Antispasmodic effect of selected Citrus flavonoids on rat isolated jejunum specimens.

Abstract:

:Citrus flavonoids are acknowledged for numerous pharmacological activities, including the myorelaxant effect on various smooth muscles. However, there is no data on their effect on jejunum contractility. Therefore, the aim of the study at hand was to evaluate the impact of hesperetin and diosmetin along with their glycosides on the motoric activity of intestine and to verify the possible mechanism of hesperetin-induced effect. The experiments were performed on rat isolated jejunum strips and were conducted under isometric conditions. Hesperetin and diosmetin, but not hesperidin and diosmin, dose-dependently (10-100µM) and reversibly inhibited acetylcholine (1µM) and KCl (80mM) induced contractile activity. The antispasmodic effect of hesperetin was partially blocked by 4-aminopyridine (100µM), glibenclamide (100µM) and NG-nitro-L-arginine methyl ester (L-NAME, 100µM). By contrast, apamin (0.1µM), tetraethylammonium (500µM) and methylene blue (10µM) did not affect the magnitude of hesperetin-induced myorelaxant effect. Indomethacin (10µM) increased the force of hesperetin-evoked reaction. In conclusion, hesperetin and diosmetin are potent myorelaxant agents. The antispasmodic effect of hesperetin is partially mediated by fast current low-voltage activated K+ channels, voltage-independent K+ channels and involves the nitric oxide pathway. Finally, hesperetin shows a synergistic effect with indomethacin towards jejunal KCl-precontracted smooth muscle.

journal_name

Eur J Pharmacol

authors

Mendel M,Chłopecka M,Dziekan N,Karlik W

doi

10.1016/j.ejphar.2016.10.006

subject

Has Abstract

pub_date

2016-11-15 00:00:00

pages

640-646

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(16)30647-1

journal_volume

791

pub_type

杂志文章
  • Modulation of nitric oxide pathways: therapeutic potential in asthma and chronic obstructive pulmonary disease.

    abstract::Nitric oxide (NO) is present in the exhaled breath of humans and other mammalian species. It is generated in the lower airways by enzymes of the nitric oxide synthase (NOS) family, although nonenzymatic synthesis and consumptive processes may also influence levels of NO in exhaled breath. The biological properties of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2005.12.069

    authors: Redington AE

    更新日期:2006-03-08 00:00:00

  • Resveratrol augments nitric oxide generation and causes store calcium release in chromaffin cells.

    abstract::The cardiovascular protecting effect of the grape fruit trans-resveratrol has been explained among other factors, through augmentation of nitric oxide (NO) production in cardiovascular tissues. Another effect of low resveratrol concentration is the inhibition of single-vesicle quantal release of catecholamine from bov...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.03.040

    authors: Padín JF,de Diego AM,Fernández-Morales JC,Merino C,Maroto M,Calvo-Gallardo E,Arranz JA,Yáñez M,García AG

    更新日期:2012-06-15 00:00:00

  • Are angiotensin receptors in vascular smooth muscles a homogeneous population?

    abstract::The effects of angiotensin II (AII) and angiotensin III (AIII) on mean arterial pressure (MAP) and mean circulatory filling pressure (MCFP), an index of total body venous tone, in the presence and absence of [Sar1,Ile8]AII in conscious rats were examined. The infusion of AII caused dose-dependent increases in MAP and ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90074-4

    authors: Tabrizchi R,Pang CC

    更新日期:1987-10-27 00:00:00

  • A role for cannabinoid receptors, but not endogenous opioids, in the antinociceptive activity of the CB2-selective agonist, GW405833.

    abstract::Several recent reports have demonstrated a role for selective cannabinoid CB2 receptor agonists in pain modulation, showing both analgesic and antihyperalgesic activities. While the mechanism of action is poorly understood, it has been postulated that these effects may be indirect, involving release of endogenous opio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.10.043

    authors: Whiteside GT,Gottshall SL,Boulet JM,Chaffer SM,Harrison JE,Pearson MS,Turchin PI,Mark L,Garrison AE,Valenzano KJ

    更新日期:2005-12-28 00:00:00

  • EMCD, a hypoglycemic triterpene isolated from Momordica charantia wild variant, attenuates TNF-α-induced inflammation in FL83B cells in an AMP-activated protein kinase-independent manner.

    abstract::Insulin resistance is a causative factor for type 2 diabetes, whereas the development of insulin resistance is closely related to chronic inflammation induced by factors such as tumor necrosis factor-α (TNF-α). Momordica charantia, also known as bitter melon, has been used as an herbal medicine and reported to amelior...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.05.033

    authors: Cheng HL,Kuo CY,Liao YW,Lin CC

    更新日期:2012-08-15 00:00:00

  • Substance P suppresses stress-induced eating.

