Yan G H, Wang G J, Li Y C
Institute of Microbiology and Epidemiology, Academy of Military Medical Sciences, Beijing, China.
Zhongguo Yao Li Xue Bao. 1991 Nov;12(6):530-3.
The effects of alpha-dimethylamino-cyclohexoxyl-dimethyl gallium (DCDG), a new antimalarial drug developed in China, on the ultrastructure of murine malaria parasites in vivo was studied in comparison with those of chloroquine (CQ) and artemisinin (Art). All these 3 antimalarials were administered ig to mice at dosages of 1-3, 40-80, and 200-400 mg.kg-1 for DCDG, CQ, and Art respectively, based on a similar intensity of morphological changes in the parasites. Blood samples were collected for electron microscopy from 15 min to 48 h after medication. The results showed that DCDG killed the malaria parasites (both asexual and sexual forms) rapidly. The most prominent changes in DCDG-treated parasites were serious dilation of perinuclear space, endoplasmic reticulum, mitochondrion and some other vesicles or intermembranous spaces. These led to the formation of large autophagic vacuoles containing some membranous materials, which were subsequently extruded. Then the parasite cells became more concentrated, finally pyknotic and died. The mode of action was very different from that of CQ and Art.
研究了我国研制的新型抗疟药α-二甲基氨基-环己氧基-二甲基镓(DCDG)对体内鼠疟原虫超微结构的影响,并与氯喹(CQ)和青蒿素(Art)进行了比较。根据寄生虫形态变化的相似程度,分别以1-3、40-80和200-400mg·kg-1的剂量对小鼠进行灌胃给药,DCDG、CQ和Art的剂量分别为上述数值。给药后15分钟至48小时采集血样进行电子显微镜检查。结果表明,DCDG能迅速杀死疟原虫(无性和有性形式)。经DCDG处理的寄生虫最显著的变化是核周间隙、内质网、线粒体和其他一些囊泡或膜间空间严重扩张。这些变化导致形成含有一些膜性物质的大型自噬泡,随后这些自噬泡被排出。然后寄生虫细胞变得更加浓缩,最终固缩并死亡。其作用方式与CQ和Art非常不同。