Anti-acetylcholinesterase Active Ingredients from Aconitum tanguticum by UPLC-Q-TOF-MS/MS / 中国实验方剂学杂志

Objective:To identify the anti-acetylcholinesterase active ingredients in <italic>Aconitum tanguticum</italic>， so as to lay the foundation for finding new anti-Alzheimer's disease （AD） drugs. Method:The anti-acetylcholinesterase active fractions of <italic>A. tanguticum</italic> were screened by the modified Ellman's method， and the chemical composition of the active fraction was analyzed by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry （UPLC-Q-TOF-MS/MS）. The chromatographic separation was performed on an ACQUITY UPLC BEH C₁₈ column （2.1 mm×50 mm， 1.7 μm） with acetonitrile （A）-0.4% ammonia aqueous solution （B） as mobile phase for gradient elution， and the column temperature was set at 30 ℃ with the flow rate of 0.4 mL·min^-1. Phase A of the dichloromethane fraction changed with time as follows：0-3 min， 5%A； 3-7 min， 5%-20%A； 7-11.5 min， 20%-33%A； 11.5-15.5 min， 33%-50%A； 15.5-20.5 min， 50%-80%A； 20.5-23 min， 80%-85%A； 23-25 min， 85%-95%A. Phase A of the <italic>n</italic>-butanol fraction changed with time as follows：0-2 min， 5%A； 2-8 min， 5%-20%A； 8-11 min， 20%-33%A； 11-15 min， 33%-95%A. Mass spectrometry was performed on electrospray ionization， data were collected in positive ion mode， and the detection range was <italic>m</italic>/<italic>z</italic> 100-1 500. Result:Both the dichloromethane and <italic>n</italic>-butanol fractions had a certain inhibitory effect on acetylcholinesterase， their half inhibitory concentration （IC₅₀） values were （64±4.4） mg·L^-1 and （85.7±3.8） mg·L^-1， respectively. By UPLC-Q-TOF-MS/MS analysis， a total of 21 alkaloids were identified from the dichloromethane fraction， and 11 alkaloids were identified from <italic>n</italic>-butanol fraction. Guan-fu base Ⅰ， found in both fractions， was first discovered in <italic>A. tanguticum</italic>. Conclusion:Diterpene alkaloids are the main anti-acetylcholinesterase substances of <italic>A. tanguticum</italic>， which is worth further exploration.

Cardiotoxicity in Zebrafish Embryos of Euphorbiae Pekinensis Radix Before and After Processing with Vinegar / 中国实验方剂学杂志

Objective:Taking zebrafish embryos as research model, to investigate the toxic effect of different polar fractions of Euphorbiae Pekinensis Radix before and after processing with vinegar on heart. Method:Zebrafish embryos with normal development at 12 h after fertilization were treated with petroleum ether, dichloromethane and ethyl acetate extracts of Euphorbiae Pekinensis Radix before and after processing with vinegar for observation of cardiac development and function at 72 h. Result:Various polar fractions of Euphorbiae Pekinensis Radix before and after processing with vinegar had the cardiotoxicity on zebrafish embryos in a dose-dependent manner. In addition, the cardiotoxicity of different polar fractions was followed by petroleum ether, dichloromethane and ethyl acetate. The cardiotoxicity was mainly manifested as slow cardiac development, pericardial edema, decrease of heart rate and apoptosis of cardiac cells. Compared with the corresponding polar fraction of raw products, the cardiotoxicity of the same polar fraction of vinegar-processed products with similar doses decreased. Conclusion:Euphorbiae Pekinensis Radix has cardiotoxicity to zebrafish embryos and the cardiotoxicity is reduced after processing with vinegar, which can provide some experimental basis for further elucidation of the detoxication mechanism of Euphorbiae Pekinensis Radix processed with vinegar.