Purwanto, Ambar Mudigdo, Hery Suwito, Paramasari Dirgahayu, Mustofa Mustofa

Lilik Wijayanti
Doctoral Program in Medical Sciences, Postgraduate Program, Universitas Sebelas Maret, Surakarta, Indonesia

Kristanto Yuli Yarso
Department of Surgery, Oncology Division, Faculty of Medicine, Universitas Sebelas Maret/RSUD Dr. Moerwadi, Surakarta, Indonesia

Bambang Purwanto
Department of Internal Medicine Dr Moewardi Hospital/ Facuty of Medicine, Universitas Sebelas Maret Surakarta, Indonesia

Ambar Mudigdo
Department of Anatomic Pathology, Medical Study Program, Faculty of Medicine, Universitas Sebelas Maret Surakarta, Indonesia

Hery Suwito
Department of Chemistry, Faculty of Science and Technology, Universitas Airlangga, Surabaya, Indonesia

Paramasari Dirgahayu
Department of Parasitology, Medical Study Program, Faculty of Medicine, Universitas Sebelas Maret, Surakarta, Indonesia

Mustofa Mustofa
Department of Pharmacology and Therapy, Faculty of Medicine, Public Health and Nursing, Universitas Gajah Mada, Yogyakarta, Indonesia. Email: mustofafk@ugm.ac.id
Online First: April 01, 2019 | Cite this Article
Wijayanti, L., Yarso, K., Purwanto, B., Mudigdo, A., Suwito, H., Dirgahayu, P., Mustofa, M. 2019. The antiplasmodial activity of chalcone derivative through the inhibition of haemozoin formation and the induction of stomatocytes formation. Bali Medical Journal 8(1): 365-370. DOI:10.15562/bmj.v8i1.1196


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 induction of stomatocytes formation. This compound might be developed into a new antimalarial drug.

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