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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 the toxic and pharmacological components before and after the processing of A. chinensis, to explore the relationship between toxicity and efficacy, and to provide a scientific basis for the rational processing of attenuated high-level aconite. Methods: Acute toxicity test in mice was used to compare the toxicities of different solvent extraction parts. Screening of the toxic parts of Aconitum kusnezoffii and Aconitum kusnezoffii was carried out. The hot plate method, writhing method, Analgesic and anti-inflammatory effects of aconitum toxicity on mice; screening of the efficacy site to explore whether the toxic site is a medicinal site. Results: The results showed that the toxicity of chloroform and chloroform was the highest among the raw materials, and the secondary components of chloroform and chloroform were the second, with the LD50 of 0.09, 1.81 and 24.41 g / kg respectively, and the LD50 of products were 0.11 and 2.42 , 0.87 g / kg respectively; while the partial toxicity of petroleum ether, ethyl acetate and ethanol was the smallest. The maximum dosage of crude product was 2.69,3.11,28.38 g / kg, the maximum dosage of product was 13.12,1.98,20.32 g / kg. At 120 min after administration, the trichloromethane fractions of 1.5 and 4.5 mg / kg and the trichloromethane fraction of 4.5 mg / kg all increased the threshold of thermotolerance in mice with dose-effect and analgesic effects At 1.6 mg / kg lappaconitine hydrobromide group. The chloroform and chloroform fractions of mice injected with glacial acetic acid for 15-30 min, 1.5 and 4.5 mg / kg, respectively, were able to effectively inhibit the number of writhing induced by glacial acetic acid in mice with a dose-effect relationship and the inhibition rate was slightly lower than 1.6 mg / kg lappaconitine hydrobromide group. In xylene-induced mouse ear swelling experiments, 1.5, 4.5 mg / kg of raw and high aconite trichloromethane can effectively relieve ear swelling in mice, and the dose-response relationship, the inhibition rate of swelling slightly less than 10.0 mg / kg indomethacin group. Conclusion: The part of trichloromethane is not only a toxic part of hypericum nigrum, but also the main analgesic and anti-inflammatory part. And it has a dose-response relationship. It is presumed that analgesic and anti-inflammatory activity is related to toxicity.