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苯丙素类化合物对血管的舒张作用:丁香酚和甲基丁香酚在人脐静脉中的作用。

Vasorelaxant effect of phenylpropanoids: Methyl eugenol and eugenol in human umbilical cord vein.

机构信息

Postgraduate Program in Physiological Sciences of the Universidade Estadual do Ceará - PPGCF/UECE, Fortaleza, Ceará, Brazil; Laboratory of Physiopharmacology of Excitable Cells of the Universidade Regional do Cariri - LFCE/URCA, Crato, Ceará, Brazil.

Multicenter Postgraduate Program in Biochemistry and Molecular Biology at the Universidade Federal do Cariri - UFCA, Center for Agricultural Sciences and Biodiversity, Crato, Ceará, Brazil.

出版信息

Biomed Pharmacother. 2024 Sep;178:117227. doi: 10.1016/j.biopha.2024.117227. Epub 2024 Jul 30.

DOI:10.1016/j.biopha.2024.117227
PMID:39084083
Abstract

Methyl-eugenol (ME) and eugenol (EUG) are phenylpropanoids with vasodilatory effects. While EUG's vasorelaxant effect in human umbilical artery (HUA) is known, their action in veins is unclear. This study aimed to evaluate ME and EUG in human umbilical vein (HUV). Isolated HUV underwent tension recordings. ME and EUG caused 100 % relaxation in HUV, with EC values corresponding to: 174.3 ± 7.3 and 217.3 ± 6.2 µM for ME and EUG respectively in presence of K; 362.3 ± 5.4 and 227.7 ± 4.9 µM for ME and EUG respectively and in presence of serotonin (5-HT). It was observed that in presence of BaCl and CaCl evoked contractions, ME (800 and 1000 µM) and EUG (1000 and 1400 µM) prevent the contractions. In presence of K channel blockers it was observed that ME promoted relaxation compared to its control, except in presence of 4-AP, suggesting a possible Ca-dependent K channel activation for this molecule; EUG increased all EC in presence of the K blockers except in presence of TEA 1 mM. Greater pharmacological potency was observed for ME. This study highlights natural substances' effects on HUV contractile parameters, suggesting ME and EUG as potential vasodilators in maintaining fetal oxygenation and venous flow during gestational hypertensive syndromes.

摘要

甲基丁香酚(ME)和丁香酚(EUG)是具有血管舒张作用的苯丙烷类化合物。虽然已知 EUG 对人脐动脉(HUA)具有血管舒张作用,但它在静脉中的作用尚不清楚。本研究旨在评估 ME 和 EUG 在人脐静脉(HUV)中的作用。分离的 HUV 进行张力记录。ME 和 EUG 引起 HUV 完全松弛,EC 值分别为:K 存在时 ME 和 EUG 分别为 174.3 ± 7.3 和 217.3 ± 6.2 µM;5-HT 存在时 ME 和 EUG 分别为 362.3 ± 5.4 和 227.7 ± 4.9 µM。观察到在 BaCl 和 CaCl 引起的收缩存在下,ME(800 和 1000 µM)和 EUG(1000 和 1400 µM)可预防收缩。在 K 通道阻滞剂存在的情况下,与对照相比,ME 促进了松弛,除了在 4-AP 存在的情况下,这表明该分子可能激活了 Ca 依赖性 K 通道;EUG 增加了所有 EC 在 K 阻滞剂存在的情况下,除了 TEA 1 mM 存在的情况。ME 表现出更大的药理学效力。本研究强调了天然物质对 HUV 收缩参数的影响,提示 ME 和 EUG 可能作为维持胎儿在妊娠期高血压综合征期间氧合和静脉血流的血管扩张剂。

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