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Am. J. Trop. Med. Hyg., 46(1), 1992, pp. 15-20
Copyright © 1992 by The American Society of Tropical Medicine and Hygiene

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

Ying-Zi Yang, Allen Ranz, Hua-Zhen Pan, Zhi-Nan Zhang, Xie-Bin Lin AND Steven R. Meshnick
Department of Microbiology, City University of New York Medical School, New York, New York; Department of Biochemistry, Institute of Basic Medical Sciences and Department of Hematology, Peking Union Medical School, Beijing, People's Republic of China

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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C. NDong, D. Anzellotti, R. K. Ibrahim, N. P. A. Huner, and F. Sarhan
Daphnetin Methylation by a Novel O-Methyltransferase Is Associated with Cold Acclimation and Photosystem II Excitation Pressure in Rye
J. Biol. Chem., February 21, 2003; 278(9): 6854 - 6861.
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Copyright © 1992 by the American Society of Tropical Medicine and Hygiene.