Chen M, Theander T G, Christensen S B, Hviid L, Zhai L, Kharazmi A
Department of Clinical Microbiology, National University Hospital, Copenhagen, Denmark.
Antimicrob Agents Chemother. 1994 Jul;38(7):1470-5. doi: 10.1128/AAC.38.7.1470.
Licochalcone A, isolated from Chinese licorice roots, inhibited the in vitro growth of both chloroquine-susceptible (3D7) and chloroquine-resistant (Dd2) Plasmodium falciparum strains in a [3H]hypoxanthine uptake assay. The growth inhibition of the chloroquine-resistant strain by licochalcone A was similar to that of the chloroquine-susceptible strain. To examine the activity of licochalcone A on the different asexual blood stages of the parasite, licochalcone A was added to highly synchronized cultures containing rings, trophozoites, and schizonts. The growth of the parasites at all stages was inhibited by licochalcone A. The in vivo activity of licochalcone A was tested in a mouse model of infection with P. yoelii. Licochalcone A administered either intraperitoneally or orally for 3 to 6 days protected the mice from the otherwise lethal P. yoelii infection. These results demonstrate that licochalcone A exhibits potent antimalarial activity and might be developed into a new antimalarial drug.
从中国甘草根中分离得到的甘草查尔酮A,在一项[3H]次黄嘌呤摄取试验中,抑制了氯喹敏感(3D7)和氯喹耐药(Dd2)恶性疟原虫菌株的体外生长。甘草查尔酮A对氯喹耐药菌株的生长抑制作用与氯喹敏感菌株相似。为了检测甘草查尔酮A对疟原虫不同无性血液阶段的活性,将甘草查尔酮A添加到含有环状体、滋养体和裂殖体的高度同步化培养物中。甘草查尔酮A抑制了寄生虫在所有阶段的生长。在约氏疟原虫感染的小鼠模型中测试了甘草查尔酮A的体内活性。腹腔注射或口服甘草查尔酮A 3至6天可保护小鼠免受原本致命的约氏疟原虫感染。这些结果表明,甘草查尔酮A具有强大的抗疟活性,可能会被开发成一种新型抗疟药物。