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(,)-法尼醇通过人脐动脉中的离子通道促进血管舒张。

Vasodilation promoted by (,)-farnesol involving ion channels in human umbilical arteries.

作者信息

Batista Paulo Ricardo, Silva Andressa de Alencar, de Sena Bastos Carla Mikevely, Rodrigues da Silva Renata Evaristo, Calixto Gabriela Lucena, de Morais Luís Pereira, Delmondes Gyllyandeson de Araújo, Kerntopf Marta Regina, de Menezes Irwin Rose Alencar, Barbosa Roseli

机构信息

Biological Chemistry Department, Pimenta Campus, Regional University of Cariri, Crato, 63105-000, Ceará, Brazil.

Biological Sciences Department, Physiopharmacology of Excitable Cells Laboratory, Pimenta Campus, Regional University of Cariri, Crato, 63105-000, Ceará, Brazil.

出版信息

Heliyon. 2023 Jun 16;9(6):e17328. doi: 10.1016/j.heliyon.2023.e17328. eCollection 2023 Jun.

Abstract

BACKGROUND

(,)-farnesol is a sesquiterpene alcohol derived from plants and animals that exhibits pharmacological properties in the cardiovascular system. However, its effects on human umbilical vessels remain unknown.

PURPOSE

Thus, this study aims to characterize the vasodilatory effect of (,)-farnesol in human umbilical arteries (HUA).

STUDY DESIGN

The tissue is obtained from pregnant women over 18 years of age, normotensive, and without prepartum complications. After collected, the tissue was segmented and dissected to remove Wharton's jelly and obtain the umbilical arteries segments.

METHODS

HUA segments were isolated and sectioned into rings that were subjected to isometric tension recordings in an organ bath.

RESULTS

(,)-farnesol (1 μmol/L to 1 mmol/L) promoted vasodilatory effect in HUA preparations, affecting basal tone, and inhibiting the electromechanical coupling induced by KCl 60 mmol/L with greater potency (EC 225.3 μmol/L) than the pharmacomechanical coupling induced by 5-HT 10 μmol/L (EC 363.5 μmol/L). In the absence of extracellular calcium, pharmacomechanical coupling was also abolished, and contractions induced by CaCl or BaCl were attenuated by (,)-farnesol indicating a possible direct inhibition of L-type VOCC as a mechanism of the vasodilatory effect. The vasodilator efficacy of (,)-farnesol on reduction of vasocontraction induced by the presence of tetraethylammonium (1 or 10 mmol/L), 4-aminopyridine (1 mmol/L) and glibenclamide (10 μmol/L) suggesting a possible influence of different potassium channels (BK, K and K).

CONCLUSION

These results suggest that (,)-farnesol may be a promising pharmacological candidate for obstetric hypertensive disorders.

摘要

背景

(±)-法尼醇是一种来源于植物和动物的倍半萜醇,在心血管系统中具有药理特性。然而,其对人脐血管的作用尚不清楚。

目的

因此,本研究旨在表征(±)-法尼醇在人脐动脉(HUA)中的血管舒张作用。

研究设计

组织取自18岁以上、血压正常且无产前并发症的孕妇。采集后,将组织进行分割和解剖,去除华通氏胶,获得脐动脉段。

方法

分离HUA段并切成环,在器官浴中进行等长张力记录。

结果

(±)-法尼醇(1μmol/L至1mmol/L)在HUA制剂中促进血管舒张作用,影响基础张力,并抑制由60mmol/L KCl诱导的机电偶联,其效力(EC225.3μmol/L)高于由10μmol/L 5-HT诱导的药理机械偶联(EC363.5μmol/L)。在无细胞外钙的情况下,药理机械偶联也被消除,并且(±)-法尼醇减弱了由CaCl或BaCl诱导的收缩,表明可能直接抑制L型电压门控钙通道作为血管舒张作用的机制。(±)-法尼醇对由四乙铵(1或10mmol/L)、4-氨基吡啶(1mmol/L)和格列本脲(10μmol/L)存在诱导的血管收缩减少的血管舒张效力,提示可能对不同钾通道(BK、K和K)有影响。

结论

这些结果表明,(±)-法尼醇可能是产科高血压疾病的一种有前景的药理学候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f916/10333471/a34d73bfcdf0/gr1.jpg

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