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作 者:王开富[1] 徐丽君[1] 邹欣[1] 陆付耳[1]
机构地区:[1]华中科技大学同济医学院附属同济医院中西医结合研究所,武汉430030
出 处:《医药导报》2011年第6期699-701,共3页Herald of Medicine
基 金:国家新药创制重大专项基金资助课题(基金编号:2009zx09301-014)
摘 要:目的 观察盐酸小檗碱与结构改造后的化合物8-羟基二氢小檗碱对大鼠脑组织、血清中乙酰胆碱酯酶(AChE)活性的抑制作用.方法 大鼠腹主动脉取血后断头处死,取脑制备组织匀浆,采用双缩脲法测定脑组织匀浆中总蛋白含量,用酶法检测脑组织和血清中AChE活性.结果 盐酸小檗碱与8-羟基二氢小檗碱对大鼠脑组织中AChE活性的抑制率分别为52.57%~82.22%和32.78%~96.14%,对大鼠血清中AChE活性的抑制率分别为8.44%~99.59%和11.72%~99.59%,抑制程度与小檗碱浓度具有明显的量效关系.结论 盐酸小檗碱和8-羟基二氢小檗碱均能显著抑制脑组织和血清中AChE活性,可能是其治疗糖尿病新的作用靶点或作用途径.Objective To investigate the inhibitory effects of monomer berberine hydrochloride and its structuremodified compound 8-hydroxy dihydroberberine on the activity of acetylcholinesterase (ACHE) in the cerebral tissue and serum of rats. Methods The rats were sacrificed by cervical dislocation after the blood was collected from abdominal aorta. The cerebral tissue was homogenized and the total protein level in it was measured using biuret. The AChE activity in cerebral tissue and serum was detected by enzymatic method. Results The inhibitory rate of AChE activity in cerebral tissue by berberine hydmchloride was 52.57% -82.22% whereas 32.78% -96. 14% by 8-hydroxy dihydroberberine. The inhibitory rate of serum AChE activity by berberine hydrochloride was 8.44% -99.59% and 11.72% -99.59% by 8-hydroxy dihydroberberine. The inhibitory extent was in a dose-effect relationship with berberine . Conclusion Both berberine hydrochloride and 8-hydroxy dihydroberberine could inhibit AChE activity in cerebral tissue and serum obviously ,which may be a new target for the treatment of diabetes.
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