Cimicifugamide from Cimicifuga rhizomes functions as a nonselective beta-AR agonist for cardiac and sudorific effects
Cimicifugamide from Cimicifuga rhizomes functions as a nonselective beta-AR agonist for cardiac and sudorific effects
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升麻根茎中的升麻酰胺可作为非选择性 β-AR 激动剂，具有强心和发汗作用
DOI：
10.1016/j.biopha.2017.03.058
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发表时间：
2017
影响因子：
7.5
通讯作者：
Bai Gang
中科院分区：
文献类型：
--
作者：
Wang ZengYong;Wang Qian;Zhang Man;Hu XueYan;Ding GuoYu;Jiang Min;Bai Gang
升麻根茎（Cimicifuga rhizomes，CR）是治疗呼吸道和心血管疾病的传统中药，但其关键有效成分及其作用机制尚未报道。本研究采用蟾蜍心力衰竭模型和小鼠发热出汗模型，观察了CR的强心、解热、发汗作用。此外，采用UPLC/Q-TOF-MS结合的β2-AR荧光素酶报告基因检测系统，对CR提取物中的活性成分进行了筛选，并利用上述体外和体内模型对该活性成分进行了验证。结果表明，CR具有抗心力衰竭、解热、发汗作用，此作用可被心得安拮抗。另一方面，从CR中筛选出升麻酰胺为β2-AR激动剂，并且在β-AR选择性评估中，升麻酰胺对β1，2-AR的激活作用比β3-AR更显著。研究结果不仅揭示了CR传统使用中的关键有效成分及其作用机理，而且为CR的质量控制提供了特征性的补充成分。
Cimicifuga rhizomes (CR) are used in the treatment of respiratory and cardiovascular diseases in traditional Chinese medicine, but their key effective components and mechanism of action have not yet been reported. In this study, the cardiac, antipyretic and sudorific effects of CR were evaluated using the toad heart failurein vitromodel and mice fever and sweatingin vivomodels. Moreover, the UPLC/Q-TOF-MS-integrated β2-AR luciferase reporter gene assay system was used to screen the bioactive ingredients from CR extract, and the activity of this ingredient were verified using the above-mentionedin vitroandvivomodels. Our results showed that CR had anti-heart failure, antipyretic and sweating effects, which could be antagonized by propranolol. On the other hand, cimicifugamide was screened as β2-AR agonist from CR and cimicifugamide could activate β1, 2-ARs more significantly than β3-AR in β-ARs selectivity assessment. The results not only revealed the key effective components and mechanism of CR in traditional use but also supplied a characteristic complementary ingredient for quality control of CR.