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钙钾通道参与姜黄素对气管平滑肌舒张作用。

Calcium and potassium channels are involved in curcumin relaxant effect on tracheal smooth muscles.

机构信息

Neurogenic Inflammation Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Natural Products and Medicinal Plants Research Center, North Khorasan University of Medical Sciences, Bojnurd, Iran.

出版信息

Pharm Biol. 2020 Dec;58(1):257-264. doi: 10.1080/13880209.2020.1723647.

Abstract

Curcumin, the active component of L. (Zingiberaceae), exhibits a wide variety of biological activities including vasodilation and anti-inflammation. The relaxant effect of curcumin in tracheal smooth muscle (TSM) was not examined so far, thus, this study was designed to assess the relaxant effect of curcumin on rat TSM and examine the underlying mechanism(s) responsible for this effect. TSM was contracted by KCl (60 mM) or methacholine (10 μM), and cumulative concentrations of curcumin (12.5, 25, 50, and 100 mg/mL) or theophylline (0.2, 0.4, 0.6, and 0.8 mM, as positive control) were added to organ bath. The relaxant effect of curcumin was examined in non-incubated or incubated tissues with atropine (1 μM), chlorpheniramine (1 μM), indomethacin (1 μM), and papaverine (100 μM). In non-incubated TSM, curcumin showed significant relaxant effects on KCl-induced contraction in a concentration-dependent manner ( < 0.001 for all concentrations). The relaxant effects of curcumin 12.5, 25, and 50 mg/mL were significantly lower in atropine-incubated tissue compared to non-incubated TSM ( < 0.05 to  < 0.001). A significant difference was observed in EC between atropine-incubated (48.10 ± 2.55) and non-incubated (41.65 ± 1.81) tissues ( < 0.05). Theophylline showed a significant relaxant effect on both KCl and methacholine-induced contraction in a concentration-dependent manner ( < 0.001 for all cases). The results indicated a relatively potent relaxant effect of curcumin on TSM, which was less marked than the effect of theophylline. Calcium channel blocking and/or potassium channel opening properties of curcumin may be responsible for TSM relaxation.

摘要

姜黄,姜科(Zingiberaceae)植物的活性成分,具有多种生物活性,包括血管舒张和抗炎作用。姜黄对气管平滑肌(TSM)的松弛作用尚未被研究,因此,本研究旨在评估姜黄对大鼠 TSM 的松弛作用,并探讨其潜在机制。用 KCl(60mM)或乙酰甲胆碱(10μM)收缩 TSM,依次加入浓度为 12.5、25、50 和 100mg/mL 的姜黄或茶碱(0.2、0.4、0.6 和 0.8mM,作为阳性对照)于器官浴中。在非孵育或孵育组织中,加入阿托品(1μM)、氯苯那敏(1μM)、吲哚美辛(1μM)和罂粟碱(100μM),检测姜黄的松弛作用。在非孵育的 TSM 中,姜黄对 KCl 诱导的收缩表现出浓度依赖性的显著松弛作用(所有浓度均  < 0.001)。与非孵育的 TSM 相比,12.5、25 和 50mg/mL 的姜黄在孵育组织中的松弛作用显著降低(  < 0.05 至  < 0.001)。孵育(48.10 ± 2.55)和非孵育(41.65 ± 1.81)组织之间的 EC 存在显著差异(  < 0.05)。茶碱对 KCl 和乙酰甲胆碱诱导的收缩均呈浓度依赖性显著松弛作用(所有情况下均  < 0.001)。结果表明,姜黄对 TSM 具有相对较强的松弛作用,其作用弱于茶碱。姜黄可能通过阻断钙通道和/或开放钾通道来松弛 TSM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b8b9/7170316/bea1394de11f/IPHB_A_1723647_F0001_C.jpg

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