Hydrastine

Abstract: Goldenseal (Hydrastis canadensis L.) is used to combat inflammation and infection. Its antibacterial activity in vitRO has been attributed to its alkaloids, the most abundant of which is berberine. The goal of these studies was to compare the composition, antibacterial activity, and efflux pump inhibitory activity of ethanolic extracts prepared from roots and aerial portions of H. canadensis. Ethanolic extracts were prepared separately from roots and aerial portions of six H. canadensis plants. Extracts were analyzed for alkaloid concentration using LC-MS and tested for antimicrobial activity against Staphylococcus aureus (NCTC 8325-4) and for inhibition of ethidium bromide efflux. Synergistic antibacterial activity was observed between the aerial extract (FIC 0.375) and to a lesser extent the root extract (FIC 0.750) and berberine. The aerial extract inhibited ethidium bromide efflux from wild-type S. aureus but had no effect on the expulsion of this compound from an isogenic derivative deleted for norA. Our studies indicate that the roots of H. canadensis contain higher levels of alkaloids than the aerial portions, but the aerial portions synergize with berberine more significantly than the roots. Furthermore, extracts from the aerial portions of H. canadensis contain efflux pump inhibitors, while efflux pump inhibitory activity was not observed for the root extract. The three most abundant H. canadensis alkaloids, berberine, hydrastine, and canadine, are not responsible for the efflux pump inhibitory activity of the extracts from H. canadensis aerial portions.

Abstract: The characterization of herbal materials is a significant challenge to analytical chemists Goldenseal (Hydrastis canadensis L), which has been chosen for toxicity evaluation by NIEHS, is among the top 15 herbal supplements currently on the market and contains a complex mixture of indigenous components ranging from carbohydrates and amino acids to isoquinoline alkaloids One key component of herbal supplement production is botanical authentication, which is also recommended prior to initiation of efficacy or toxicological studies To evaluate material available to consumers, goldenseal root powder was obtained from three commercial suppliers and a strategy was developed for characterization and comparison that included Soxhlet extraction, HPLC, GC-MS, and LC-MS analyses HPLC was used to determine the weight percentages of the goldenseal alkaloids berberine, hydrastine, and canadine in the various extract residues Palmatine, an isoquinoline alkaloid native to Coptis spp and other common goldenseal adulterants, was also quantitated using HPLC GC-MS was used to identify non-alkaloid constituents in goldenseal root powder, whereas LC-MS was used to identify alkaloid components After review of the characterization data, it was determined that alkaloid content was the best biomarker for goldenseal A 20-min ambient extraction method for the determination of alkaloid content was also developed and used to analyze the commercial material All three lots of purchased material contained goldenseal alkaloids hydrastinine, berberastine, tetrahydroberberastine, canadaline, berberine, hydrastine, and canadine Material from a single supplier also contained palmatine, coptisine, and jatrorrhizine, thus indicating that the material was not pure goldenseal Comparative data for three commercial sources of goldenseal root powder are presented

Abstract: The action of strychnine, hydrastine, and apamine on neuromuscular transmission in the stomach and taenia coli was investigated. Hydrastine and strychnine increase nonadrenergic IPSPs of smooth muscle cells. Under the influence of apamine the IPSP and hyperpolarization evoked by exogenous ATP are reversibly blocked and noncholinergic EPSPs appear; ATP, however, does not cause depolarization of the cell membrane. Consequently, apamine is a specific blocker of nonadrenergic inhibition, acting on the postsynaptic membrane, and ATP is a mediator both of this inhibition and of noncholinergic synaptic excitation discovered in smooth muscle cells.