去氢骆驼蓬碱及其衍生物DH-004的急性毒性研究

Study of acute toxicity of harmine and derivative DH-004

目的研究去氢骆驼蓬碱及其衍生物DH-004的急性毒性。方法采用Bliss法测定小鼠经腹腔注射去氢骆驼蓬碱和去氢骆驼蓬碱衍生物DH-004的LD50,记录各组小鼠的中毒症状。结果去氢骆驼蓬碱经腹腔注射的LD50及95%可信限为49.40 mg/kg体质量(41.44~57.62 mg/kg体质量);去氢骆驼蓬碱衍生物DH-004经腹腔注射的LD50及95%可信限为252.66 mg/kg体质量(220.60~289.72 mg/kg体质量)。小鼠中毒症状主要表现为震颤、躁动不安、抽搐等情况。结论小鼠经腹腔注射给药去氢骆驼蓬碱衍生物DH-004毒性小于去氢骆驼蓬碱毒性,去氢骆驼蓬碱经结构修饰能达到减毒作用。

Objective To study the acute toxicity of harmine and derivative DH-004.Methods The LD50 of Harmine and derivative DH-004 intraperitoneally injected in mice were determined by Bliss method.The poisoning symptoms of toxicity reaction were observed at the same time.Results The LD50 and its 95%confidence interval of Harmine in mice were 49.40 mg/kg(41.44~57.62 mg/kg).And the LD50 and its 95%confidence interval of harmine derivatives DH-004 in mice were 252.66 mg/kg(220.60~289.72 mg/kg).The poisoning symptoms were tremor,restlessness and convulsion.Conclusion After intraperitoneally injected into mice,the toxicity of Harmine was more serious than harmine derivatives DH-004.Therefore,Toxicity of harmine can be attenuated by structural modification.