Huperzine A, a novel promising acetylcholinesterase inhibitor

被引:89
作者
Cheng, DH [1 ]
Ren, H [1 ]
Tang, XC [1 ]
机构
[1] CHINESE ACAD SCI, SHANGHAI INST MAT MED, STATE KEY LAB DRUG RES, SHANGHAI 200031, PEOPLES R CHINA
关键词
Alzheimer's disease; cholinesterase inhibitor; E2020; huperzine A; memory; radial maze; scopolamine; tacrine;
D O I
10.1097/00001756-199612200-00020
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
THE effects of huperzine A on memory impairments induced by scopolamine were evaluted using a radial maze task and inhibition of cholinesterase in vitro compared with the effects of E2020 and tacrine. Scopolamine (0.2 mg kg(-1)) significantly impaired spatial memory in rats. Huperzine A (0.1-0.4 mg kg(-1), p.o.), E2020 (0.5-1.0 mg kg(-1), p.o.) and tacrine (1.0-2.0 mg kg(-1), p.o) could reverse these scopolamine-induced memory deficits. The ratios of huperzine A, E2020 and tacrine for butyrylcholinesterase:acetylcholinesterase determined by a colourimetric method were 884.57, 489.05, and 0.80, respectively. The results demonstrated that huperzine A was the most selective acetylcholinterase inhibitor, and improved the working memory deficit induced by scopolamine significantly better than did E2020 or tacrine, suggesting it may be a promising agent for clinical therapy of cognitive impairment in patients with Alzheimer's Disease.
引用
收藏
页码:97 / 101
页数:5
相关论文
共 22 条
  • [1] THE CHOLINERGIC HYPOTHESIS OF GERIATRIC MEMORY DYSFUNCTION
    BARTUS, RT
    DEAN, RL
    BEER, B
    LIPPA, AS
    [J]. SCIENCE, 1982, 217 (4558) : 408 - 417
  • [2] NEUROTRANSMISSION - THE LINK INTEGRATING ALZHEIMER RESEARCH
    BOWEN, DM
    FRANCIS, PT
    CHESSELL, IP
    WEBSTER, MT
    [J]. TRENDS IN NEUROSCIENCES, 1994, 17 (04) : 149 - 150
  • [3] ALZHEIMERS-DISEASE - A DISORDER OF CORTICAL CHOLINERGIC INNERVATION
    COYLE, JT
    PRICE, DL
    DELONG, MR
    [J]. SCIENCE, 1983, 219 (4589) : 1184 - 1190
  • [4] CHOLINERGIC STRATEGIES IN THE TREATMENT OF ALZHEIMERS-DISEASE
    DAVIDSON, M
    STERN, RG
    BIERER, LM
    HORVATH, TB
    ZEMISHLANI, Z
    MARKOFSKY, R
    MOHS, RC
    [J]. ACTA PSYCHIATRICA SCANDINAVICA, 1991, 83 : 47 - 51
  • [5] DAVIES P, 1976, LANCET, V2, P1403
  • [6] A NEW AND RAPID COLORIMETRIC DETERMINATION OF ACETYLCHOLINESTERASE ACTIVITY
    ELLMAN, GL
    COURTNEY, KD
    ANDRES, V
    FEATHERSTONE, RM
    [J]. BIOCHEMICAL PHARMACOLOGY, 1961, 7 (02) : 88 - &
  • [7] THE CHOLINERGIC NEUROTRANSMITTER SYSTEM IN HUMAN-MEMORY AND DEMENTIA - A REVIEW
    KOPELMAN, MD
    [J]. QUARTERLY JOURNAL OF EXPERIMENTAL PSYCHOLOGY SECTION A-HUMAN EXPERIMENTAL PSYCHOLOGY, 1986, 38 (04): : 535 - 573
  • [8] Lin JH, 1996, ACTA PHARM SINIC, V17, P299
  • [9] THE STRUCTURES OF HUPERZINE-A AND HUPERZINE-B, 2 NEW ALKALOIDS EXHIBITING MARKED ANTICHOLINESTERASE ACTIVITY
    LIU, JS
    ZHU, YL
    YU, CM
    ZHOU, YZ
    HAN, YY
    WU, FW
    QI, BF
    [J]. CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE, 1986, 64 (04): : 837 - 839
  • [10] POTENCIES AND STEREOSELECTIVITIES OF ENANTIOMERS OF HUPERZINE-A FOR INHIBITION OF RAT CORTICAL ACETYLCHOLINESTERASE
    MCKINNEY, M
    MILLER, JH
    YAMADA, F
    TUCKMANTEL, W
    KOZIKOWSKI, AP
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 203 (02) : 303 - 305