食蟹猴疟原虫：抗疟化合物CDRI 80/53（依鲁喹啉）对恒河猴的配子体杀灭活性。

Plasmodium cynomolgi: gametocytocidal activity of the anti-malarial compound CDRI 80/53 (elubaquine) in rhesus monkeys.

作者信息

Puri S K, Dutta G P

机构信息

Division of Parasitology, Central Drug Research Institute, Lucknow 226001, India.

出版信息

Exp Parasitol. 2005 Sep;111(1):8-13. doi: 10.1016/j.exppara.2005.05.007.

DOI:10.1016/j.exppara.2005.05.007

PMID:16005457

Abstract

The gametocytocidal action of a new enamine analogue of primaquine, elubaquine (compound CDRI 80/53, bulaquine), has been evaluated against Plasmodium cynomolgi B in rhesus monkeys. Colony bred Anopheles stephensi mosquitoes were fed on gametocyte carrying rhesus monkeys prior to and at varying intervals after oral administration of a single dose of elubaquine at doses ranging between 0.63 and 5.00 mg/kg. Complete loss of oocyst development and mosquito infectivity was observed within 24 h after administering a single 1.25 mg/kg dose, while higher dose of 3.75 mg/kg inhibited oocyst development within 5 h, indicating gametocytocidal action of the compound. Elubaquine did not show any action against developing oocysts in the vector.

摘要

已在恒河猴中评估了一种新的伯氨喹烯胺类似物——鲁巴喹（化合物CDRI 80/53，布喹）对食蟹猴疟原虫B的配子体杀灭作用。在口服单剂量鲁巴喹（剂量范围为0.63至5.00 mg/kg）之前及之后的不同时间间隔，用携带配子体的恒河猴喂养群体饲养的斯氏按蚊。在给予单剂量1.25 mg/kg后24小时内，观察到卵囊发育和蚊子感染性完全丧失，而较高剂量3.75 mg/kg在5小时内抑制了卵囊发育，表明该化合物具有配子体杀灭作用。鲁巴喹对媒介中正在发育的卵囊没有任何作用。