目的:从毒效角度出发,比较附子、乌头、草乌不同炮制品及提取物的毒性,为研究和应用这些生药提供相关实验依据。方法:以小鼠为主要研究对象,观察急性死亡率,心电影响阈剂量来观察毒性,以镇痛及其抗室颤来观察其药效。结果:从急性毒性看,白附片和黑顺片毒性较小,其最大给药剂量均为20.52 g.kg-1。盐附子毒性较大,LD50为11.301 g.kg-1。结合相关活性综合考察,临床安全指数由大到小依次为:黑顺片>白附片>盐附子。草乌毒性较大(LD50 292.38 mg.kg-1),经炮制后毒性明显减小,约降低70.32倍。结论:附子、乌头炮制后起到了减毒存效的作用,而草乌炮制后则表现为毒效同时降低。

The study is aimed to compare toxicity of aconite roots in different preparations from the point of both toxic and pharmacological action.Related experiment basis was presented in the study and research of Chinese medicinal.Toxicity,morbidity and minimum cardiac toxic dose were assessed.Effects on acetic acid-induced abdominal constriction and trichloromethane-induced ventricular fibrillation of mice were observed.The results showed that from the morbidity of acute toxicity,the toxicity of refined aconite roots is reduced with the maximum tolerance dosage of 20.52 g/kg,except the aconite root prepared by salt(LD50 11.301 g/kg).Base on the clinic index(toxic dose/effective dose),the safety index of the root by different preparation were,from big to small,by boiling plus steaming was more than only by boiling preparation,which is more than only salt preparation without boiling and steaming,respectively.The toxicity of Aconitum kusnezoffii Reichb.(Cao Wu) was more than LD50 292.38 mg/kg.But,its toxicity was apparently reduced to 70.32 times through preparation.It is concluded that by the process of refining aconites,the result of toxicity-reducing and action-maintaining was for refined Aconitum carmichaeli Debx.Actions were attenuated in both toxicity and pharmacology in refined Aconitum kusnezoffii Reichb.

科学技术部“十一五”国家科技支撑计划(2006BAI14B01-001):药品安全关键技术研究——常见与重要药品安全标准研究,主项目负责人:马双成,子项目负责人:肖新月,科学技术部国家“重大新药创制”科技重大专项(2009ZX09308-003):中药生产技术及过程控制技术标准平台,负责人:王智民,科学技术部国家“重大新药创制”科技重大专项(2009ZX09502-002):与药效相关的中药质量评价关键技术研究,负责人:王峥涛,科学技术部国家“重大新药创制”科技重大专项(2009ZX09502-001):中药研究关键技术,负责人:梁爱华