Progress in the Research of Lycopodium Alkaloids

Progress in the Research of Lycopodium Alkaloids
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DOI:
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发表时间:
2003
影响因子:
4.6
通讯作者:
Tan Chang
Tan Chang
中科院分区:
医学2区
文献类型:
--
作者:
Tan Chang

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综述了1994年1月至2003年3月发现的石杉碱类生物碱,以及石杉碱A (HA)的研究进展。本文阐述了番茄碱型、番茄碱型、fawcettimini型和杂族这四种常见的番茄属生物碱的结构特征。药理学研究表明,透明质酸是一种有效的、高选择性的、可逆的乙酰胆碱酯酶(AChE)抑制剂。对HA的构效关系研究表明,HA具有简洁的结构,其大部分结构片段,如两个双键、吡酮环、三碳桥环和氨基的n原子是其具有高抗AchE活性所必需的。近年来,一些HA希夫碱衍生物和HA-tacrine杂交种被报道具有接近或优于HA的抗ache活性。
The Lycopodiwn alkaloids discovered from January, 1994 to March, 2003, and the research progress of huperzine A (HA) were reviewed. This paper illustrated the structure characters of lycopodine-type, lycodine-type, fawcettimine-type and miscellaneous group, common four types of Lycopodium alkaloids. Pharmacological studies showed HA was a potent, high selective, and reversible acetycholinesterase(AChE) inhibitor. The structure-activity relationship studies on HA disclosed that HA possesses a concise structure, in which most of structure fragments, such as two double bonds, pyridone ring, tri-carbon bridge ring, and the N-atom of the amino group were necessary for its high anti- AchE activity. Recently, some HA Schiff base derivatives and HA-tacrine hybrids were reported that they had near or better anti-AChE activity than HA.