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作为DNA拓扑异构酶抑制剂的次生代谢产物:抗癌药物设计的新时代。

Secondary metabolites as DNA topoisomerase inhibitors: A new era towards designing of anticancer drugs.

作者信息

Baikar Supriya, Malpathak Nutan

机构信息

Department of Botany, University of Pune, Pune, India.

出版信息

Pharmacogn Rev. 2010 Jan;4(7):12-26. doi: 10.4103/0973-7847.65320.

Abstract

A large number of secondary metabolites like alkaloids, terpenoids, polyphenols and quinones are produced by the plants. These metabolites can be utilized as natural medicines for the reason that they inhibit the activity of DNA topoisomerase which are the clinical targets for anticancer drugs. DNA topoisomerases are the cellular enzymes that change the topological state of DNA through the breaking and rejoining of DNA strands. Synthetic drugs as inhibitors of topoisomerases have been developed and used in the clinical trials but severe side effects are a serious problem for them therefore, there is a need for the development of novel plant-derived natural drugs and their analogs which may serve as appropriate inhibitors with respect to drug designing. The theme for this review is how secondary metabolites or natural products inactivate the action of DNA topoisomerases and open new avenues towards isolation and characterization of compounds for the development of novel drugs with anticancer potential.

摘要

植物会产生大量的次生代谢产物,如生物碱、萜类化合物、多酚和醌类。这些代谢产物可被用作天然药物,因为它们能抑制DNA拓扑异构酶的活性,而DNA拓扑异构酶是抗癌药物的临床靶点。DNA拓扑异构酶是一种细胞酶,通过DNA链的断裂和重新连接来改变DNA的拓扑状态。作为拓扑异构酶抑制剂的合成药物已被开发并用于临床试验,但严重的副作用是它们面临的一个严重问题。因此,需要开发新型的植物源天然药物及其类似物,这些药物在药物设计方面可能是合适的抑制剂。本综述的主题是次生代谢产物或天然产物如何使DNA拓扑异构酶的作用失活,并为分离和鉴定具有抗癌潜力的新型药物的化合物开辟新途径。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b40/3249898/c894413e0d8b/PRev-4-12-g002.jpg

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