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香桃木油主要成分 1-硝基-2-苯乙烷对自发性高血压大鼠肠系膜上动脉的血管舒张作用。

Vasorelaxant effects of 1-nitro-2-phenylethane, the main constituent of the essential oil of Aniba canelilla, in superior mesenteric arteries from spontaneously hypertensive rats.

机构信息

Department of Physiology and Pharmacology, Federal University of Pernambuco, Recife, PE, Brazil.

出版信息

Eur J Pharm Sci. 2013 Mar 12;48(4-5):709-16. doi: 10.1016/j.ejps.2012.12.033. Epub 2013 Jan 10.

Abstract

The present study investigated the mechanisms underlying the vasorelaxant effects of the essential oil of Aniba canelilla (EOAC) and its main constituent 1-nitro-2-phenylethane (NP) in isolated superior mesenteric artery from spontaneously hypertensive rats (SHRs). At 0.1-1000 μg/mL, EOAC and NP relaxed SMA preparations pre-contracted with 75 mMKCl with IC(50) (geometric mean [95% confidence interval]) values of 294.19 [158.20-94.64] and 501.27 [378.60-624.00] μg/mL, respectively); or with phenylephrine (PHE) (IC(50)s=11.07 [6.40-15.68] and 7.91 [4.08-11.74) μg/mL, respectively). All these effects were reversible and remained unaltered by vascular endothelium removal. In preparations maintained under Ca(2+)-free conditions, EOAC and NP (both at 600 μg/mL) reduced the PHE-, but not the caffeine-induced contraction. In Ca(2+)-free and high K(+) (75 mM) medium, the contractions produced by CaCl(2) or BaCl(2) were reduced or even abolished by EOAC and NP at 100 and 600 μg/mL, respectively. EOAC and NP (both at 10-1000 μg/mL) also relaxed the contraction evoked by phorbol dibutyrate (IC(50)=52.66 [10.82-94.64] and 39.13 [31.55-46.72] μg/mL, respectively). It is concluded that NP has a myogenic endothelium-independent vasorelaxant effects and appears to be the active principle of the EOAC. Vasorelaxant effect induced by both EOAC and NP is preferential to receptor-activated pathways and it appears to occur intracellularly more than a superficial action restricted to the membrane environment such as a simple blocking activity on a given receptor or ion channel.

摘要

本研究旨在探讨香桃木油(EOAC)及其主要成分 1-硝基-2-苯乙烷(NP)在自发性高血压大鼠(SHR)离体肠系膜上动脉中的血管舒张作用机制。在 0.1-1000μg/mL 浓度下,EOAC 和 NP 分别以 294.19[158.20-94.64]和 501.27[378.60-624.00]μg/mL 的 IC50 值舒张预收缩于 75mM KCl 的 SMA 标本;或预收缩于苯肾上腺素(PHE)(IC50 分别为 11.07[6.40-15.68]和 7.91[4.08-11.74]μg/mL)的 SMA 标本。所有这些作用均为可逆的,且不受血管内皮去除的影响。在维持于无钙条件下的标本中,EOAC 和 NP(均为 600μg/mL)降低 PHE 引起的收缩,但不降低咖啡因引起的收缩。在无钙和高钾(75mM)介质中,100 和 600μg/mL 的 EOAC 和 NP 分别降低或甚至消除由 CaCl2 或 BaCl2 引起的收缩。EOAC 和 NP(均为 10-1000μg/mL)也舒张佛波醇二丁酸(PDBu)引起的收缩(IC50 分别为 52.66[10.82-94.64]和 39.13[31.55-46.72]μg/mL)。综上所述,NP 具有肌源性内皮非依赖性血管舒张作用,似乎是 EOAC 的活性成分。EOAC 和 NP 引起的血管舒张作用优先于受体激活途径,似乎发生在细胞内,而不是仅限于膜环境的浅表作用,例如对特定受体或离子通道的简单阻断作用。

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