Daphnetin: a Novel Antimalarial Agent with in Vitro and in Vivo Activity

Ying-Zi YangDepartment of Microbiology, City University of New York Medical School, Department of Biochemistry, Institute of Basic Medical Sciences and Department of Hematology, Peking Union Medical School, New York, New York, People's Republic of China

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Allen RanzDepartment of Microbiology, City University of New York Medical School, Department of Biochemistry, Institute of Basic Medical Sciences and Department of Hematology, Peking Union Medical School, New York, New York, People's Republic of China

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Hua-Zhen PanDepartment of Microbiology, City University of New York Medical School, Department of Biochemistry, Institute of Basic Medical Sciences and Department of Hematology, Peking Union Medical School, New York, New York, People's Republic of China

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Zhi-Nan ZhangDepartment of Microbiology, City University of New York Medical School, Department of Biochemistry, Institute of Basic Medical Sciences and Department of Hematology, Peking Union Medical School, New York, New York, People's Republic of China

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Xie-Bin LinDepartment of Microbiology, City University of New York Medical School, Department of Biochemistry, Institute of Basic Medical Sciences and Department of Hematology, Peking Union Medical School, New York, New York, People's Republic of China

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Steven R. MeshnickDepartment of Microbiology, City University of New York Medical School, Department of Biochemistry, Institute of Basic Medical Sciences and Department of Hematology, Peking Union Medical School, New York, New York, People's Republic of China

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Daphnetin is a dihydroxycoumarin that is being used in China for the treatment of coagulation disorders. It is also a chelator and an antioxidant. In vitro, daphnetin causes a 50% inhibition (IC50) of 3H-hypoxanthine incorporation by Plasmodium falciparum at concentrations between 25 and 40 µM. Several related compounds, such as scopoletin, 2, 3-dihydroxybenzoic acid and 3, 4-dihydroxybenzoic acid show no inhibitory activity. The antimalarial activity of daphnetin is inhibited by the addition of iron. Daphnetin does not appear to be an oxidant drug, since it does not spontaneously generate superoxide in vitro. However, it does alkylate bovine serum albumin when incubated in the presence of iron. In vivo, daphnetin significantly prolongs survival of P. yoelli—infected mice.

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