摘要
以肝细胞表面的无唾液酸糖蛋白受体的特异性配基──半乳糖基拟糖白蛋白(Neoglycoalbumin.NGA)作为载体,通过丁二酰胺桥,成功地与抗疟药伯氨喹(PQ)偶联,制备了肝靶向抗疟药NGA-PQ,药密度达到16.8±0.85,糖密度达到21.7±1.73.经药效学试验,NGA-PQ的抗疟作用明显优于同剂量的PQ。
Neoglycoalbumin(NGA),the special ligend of asialoglycoprotein receptor on the hepatocyte,was linked via a butanediamide bridge to the free amino group of primaquine to form a conjugator NGA-PQ,The drug density and carbohydrate density of the NGA-PQ which was used as a hepatic antimalarial agent were 16.8±0.85 and 21.7±1. 73 respectively. The study on its therapeutic activity demonstrated that the antimalaria activity of half dose of PQ in NGA-PQ was more effective than that of the same dose of PQ.
出处
《中国药物化学杂志》
CAS
CSCD
1994年第4期240-244,共5页
Chinese Journal of Medicinal Chemistry
基金
卫生部科学研究课题
关键词
半乳糖基
拟糖白蛋白
磷酸伯氨喹
抗疟药
Asialoglycoprotein receptor
Galactocyl neoglycoalbumin
Primaquine phosphate
Hepatic targeting