文献类型：期刊文献

中文题名：高乌头炮制前后毒性部位与镇痛抗炎药效部位筛选研究

英文题名：Screening of toxic,analgesic and anti-inflammatory compounds from crude and processed Aconitum sinomontanum Nakai

作者：张立军[1];戴海蓉[1];杨志军[2];夏鹏飞[2];马骏[2];李芸[1]

第一作者：张立军

机构：[1]甘肃中医药大学;[2]甘肃中医药大学甘肃省中药药理与毒理学重点实验室

第一机构：甘肃中医药大学

年份：2017

卷号：33

期号：4

起止页码：78

中文期刊名：中药药理与临床

外文期刊名：Pharmacology and Clinics of Chinese Materia Medica

收录：北大核心:【北大核心2014】；CSCD:【CSCD2017_2018】；

基金：国家自然科学基金项目(81560650);甘肃省自然科学基金项目(1107RJZA242)

语种：中文

中文关键词：高乌头;高乌头制品;三氯甲烷部分;急性毒性;镇痛;抗炎

外文关键词：Aconitum sinomontanum Nakai（高乌头）; chloroform extract; acute toxicity; analgesic activity; anti-inflammatory activity

摘要：目的:筛选高乌头炮制前后毒性及药效部位,探讨毒性与药效的关系,为高乌头减毒存效合理炮制提供科学依据。方法:采用小鼠急性毒性实验比较不同溶剂萃取部分的毒性,筛选生、制高乌头的毒性部位,以热板法、扭体法及二甲苯致鼠耳肿胀实验考察不同剂量生、制高乌头毒性部分对小鼠的镇痛抗炎作用;筛选药效部位,探究毒性部位是否为药效部位。结果:生、制高乌头均为三氯甲烷部分的毒性最强,水提及正丁醇部分次之,生品LD50分别为0.09、1.81、24.41 g/kg,制品LD50分别为0.11、2.42、0.87 g/kg;而石油醚、乙酸乙酯及乙醇部分毒性均最小,生品最大给药量分别为2.69、3.11、28.38 g/kg,制品最大给药量分别为13.12、1.98、20.32 g/kg。给药后120 min、1.5、4.5 mg/kg的生品三氯甲烷部分与4.5 mg/kg的制品三氯甲烷部分均能提高小鼠热板痛阈值,且呈量效关系,镇痛作用优于1.6 mg/kg氢溴酸高乌甲素组。注射冰醋酸15~30 min,1.5、4.5 mg/kg的生、制品三氯甲烷部分均能有效抑制冰醋酸所致小鼠的扭体次数,且呈量效关系,抑制率略低于1.6 mg/kg氢溴酸高乌甲素组。在二甲苯致鼠耳肿胀实验中,1.5、4.5 mg/kg的生、制高乌头三氯甲烷部分均能有效缓解小鼠耳肿胀度,且呈量效关系,肿胀抑制率略低于10.0 mg/kg消炎痛组。结论:三氯甲烷部分既是生、制高乌头的毒性部位,又是其镇痛抗炎的主要药效部位,且呈量效关系,推测其镇痛抗炎活性与毒性存在一定的关联。
Objective： To screen toxic,analgesic and anti-inflammatory compounds from crude and processed Aconitum Sinomontanum Nakai,and to study the relationship between the toxicity and efficacy,and to provide the scientific basis for reasonable processing to ＂ toxicity reducing and efficacy existing＂ on Aconitum sinomontanum Nakai. Methods： An acute toxicity test was used to compare the toxicity of different extracts to screen the ＂ toxic＂ group,then the hot-plate test,acid-induced writhing test,and dimethylbenzene-induced auricular swelling test were used to assess respectively the analgesic and anti-inflammatory effect of the ＂ toxic＂ group to screen ＂ effect＂ group,further to study whether toxic and effective compounds are the same. Results： The chloroform extracts of crude and processed Aconitum Sinomontanum Nakai had maximum toxicity,followed by water and butanol extracts,LD50 of different extracts of crude product were 0. 09,1. 81 and 24. 41 g/kg,LD50 of different extracts of processed product were 0. 11,2. 42,0. 87 g/kg,respectively. The extracts of petroleum ether,ethyl acetate and alcohol had minimal toxicity,the maximum dose of different extracts of crude product were 2. 69,3. 11 and 28. 38 g/kg,the maximum dose of different extracts of processed product were 13. 12,1. 98,20. 32 g/kg,respectively. The pain threshold in mice were increased by 1. 5and 4. 5 mg/kg dose of chloroform extract of crude product,4. 5 mg/kg dose of chloroform extract of processed product Aconitum Sinomontanum Nakai at 120 minutes after the last administration,and their analgesic activities were better than that of 1. 6 mg/kg dose of Lappaconitine hydrobromide. Writhing times were reduce by 1. 5 and 4. 5 mg/kg dose of chloroform extract of crude and processed Aconitum Sinomontanum Nakai at 15 ~ 30 minutes after administration,and their inhibition rates were slightly lower than 1. 6 mg/kg dose of Lappaconitine hydrobromide. In the auricular swelling induced by dimethylbenzene test,the swelling degree was relieved by 1. 5 and 4. 5 mg/kg dose of chloroform extract of crude and processed Aconitum Sinomontanum Nakai,and their swelling inhibition rates were slightly lower than 1. 6 mg/kg dose of indomethacin. Conclusion： The chloroform extract of Aconitum sinomontanum Nakai was both a toxic and an active group,it showed that there was a dose-effect relationship between them,there was probably some correlation between the analgesic,anti-inflammatory and toxicity.