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

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.

Objective To investigate the anti-inflammatory and analgesic activity and acute toxicity of Bulleyaconitine A and Foresaconitine and Yunaconitine from Aeonitum 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 LD50o 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） Bulleyaeonitine 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.