Chen M, Brøgger Christensen S, Zhai L, Rasmussen M H, Theander T G, Frøkjaer S, Steffansen B, Davidsen J, Kharazmi A
Centre for Medical Parasitology, Department of Clinical Microbiology, University Hospital of Copenhagen, Denmark.
J Infect Dis. 1997 Nov;176(5):1327-33. doi: 10.1086/514129.
Previous studies have shown that licochalcone A, an oxygenated chalcone, exhibits antileishmanial and antimalarial activities. The present study was designed to examine the antimalarial activity of an analog of licochalcone A, 2,4-dimethoxy-4'-butoxychalcone (2,4mbc). 2,4mbc inhibited the in vitro growth of both a chloroquine-susceptible (3D7) and a chloroquine-resistant (Dd2) strain of Plasmodium falciparum in a [3H]hypoxanthine uptake assay. The in vivo activity of 2,4mbc was tested in mice infected with Plasmodium berghei or Plasmodium yoelii and in rats infected with P. berghei. 2,4mbc administered either orally, intraperitoneally, or subcutaneously for 5 days protected the mice from otherwise lethal infections of these parasites. 2,4mbc administered orally for 5 days reduced parasitemia in the rats infected with P. berghei. These results demonstrate that 2,4mbc exhibits potent antimalarial activity and might be developed into a new antimalarial drug.
先前的研究表明，氧化查耳酮地锦草查耳酮A具有抗利什曼原虫和抗疟活性。本研究旨在检测地锦草查耳酮A类似物2,4-二甲氧基-4'-丁氧基查耳酮（2,4mbc）的抗疟活性。在[3H]次黄嘌呤摄取试验中，2,4mbc抑制了恶性疟原虫氯喹敏感株（3D7）和氯喹耐药株（Dd2）的体外生长。在感染伯氏疟原虫或约氏疟原虫的小鼠以及感染伯氏疟原虫的大鼠中测试了2,4mbc的体内活性。口服、腹腔注射或皮下注射2,4mbc 5天可保护小鼠免受这些寄生虫的致命感染。口服2,4mbc 5天可降低感染伯氏疟原虫大鼠的寄生虫血症。这些结果表明，2,4mbc具有强大的抗疟活性，可能会被开发成一种新型抗疟药物。
