关键词: Chamaecyparis lawsoniana L-type voltage-dependent Ca2+ channels airway smooth muscle relaxation quercetin store-operated Ca2+ channels

Mesh : Animals Guinea Pigs Muscle, Smooth / drug effects metabolism Muscle Contraction / drug effects Quercetin / pharmacology chemistry Trachea / drug effects metabolism Plant Extracts / pharmacology chemistry Chamaecyparis / chemistry Calcium / metabolism Male Calcium Channel Blockers / pharmacology Histamine / metabolism Calcium Channels, L-Type / metabolism Plant Leaves / chemistry

来  源:   DOI:10.3390/molecules29102284   PDF(Pubmed)

Abstract:
The Cupressaceae family includes species considered to be medicinal. Their essential oil is used for headaches, colds, cough, and bronchitis. Cedar trees like Chamaecyparis lawsoniana (C. lawsoniana) are commonly found in urban areas. We investigated whether C. lawsoniana exerts some of its effects by modifying airway smooth muscle (ASM) contractility. The leaves of C. lawsoniana (363 g) were pulverized mechanically, and extracts were obtained by successive maceration 1:10 (w:w) with methanol/CHCl3. 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 Ca2+ channels (L-VDCC) before the addition of C. lawsoniana. Interestingly, at different concentrations, C. lawsoniana diminished the tracheal contractions induced by KCl, TEA, HIS, and Cch. In ASM cells, C. lawsoniana significantly diminished L-type Ca2+ currents. ASM cells stimulated with Cch produced a transient Ca2+ peak followed by a sustained plateau maintained by L-VDCC and store-operated Ca2+ channels (SOCC). C. lawsoniana almost abolished this last response. These results show that C. lawsoniana, 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.
摘要:
柏科包括被认为是药用的物种。他们的精油用于治疗头痛,感冒,咳嗽,还有支气管炎.雪松树,如Chamaecyprislawsoniana(C.lawsoniana)常见于城市地区。我们调查了C.lawsoniana是否通过改变气道平滑肌(ASM)收缩力来发挥其某些作用。将C.lawsoniana(363g)的叶子进行机械粉碎,通过用甲醇/CHCl3连续浸渍1:10(w:w)获得提取物。豚鼠气管环用氯化钾收缩,四乙基铵(TEA),组胺(HIS),或器官浴中的卡巴胆碱(Cch)。在Cch实验中,在添加C.lawsoniana之前,将组织与D-600预孵育,D-600是L型电压依赖性Ca2通道(L-VDCC)的拮抗剂。有趣的是,在不同的浓度下,C.lawsoniana减少了KCl引起的气管收缩,茶,HIS,还有Cch.在ASM单元格中,C.lawsoniana显着降低了L型Ca2电流。用Cch刺激的ASM细胞产生瞬时Ca2峰,随后是由L-VDCC和储存操作的Ca2通道(SOCC)维持的持续平台。C.lawsoniana几乎废除了这最后的回应。这些结果表明C.lawsoniana,及其活性代谢物槲皮素,通过抑制L-VDCC和SOCC来放松ASM;必须进行进一步的研究以获得提取物的完整代谢物集,并详细研究其药理学性质。
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