Study on the preparation of ligand of hepatic asialoglycoprotein receptor / 国际生物医学工程杂志

ABSTRACT

Objective To optimize the preparation of high-efficiency galactocylated poly-L-lysine (Gal-PLL) ligand of the asialoglycoprotein receptor in liver, providing premise and foundation for upper preparation of ultrasound contrast agent of liver targeted nanoscale perfluorocarbon microballoon and the liver targeted molecular imaging. Methods Chemical reactions of reductive amination were carried out on group A and group B according to different proportions of reaction component. Each group was subdivided into three subgroups. In group A, three different molar ratios of D-galactose and poly-L-lysine (PLL) were compounded respectively with equivalent and sufficient reductant borohydride. In group B, identical molar ratios of D-galactose and PLL were compounded respectively with three unequal reductants borohydride. Products of each group were separated and purified by sephadex column to acquire different molecular weight distributions and the results were analyzed. Results In the condition of identical reductant, the peak curve of compound's molecular weight appeared earlier when D-galactose decreased properly. In the condition of identical molar ratio of D-galactose and PLL,the peak curve of compound's molecular weight appeared also earlier when reductant decreased properly. When the molar ratio of D-galactose and reductant was 1∶1, the peak curve of compound Gal-PLL and free components was more obvious, and the quantity of compound Gal-PLL increased to maximum. Conclusions In the condition of identical reductant, coupling effect of D-galactose and PLL increased when D-galactose decreased properly. In the condition of identical molar ratio of D-galactose and PLL, coupling effect was better when reductant decreased properly. When the molar ratio of D-galactose and reductant was 1∶1, coupling effect of them was the best. The coupling of D-galactose and PLL was related to not only the proportion of D-galactose and PLL, but also the proportion of D-galactose and reductant.