99Tcm标记抗疟药NGA─PQ的肝靶向性研究

STUDY ON HEPATIC TARGETING OF ANTIMALARIAL DRUG NGA PQ LABELLED WITH 99 Tc m

以肝细胞膜无唾液酸糖蛋白受体的特异性配体半乳糖新糖白蛋白（ＮＧＡ）作载体，通过丁二酰胺桥将其与抗疟药磷酸伯氨喹（ＰＱ）偶联，制备了一种肝靶向抗疟药ＮＧＡ－ＰＱ。经放射性核素显像研究证实，ＮＧＡ－ＰＱ具有明显的趋肝性和受体介导结合特性，肝最大摄取率高达８０．０％，且保留时间较长，ＮＧＡ－ＰＱ可能成为优良的受体介导肝靶向抗疟药。

Neoglycoalbumin(NGA), the special ligand of asialoglycoprotein receptor on the hepatocyte is linked via a butanediamide bridge to the free amino group of primaquine(PQ) to form a conjugator NGA PQ. To verify its property of targeting to hepatocytes, NGA PQ is labelled with 99 Tc m, then rabbits and chickens imaging are performed. The results indicate that NGA PQ has remarkable livertaxis and the uptake of NGA PQ in liver is over 80.0% with feature of receptor mediated binding to hepatocytes in vivo. Therefore, the NGA PQ is considered to be a potential receptor mediated hepatic targeting antimalarial drug.