Structural characterization,in vivo toxicity and biological activity of two new pyro-type diterpenoid alkaloids derived from 3-acetylaconitine

作     者：Yu-jie Wang Yan Wang Pei Tao Yu-jie Wang;Yan Wang;Pei Tao

作者机构：School of Ethnic MedicineChengdu University of Traditional Chinese MedicineChengdu 611137Sichuan ProvinceChina School of PharmacyChengdu University of Traditional Chinese MedicineChengdu 611137Sichuan ProvinceChina 

出 版 物：《Journal of Integrative Medicine》 (结合医学学报（英文版）)

年 卷 期：2023年第21卷第3期

页      面：302-314页

核心收录：

学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(No.81403104) the Sichuan Science and Technology Program(No.2020YJ0131) Xinglin Scholar Research Promotion Project of Chengdu University of Traditional Chinese Medicine,China(No.QNXZ2018042,No.QJRC2022046) 

主　　题：3-Acetylaconitine Acute toxicity Antiarrhythmic agents 16-Epi-pyroacetylaconitine Pyroacetylaconitine Processing 

摘      要：Objective:The transformations that occur in diterpenoid alkaloids during the process of sand frying for Chinese herbal medicine preparation have yet to be *** study investigated the structural changes that take place in 3-acetylaconitine during a simulation of heat-processing and evaluated the toxicity and biological activity of the pyrolysis ***:The diterpenoid alkaloid 3-acetylaconitine was heated at 180°C for 15 min to simulate the process of sand *** pyrolysis products were separated using column chromatography,and their structures were investigated using high-resolution electrospray ionization mass spectroscopy and nuclear magnetic resonance ***,in vivo cardiotoxicity and acute toxicity of 3-acetylaconitine and its pyrolysis products were compared,and the aconitine-induced arrhythmia model was employed to evaluate the antiarrhythmic effect of the pyrolysis ***:Two new diterpenoid alkaloids,pyroacetylaconitine and 16-epi-pyroacetylaconitine,a pair of epimers at C-16,were *** comparing the structures of these compounds,possible transformation pathways were *** with the prototype compound,3-acetylaconitine,the cardiotoxicity and acute toxicity of the heat-transformed products were significantly *** the biological activity assay,the two pyrolysis products exhibited an effective increase in ventricular premature beat latency,a reduction in the occurrence of ventricular tachycardia,as well as an increase in the rate of arrhythmia inhibition,implying strong antiarrhythmic ***:Compared with 3-acetylaconitine,its pyrolysis products displayed lower toxicity and good antiarrhythmic effects;thus,they have potential for being developed into antiarrhythmic medicines.