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Semen cassiae Extract Inhibits Contraction of Airway Smooth Muscle

机译:精液提取物抑制气道平滑肌收缩

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摘要

β2-adrenoceptor agonists are commonly used as bronchodilators to treat obstructive lung diseases such as asthma and chronic obstructive pulmonary disease (COPD), however, they induce severe side effects. Therefore, developing new bronchodilators is essential. Herbal plants were extracted and the extracts’ effect on airway smooth muscle (ASM) precontraction was assessed. The ethyl alcohol extract of semen cassiae (EESC) was extracted from Semen cassia. The effects of EESC on the ACh- and 80 mM K+-induced sustained precontraction in mouse and human ASM were evaluated. Ca2+ permeant ion channel currents and intracellular Ca2+ concentration were measured. HPLC analysis was employed to determine which compound was responsible for the EESC-induced relaxation. The EESC reversibly inhibited the ACh- and 80 mM K+-induced precontraction. The sustained precontraction depends on Ca2+ influx, and it was mediated by voltage-dependent L-type Ca2+ channels (LVDCCs), store-operated channels (SOCs), TRPC3/STIM/Orai channels. These channels were inhibited by aurantio-obtusin, one component of EESC. When aurantio-obtusin removed, EESC’s action disappeared. In addition, aurantio-obtusin inhibited the precontraction of mouse and human ASM and intracellular Ca2+ increases. These results indicate that Semen cassia-contained aurantio-obtusin inhibits sustained precontraction of ASM via inhibiting Ca2+-permeant ion channels, thereby, which could be used to develop new bronchodilators.
机译:β2-肾上腺素受体激动剂通常用作支气管扩张剂,用于治疗阻塞性肺部疾病,例如哮喘和慢性阻塞性肺部疾病(COPD),但是它们会引起严重的副作用。因此,开发新的支气管扩张剂至关重要。提取草药植物,并评估提取物对气道平滑肌(ASM)预收缩的作用。从决明子提取精液的乙醇提取物(EESC)。评估了EESC对ACh-和80 mM K + 诱导的小鼠和人ASM持续预收缩的作用。测量Ca 2 + 离子通道电流和细胞内Ca 2 + 浓度。 HPLC分析用于确定哪种化合物引起了ESCC诱导的松弛。 EESC可逆地抑制ACh-和80 mM K + 诱导的预收缩。持续的预收缩取决于Ca 2 + 的涌入,它是由电压依赖性L型Ca 2 + 通道(LVDCC),存储操作通道(SOC)介导的,TRPC3 / STIM / Orai频道。这些通道被EESC的一种成分aurantio-obtusin抑制。去除金黄色-小tus素后,ESC的动作消失了。此外,aurantio-obtusin抑制了小鼠和人ASM的预收缩,并且细胞内Ca 2 + 升高。这些结果表明,精子决明子中的aurantio-obtusin通过抑制Ca 2 + 渗透离子通道而抑制了ASM的持续预收缩,从而可用于开发新的支气管扩张剂。

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