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大豆黄酮对正常和高收缩状态下肠道蠕动的抑制作用。

Inhibitory effects of daidzein on intestinal motility in normal and high contractile states.

机构信息

Department of Pharmacology, Dalian Medical University, Dalian, China.

出版信息

Pharm Biol. 2012 Dec;50(12):1561-6. doi: 10.3109/13880209.2012.698285. Epub 2012 Sep 15.

Abstract

CONTEXT

Daidzein is a naturally occurring compound and has various health benefits. However, its effects on intestinal smooth muscle contractility remain unknown.

AIMS

The present study was to characterize the effects of daidzein on the contractility of isolated jejunal smooth muscle and its underlying mechanisms.

METHODS

Ex vivo assay was selected as the major method to determine the effects of daidzein on the contractility of isolated jejunal smooth muscle fragment (JSMF).

RESULTS

Daidzein (5-160 µmol/L) inhibited the contractility of JSMF in normal contractile state and in a dose-dependent manner. Daidzein also inhibited the contractility of JSMF induced by ACh, histamine, erythromycin and high Ca²⁺, respectively, and decreased charcoal propulsion in the small intestine in vivo. The inhibitory effects of daidzein were partially blocked by phentolamine or propranolol and were abolished in the presence of varapamil or at Ca²⁺-free assay condition. However, the inhibitory effects of daidzein on jejunal contraction were not significantly influenced by nitric oxide (NO) synthase inhibitor L-NG-nitro-arginine (L-NNA). Daidzein was also found to directly inhibit the phosphorylation and Mg²⁺-ATPase activity of smooth muscle myosin.

DISCUSSION AND CONCLUSION

The results implicated that α- and β-adrenergic receptors were involved in the inhibitory effects produced by daidzein rather than via NO pathway. As a phytoestrogen, daidzein has shown its potential value in relieving the hypercontractility of small intestine.

摘要

背景

大豆黄苷是一种天然存在的化合物,具有多种健康益处。然而,其对肠道平滑肌收缩性的影响尚不清楚。

目的

本研究旨在研究大豆黄苷对离体空肠平滑肌收缩性的影响及其潜在机制。

方法

采用离体实验方法,选择空肠平滑肌片段(JSMF)作为主要方法,确定大豆黄苷对 JSMF 收缩性的影响。

结果

大豆黄苷(5-160 μmol/L)以剂量依赖性方式抑制正常收缩状态和 ACh、组胺、红霉素和高 Ca²⁺诱导的 JSMF 收缩性,并降低体内小肠炭推进。大豆黄苷的抑制作用可被酚妥拉明或普萘洛尔部分阻断,并在存在维拉帕米或无 Ca²⁺条件下被消除。然而,一氧化氮(NO)合酶抑制剂 L-NG-硝基-精氨酸(L-NNA)对大豆黄苷抑制空肠收缩的作用影响不大。大豆黄苷还被发现直接抑制平滑肌肌球蛋白的磷酸化和 Mg²⁺-ATP 酶活性。

讨论与结论

结果表明,α-和β-肾上腺素能受体参与了大豆黄苷产生的抑制作用,而不是通过 NO 途径。作为一种植物雌激素,大豆黄苷在缓解小肠过度收缩方面显示出了潜在的价值。

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