[Preparation of galactosyl-insulin with double saccharide density and a study of its hepatic targeting property].
This study was intended to improve the technical procedure so as to increase the saccharide density of galactosyl-recombinant insulin and elevate its liver targeting property. Using a branched compound 3,5-dihydroxy benzoic acid as the base of a conjugating bridge, the authors prepared a new double galactosyl-recombinant insulin, whose saccharide density being two times as high as that of galactosyl-recombinant insulin. The double gal-insulin conjugate, gal-insulin conjugate and original insulin were labeled with 131I, and then the three kinds of 131I labeled compounds were tested in rabbit whole body imaging to measure their properties of liver targeting. The peak values of rabbit liver concentration for double gal-insulin, gal-insulin and original insulin were 59.5%, 43.8% and 21.5%, respectively. These results demonstrate that for elevating the liver targeting property of galactosyl-recombinant compounds, a branched agent like 3,5-dihydroxyl benzoic acid can be adopted as an effective medium.
Liang
Z
Z
Department of Nuclear Medicine, First Affiliated Hospital, WCUMS, Chengdu 610041.
Fu
X
X
Guan
C
C
Zhong
Y
Y
Li
Y
Y
D000818:Animals; D002645:Chickens; D038983:Galactolipids; D005690:Galactose / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D007328:Insulin / Q000096:biosynthesis / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D008099:Liver / Q000378:metabolism*; D008297:Male; D011817:Rabbits; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000138:chemical synthesis / Q000493:pharmacokinetics*
D038983:Galactolipids; D007328:Insulin; D011994:Recombinant Proteins; C008543:galactosylglyceride; D005690:Galactose