    abstract::Parenterally administered substance P suppressed stress-induced eating (resulting from mild tail pinch) in a dose-related manner, whereas at similar or higher doses of substance P starvation-induced eating was uneffected. This specific effect of substance P on stress-induced eating is possibly associated with alterati...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(80)90514-2

    authors: Morley JE,Levine AS

    更新日期:1980-10-17 00:00:00

  • The effect of a Rho kinase inhibitor Y-27632 on superoxide production, aggregation and adhesion in human polymorphonuclear leukocytes.

    abstract::We investigated the involvement of p160ROCK (a Rho-associated coiled coil-forming protein kinase), one of Rho kinases on superoxide anion production (O(2)(-) production), aggregation and adhesion of human polymorphonuclear leukocytes under physiological condition, using a selective p160ROCK inhibitor, (+)-(R)-trans-4-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00593-8

    authors: Kawaguchi A,Ohmori M,Harada K,Tsuruoka S,Sugimoto K,Fujimura A

    更新日期:2000-09-08 00:00:00

  • Brivaracetam and seletracetam, two new SV2A ligands, improve paroxysmal dystonia in the dt sz mutant hamster.

    abstract::Previous examinations demonstrated antidystonic effects of the synaptic vesicle protein 2A (SV2A) ligand levetiracetam in the dt(sz) mutant hamster, an animal model of paroxysmal non-kinesiogenic dyskinesia in which dystonic episodes can be induced by stress. In the present study, we examined the effects of the two ne...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.10.048

    authors: Hamann M,Sander SE,Richter A

    更新日期:2008-12-28 00:00:00

  • Contribution of different opioid systems to footshock-induced analgesia and motor suppression.

    abstract::Mice, subjected footshock, showed a significant increase of pain threshold and motor suppression immediately after the footshock and both effects were partially antagonized by pretreatment with naloxone at high doses. The magnitude of footshock-induced analgesia, but not motor suppression, was significantly less in mo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90287-x

    authors: Nabeshima T,Yamada K,Kameyama T

    更新日期:1983-09-02 00:00:00

  • Electrophysiological and neurochemical investigations on the action of carbamazepine on the rat hippocampus.

    abstract::Carbamazepine moderately depressed the input fiber volley resulting in attenuation of the dendritic epsp and the population spike in CA1 of rat hippocampal slices with a threshold concentration of 20 microM. The depressant effect on the population spike was not antagonized by the adenosine receptor blocker caffeine. P...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90030-5

    authors: Olpe HR,Baudry M,Jones RS

    更新日期:1985-03-26 00:00:00

  • Donepezil blocks voltage-gated ion channels in rat dissociated hippocampal neurons.

    abstract::Donepezil (E2020) is a novel cholinesterase inhibitor for the treatment of Alzheimer's disease. Recent studies show that it may act on targets other than acetylcholinesterase in the brain. In the present study, the actions of donepezil on voltage-gated Na+ and K+ channels were investigated in rat dissociated hippocamp...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.12.004

    authors: Yu B,Hu GY

    更新日期:2005-01-31 00:00:00

  • Silibinin ameliorates diabetic nephropathy via improving diabetic condition in the mice.

    abstract::Diabetic nephropathy (DN) is a major cause of end-stage renal disease and one of the most severe diabetic complications. However, there is lack of effective treatments for DN and the underlying mechanisms of the renal injury remain unclear. In current study, we evaluated the effects of silibinin on DN and further expl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.12.031

    authors: Liu Y,Ye J,Cao Y,Zhang R,Wang Y,Zhang S,Dai W,Ye S

    更新日期:2019-02-15 00:00:00

  • Broad therapeutic treatment window of [Nle(4), D-Phe(7)]alpha-melanocyte-stimulating hormone for long-lasting protection against ischemic stroke, in Mongolian gerbils.

    abstract::Melanocortin peptides have been shown to produce neuroprotection in experimental ischemic stroke. The aim of the present investigation was to identify the therapeutic treatment window of melanocortins, and to determine whether these neuropeptides chronically protect against damage consequent to brain ischemia. A 10-mi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.03.038

    authors: Giuliani D,Leone S,Mioni C,Bazzani C,Zaffe D,Botticelli AR,Altavilla D,Galantucci M,Minutoli L,Bitto A,Squadrito F,Guarini S

    更新日期:2006-05-24 00:00:00

  • Regulation of urokinase plasminogen activator by epigallocatechin-3-gallate in human fibrosarcoma cells.

