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特曲霉素B衍生物对乙酰胆碱酯酶的抑制作用。

Acetylcholinesterase inhibition by territrem B derivatives.

作者信息

Peng F C

机构信息

Institute of Toxicology, College of Medicine, National Taiwan University, Taipei, Republic of China.

出版信息

J Nat Prod. 1995 Jun;58(6):857-62. doi: 10.1021/np50120a006.

Abstract

Five derivatives of territrem B [2], a potent acetylcholinesterase inhibitor isolated from a rice culture of Aspergillus terreus, were prepared from 2 as well as from its major metabolite, 4 beta-hydroxymethyl-4 beta-demethylterritrem B [4]. The inhibitory activities of these derivatives against electric eel acetylcholinesterase (E.C. 3.1.1.7) were tested and it was concluded that the enone and the pyrone groups present in 2 may play an important biological role.

摘要

从土曲霉水稻培养物中分离得到的强效乙酰胆碱酯酶抑制剂土曲霉震颤素B [2] 的5种衍生物,是由2及其主要代谢产物4β-羟甲基-4β-去甲基土曲霉震颤素B [4] 制备而成。测试了这些衍生物对电鳗乙酰胆碱酯酶(E.C. 3.1.1.7)的抑制活性,得出结论:2中存在的烯酮和吡喃酮基团可能起着重要的生物学作用。

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