Gastric relaxation induced by apigenin and quercetin: analysis of the mechanism of action.

Rosa Maria Serio, Flavia Mule', Alessandra Rotondo

Risultato della ricerca: Article

16 Citazioni (Scopus)

Abstract

AIMS: Recently, flavonoids have been shown to cause murine gastric relaxation. In the present study we examined the mechanism of action underlying gastric relaxation induced by apigenin and quercetin in isolated mouse stomach. MAIN METHODS: The mechanical activity from the whole stomach was detected as changes in the endoluminal pressure and the response to increasing concentrations of both flavonoids were tested before and after different pharmacological treatments. KEY FINDINGS: Apigenin and quercetin-induced a concentration-dependent gastric relaxation, apigenin being more potent than quercetin. The responses were unaffected by 2'5'dideoxyadenosine, an inhibitor of adenylate cyclase, 3-isobutyl-1-methylxanthine, a non selective inhibitor of cyclic nucleotide phosphodiesterase, or ryanodine, an inhibitor of calcium release from ryanodine-sensitive intracellular stores, whereas they were significantly decreased in Ca(2+)-free solution or in the presence of nifedipine, a blocker of L-type voltage-dependent Ca(2+) channels, which did not modify the relaxation induced by isoproterenol. Moreover, both flavonoids caused concentration-dependent inhibition of the contractile responses caused by exogenous application of Ca(2+) in a Ca(2+)-free solution, high K(+) or carbachol. SIGNIFICANCE: Our results support the hypothesis that the gastric myorelaxant effects of apigenin and quercetin arise from their negative modulation of calcium influx through voltage-dependent Ca(2+) channels, however intracellular modulation of signalling cascade leading to contraction could be involved.
Lingua originaleEnglish
pagine (da-a)85-90
Numero di pagine6
RivistaLife Sciences
Volume85
Stato di pubblicazionePublished - 2009

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Apigenin
Quercetin
Stomach
Flavonoids
Ryanodine
Dideoxyadenosine
Modulation
Calcium
1-Methyl-3-isobutylxanthine
Cyclic Nucleotides
Phosphoric Diester Hydrolases
Carbachol
Electric potential
Nifedipine
Isoproterenol
Pharmacology
Pressure

All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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Gastric relaxation induced by apigenin and quercetin: analysis of the mechanism of action. / Serio, Rosa Maria; Mule', Flavia; Rotondo, Alessandra.

In: Life Sciences, Vol. 85, 2009, pag. 85-90.

Risultato della ricerca: Article

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title = "Gastric relaxation induced by apigenin and quercetin: analysis of the mechanism of action.",
abstract = "AIMS: Recently, flavonoids have been shown to cause murine gastric relaxation. In the present study we examined the mechanism of action underlying gastric relaxation induced by apigenin and quercetin in isolated mouse stomach. MAIN METHODS: The mechanical activity from the whole stomach was detected as changes in the endoluminal pressure and the response to increasing concentrations of both flavonoids were tested before and after different pharmacological treatments. KEY FINDINGS: Apigenin and quercetin-induced a concentration-dependent gastric relaxation, apigenin being more potent than quercetin. The responses were unaffected by 2'5'dideoxyadenosine, an inhibitor of adenylate cyclase, 3-isobutyl-1-methylxanthine, a non selective inhibitor of cyclic nucleotide phosphodiesterase, or ryanodine, an inhibitor of calcium release from ryanodine-sensitive intracellular stores, whereas they were significantly decreased in Ca(2+)-free solution or in the presence of nifedipine, a blocker of L-type voltage-dependent Ca(2+) channels, which did not modify the relaxation induced by isoproterenol. Moreover, both flavonoids caused concentration-dependent inhibition of the contractile responses caused by exogenous application of Ca(2+) in a Ca(2+)-free solution, high K(+) or carbachol. SIGNIFICANCE: Our results support the hypothesis that the gastric myorelaxant effects of apigenin and quercetin arise from their negative modulation of calcium influx through voltage-dependent Ca(2+) channels, however intracellular modulation of signalling cascade leading to contraction could be involved.",
keywords = "Apigenin, Calcium antagonists, Flavonoids, Gastric tone, Quercetin, Smooth muscle",
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T1 - Gastric relaxation induced by apigenin and quercetin: analysis of the mechanism of action.

