文献类型：期刊文献

中文题名：高乌头“毒性”部位及镇痛抗炎“药效”部位的筛选

英文题名：Screening of high “toxicity”parts and effectively analgesic and anti-inflammatory parts from 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,甘肃兰州730000;[2]甘肃中医药大学甘肃省中药药理与毒理学重点实验室,甘肃兰州730000

第一机构：甘肃中医药大学

年份：2017

卷号：37

期号：24

起止页码：2424

中文期刊名：中国医院药学杂志

外文期刊名：Chinese Journal of Hospital Pharmacy

收录：CSTPCD;;北大核心:【北大核心2014】；

基金：国家自然科学基金项目(编号:81560650)

语种：中文

中文关键词：高乌头;三氯甲烷部分;急性毒性;镇痛;抗炎

外文关键词：Aconitum Sinomontanum Nakai; chloroform extract; acute toxicity; analgesic activity; anti-inflammatory activity

摘要：目的:筛选高乌头的毒性及药效部位,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高乌头"毒性"部分对小鼠的镇痛抗炎作用。结果:高乌头不同溶剂萃取部分急性毒性强度差别较大,三氯甲烷部分的毒性最强,水提及正丁醇部分次之,LD_(50)分别为89.65,1 805.40,24 409.41 mg·kg^(-1);石油醚、乙酸乙酯及乙醇部分毒性最小,最大给药量分别为2 686.01,3 108.13,28 376.21 mg·kg^(-1)。给药后120 min,1.5,4.5 mg·kg^(-1)的高乌头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^(-1)氢溴酸高乌甲素组。注射乙酸15 min后,1.5,4.5mg·kg^(-1)的高乌头三氯甲烷部分均能有效抑制乙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^(-1)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^(-1)的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1.6 mg·kg^(-1)消炎痛组。结论:高乌头三氯甲烷部分既是其毒性部位,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 toxicity and effect parts from Aconitum Sinomontanum Nakai,study the relationship between the toxicity and efficacy,and provide a scientific basis for reasonable processing to＂toxicity reducing and efficacy existing＂for Aconitum sinomontanum Nakai.METHODS An acute toxicity test was used to compare the toxicity of different extracts to screen the＂toxic＂groups,then hot-plate test,acid-induced writhing test and dimethylbenzene-induced auricular swelling test were used to assess the analgesic and anti-inflammatory effects of the＂toxic＂groups to screen＂effect＂groups,and to study whether the toxicity and effect parts were the same.RESULTS There were significantly differences in the toxicity of different extracts of Aconitum Sinomontanum Nakai.The extract of chloroform had maximum toxicity,followed by water and butanol extracts,and the LD50were 89.65,1 805.40 and 24 409.41 mg·kg^-1,respectively.The extracts of petroleum ether,ethyl acetate and alcohol had minimal toxicity at the maximum doses of 2 686.01,3 108.13 and 28 376.21 mg·kg^-1,respectively.The pain threshold was increased in1.5 and 4.5 mg·kg^-1dose groups of chloroform extract of Aconitum Sinomontanum Nakai120 min after the last administration,analgesic activity was higher than in 1.6 mg·kg^-1 dose group of lappaconitine hydrobromide.Writhing times were reduced in1.5 and4.5 mg·kg^-1dose groups of chloroform extract of Aconitum Sinomontanum Naka15 min after administration,inhibition rate was slightly lower than that in1.6 mg·kg^-1dose group of Lappaconitine hydrobromide.In the auricular swelling induced by dimethylbenzene test,the swelling degrees were relieved in1.5 and4.5 mg·kg^-1dose groups of chloroform extract of Aconitum Sinomontanum Naka,swelling inhibition rate was slightly lower than that in1.6 mg·kg^-1dose group of indomethacin.CONCLUSION The chloroform extract of Aconitum sinomontanum Nakai is both a toxic and an active group,with a dose-effect relationship.Its analgesic,anti-inflammatory and toxic effects are probably correlated.