Resveratrol and genistein inhibition of rat isolated gastrointestinal contractions and related mechanisms

Zhang, Lixue; Li, Hongfang; Wang, Longde; Jin, Songqing; Dou, Xing-Cheng; Tian, Zhongmin; Ma, Qin

doi:10.3748/wjg.v20.i41.15335

Cited by 9 publications

(16 citation statements)

References 26 publications

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“…This observation is consistent with those reported for the effects of flavonoids on GI smooth muscles of rats and guinea pigs. 9,10,36,39,40 Modulation of NO metabolism is one of the possible mechanisms that may contribute to the explanation of polyphenol activity observed in vivo. In the stomach, polyphenols in the diet may not only promote the reduction of nitrites toward NO, but also deal with a complex network of chemical reactions to produce NO with its signaling functions.…”

Section: Discussionmentioning

confidence: 99%

Quercetin relaxes human gastric smooth muscles directly through ATP‐sensitive potassium channels and not depending on the nitric oxide pathway

Modzelewska

Drygalski

Kleszczewski

et al. 2021

Neurogastroenterology Motil

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Background: Quercetin has recently become a remarkably popular subject of research due to its broad beneficial pharmacological properties. The goal of our study was to observe its effects on contractility of human gastric smooth muscles in reference to the NO pathway and direct influence of potassium channels.Methods: Tissues were obtained from patients undergoing sleeve gastrectomy due to morbid obesity (n = 10 aged 24-56; BMI 47.16 ± 1.84). The following parameters were evaluated in the recordings: area under the curve (AUC), average baseline muscle tone, and relative change in muscle contraction. Key Results: Quercetin induced noticeable, dose-dependent relaxation of the carbachol treated gastric strips. The substantial effect was noted at concentrations higher than 10 −7 mol/L and maximal at 10 −4 mol/L (81.82 ± 3.32%; n = 10; p < 0.0001) of the control.Neither NOS blockers nor guanylyl cyclase blockers had inhibitory effects on the relaxation of strips induced by examined polyphenol. Glibenclamide inhibited the relaxing effect of quercetin, significant at concentrations higher than 5⋅10 −5 mol/L. Preincubation with charybdotoxin or apamin extended the relaxing effect of quercetin (from 10 −6 mol/L).Tamoxifen, in turn, significantly increased muscle relaxation at all quercetin concentrations. Conclusions & Inferences:In conclusion, the current study was the first to show that quercetin-induced relaxation of human gastric smooth muscle occurs directly through K + ATP channels and independently to NO pathways. The present results suggest that quercetin is a potential nutraceutical in the treatment of functional gastrointestinal dyspepsia and other minor gastric muscle motility disturbance.

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Section: Discussionmentioning

confidence: 99%

Quercetin relaxes human gastric smooth muscles directly through ATP‐sensitive potassium channels and not depending on the nitric oxide pathway

Modzelewska

Drygalski

Kleszczewski

et al. 2021

Neurogastroenterology Motil

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“…The proposed mechanism in this study included K ATP channels as target site for RSV. Additionally, another study conducted on gastrointestinal smooth muscle from rats, also confirms that RSV and genistein relax those muscle and confirm that K ATP channels are included in the reduction of the mean contractile amplitude (61). Furthermore, it has been shown that in RSV-induced relaxation of human gallbladder smooth muscle K ATP channels are involved (62).…”

Section: Effects Of Resveratrol On the Smooth Muscle K Atp Channelsmentioning

confidence: 62%

“…However, growing number of studies tends to evaluate more efficacy approaches in the treatment of such diseases and the natural products with anti-inflammatory properties have very promising potential. In studies evaluating potential use of RSV for the treatment of biliary colic and other gastrointestinal colic-like pain (61), it was shown that K ATP and BK Ca channels are directly involved in the RSV-mediated relaxation pathways. Certain proportion in this response plays K-independent mechanisms which include NO, cAMP and cGMP signal pathways (62).…”

Section: Effects Of Resveratrol On the Smooth Muscle Potassium Channels In The Gastrointestinal Systemmentioning

confidence: 99%

Potassium channels on smooth muscle as a molecular target for plant-derived Resveratrol

Rajković

Djokic

Gostimirović

et al. 2020

Cell Mol Biol (Noisy-le-grand)

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Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a phytoalexin present in a variety of plant species. Resveratrol has a wide spectrum of pharmacologic properties, and it exhibits versatile biological effects on different human and animal models. The studies have shown that potassium (K) channels can be potential targets in the mechanism of resveratrol action. K channels play a crucial role in maintaining membrane potential. Inhibition of K channels causes membrane depolarization and then contraction of smooth muscles, while the activation leads to membrane hyperpolarization and subsequently, relaxation. Five diverse types of K channels have been identified in smooth muscle cells in different tissue: ATP-sensitive K channels (K ATP ), voltage-dependent K channels (Kv), Ca 2+ -and voltagedependent K channels (BK Ca ), inward rectifier K channels (Kir), and tandem two-pore K channels (K 2P ). The expression and activity of K channels altered in many types of diseases. Aberrant function or expression of K channels can be underlying in pathologies such as cardiac arrhythmia, diabetes mellitus, hypertension, preterm birth, preeclampsia, and various types of cancer. Modulation of K channel activity by molecular approaches and selective drug development may be a novel treatment modality for these dysfunctions in the future. The plant-derived non-toxic polyphenols, such as resveratrol, can alter K channel activity and lead to the desired outcome. This review presents the basic properties, physiological, pathophysiological functions of K channels, and pharmacological roles of resveratrol on the major types of K channels that have been determined in smooth muscle cells.

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“…In other tissues, resveratrol relaxations could be partially blocked by glibenclamide or 4-AP, even when TEA failed to block the relaxation. 26,38 However, this was not the case with bovine retinal arteries. All used K þ blockers failed to block the relaxation of resveratrol.…”

Section: Discussionmentioning

confidence: 98%

Vasorelaxing Effect of Resveratrol on Bovine Retinal Arteries

Daele

Boydens

Pauwels

et al. 2016

Invest. Ophthalmol. Vis. Sci.

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Resveratrol and genistein inhibition of rat isolated gastrointestinal contractions and related mechanisms

Abstract: Resveratrol and genistein relax gastrointestinal smooth muscle via α-adrenergic receptors, nitric oxide and cyclic adenosine monophosphate pathways, ATP-sensitive potassium channels, and inhibition of L-type Ca(2+) channels.

Cited by 9 publications

References 26 publications

Quercetin relaxes human gastric smooth muscles directly through ATP‐sensitive potassium channels and not depending on the nitric oxide pathway

Quercetin relaxes human gastric smooth muscles directly through ATP‐sensitive potassium channels and not depending on the nitric oxide pathway

Potassium channels on smooth muscle as a molecular target for plant-derived Resveratrol

Vasorelaxing Effect of Resveratrol on Bovine Retinal Arteries

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