滇西乌头中三种二萜生物碱相关药效和毒性的对比
Comparation of Three Kinds of Diterpenoid Alkaloid from Aconitum bulleyanum Diels in Related Pharmacodynamics and Toxicity
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摘要: 目的 对滇西乌头中分离的二萜生物碱草乌甲素、黑乌弱碱和滇乌碱抗炎镇痛活性和急性毒性进行比较研究.方法 灌胃给药后, 通过小鼠醋酸扭体和二甲苯耳肿胀实验, 考察3种生物碱的抗炎镇痛效果, 并比较3者的急性毒性.结果 (1) 草乌甲素、滇乌碱和黑乌弱碱的LD50分别为:4.06 mg/kg、2.81 mg/kg、12.00mg/kg; (2) 3种生物碱单次灌胃给药, 对醋酸致小鼠扭体性疼痛均有不同程度的抑制作用, 2.0 mg/kg的草乌甲素作用最强, 抑制率高于相同剂量的滇乌碱和黑乌弱碱, 与同剂量的黑乌弱碱组比较, 有统计学意义 (P<0.05) ; (3) 草乌甲素、滇乌碱对二甲苯致耳廓肿胀有明显抑制作用, 与溶媒组比较有统计学意义 (P<0.05) , 同等剂量的黑乌弱碱抗炎作用不明显;0.4 mg/kg滇乌碱抗炎作用最强, 与同剂量的草乌甲素和黑乌弱碱组比较有统计学意义 (P<0.01) .结论 (1) 急性毒性比较:滇乌碱>草乌甲素>黑乌弱碱; (2) 3种生物碱都有不同程度的镇痛作用, 草乌甲素镇痛作用最强; (3) 滇乌碱抗炎作用优于同浓度的草乌甲素和黑乌弱碱.Abstract: Objective To investigate the anti-inflammatory and analgesic activity and acute toxicity of Bulleyaconitine A and Foresaconitine and Yunaconitine from Aconitum bulleyanum Diels.Methods After intragastric administration, the anti-inflammatory and analgesic activities of Bulleyaconitine A and Foresaconitine and Yunaconitine using Acetic acid writhing test and Dimethylbenzene auricle swelling test in mice were compared.The acute toxicities of three iterpenoidalkaloids were also compared according to LD50.Results (1) The LD50 values of Bulleyaconitine A and Foresaconitine and Yunaconitine were:4.06 mg/kg, 2.81 mg/kg and 12 mg/kg; (2) Single intragastric administration of three kinds of alkaloids all had obvious inhibitory effect on acetic acid-induced writhing pain.The 2 mg/kg group of Bulleyaconitine A had the strongest effect, the inhibition rate was higher than the same dose of Foresaconitine and Yunaconitine, there was significant difference compared with Foresaconitine group (P<0.05) ; (3) Bulleyaconitine A and Yunaconitine had obvious inhibiting effect on auricle swelling induced by dimethylbenzene, there were significant differences compared with the vehicle group (P <0.05) , Foresaconitine with the same dose had no obvious effect; 0.4 mg/kg Yunaconitine had the strongest anti-inflammatory effects, there were significant differences compared with the same dose of Bulleyaconitine A and Foresaconitine groups ( P <0.01) .Conclusion ( 1) Comparison of acute toxicity: Yunaconitine >Bulleyaconitine A >Foresaconitine; (2) Three alkaloids all have analgesic effects in different degree, Bulleyaconitine A is the strongest; (3) Yunaconitine is better than Bulleyaconitine A and Foresaconitine in anti-inflammatory effect with same concentration.
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Key words:
- Aconitum bulleyanum Diels /
- Diterpenoidalkaloid /
- Anti-inflammatory /
- Analgesic /
- Acute toxicity
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[1]马晓强, 蒋山好, 朱大元.滇西乌头中的二萜生物碱[J].中国中药杂志, 1998, 23 (11) :679-680. [2]袁梅, 马晓霞, 杨树德, 等.滇西乌头化学成分研究[J].中药材, 2013, 36 (6) :938-940. [3]蔡超群, 杨春华, 梁敬钰, 等.乌头属二萜生物碱成分构效关系研究进展[J].海峡药学, 2013, 25 (3) :1-5. [4]张为亮, 徐楚江, 杨明, 等.附子毒效关系的实验研究[J].广西中医药, 1997, 6 (20) :43-51. [5]俞昌喜, 黄凌燕, 唐希灿.滇乌碱及其类似物镇痛效应的构效关系[J].福建医学院学报, 1996, 30 (1) :10-12. [6]郑平, 杨煜荣, 张炜平, 等.3, 15-二乙酰苯甲酰乌头原碱的镇痛作用, 毒性及与其类似物的比较[J].中国药理学报, 1994, 15 (3) :239-243. [7]张慧灵, 杨煌荣, 王勇, 等.3, 15-二乙酰苯甲酰鲺头原碱镇痛的作用部位[J].中国药理学报, 1994, 15 (2) :176-180. [8] [8]AMERI A.Effects of the aconitum alkaloid mesaconitine in rat hippocampal slices and the involvement of adrenoceptor[J].British Journal of Pharmacology, 1998, 123 (2) :243-250. [9] 董月丽, 陈维洲, 丁光生.乌头碱及其同系物诱发心律失常作用的比较[J].中国药理学报, 1981, 2 (3) :173-176. [10] [10]KISS T, ORVOS P, BANSAGHI S, et al.Identification of diterpene alkaloids from Aconitum napellus subsp.Firmum and GIRK channel activities of some Aconitum alkaloids[J].Fitoterapia, 2013, 90 (20) :85-93. [11]林志共, 蔡文, 唐希灿.滇乌碱的抗炎和镇痛作用[J].中国药理学与毒理学志, 1987, 1 (2) :93-99. [12]高黎明, 毛学峰, 魏小梅, 等.二萜类生物碱的药理作用及构效关系研究概况[J].西北师范大学学报 (自然科学版) , 1999, 15 (19) :102-107. [13]杨姝, 金振辉, 羊晓东, 等.乌头属植物的化学成分及药理作用研究进展[J].云南农业大学学报, 2007, 22 (2) :293-298. [14]安婧娴, 刘芳, 刘芳, 等.近年来乌头属植物二萜生物碱化学成分及其镇痛活性研究进展[J].中南药学, 2016, 14 (5) :521-525. -
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