Gastric retention and stability of lipidized Bowman-Birk protease inhibitor in mice.
Bowman-Birk protease inhibitor (BBI) was modified with a reversible lipidizing agent. The palmitoylated product, Pal-BBI, and BBI were iodinated and orally administered to mice using a gavage needle. A prolonged retention of Pal-BBI was found in the stomach. Furthermore, a significant amount of Pal-BBI was detected as intact polypeptide in the stomach of mice fed with Pal-BBI, while only degradation products were detected with BBI. There was also a significant increase of radioactivity in the blood and liver in mice 1.5 h post-administration of Pal-BBI. These results indicate that lipidized polypeptide can have a longer retention and lower digestion in the stomach. They also suggest that the Pal-BBI may have a higher gastrointestinal absorption than the original polypeptide.
Wang
J
J
Department of Pharmaceutical Sciences, University of Southern California School of Pharmacy, Los Angeles 90033, USA.
Shen
W C
WC
D000818:Animals; D005260:Female; D005753:Gastric Mucosa / Q000378:metabolism*; D007420:Intestine, Large / Q000378:metabolism; D007421:Intestine, Small / Q000378:metabolism; D007668:Kidney / Q000378:metabolism; D008055:Lipids / Q000493:pharmacokinetics*; D008099:Liver / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D014358:Trypsin Inhibitor, Bowman-Birk Soybean / Q000493:pharmacokinetics*; D014361:Trypsin Inhibitors / Q000493:pharmacokinetics*
D008055:Lipids; D014358:Trypsin Inhibitor, Bowman-Birk Soybean; D014361:Trypsin Inhibitors