[01] Koto-te-Nyiwa Ngbolua, Department of Biology, University of Kinshasa, Kinshasa, Democratic Republic of the Congo; Faculty of Medicine, University of Gbado-Lite, Gbado-Lite, Democratic Republic of the Congo; Physical Chemistry of Biological Macromolecules Laboratory, University of Kinshasa, Kinshasa, Democratic Republic of the Congo. [02] Zephirin Yav Gushimana, Physical Chemistry of Biological Macromolecules Laboratory, University of Kinshasa, Kinshasa, Democratic Republic of the Congo. [03] Pius Tshimankinda Mpiana, Physical Chemistry of Biological Macromolecules Laboratory, University of Kinshasa, Kinshasa, Democratic Republic of the Congo.

Malaria is a serious public health problem in developing countries and affects about 500 million people per year. However, resistance of some plasmodial strains to the chemotherapy effect of quinoline based-antimalarial drugs has caused the resurgence of malaria in endemic areas. The aim of this study was to evaluate the antimalarial activity of complexes of hemin with chloroquine, amodiaquine, quinine, quinidine and mefloquine. The complexes of hemin with chloroquine, amodiaquine, quinine, quinidine and mefloquine were prepared in vitro, using water-propylène glycol 30% mixture as solvent. The n vitro antimalarial assays were carried out according to WHO protocol and expressed as IC₅₀ i.e concentration of drug which kills 50% of the parasite. The in vivo antiplasmodial activity was evaluated by thick smear while the average weights of mice before and after the exposure to the hemin-amodiaquin complex were used to evaluate the complex toxicity. The IC₅₀ shows a relatively high activity for all complexes tested, in comparison with the corresponding quinoline antimalarial based drug alone (p<005). The in vivo antimalarial assay with hemin-amodiaquine complex (H-AQ) shows a total disappearance of parasitaemia at day 7 after infection of Balb/c mice with P. berghei. The preliminary toxicity test on mice has revealed that H-AQ is not toxic. Besides, any correlation was found between the antimalarial activity and the thermodynamic stability considering all complexes. This could be explained by the great discrepancy observed in susceptibility of used parasite strains. It is therefore desirable that the antiplasmodial test be carried on standardized strains using the isotopic test. It would be interesting to include other quinoline derivatives and corresponding complexes in order to confirm the thermodynamic-biological activity correlation of complexes by determining an area of temperature, pH, ionic strength, etc. to which the complexation constant would respect the order of parasitological activity.

Malaria, Quinoline Antimalarial Based Drugs, Ferriprotoporphyrin IX, Complex, Thermodynamic Stability

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