Differential receptor targeting of liver cells using 99mTc- neoglycosylated human serum albumins

Sungeun Kim, Jae Min Jeong, Mee Kyung Hong, Ja June Jang, Jaetae Lee, Dong Soo Lee, June Key Chung, Myung Chul Lee

    Research output: Contribution to journalArticlepeer-review

    17 Citations (Scopus)

    Abstract

    Neolactosyl human serum albumin (LSA) targets asialoglycoprotein receptor and shows high liver uptake due to accumulation in hepatocytes. Although neomannosyl human serum albumin (MSA) also shows high liver uptake, it has been reported to be taken up by Kupffer cells and endothelial cells. We compared the biological properties of LSA and MSA. 99mTc-LSA and 99mTc-MSA biodistribution in mice were investigated after intravenous injection. In vivo localization of rhodaminisothiocyanate (RITC)-LSA and fluoresceineisothiocyanate (FITC)-MSA were investigated in mouse liver. Excretion routes of 99mTc-LSA and 99mTc-MSA metabolites were examined. Both 99mTc-LSA and 99mTc-MSA showed high liver uptakes. RITC-LSA was taken up by hepatocytes whereas FITC-MSA was taken up by Kupffer cells and endothelial cells. 99mTc-MSA showed higher spleen and kidney uptakes than 99mTc-LSA. 99mTc-LSA metabolites excreted in urine and feces accounted for 44.4 and 50.0% of 99mTc-LSA injected, respectively, while 99mTc-MSA metabolites accounted for 51.5 and 10.3%, respectively. In conclusion, LSA is specifically taken up by hepatcytes while MSA by Kupffer cells and endothelial cells. After taken up by the liver, LSA is metabolized by the hepatocytes and then excreted through both the hepatobiliary tract and kidney, whereas MSA is metabolized by Kupffer cells and endoghelial cells and then excreted mainly through the kidney.

    Original languageEnglish
    Pages (from-to)60-66
    Number of pages7
    JournalArchives of pharmacal research
    Volume31
    Issue number1
    DOIs
    Publication statusPublished - 2008 Jan

    Keywords

    • FITC
    • Fluorescence
    • Galactose
    • Hepatocyte
    • Kupffer cell
    • LSA
    • MSA
    • Mannose
    • Technetium

    ASJC Scopus subject areas

    • Molecular Medicine
    • Drug Discovery
    • Organic Chemistry

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