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Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine
文献类型：期刊论文
| 作者 | Wang, R; Yan, H; Tang, XC
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2006-01 |
| 卷号 | 27期号:1页码:1-26 |
| ISSN号 | 1671-4083 |
| 关键词 | huperzine A Alzheimer disease acetylcholinesterase cholinesterase inhibitors cognitive enhancer neuroprotect agents oxidative stress apoptosis |
| DOI | 10.1111/j.1745-7254.2006.00255.x |
| 文献子类 | Review |
| 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. |
| WOS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 |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| WOS记录号 | WOS:000234427200001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273692]  |
| 专题 | 院士及顾问专家 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Tang, XC |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, R,Yan, H,Tang, XC. Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine[J]. ACTA PHARMACOLOGICA SINICA,2006,27(1):1-26. |
| APA | Wang, R,Yan, H,&Tang, XC.(2006).Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine.ACTA PHARMACOLOGICA SINICA,27(1),1-26. |
| MLA | Wang, R,et al."Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine".ACTA PHARMACOLOGICA SINICA 27.1(2006):1-26. |
入库方式： OAI收割
来源：上海药物研究所
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