Yang Y Z, Ranz A, Pan H Z, Zhang Z N, Lin X B, Meshnick S R
Department of Microbiology, City University of New York Medical School, New York.
Am J Trop Med Hyg. 1992 Jan;46(1):15-20. doi: 10.4269/ajtmh.1992.46.15.
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 microM. 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.
瑞香素是一种二羟基香豆素，在中国用于治疗凝血障碍。它也是一种螯合剂和抗氧化剂。在体外，瑞香素在25至40微摩尔浓度之间可使恶性疟原虫掺入3H-次黄嘌呤的量受到50%的抑制（IC50）。几种相关化合物，如东莨菪素、2,3-二羟基苯甲酸和3,4-二羟基苯甲酸均无抑制活性。添加铁会抑制瑞香素的抗疟活性。瑞香素似乎不是一种氧化药物，因为它在体外不会自发产生超氧化物。然而，当在铁存在的情况下孵育时，它会使牛血清白蛋白烷基化。在体内，瑞香素可显著延长约氏疟原虫感染小鼠的存活时间。
