rdf:type |
|
lifeskim:mentions |
umls-concept:C0007634,
umls-concept:C0008429,
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0026809,
umls-concept:C0063033,
umls-concept:C0168307,
umls-concept:C0175677,
umls-concept:C0205263,
umls-concept:C0599473,
umls-concept:C1545588
|
pubmed:issue |
3
|
pubmed:dateCreated |
2001-12-28
|
pubmed:abstractText |
Recently, the potent cholinesterase inhibitor (-)-huperzine A (HupA) was demonstrated to protect neuronal and glial cells against the cytotoxicity of beta-amyloid (Abeta). Since the unnatural (+)-HupA is a much less potent inhibitor, it was of interest to examine the stereoselectivity of cellular protection by the two isomers. In the present study, effects of (+)- and (-)-HupA on Abeta(25-35)-induced injury were compared in PC12 and NG108-15 neuroblastoma cell lines. Following a 24 h exposure to 1 microM Abeta(25-35), cell survival was markedly reduced, but preincubation with (+)-HupA or (-)-HupA (0.1-10 microM) enhanced survival significantly. The potency of (-)-HupA and (+)-HupA in protecting against Abeta toxicity was similar. This result contrasted with the stereoselectivity of cholinesterase inhibition in vitro and in vivo, in which (-)-HupA is about 50-fold more potent than (+)-HupA. It is concluded that the neuroprotective properties of HupA enantiomers have no relation to anti-cholinesterase activity.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
0304-3940
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
14
|
pubmed:volume |
317
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
143-6
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:11755260-Acetylcholine,
pubmed-meshheading:11755260-Alkaloids,
pubmed-meshheading:11755260-Alzheimer Disease,
pubmed-meshheading:11755260-Amyloid beta-Peptides,
pubmed-meshheading:11755260-Animals,
pubmed-meshheading:11755260-Cerebral Cortex,
pubmed-meshheading:11755260-Cholinesterase Inhibitors,
pubmed-meshheading:11755260-Dose-Response Relationship, Drug,
pubmed-meshheading:11755260-Mice,
pubmed-meshheading:11755260-Neurons,
pubmed-meshheading:11755260-Neuroprotective Agents,
pubmed-meshheading:11755260-Neurotoxins,
pubmed-meshheading:11755260-PC12 Cells,
pubmed-meshheading:11755260-Peptide Fragments,
pubmed-meshheading:11755260-Rats,
pubmed-meshheading:11755260-Sesquiterpenes,
pubmed-meshheading:11755260-Stereoisomerism
|
pubmed:year |
2002
|
pubmed:articleTitle |
Stereoselectivities of enantiomers of huperzine A in protection against beta-amyloid(25-35)-induced injury in PC12 and NG108-15 cells and cholinesterase inhibition in mice.
|
pubmed:affiliation |
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 294 Tai Yuan Road, Shanghai 200031, PR China.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|