Chen P Q, Yuan J, Du Q Y, Chen L, Li G Q, Huang Z Y, Yang D D, Wu L N
Tropical Medicine Institute, Guangzhou University of Traditional Chinese Medicine, Guangzhou 510405, China.
Acta Pharmacol Sin. 2000 Mar;21(3):234-8.
The fine structural changes of Plasmodium berghei ANKA strain after treatment with the dihydroartemisinin (DATM) were observed.
DATM 180 mg.kg-1.d-1 was given ig to outbreed NIH mice infected with P. berghei ANKA strain. Blood samples were collected, embedded and examined by electron microscopy.
In P. berghei ANKA strain, 1 h after drug administration, the parasites food vacuole membranes were destroyed, and the pigment grains showed some changes. The nucleus membrane, cytomembrane, and food vacuole membranes were stratified 2 h after administration. At the same time, swelling and separation of the outer and inner membrane or shrinking of the mitochondria were seen. Stripped nuclear and cytoplasm membrane were developed and vacuolizations were seen 4 h later. Eight hours after administration, a large number of parasite structures were destroyed except for a few parasite autophagic vacuoles.
DATM was a fast-acting and effective antimalarial drug. Its primary target is the membrane system. No obvious resistant characteristics were found upto 24 generations after resistant induction test for 4 months.
观察双氢青蒿素（DATM）作用后伯氏疟原虫ANKA株的超微结构变化。
以180mg·kg-1·d-1的剂量将双氢青蒿素灌胃给予感染伯氏疟原虫ANKA株的远交系NIH小鼠。采集血样，进行包埋并通过电子显微镜检查。
在伯氏疟原虫ANKA株中，给药1小时后，疟原虫的食物泡膜被破坏，色素颗粒出现一些变化。给药2小时后，核膜、细胞膜和食物泡膜出现分层。同时，可见线粒体外膜与内膜肿胀分离或线粒体皱缩。4小时后出现核膜和细胞质膜剥离以及空泡化。给药8小时后，除少数疟原虫自噬泡外，大量疟原虫结构被破坏。
双氢青蒿素是一种速效、有效的抗疟药物。其主要作用靶点是膜系统。在进行4个月的抗性诱导试验后，直至第24代均未发现明显的抗性特征。
