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8-异前列腺素F2α在大鼠肺动脉中的舒张功能证据。

Evidence for a dilator function of 8-iso prostaglandin F2 alpha in rat pulmonary artery.

作者信息

Jourdan K B, Evans T W, Curzen N P, Mitchell J A

机构信息

Unit of Critical Care Medicine, Royal Brompton Hospital, London.

出版信息

Br J Pharmacol. 1997 Apr;120(7):1280-5. doi: 10.1038/sj.bjp.0701052.

Abstract
  1. 8-Iso prostaglandin F2 alpha (8-iso PGF2 alpha) is one of a series of prostanoids formed independently of the cyclo-oxygenase pathway. It has been shown to be upregulated in many conditions of oxidant stress where its formation is induced by free radical-catalysed actions on arachidonic acid. As 8-iso PGF2 alpha is formed in vivo in diseases in which oxidant stress is high such as septic shock, we have assessed the relative potency and efficacy of this compound in pulmonary arteries from control and lipopolysaccharide (LPS)-treated rats. 2. Several studies have characterized the contractile actions of 8-iso PGF2 alpha on various smooth muscle preparations, but its potential dilator actions have not been addressed. Thus these studies examined both the contractile and dilator actions of 8-iso PGF2 alpha in rat pulmonary artery rings. The thromboxane mimetic U46619, PGE2 sodium nitroprusside (SNP) and acetyl choline (ACh) were used for comparison. Each prostanoid had to be dissolved in ethanol to a maximum concentration of 1 x 10-2 M. At high concentrations, ethanol directly contracted pulmonary vessels. We were therefore limited by the actions of the vehicle such that we were unable to add prostanoids at concentrations higher than 1 x 10-4 M. In some cases this meant that maximum responses were not achieved and in these cases the Emax and pD2 values are apparent estimates. 3. The following rank order of potency was obtained from contractile studies; U46619 > 8-iso PGF2 alpha > PGE2, each prostanoid producing concentration-dependent contractions (10(-10)-3 x 10(-4) M, 10(-9)-10(-4) M, 10(-8)-10(-4) M, respectively). As has been shown previously for other smooth muscle preparations, the thromboxane receptor (TP) antagonist ICI 192605, (1 x 10(-6), 1 x 10(-5) and 1 x 10(-4) M), inhibited the contractions of 8-iso PGF2 alpha in a concentration-dependent fashion. 4. The nitric oxide synthase inhibitor, NG-nitro-L-arginine methyl ester (L-NAME; 1 x 10(-4) M), enhanced the contractile function of both 8-iso PGF2 alpha and PGE2, but had no effect on that caused by U46619. Similarly, L-NAME inhibited the dilator function of all agents tested except the exogenous nitric oxide (NO) donor SNP indicating that PGE2 and 8-iso PGF2 alpha like ACh, act through the release of NO. The specificity of the effects of L-NAME were confirmed in studies with the inactive enantiomer D-NAME (1 x 10(-4) M), which did not affect the contractile or the dilator actions of 8-iso PGF2 alpha. Furthermore, ICI 192605 enhanced the dilator actions of 8-iso PGF2 alpha, suggesting that the dilator component of 8-iso PGF2 alpha was achieved via activation of a non-TP receptor. 5. Isoprostanes may modulate vascular tone by a direct action on TP receptors to cause contraction and via a distinct receptor leading to the release of NO to cause dilation.
摘要
  1. 8-异前列腺素F2α(8-iso PGF2α)是一系列独立于环氧化酶途径形成的前列腺素类物质之一。已表明在许多氧化应激条件下其表达上调,在这些条件下,其形成是由自由基对花生四烯酸的催化作用诱导的。由于8-iso PGF2α在体内高氧化应激的疾病如脓毒性休克中形成,我们评估了该化合物在对照大鼠和脂多糖(LPS)处理大鼠肺动脉中的相对效价和功效。2. 多项研究已对8-iso PGF2α对各种平滑肌制剂的收缩作用进行了表征,但其潜在的舒张作用尚未得到研究。因此,这些研究考察了8-iso PGF2α在大鼠肺动脉环中的收缩和舒张作用。使用血栓素类似物U46619、前列腺素E2、硝普钠(SNP)和乙酰胆碱(ACh)作为对照。每种前列腺素必须溶解在乙醇中,最大浓度为1×10-2 M。在高浓度时,乙醇会直接使肺血管收缩。因此,我们受到溶剂作用的限制,无法添加浓度高于1×10-4 M的前列腺素。在某些情况下,这意味着无法达到最大反应,在这些情况下,Emax和pD2值是表观估计值。3. 从收缩研究中得到以下效价顺序:U46619>8-iso PGF2α>前列腺素E2,每种前列腺素均产生浓度依赖性收缩(分别为10(-10)-3×10(-4)M、10(-9)-10(-4)M、10(-8)-10(-4)M)。如先前在其他平滑肌制剂中所示,血栓素受体(TP)拮抗剂ICI 192605(1×10(-6)、1×10(-5)和1×10(-4)M)以浓度依赖性方式抑制8-iso PGF2α的收缩。4. 一氧化氮合酶抑制剂NG-硝基-L-精氨酸甲酯(L-NAME;1×10(-4)M)增强了8-iso PGF2α和前列腺素E2的收缩功能,但对U46619引起的收缩无影响。同样,L-NAME抑制了除外源性一氧化氮(NO)供体SNP外所有测试药物的舒张功能,表明前列腺素E2和8-iso PGF2α与ACh一样,通过释放NO起作用。L-NAME作用的特异性在使用无活性对映体D-NAME(1×10(-4)M)的研究中得到证实,D-NAME不影响8-iso PGF2α的收缩或舒张作用。此外,ICI 192605增强了8-iso PGF2α的舒张作用,表明8-iso PGF2α的舒张成分是通过激活非TP受体实现的。5. 异前列腺素可能通过直接作用于TP受体引起收缩以及通过不同受体导致NO释放引起舒张来调节血管张力。

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