Document Detail

Inhibition of guinea pig intestinal peristalsis by the flavonoids quercetin, naringenin, apigenin and genistein.
MedLine Citation:
PMID:  14646351     Owner:  NLM     Status:  MEDLINE    
Flavonoids are known to relax precontracted intestinal smooth muscle and to delay intestinal transit. We therefore investigated the effects of quercetin, naringenin, apigenin and genistein on intestinal peristalsis in vitro. Peristalsis in fluid-perfused segments of the guinea pig small intestine was recorded through the intraluminal pressure changes associated with the peristaltic waves. Alterations of distension sensitivity were reflected by changes in the peristaltic pressure threshold and alterations of peristaltic performance by changes in the maximal acceleration, amplitude and residual baseline pressure of the peristaltic waves. Quercetin, naringenin, apigenin and genistein (10-300 micromol/l) depressed intestinal peristalsis in a structure- and concentration-dependent manner. The flavonoid-evoked changes in peristalsis parameters made it possible to distinguish between two patterns of peristaltic motor inhibition: a decrease in distension sensitivity and peristaltic performance (apigenin and genistein) and a decrease in distension sensitivity without a major change in peristaltic performance (quercetin and naringenin). The antiperistaltic effect of quercetin was partially prevented by apamin (0.5 micromol/l), N-nitro-L-arginine methylester (100 micromol/l) and naloxone (0.5 micromol/l), whereas the effect of genistein was hardly affected by these drugs. Peristaltic motor activity suppressed by quercetin (300 micromol/l), but not genistein (100 micromol/l), was partially restored by apamin. In contrast, neostigmine (0.3 micromol/l) caused a significant recovery of peristalsis from blockade by genistein but failed to reverse peristaltic motor blockade due to quercetin. These observations suggest that naringenin and quercetin inhibit peristalsis by facilitating inhibitory enteric pathways, whereas apigenin and genistein interfere with muscle excitation or excitation-contraction coupling.
Kamel Gharzouli; Peter Holzer
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Pharmacology     Volume:  70     ISSN:  0031-7012     ISO Abbreviation:  Pharmacology     Publication Date:  2004 Jan 
Date Detail:
Created Date:  2003-12-03     Completed Date:  2004-05-28     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0152016     Medline TA:  Pharmacology     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  5-14     Citation Subset:  IM    
Copyright Information:
Copyright 2004 S. Karger AG, Basel
Department of Experimental and Clinical Pharmacology, University of Graz, Austria.
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MeSH Terms
Antidiarrheals / pharmacology
Apamin / pharmacology
Caerulein / pharmacology
Dimethylphenylpiperazinium Iodide / pharmacology
Dose-Response Relationship, Drug
Flavanones / pharmacology
Flavonoids / administration & dosage,  pharmacokinetics*,  pharmacology
Genistein / pharmacology
Guinea Pigs
Intestine, Small / drug effects*,  physiology
Muscle Contraction / drug effects
Muscle, Smooth / drug effects
NG-Nitroarginine Methyl Ester / pharmacology
Naloxone / pharmacology
Neostigmine / pharmacology
Peristalsis / drug effects*,  physiology
Quercetin / pharmacology
Reg. No./Substance:
0/Antidiarrheals; 0/Flavanones; 0/Flavonoids; 117-39-5/Quercetin; 17650-98-5/Caerulein; 24345-16-2/Apamin; 446-72-0/Genistein; 465-65-6/Naloxone; 480-41-1/naringenin; 50903-99-6/NG-Nitroarginine Methyl Ester; 520-36-5/Apigenin; 54-77-3/Dimethylphenylpiperazinium Iodide; 59-99-4/Neostigmine

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