Abstract
OBJECTIVE:To prepare galactosyl recombinant human growth hormone (Gal-rhGH) and to study its distribution in mice.METHODS:A double-function agent,2-imino-2-methoxyethyl-1-thio-β-D-glycosides(IME) was prepared by D-galactose through acetylation,bromination,condensation,displacement and addition reactions.Gal-rhGH was prepared via IME attaching to the lysine residues on rhGH.RESULTS:Differential thermal analysis (DTA) verified that Gal-rhGH was a covalent compound with mean 5 galactosyl residues per rhGH molecule.The comparative study of distribution in mice after iv showed that the radioactivity of 125I-rhGH-Gal was concentrated in liver,whose maximum quantity was 2.3 times as that of 125I-rhGH.The distribution of 125I-rhGH-Gal in kidney was 43% as that of 125I-rhGH.The AUC of whole tissue relative radioactivity distribution of 125I-rhGH-Gal in blood,liver,kidney,heart,lung,spleen and intestine,were 60%,155%,58%,31%,95%,43%,67% as that of 125I-rhGH,respectively.CONCLUSION:A hepatic targeting agent Gal-rhGH was prepared successfully.
Key words
Recombinant human growth hormone /
Galactosyl recombinant human growth hormone /
hepatic targeting
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Li Tongling .
Preparation of galactosyl recombinant human growth hormone and its hepatic targeting[J]. Chinese Pharmaceutical Journal, 1999, 34(09): 600-603
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