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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2007-3-1
pubmed:abstractText
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 microM, 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 microM 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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0918-6158
pubmed:author
pubmed:issnType
Print
pubmed:volume
30
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
547-51
pubmed:meshHeading
pubmed-meshheading:17329854-Analgesics, Non-Narcotic, pubmed-meshheading:17329854-Animals, pubmed-meshheading:17329854-Anti-Bacterial Agents, pubmed-meshheading:17329854-Capsaicin, pubmed-meshheading:17329854-Cell Membrane Permeability, pubmed-meshheading:17329854-Cephalexin, pubmed-meshheading:17329854-Dipeptides, pubmed-meshheading:17329854-Dose-Response Relationship, Drug, pubmed-meshheading:17329854-Ileum, pubmed-meshheading:17329854-Intestinal Absorption, pubmed-meshheading:17329854-Jejunum, pubmed-meshheading:17329854-Male, pubmed-meshheading:17329854-Metabolic Clearance Rate, pubmed-meshheading:17329854-Perfusion, pubmed-meshheading:17329854-Rats, pubmed-meshheading:17329854-Rats, Wistar, pubmed-meshheading:17329854-Ruthenium Red, pubmed-meshheading:17329854-Symporters, pubmed-meshheading:17329854-TRPV Cation Channels
pubmed:year
2007
pubmed:articleTitle
Effects of capsaicin on intestinal cephalexin absorption in rats.
pubmed:affiliation
Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Okayama 700-8530, Japan.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't