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从化学 bench 到临床前试验的 Annonaceous acetogenins 的历史观点。

Historic perspectives on Annonaceous acetogenins from the chemical bench to preclinical trials.

机构信息

Graduate Institute of Pharmaceutical Chemistry, College of Pharmacy, China Medical University, Taichung, Taiwan.

出版信息

Planta Med. 2010 Sep;76(13):1390-404. doi: 10.1055/s-0030-1250006. Epub 2010 Jun 24.

DOI:10.1055/s-0030-1250006
PMID:20577943
Abstract

Studies on the Annonaceous acetogenins began after the first cytotoxic acetogenin, uvaricin, was isolated in 1982. This attractive finding made many medicinal and natural product chemists direct their efforts on the isolation and identification of these classes of compounds. As more Annonaceous acetogenins were isolated, more information about them was uncovered. From their structural identification to the total synthesis of natural product analogues and from cell-based screening and molecular-based targeting to animal testing, the mechanisms of action of the Annonaceous acetogenins became clearer. The purpose of this review is to give an account of recent studies on this class of compounds and their analogues, which will aid us not only in clarifying how the Annonaceous acetogenins act but also in establishing principles for the further development of this class of compounds.

摘要

在 1982 年分离出第一个细胞毒性的醋酸酯酶抑制剂乌伐他汀后,人们开始对番荔枝科醋酸酯酶抑制剂进行研究。这一诱人的发现促使许多药物和天然产物化学家致力于这些化合物的分离和鉴定。随着更多的番荔枝科醋酸酯酶抑制剂被分离出来,人们对它们的了解也越来越多。从结构鉴定到天然产物类似物的全合成,从基于细胞的筛选到基于分子的靶向到动物试验,番荔枝科醋酸酯酶抑制剂的作用机制变得更加清晰。本文的目的是介绍该类化合物及其类似物的最新研究进展,这不仅有助于阐明番荔枝科醋酸酯酶抑制剂的作用机制,也有助于为该类化合物的进一步发展奠定基础。

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