AU - Serio, Rosa Maria

AU - Mule', Flavia

AU - Rotondo, Alessandra

PY - 2009

Y1 - 2009

N2 - AIMS: Recently, flavonoids have been shown to cause murine gastric relaxation. In the present study we examined the mechanism of action underlying gastric relaxation induced by apigenin and quercetin in isolated mouse stomach. MAIN METHODS: The mechanical activity from the whole stomach was detected as changes in the endoluminal pressure and the response to increasing concentrations of both flavonoids were tested before and after different pharmacological treatments. KEY FINDINGS: Apigenin and quercetin-induced a concentration-dependent gastric relaxation, apigenin being more potent than quercetin. The responses were unaffected by 2'5'dideoxyadenosine, an inhibitor of adenylate cyclase, 3-isobutyl-1-methylxanthine, a non selective inhibitor of cyclic nucleotide phosphodiesterase, or ryanodine, an inhibitor of calcium release from ryanodine-sensitive intracellular stores, whereas they were significantly decreased in Ca(2+)-free solution or in the presence of nifedipine, a blocker of L-type voltage-dependent Ca(2+) channels, which did not modify the relaxation induced by isoproterenol. Moreover, both flavonoids caused concentration-dependent inhibition of the contractile responses caused by exogenous application of Ca(2+) in a Ca(2+)-free solution, high K(+) or carbachol. SIGNIFICANCE: Our results support the hypothesis that the gastric myorelaxant effects of apigenin and quercetin arise from their negative modulation of calcium influx through voltage-dependent Ca(2+) channels, however intracellular modulation of signalling cascade leading to contraction could be involved.

AB - AIMS: Recently, flavonoids have been shown to cause murine gastric relaxation. In the present study we examined the mechanism of action underlying gastric relaxation induced by apigenin and quercetin in isolated mouse stomach. MAIN METHODS: The mechanical activity from the whole stomach was detected as changes in the endoluminal pressure and the response to increasing concentrations of both flavonoids were tested before and after different pharmacological treatments. KEY FINDINGS: Apigenin and quercetin-induced a concentration-dependent gastric relaxation, apigenin being more potent than quercetin. The responses were unaffected by 2'5'dideoxyadenosine, an inhibitor of adenylate cyclase, 3-isobutyl-1-methylxanthine, a non selective inhibitor of cyclic nucleotide phosphodiesterase, or ryanodine, an inhibitor of calcium release from ryanodine-sensitive intracellular stores, whereas they were significantly decreased in Ca(2+)-free solution or in the presence of nifedipine, a blocker of L-type voltage-dependent Ca(2+) channels, which did not modify the relaxation induced by isoproterenol. Moreover, both flavonoids caused concentration-dependent inhibition of the contractile responses caused by exogenous application of Ca(2+) in a Ca(2+)-free solution, high K(+) or carbachol. SIGNIFICANCE: Our results support the hypothesis that the gastric myorelaxant effects of apigenin and quercetin arise from their negative modulation of calcium influx through voltage-dependent Ca(2+) channels, however intracellular modulation of signalling cascade leading to contraction could be involved.

KW - Apigenin

KW - Calcium antagonists

KW - Flavonoids

KW - Gastric tone

KW - Quercetin

KW - Smooth muscle

UR - http://hdl.handle.net/10447/42765

M3 - Article

VL - 85

SP - 85

EP - 90

JO - Life Sciences

JF - Life Sciences

SN - 0024-3205

ER -