    abstract::(-)-Epigallocatechin-3-gallate (EGCG), a main flavanol of green tea, potently suppressed the urokinase-type plasminogen activator (uPA) expression in human fibrosarcoma HT 1080 cells. EGCG induced not only the suppression of the uPA promoter activity but also the destabilization of uPA mRNA. EGCG inhibited the phospho...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2003.12.031

    authors: Kim MH,Jung MA,Hwang YS,Jeong M,Kim SM,Ahn SJ,Shin BA,Ahn BW,Jung YD

    更新日期:2004-03-08 00:00:00

  • Metalloporphyrins inhibit nitric oxide-dependent cGMP formation in vivo.

    abstract::Sodium nitroprusside produced a dose-dependent increase in extracellular levels of cGMP in the cerebellar cortex in vivo. This was independent of nitric oxide synthase activity. The metalloporphyrins zinc-protoporphyrin-IX, tin-protoporphyrin-IX and zinc-deuteroporphyrin-IX,2,4-bis glycol prevented the increase in cGM...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90149-x

    authors: Luo D,Vincent SR

    更新日期:1994-05-17 00:00:00

  • Guanabenz, an alpha2-selective adrenergic agonist, activates Ca2+-dependent chloride currents in cystic fibrosis human airway epithelial cells.

    abstract::In cystic fibrosis respiratory epithelial cells, the absence or dysfunction of the chloride channel CFTR (Cystic Fibrosis Transmembrane conductance Regulator) results in reduced chloride ion transport. In contrast, Ca2+-stimulated Cl- secretion is intact in cystic fibrosis airway epithelia. One possible target for dru...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.06.103

    authors: Norez C,Vandebrouck C,Antigny F,Dannhoffer L,Blondel M,Becq F

    更新日期:2008-09-11 00:00:00

  • Characterization of C-terminal tail determinants involved in CRTH2 receptor trafficking: identification of a recycling motif.

    abstract::The molecular mechanisms regulating the trafficking of the CRTH2 receptor are poorly understood. In the present study, we characterize C-terminal tail determinants involved in the agonist-induced trafficking of the CRTH2 receptor for prostaglandin D(2). Our results showed that progressive deletion of C-terminal tail r...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.12.022

    authors: Roy SJ,Parent A,Gallant MA,de Brum-Fernandes AJ,Stanková J,Parent JL

    更新日期:2010-03-25 00:00:00

  • A research update on the therapeutic potential of rhein and its derivatives.

    abstract::Rhein is one of the anthraquinones components of Rheum. It shows excellent clinical efficacy and is widely used in the management of several disease conditions including tumors, inflammation, diabetic nephropathy, and viral infections. In this review, we summarize the recent studies on the pharmacological activities o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2021.173908

    authors: Cheng L,Chen Q,Pi R,Chen J

    更新日期:2021-01-27 00:00:00

  • Reserpine-induced locomotor stimulation in mice chronically treated with typical and atypical antidepressants.

    abstract::Previous studies have shown that chronic treatment with antidepressants (AD) leads to an increased responsiveness of NA systems to noradrenaline (NA) or its agonist. In the present paper the influence is described of a prolonged treatment with AD of different pharmacological profiles on the effect of reserpine in the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90087-0

    authors: Maj J,Rogóz Z,Skuza G,Sowińska H

    更新日期:1983-03-04 00:00:00

  • Design and screening of ASIC inhibitors based on aromatic diamidines for combating neurological disorders.

    abstract::Acid sensing ion channels (ASICs) are implicated in various brain functions including learning and memory and are involved in a number of neurological disorders such as pain, ischemic stroke, depression, and multiple sclerosis. We have recently defined ASICs as one of receptor targets of aromatic diamidines in neurons...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2010.09.005

    authors: Chen X,Orser BA,MacDonald JF

    更新日期:2010-12-01 00:00:00

  • Apoptotic, necrotic, and antiproliferative activity of diosgenin and diosgenin glycosides on cervical cancer cells.

    abstract::(25R)-spirost-5-en-3β-ol, also known as diosgenin (DSG), exerts antiproliferative activity on diverse cell lines, induces apoptosis, and acts as a chemopreventative agent. However, the relationship between DSG glycosides and apoptotic, necrotic, and antiproliferative activity remains unclear. It is in this regard that...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.172942

    authors: Hernández-Vázquez JMV,López-Muñoz H,Escobar-Sánchez ML,Flores-Guzmán F,Weiss-Steider B,Hilario-Martínez JC,Sandoval-Ramírez J,Fernández-Herrera MA,Sánchez Sánchez L

    更新日期:2020-03-15 00:00:00

  • Antithrombin increases pulmonary endothelins: inhibition by heparin and Ca2+ channel antagonism.

    abstract::We investigated the mechanism of antithrombin III-induced vascular release of endothelins in rat isolated lung. The antithrombin III-stimulated release of big endothelin-1 and endothelin-1 (1.7-fold and 1.3-fold over baseline) was abolished by nicardipine (L-type Ca2+ channel blocker), heparin, and N-acetyl heparin (a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00124-7

    authors: Stangl K,Dschietzig T,Alexiou K,Brunner F

    更新日期:1999-04-01 00:00:00

  • Neuroprotective effects of vildagliptin on drug induced Alzheimer's disease in rats with metabolic syndrome: Role of hippocampal klotho and AKT signaling pathways.

