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Ephedrine alkaloids-free Ephedra Herb extract: a safer alternative to ephedra with comparable analgesic anticancer and anti-influenza activities

机译:不含麻黄碱的生物碱麻黄提取物:具有可比的止痛抗癌和抗流感活性是麻黄的安全替代品

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摘要

It is generally accepted that the primary pharmacological activities and adverse effects of Ephedra Herb are caused by ephedrine alkaloids. Interestingly, our research shows that Ephedra Herb also has ephedrine alkaloid-independent pharmacological actions, such as c-MET inhibitory activity. This study describes the preparation of an ephedrine alkaloids-free Ephedra Herb extract (EFE) by ion-exchange column chromatography, as well as in vitro and in vivo evaluation of its pharmacological actions and toxicity. We confirmed that EFE suppressed hepatocyte growth factor (HGF)-induced cancer cell motility by preventing both HGF-induced phosphorylation of c-Met and its tyrosine kinase activity. We also investigated the analgesic effect of EFE. Although the analgesic effect of Ephedra Herb has traditionally been attributed to pseudoephedrine, oral administration of EFE reduced formalin-induced pain in a dose-dependent manner in mice. Furthermore, we confirmed the anti-influenza virus activity of EFE by showing inhibition of MDCK cell infection in a concentration-dependent manner. All assessments of toxicity, even after repeated oral administration, suggest that EFE would be a safer alternative to Ephedra Herb. The findings described here suggest that EFE has c-Met inhibitory action, analgesic effect, and anti-influenza activity, and that it is safer than Ephedra Herb extract itself. Therefore, EFE could be a useful pharmacological agent.Electronic supplementary materialThe online version of this article (doi:10.1007/s11418-016-0979-z) contains supplementary material, which is available to authorized users.
机译:人们普遍认为麻黄碱的主要药理活性和不良反应是由麻黄碱生物碱引起的。有趣的是,我们的研究表明麻黄还具有非麻黄碱非生物碱药理作用,例如c-MET抑制活性。这项研究描述了通过离子交换柱色谱法制备不含麻黄碱的生物碱麻黄提取物(EFE),以及对其药理作用和毒性的体内和体外评估。我们证实,EFE通过阻止HGF诱导的c-Met磷酸化及其酪氨酸激酶活性,抑制了肝细胞生长因子(HGF)诱导的癌细胞运动。我们还研究了EFE的镇痛作用。尽管传统上将麻黄药草的镇痛作用归因于伪麻黄碱,但口服EFE可以剂量依赖的方式减轻小鼠的福尔马林诱发的疼痛。此外,我们通过以浓度依赖性方式显示出对MDCK细胞感染的抑制作用,证实了EFE的抗流感病毒活性。所有的毒性评估,甚至在重复口服后也表明,EFE将是麻黄药草的更安全替代品。这里描述的发现表明EFE具有c-Met抑制作用,止痛作用和抗流感活性,并且它比麻黄提取物本身更安全。电子补充材料本文的在线版本(doi:10.1007 / s11418-016-0979-z)包含补充材料,授权用户可以使用。

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