Elucidation of pemeable mechanism of new intestinal permeable peptide

2017 Fiscal Year Final Research Report

• Project/Area Number: 16K15162
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Kumamoto University
• Principal Investigator: OHTSUKI Sumio 熊本大学, 大学院生命科学研究部(薬), 教授 (60323036)
• Project Period (FY): 2016-04-01 – 2018-03-31
• Keywords: 環状ペプチド / 小腸透過 / Caco-2細胞

Outline of Final Research Achievements

In order to develop macromolecular drugs, it has been desired to realize carriers that allow macromolecule to permeate the small intestine. Using a newly identified cyclic peptide that promotes penetration of the small intestine, the purpose of this study was to elucidate the characteristics and mechanism of cyclic peptide permeation through the small intestine. Phage penetration was inhibited by synthetic peptides in both Caco-2 cells and mouse small intestine closed loop. In addition, it was suggested that the fluorescence labeled cyclic peptide was internalized into Caco-2 cells and its internalization was mediated by energy-dependent process, and macro-pinocytosis was involved. In addition, it was revealed that cyclic structure is necessary for promoting the penetration, and that small the cyclic peptides do not weaken tight junctions and have low toxicity to small intestinal epithelial cells.

Free Research Field

生物薬剤学