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KMID : 0043320070300091162
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Archives of Pharmacal Research
2007 Volume.30 No. 9 p.1162 ~ p.1167
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Pharmacokinetics of GST-TatdMt, a Recombinant Fusion Protein Possessing Potent Anti-obesity Activity, in Mice
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Shin Beom-Soo
Seo Jin-Hyuk
Hur Man-Wook
Lee Min-Nyung
Yoo Sun-Dong
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Abstract
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This study examined the absorption and pharmacokinetic disposition of 125I-GST-TatdMt, a recombinant Tat protein possessing potent anti-obesity activity, in mice after vascular and extravascular administration. GST-TatdMt was over-expressed in E. coli, purified, and radioiodinated using the IODO-GEN method. 125I-GST-TatdMt was administered to mice by i.v., i.p. and oral administration at doses of 652.7 nCi (102.3 킽). Upon i.v. injection, the average terminal elimination half-life (t1/2,?), AUC and AUMC were 6.4 h, 318.2 nCi톒/mL and 2518 nCi톒2/ mL, respectively. The highest radioactivity was observed in lung followed by liver, spleen, heart and kidney. The t1/2,? values obtained from i.v., i.p., and oral administration were comparable from each other (range 5.8-6.4 h). The absolute bioavailability of 125I-GST-TatdMt was 42.8% and 60.5% after p.o. and i.p. administration, respectively. Given the cell-penetrating nature, 125I-GST-TatdMt may be absorbed into the systemic circulation to a relatively high extent after extravascular administration.
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KEYWORD
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Tat, Pharmacokinetics, Bioavailability, Distribution, Obesity
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