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背景:从天然药物中寻求安全有效的镇静安定类药物为逐年增加的神经精神类疾病的治疗提供了新的思路。前期研究发现草问荆总生物碱具有良好的镇静安定作用。目的:研究草问荆总生物碱对小鼠脑单胺氧化酶-B活性的影响以揭示草问荆总生物碱对中枢神经系统抑制作用的作用机制。设计:以实验动物为观察对象的随机对照实验。单位:哈尔滨商业大学药物研究所博士后科研工作站。材料:实验于2002-03/2003-01在黑龙江中医药大学药理研究室完成。药物选用草问荆总生物碱;烟肼酰胺;选用昆明种小白鼠100只,体质量(20±2)g,雌雄各半。方法:草问荆总生物碱对小鼠脑单胺氧化酶-B活性实验:小白鼠随机分为生理盐水对照组,不同剂量(15mg/kg,30mg/kg,45mg/kg,60mg/kg)的草问荆总生物碱组,每组10只。给药30min后,处死小鼠。采用紫外分光光度法测定单胺氧化酶-B的活性。草问荆总生物碱对烟肼酰胺抑制小鼠脑单胺氧化酶-B活性实验:小白鼠随机分为生理盐水对照组,烟肼酰胺组,烟肼酰胺加草问荆总生物碱不同剂量组(20mg/kg+15mg/kg,20mg/kg+30mg/kg,20mg/kg+45mg/kg,20mg/kg+60mg/kg)。每组10只。给药30min后,立即采用脊髓脱臼法处死小鼠。采用紫外分光光度法测定单胺氧化酶-B的活性。主要观察指标:小鼠脑单胺氧化酶-B活力,计算单胺氧化酶-B相对活力和单胺氧化酶-B活力提高(或抑制)百分率。结果:给药前后动物数均为每组10只,无异常或死亡现象。①草问荆总生物碱对小鼠脑单胺氧化酶-B活性的影响:草问荆总生物碱15mg/kg,30mg/kg,45mg/kg,60mg/kg组单胺氧化酶-B活力均高于生理盐水对照组(15.57±1.14),(16.78±1.10),(18.16±0.50),(22.72±1.26),(13.74±0.81)mkat/g。②草问荆总生物碱对烟肼酰胺抑制小鼠脑单胺氧化酶-B活力的影响:草问荆总生物碱可对抗烟肼酰胺抑制小鼠脑单胺氧化酶-B活性作用,当草问荆总生物碱45mg/kg时可完全对抗烟酰胺的抑制作用(酶活力抑制百分率为-4.62%),当草问荆总生物碱60mg/kg时则可将其抑制作用翻转为激活作用(酶活力抑制百分率为-77.92%)。结论:草问荆总生物碱可显著提高小鼠脑单胺氧化酶-B的活性,能够对抗单胺氧化酶抑制剂烟肼酰胺抑制单胺氧化酶-B的作用。大剂量草问荆总生物碱(60mg/kg)可将烟肼酰胺对单胺氧化酶-B的抑制作用翻转为激活作用。
Background: The search for safe and effective sedative and tranquilizing drugs from natural medicines has provided new ideas for the treatment of neuropsychiatric diseases that are increasing year by year. The previous study found that alkaloids from Caojingjing had good sedative and stability effects. OBJECTIVE: To study the effect of total alkaloids from Caojingjing on the activity of brain monoamine oxidase-B in mice to reveal the mechanism of the inhibitory effect of total alkaloids from Caojingjing on the central nervous system. Design: A randomized controlled trial using experimental animals as the subject of observation. Unit: Postdoctoral Research Station of Harbin Institute of Commerce. MATERIALS: The experiment was performed at the Department of Pharmacology, Heilongjiang University of Traditional Chinese Medicine from March 2002 to January 2003. The drug selected grass alkaloid alkaloids; smoke amide; selected Kunming species of mice 100, body weight (20 ± 2) g, male and female. METHODS: The activity of monoamine oxidase-B in brain of alkaloids from M. punctata was tested in mice: The mice were randomly divided into normal saline control group and different doses (15 mg/kg, 30 mg/kg, 45 mg/kg, 60 mg/kg). Total alkaloid group, 10 in each group. After 30 minutes of administration, the mice were sacrificed. UV spectrophotometry was used to determine the activity of monoamine oxidase-B. Effect of total alkaloids from alkaloids on the inhibition of monoamine oxidase-B activity in mice brain by alkaloids: The mice were randomly divided into normal saline control group, nicotinamide group, and nicotinamide plus grasshopper alkaloids different dose groups (20 mg /kg+15mg/kg, 20mg/kg+30mg/kg, 20mg/kg+45mg/kg, 20mg/kg+60mg/kg). 10 in each group. Immediately after 30 minutes of administration, the mice were sacrificed by spinal cord deodorization. UV spectrophotometry was used to determine the activity of monoamine oxidase-B. MAIN OUTCOME MEASURES: Monoamine oxidase-B activity in mouse brains, and the relative activity of monoamine oxidase-B and percentage of monoamine oxidase-B activity increase (or inhibition) were calculated. RESULTS: The number of animals before and after administration was 10 in each group. There was no abnormality or death. 1 Effect of alkaloids from alkaloids on the activity of monoamine oxidase-B in mice brain: The total alkaloids oxidase-B activity in the alkaloids of 15 mg/kg, 30 mg/kg, 45 mg/kg, and 60 mg/kg were higher than that of physiological saline. Group (15.57±1.14), (16.78±1.10), (18.16±0.50), (22.72±1.26), (13.74±0.81) mkat/g. 2 The effect of alkaloids from alkaloids on inhibiting the activity of monoamine oxidase-B in mice brain by alkaloids from alkaloids: Caojing alkaloids can inhibit the effect of nicotinamide on monoamine oxidase-B activity in mice brain, when grass alkaloid alkaloids At 45 mg/kg, it completely inhibited the nicotinamide inhibition (percentage inhibition of the enzyme activity was -4.62%). When the total alkaloid 60 mg/kg was challenged, the inhibitory effect was reversed to activate (the percentage inhibition of enzyme activity was -77.92%). CONCLUSION: The total alkaloids of E. quinquefasciatus can significantly increase the activity of monoamine oxidase-B in the brain of mice, and can inhibit the effect of monoamine oxidase inhibitor nicotinamide on the inhibition of monoamine oxidase-B. Large doses of quercus alkaloids (60 mg/kg) reversed the inhibitory effect of nicotinamide on monoamine oxidase-B activation.