Liu Y G, Wang Q M, Xu Y Q, Ni Q Z, Ni Y C
Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, Shanghai 200025.
Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 2001;19(1):30-2.
To investigate the activity of daphnetin(DPNT) against the exo-erythrocytic stage of rodent malaria.
Groups of ten male ICR mice were infected by intraperitoneal injection with sporozoites of P. yoelii. Mice were administered daphnetin 0.5 hr postinfection on d0 and once per day for three additional consecutive days(d1-d3) by the i.g. route. The effects of daphnetin at various dosages and those of the combination of daphnetin with primaquine were assessed by the number of mice with negative Giemsa-stained slides from tail blood on the seventh day after infection and by the average number of red blood cells (RBC) infected in 1,000 RBC observed on the eleventh or twelfth day after infection. We also observed the effect of daphnetin on the concentration of Hb in ICR mice.
Daphnetin exhibited no detectable antimalarial effect on the exo-erythrocytic stage of P. yoelii, while the antimalarial efficacy of DPNT 50 mg/(kg.d) combined with 5 mg/(kg.d) PQ, was comparable to PQ 10 mg/(kg.d) x 4 d i.g. in mice infected with sporozoites of P. yoelii. The concentration of Hb in ICR mice administered with DPNT 50 mg/(kg.d) x 4 d decreased on the eighth day after administration.
Daphnetin alone showed no anti-exoerythrocytic activity in vivo. The combination of DPNT 50 mg/(kg.d) with PQ 5 mg/(kg.d) showed promising antimalarial efficacy comparable to that of PQ 10 mg/(kg.d). Administration of DPNT caused anemia in ICR mice.
研究瑞香素(DPNT)对啮齿类动物疟疾红细胞外期的作用。
将10只雄性ICR小鼠分为一组,通过腹腔注射约氏疟原虫子孢子进行感染。感染后0.5小时,经口给予小鼠瑞香素,于第0天给药,随后连续3天(第1 - 3天)每天给药1次。通过感染后第7天尾血涂片吉姆萨染色阴性的小鼠数量,以及感染后第11天或第12天在1000个红细胞中观察到的平均感染红细胞数,评估不同剂量瑞香素以及瑞香素与伯氨喹联合用药的效果。我们还观察了瑞香素对ICR小鼠血红蛋白浓度的影响。
瑞香素对约氏疟原虫红细胞外期未表现出可检测到的抗疟作用,而50 mg/(kg·d)瑞香素与5 mg/(kg·d)伯氨喹联合用药的抗疟效果,与10 mg/(kg·d)×4 d经口给予伯氨喹对感染约氏疟原虫子孢子小鼠的抗疟效果相当。给予50 mg/(kg·d)×4 d瑞香素的ICR小鼠,给药后第8天血红蛋白浓度降低。
单独使用瑞香素在体内未表现出抗红细胞外期活性。50 mg/(kg·d)瑞香素与5 mg/(kg·d)伯氨喹联合用药显示出有前景的抗疟效果,与10 mg/(kg·d)伯氨喹相当。给予瑞香素会导致ICR小鼠贫血。