Nabeshima T
Department of Neuropsychopharmacology & Hospital Pharmacy, Nagoya University School of Medicine, Japan.
Yakugaku Zasshi. 1995 Jul;115(7):499-512. doi: 10.1248/yakushi1947.115.7_499.
Nerve growth factor (NGF) plays an important role in the survival and maintenance of cholinergic neurons in the central nervous system. In senile dementia of the Alzheimer type (SDAT), learning and memory are impaired by the loss of neurons in the magnocellular cholinergic neuronal system. It is, therefore, of interest to investigate the role of NGF in this degenerative disorder. Since NGF does not cross the blood-brain barrier and is easily metabolized by peptidases when administered peripherally, it can be used for medical treatment only when directly injected into the brain. We tried to develop drugs which could be taken orally and stimulate the NGF synthesis in the brain. In addition, we attempted to develop a SDAT animal model using osmotic minipump to infuse beta-amyloid protein into cerebral ventricle, since there are no SDAT model animals accompanied with various pathophysiological changes. We demonstrate here that the oral administration of propentofylline, idebenone and trimethylquinone derivative, potent in vitro NGF synthesis stimulators, induced the increase in NGF protein and mRNA, and in choline acetyltransferase activity, in basal forebrain-lesioned and aged rats, but not in intact young rats. These drugs also ameliorated the behavioral deficits in habituation, water maze, and passive avoidance tasks in these animals. These results suggest that these drugs stimulated NGF synthesis in vivo and ameliorated the behavioral deficits which were accompanied with the reduced choline acetyltransferase activity in the basal forebrain-lesioned and aged rats. In terms of the SDAT animal model, the performance of the water maze and passive avoidance tasks was impaired and choline acetyltransferase activity significantly decreased in beta-amyloid protein-treated rats. Histochemical results showed the deposition of beta-amyloid protein in the cortex and hippocampus and atrophy and loss of hippocampal neurons. These results suggest that the deposition of beta-amyloid protein in the brain is related to the impairment of learning and cholinergic neuronal degeneration, and that beta-amyloid protein-treated rats could be an animal model for SDAT and used for the screening of drugs for SDAT.
神经生长因子(NGF)在中枢神经系统胆碱能神经元的存活和维持中起着重要作用。在阿尔茨海默型老年痴呆症(SDAT)中,大细胞胆碱能神经元系统中神经元的丧失会损害学习和记忆。因此,研究NGF在这种退行性疾病中的作用具有重要意义。由于NGF不能穿过血脑屏障,且在外周给药时容易被肽酶代谢,因此只有直接注入大脑才能用于医学治疗。我们试图开发可以口服并刺激大脑中NGF合成的药物。此外,由于没有伴有各种病理生理变化的SDAT模型动物,我们尝试使用渗透微型泵将β-淀粉样蛋白注入脑室来建立SDAT动物模型。我们在此证明,口服丙戊茶碱、艾地苯醌和三甲基醌衍生物(这些在体外是有效的NGF合成刺激剂),可诱导基底前脑损伤和老龄大鼠的NGF蛋白和mRNA增加,以及胆碱乙酰转移酶活性增加,但对完整的年轻大鼠无效。这些药物还改善了这些动物在习惯化、水迷宫和被动回避任务中的行为缺陷。这些结果表明,这些药物在体内刺激了NGF合成,并改善了与基底前脑损伤和老龄大鼠胆碱乙酰转移酶活性降低相关的行为缺陷。就SDAT动物模型而言,β-淀粉样蛋白处理的大鼠在水迷宫和被动回避任务中的表现受损,胆碱乙酰转移酶活性显著降低。组织化学结果显示β-淀粉样蛋白在皮质和海马中沉积,海马神经元萎缩和丢失。这些结果表明,大脑中β-淀粉样蛋白的沉积与学习障碍和胆碱能神经元变性有关,β-淀粉样蛋白处理的大鼠可以作为SDAT的动物模型,用于筛选治疗SDAT的药物。