Song J, Wang X, Huang F, Feng C, Zhang Z, Huo Y, Pang Q
Department of Parasitology, Third Military Medical University, Chongqing.
Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 1995;13(2):117-9.
Target-primaquine (TPQ)--the primaquine entrapped by galactosylneoglycoalbumin (G-NGA), was given intravenously (iv) to Wistar rats 2 h after sporozoite inoculation. The sporozoite viability (SPV) of TPQ 20 mg/kg group was revealed to be 1.2% 42 h after inoculation, which showed a decline of about 6% as compared to the control; besides, degeneration or retardation of development was present in 90% of EEF. In TPQ 10 mg/kg and PQ 20 mg/kg groups, the SPV were 2.8% and 5.0%, respectively, showing drops by 15% and 26% as compared with that of the control. Degeneration or retardation in development was also visible in about half of the EEF. In mice which were treated iv with TPQ 10 mg/kg or PQ 20 mg/kg 2 h after sporozoite inoculation, the prepatent periods were delayed markedly as compared with that of the control. Parasitemia did not appear in 2 mice in 10 mg/kg TPQ group further indicated the effectiveness of the drug. The results suggest that the anti-EEF effect of TPQ is apparently more promising than that of PQ.
靶向伯氨喹(TPQ)——即被半乳糖基新糖白蛋白(G-NGA)包裹的伯氨喹,在子孢子接种2小时后经静脉注射(iv)给予Wistar大鼠。接种后42小时,TPQ 20mg/kg组的子孢子活力(SPV)为1.2%,与对照组相比下降了约6%;此外,90%的早期滋养体(EEF)出现发育退化或迟缓。在TPQ 10mg/kg组和PQ 20mg/kg组中,SPV分别为2.8%和5.0%,与对照组相比分别下降了15%和26%。约一半的EEF也可见发育退化或迟缓。在子孢子接种2小时后经静脉注射TPQ 10mg/kg或PQ 20mg/kg治疗的小鼠中,与对照组相比,潜隐期明显延长。10mg/kg TPQ组的2只小鼠未出现寄生虫血症,进一步表明了该药物的有效性。结果表明,TPQ的抗EEF作用显然比PQ更有前景。