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progressinstudiesofhuperzineaanaturalcholinesteraseinhibitorfromchineseherbalmedicine

文献类型:期刊论文

作者Rui Wang; Han Yan; Xican Tang
刊名actapharmacologicasinica
出版日期2006
卷号27期号:1页码:1
关键词RAT PHEOCHROMOCYTOMA CELLS NERVE GROWTH-FACTOR AMYLOID PRECURSOR PROTEIN SPATIAL WORKING-MEMORY LONG-TERM POTENTIATION EXPERIMENTAL COGNITIVE IMPAIRMENT DISSOCIATED HIPPOCAMPAL-NEURONS ALZHEIMERS-DISEASE THERAPY OXYGEN-GLUCOSE DEPRIVATION CENTRAL CHOLINERGIC SYSTEM huperzine A Alzheimer disease acetylcholinesterase cholinesterase inhibitors cognitive enhancer neuroprotect agents oxidative stress apoptosis
ISSN号1671-4083
DOI10.1111/j.1745-7254.2006.00255.x
英文摘要Huperzine A (HupA), a novel alkaloid isolated from the Chinese herb Huperzia serrata, is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE). Compared with tacrine, donepezil, and rivastigmine, HupA has better penetration through the blood-brain barrier, higher oral bioavailability, and longer duration of AChE inhibitory action. HupA has been found to improve cognitive deficits in a broad range of animal models. HupA possesses the ability to protect cells against hydrogen peroxide, P-amyloid protein (or peptide), glutamate, ischemia and staurosporine-induced cytotoxicity and apoptosis. These protective effects are related to its ability to attenuate oxidative stress regulate the, expression of apoptotic proteins Bcl-2, Bax, P53, and caspase-3, protect mitochondria, upregulate nerve growth factor and its receptors, and interfere with amyloid precursor protein metabolism. Antagonizing effects of HupA on N-methyl-D-aspartate receptors and potassium currents may also contribute to its neuroprotection as well. Pharmacokinetic studies in rodents, canines, and healthy human volunteers indicated that HupA was. absorbed rapidly, distributed widely in the body, and eliminated at a moderate rate with the property of slow and prolonged release after oral administration. Animal and clinical safety tests showed that HupA had no unexpected toxicity, particularly the dose-limiting hepatotoxicity induced by tacrine. The phase IV clinical trials in China have demonstrated that HupA significantly improved memory deficits in elderly people with benign senescent forgetfulness, and patients with Alzheimer disease and vascular dementia, with minimal peripheral cholinergic side effects and no unexpected toxicity. HupA can also be used as a protective agent against organophosphate intoxication.
语种英语
源URL[http://119.78.100.183/handle/2S10ELR8/286758]  
专题中国科学院上海药物研究所
作者单位中国科学院上海药物研究所
推荐引用方式
GB/T 7714
Rui Wang,Han Yan,Xican Tang. progressinstudiesofhuperzineaanaturalcholinesteraseinhibitorfromchineseherbalmedicine[J]. actapharmacologicasinica,2006,27(1):1.
APA Rui Wang,Han Yan,&Xican Tang.(2006).progressinstudiesofhuperzineaanaturalcholinesteraseinhibitorfromchineseherbalmedicine.actapharmacologicasinica,27(1),1.
MLA Rui Wang,et al."progressinstudiesofhuperzineaanaturalcholinesteraseinhibitorfromchineseherbalmedicine".actapharmacologicasinica 27.1(2006):1.

入库方式: OAI收割

来源:上海药物研究所

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