Biological Chemistry Department, Pimenta Campus, Regional University of Cariri, Crato 63105-000, Ceará, Brazil.
Physiopharmacology of Excitable Cells Laboratory, Biological Sciences Department, Pimenta Campus, Regional University of Cariri, Crato 63105-000, Ceará, Brazil.
Curr Med Chem. 2024;31(42):7072-7082. doi: 10.2174/0109298673269428231204064101.
Perillyl alcohol (POH) is a monoterpenoid found in plant essential oils and has been shown to relax murine vessels, but its effect on human vessels remains poorly studied.
The study aimed to characterize the effect of POH on human umbilical arteries (HUA).
Rings of HUA were obtained from uncomplicated patients and suspended in an organ bath for isometric recording. The vasorelaxant effect of POH in HUA was evaluated on basal tone and electromechanical or pharmacomechanical contractions, and possible mechanisms of action were also investigated.
POH (1-1000 μM) altered the basal tone of HUA and completely relaxed HUA rings precontracted with KCl (60 mM) or 5-HT (10 μM), obtaining greater potency in the pharmacomechanical pathway (EC 110.1 μM), suggesting a complex interference in the mobilization of extra- and intracellular Ca. POH (1000 μM) inhibited contractions induced by BaCl (0.1-30 mM) in a similar way to nifedipine (10 μM), indicating a possible blockade of L-type VOCC. In the presence of potassium channel blockers, tetraethylammonium (1 mM), 4-aminopyridine (1 mM), or glibenclamide (10 μM), an increase in the EC value of the POH was observed, suggesting a modulation of the activity of BK, K, and K channels.
The data from this study suggest that POH modulates Ca and K ion channels to induce a relaxant response in HUA.
芳樟醇(POH)是植物精油中的单萜烯,已被证明可使小鼠血管舒张,但对人血管的影响仍研究甚少。
本研究旨在研究 POH 对人脐动脉(HUA)的作用。
从无并发症的患者中获得 HUA 环,并将其悬挂在器官浴中进行等长记录。评估 POH 对 HUA 基础张力和机电或药理机械收缩的血管舒张作用,并研究可能的作用机制。
POH(1-1000μM)改变了 HUA 的基础张力,并完全松弛了用 KCl(60mM)或 5-HT(10μM)预收缩的 HUA 环,在药理机械途径中获得更大的效力(EC 110.1μM),表明对细胞内外 Ca 的动员有复杂的干扰。POH(1000μM)以类似于硝苯地平(10μM)的方式抑制由 BaCl(0.1-30mM)引起的收缩,表明可能对 L 型 VOCC 有阻滞作用。在钾通道阻滞剂四乙铵(1mM)、4-氨基吡啶(1mM)或格列本脲(10μM)存在的情况下,观察到 POH 的 EC 值增加,表明 BK、K 和 K 通道活性的调节。
本研究的数据表明,POH 通过调节 Ca 和 K 离子通道诱导 HUA 产生舒张反应。