Abstract
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.
Highlights
Electronic supplementary material The online version of this article contains supplementary material, which is available to authorized users.Ephedra Herb is a crude drug containing ephedrine alkaloids, and is used in Japan as a component in many Kampo formulae, including maoto, kakkonto, shoseiryuto, and eppikajutsubuto
Recent data suggest that Ephedra Herb contains active ingredients other than ephedrine alkaloids, such as herbacetin glycosides [12], and possesses ephedrine alkaloid-independent pharmacological actions [13]
We show that EFE has a c-Met inhibitory action, analgesic effect, and anti-influenza activity without toxicity
Summary
Electronic supplementary material The online version of this article (doi:10.1007/s11418-016-0979-z) contains supplementary material, which is available to authorized users. Our studies confirmed that the c-Met inhibitory activity of maoto derives from Ephedra Herb, which impairs HGF-induced cancer cell motility by suppressing the HGF-c-Met signaling pathway through inhibition of c-Met tyrosine kinase activity [4]. Herbacetin, the aglycone of these herbacetinglycosides, inhibits HGF-induced cell migration and phosphorylation of c-Met [13] These findings suggest that herbacetin-glycosides are bioactive constituents of Ephedra Herb that may be responsible for its pharmacological actions not mediated by ephedrine alkaloids. We predicted that c-Met inhibitory activity may be produced by the non-alkaloidal fraction of Ephedra Herb extract, which contains herbacetin-glycosides and other bioactive molecules that produce synergistic effects. The non-alkaloidal fraction of Ephedra Herb is useful for cancer patients, because adverse effects caused by ephedrine alkaloids are avoided. We report the pharmacological and toxicological properties of EFE
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