并且它的活性化合物槲皮素作为气道平滑肌收缩的钙抑制剂。
and Its Active Compound Quercetin as Ca Inhibitors in the Contraction of Airway Smooth Muscle.
机构信息
Departamento de Farmacología, Facultad de Medicina, Universidad Nacional Autónoma de México, Avenida Universidad No. 3000, Alcaldía de Coyoacán, C.P., Mexico City 04510, Mexico.
Centro de Investigación en Ciencias Cognitivas, Universidad Autónoma del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, C.P., Cuernavaca 62209, Mexico.
出版信息
Molecules. 2024 May 12;29(10):2284. doi: 10.3390/molecules29102284.
The family includes species considered to be medicinal. Their essential oil is used for headaches, colds, cough, and bronchitis. Cedar trees like () are commonly found in urban areas. We investigated whether exerts some of its effects by modifying airway smooth muscle (ASM) contractility. The leaves of (363 g) were pulverized mechanically, and extracts were obtained by successive maceration 1:10 (:) with methanol/CHCl. Guinea pig tracheal rings were contracted with KCl, tetraethylammonium (TEA), histamine (HIS), or carbachol (Cch) in organ baths. In the Cch experiments, tissues were pre-incubated with D-600, an antagonist of L-type voltage-dependent Ca channels (L-VDCC) before the addition of . Interestingly, at different concentrations, diminished the tracheal contractions induced by KCl, TEA, HIS, and Cch. In ASM cells, significantly diminished L-type Ca currents. ASM cells stimulated with Cch produced a transient Ca peak followed by a sustained plateau maintained by L-VDCC and store-operated Ca channels (SOCC). almost abolished this last response. These results show that , and its active metabolite quercetin, relax the ASM by inhibiting the L-VDCC and SOCC; further studies must be performed to obtain the complete set of metabolites of the extract and study at length their pharmacological properties.
该属植物包含一些被认为具有药用价值的物种。它们的精油可用于治疗头痛、感冒、咳嗽和支气管炎。像 () 这样的雪松通常在城市地区很常见。我们研究了 () 是否通过改变气道平滑肌 (ASM) 的收缩性来发挥其部分作用。将 () 的叶子(363 克)机械粉碎,然后用甲醇/CHCl 以 1:10(:)的比例连续浸渍提取。在器官浴中,用 KCl、四乙铵 (TEA)、组胺 (HIS) 或卡巴胆碱 (Cch) 收缩豚鼠气管环。在 Cch 实验中,组织在加入 () 之前用 L 型电压依赖性钙通道 (L-VDCC) 拮抗剂 D-600 预孵育。有趣的是,在不同浓度下,() 可减弱 KCl、TEA、HIS 和 Cch 诱导的气管收缩。在 ASM 细胞中,() 显著减少 L 型钙电流。用 Cch 刺激的 ASM 细胞产生一个短暂的 Ca 峰,随后由 L-VDCC 和储存操作的钙通道 (SOCC) 维持持续的平台。() 几乎完全消除了这种最后反应。这些结果表明,() 和其活性代谢物槲皮素通过抑制 L-VDCC 和 SOCC 来松弛 ASM;必须进行进一步的研究以获得提取物的完整代谢物组,并深入研究它们的药理学特性。