Inhibitory Potency of Marketed Drugs for Ulcerative Colitis and Crohn’s Disease on PEPT1

• Miyake Masateru

  Department of Pharmacy, Uppsala University BA Project, Formulation Research Institute, Otsuka Pharmaceutical Co., Ltd.

• Fujishima Miki

  ADME/TOX Research Institute, Sekisui Medical Co., Ltd.

• Nakai Daisuke

  Department of Pharmacy, Uppsala University

抄録

We investigate the inhibitory effect of marketed drugs for treatment of inflammatory bowel disease (IBD) such as ulcerative colitis (UC) and Crohn’s disease (CD) on the uptake transporters of peptide transporter 1 (PEPT1), which are up-regulated under the inflamed condition. The uptake transport of glycylsarcosine, a typical substrate for PEPT1, was reduced to 60% only by 5-aminosalicylate at the clinically relevant concentration among tested marketed drugs in PEPT1 transfected HEK293 cell lines. These findings suggest that the inhibition of PEPT1, which were up-regulated in inflamed or non-inflamed site on UC and CD patients, contribute to the clinical effect of commercially available drugs for IBD patients through the inhibition of uptake of antigenic proinflammatory oligopeptides such as formyl-methionine (Met)-leucine (Leu)-phenylalanine (Phe) via PEPT1.

収録刊行物

• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ

  Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 40 (9), 1572-1575, 2017

  公益社団法人 日本薬学会

キーワード

• peptide transporter 1
• 5-aminosalicylate
• ulcerative colitis
• Crohn’s disease
• intestinal absorption

詳細情報

• CRID: 1390001204631175808
• NII論文ID: 130006038760
• NII書誌ID: AA10885497
• DOI: 10.1248/bpb.b17-00181
• ISSN: 13475215
• ISSN: 09186158
• NDL書誌ID: 028470774
• PubMed: 28867741
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I028470774
• Web Site: https://www.jstage.jst.go.jp/article/bpb/40/9/40_b17-00181/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2018146337
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可