Effects of Capsaicin on Intestinal Cephalexin Absorption in Rats

• Komori Yukiko

  Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University

• Aiba Tetsuya

  Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University

• Sugiyama Risa

  Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University

• Nakai Chie

  Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University

• Kawasaki Hiromu

  Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University

• Kurosaki Yuji

  Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University

Abstract

The effects of capsaicin on intestinal cephalexin absorption were investigated by means of in situ single pass perfusion in rats to clarify whether this pungent compound present in spice is a potential factor altering the intestinal drug absorption processes. Under the control condition, cephalexin was absorbed at a rate of 1.16±0.08 and 0.90±0.06 nmol/min/cm in the jejunum and ileum, respectively. The intestinal cephalexin absorption rate was decreased when capsaicin was dissolved in the perfusate at a concentration of 400 μM, being 0.54±0.07 and 0.46±0.10 nmol/min/cm in the jejunum and ileum, respectively. The inhibitive effect of capsaicin on intestinal cephalexin absorption was diminished when ruthenium red, a non-selective inhibitor of the transient receptor potential (TRP) cation channels, was intravenously infused into the rat during the experiment. Moreover, when we evaluated the paracellular permeability of cephalexin by utilizing a competitive inhibitor, glycylsarcosine, it was demonstrated that glycylsarcosine-insensitive intestinal cephalexin absorption in the jejunum was increased by 4.5 times in the presence of 400 μM capsaicin. These findings indicate that capsaicin affects both transcellular and paracellular pathways of intestinal cephalexin absorption by interacting with the TRP cation channels in intestinal tissues, in which capsaicin seems to change the transport activity of H⁺/peptide co-transporter 1 (PEPT1), and to a lesser degree, it seems to alter the paracellular permeability of the intestinal epithelia.

Journal

• Biological and Pharmaceutical Bulletin

  Biological and Pharmaceutical Bulletin 30 (3), 547-551, 2007

  The Pharmaceutical Society of Japan

Keywords

• capsaicin
• cephalexin
• absorption
• transient receptor potential (TRP)
• peptide co-transporter (PEPT)1
• paracellular permeability

Details

• CRID: 1390282679600926464
• NII Article ID: 110006239201
• NII Book ID: AA10885497
• DOI: 10.1248/bpb.30.547
• ISSN: 13475215
• ISSN: 09186158
• NDL BIB ID: 8658236
• Web Site: http://id.ndl.go.jp/bib/8658236
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I8658236
• Web Site: http://www.jstage.jst.go.jp/article/bpb/30/3/30_3_547/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2007232820
• Text Lang: en
• Data Source:
  • JaLC
  • NDL
  • Crossref
  • CiNii Articles
  • KAKEN
• Abstract License Flag: Disallowed