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KMID : 0043320080310010060
Archives of Pharmacal Research
2008 Volume.31 No. 1 p.60 ~ p.66
Differential Receptor Targeting of Liver Cells Using 99mTc-Neoglycosylated Human Serum Albumins
Kim Sung-Eun

Jang Ja-June
Chung June-Key
Lee Myung-Chul
Lee Jae-Tae
Jeong Jae-Min
Lee Dong-Soon
Hong Mee-Kyung
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. 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.
KEYWORD
Fluorescence, Technetium, Kupffer cell, Hepatocyte, LSA, MSA, FITC, Mannose, Galactose
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