Novel cognitive improving and neuroprotective activities of Polygala tenuifolia Willdenow extract, BT-11

Novel cognitive improving and neuroprotective activities of Polygala tenuifolia Willdenow extract, BT-11
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DOI:
10.1002/jnr.10429
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发表时间:
2002-11-01
影响因子:
4.2
通讯作者:
Suh, YH
Suh, YH
中科院分区:
医学3区
文献类型:
--
作者:
Park, CH;Choi, SH;Suh, YH

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本研究旨在从天然来源中寻找一种新的具有认知增强活性且副作用小的活性成分。结果表明,远志(Polygala tenuifolia Willdenow)干根提取物(BT-11,10 mg/kg,i. p.)采用被动回避法和水迷宫法,观察了东莨菪碱对大鼠认知功能的影响。我们还研究了BT-11对谷氨酸(Glu)和淀粉样前体蛋白(APP)的毒性代谢产物如淀粉样β蛋白(Abeta)和APP的C端片段(CT)诱导的原代培养大鼠神经元毒性的影响。BT-11(0.5、3和5 μ g/ml)的预处理以剂量依赖性方式显著减少由Glu(1 mM)、Abeta(10 μ M)和CT 105(10 μ M)诱导的细胞死亡。此外,BT-11以剂量依赖性和非竞争性方式抑制乙酰胆碱酯酶(AChE)活性(IC 50值; 263.7 μ g/ml)。我们的新发现表明,这种提取物可能对阿尔茨海默病(AD)或其他与兴奋性毒性和中枢胆碱能功能障碍相关的神经退行性疾病中的神经元死亡和认知障碍具有一定的保护作用。(C)2002 Wiley-Liss,Inc.
We carried out this study to search a new active constituent that had cognitive enhancing activity and low side effects from natural source. We found that the extract of dried root of Polygala tenuifolia Willdenow (BT-11, 10 mg/kg, i.p.) could significantly reverse scopolamine-induced cognitive impairments in rat, using a passive avoidance and a water maze test. We also investigated the effects of BT-11 on neurotoxicity induced by glutamate (Glu) and toxic metabolites of amyloid precursor protein (APP) such as amyloid beta protein (Abeta) and C-terminal fragment of APP (CT) in primary cultured neurons of rat. The pretreatment of BT-11 (0.5, 3, and 5 mug/ml) significantly reduced cell death induced by Glu (1 mM), Abeta (10 muM) and CT105 (10 muM) in a dose-dependent manner. In addition, BT-11 inhibited acetylcholinesterase (AChE) activity in a dose-dependent and noncompetitive manner (IC50 value; 263.7 mug/ml). Our novel findings suggest the possibility that this extract may have some protective effects against neuronal death and cognitive impairments in Alzheimer's disease (AD), or other neurodegenerative diseases related to excitotoxicity and central cholinergic dysfunction. (C) 2002 Wiley-Liss, Inc.