    abstract::Growing evidences suggest the presence of several similarities in the molecular mechanisms underlying the neurodegenerative diseases and metabolic abnormalities. Adults who develop Metabolic Syndrome (MS) are at a higher risk of developing Alzheimer's disease (AD). Pharmacological agents, like dipeptidyl peptidase-4 (...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173612

    authors: Yossef RR,Al-Yamany MF,Saad MA,El-Sahar AE

    更新日期:2020-12-15 00:00:00

  • Sodium salicylate acts through direct inhibition of phosphoinositide 3-kinase-like kinases to modulate topoisomerase-mediated DNA damage responses.

    abstract::Chemopreventive non-steroidal anti-inflammatory drugs (NSAIDs) exhibit diverse pharmacological and biological activities mainly through their inhibitory effect on cyclooxygenase (COX). However, COX-independent mechanisms involving kinase inhibition have been proposed to explain certain therapeutic effects of NSAIDs. H...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.04.012

    authors: Fan JR,Huang TH,Wen CY,Shen TL,Li TK

    更新日期:2010-07-25 00:00:00

  • Dinitrosyl iron complexes with glutathione suppress experimental endometriosis in rats.

    abstract::Dinitrosyl iron complexes (DNIC) with glutathione exert a cytotoxic effect on endometrioid tumours in rats with surgically induced experimental endometriosis. Intraperitoneal treatment of rats (Group 1) with DNIC (12.5μmoles/kg, daily, for 12 days), beginning with day 4 after the surgical operation (implantation of tw...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.01.002

    authors: Burgova EN,Tkachev NА,Adamyan LV,Mikoyan VD,Paklina OV,Stepanyan AA,Vanin AF

    更新日期:2014-03-15 00:00:00

  • Comparative effects of dexamethasone and L-canavanine in experimental septic shock.

    abstract::Glucocorticoids can reverse hemodynamic disturbances and dependence on catecholamines in septic shock. The relevant beneficial mechanisms of steroids in septic shock are unknown, although inducible nitric oxide synthase could account for them. The aim of this study was to compare the effects of dexamethasone, a glucoc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)02035-1

    authors: Mansart A,Bollaert PE,Levy B,Nicolas MB,Mallié JP

    更新日期:2003-08-15 00:00:00

  • Decreased peripheral benzodiazepine binding sites in platelets of neuroleptic-treated schizophrenics.

    abstract::A decrease of 30% was observed in the density of peripheral-type benzodiazepine binding sites in platelets of nine schizophrenics maintained on chronic neuroleptic treatment as compared to platelets of six untreated schizophrenics and 15 healthy volunteers. The equilibrium dissociation constant for binding by [3H]PK 1...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90500-5

    authors: Gavish M,Weizman A,Karp L,Tyano S,Tanne Z

    更新日期:1986-02-18 00:00:00

  • Influence of 7-nitroindazole on the anticonvulsive action of conventional antiepileptic drugs.

    abstract::7-Nitroindazole (a selective neuronal nitric oxide (NO) synthase inhibitor) at 25 and 50 mg/kg, 30 min before the test, did not influence the electroconvulsive threshold. However, at 50 mg/kg, it enhanced the anticonvulsive activity of phenobarbital against maximal electroshock and did not affect that of carbamazepine...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01034-0

    authors: Borowicz KK,Kleinrok Z,Czuczwar SJ

    更新日期:1997-07-23 00:00:00

  • Metabotropic glutamate mGlu1 receptor stimulation and blockade: therapeutic opportunities in psychiatric illness.

    abstract::Metabotropic glutamate mGlu(1) receptors play a modulatory role in the nervous system. They enhance cell excitability, modulate synaptic neurotransmission and are involved in synaptic plasticity. During the last 10 years, several selective metabotropic glutamate mGlu(1) receptor competitive antagonists and potentiator...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2009.12.043

    authors: Lesage A,Steckler T

    更新日期:2010-08-10 00:00:00

  • Critical reevaluation of spiperone and benzamide binding to dopamine D2 receptors: evidence for identical binding sites.

    abstract::There are several inconsistencies in the literature as regards the characteristics of benzamide and butyrophenone binding to dopamine D2-like receptors. The variations observed in Bmax, Kd and Ki values have led to hypotheses, such as the existence of a specific "benzamide binding site' and that dopamine D2 receptors ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(96)00080-5

    authors: Malmberg A,Jerning E,Mohell N

    更新日期:1996-05-06 00:00:00