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天然来源抗疟药的最新进展:隐丹参酮类似物

Recent developments in naturally derived antimalarials: cryptolepine analogues.

作者信息

Wright Colin W

机构信息

The School of Pharmacy, University of Bradford, West Yorkshire, BD7 1DP, UK.

出版信息

J Pharm Pharmacol. 2007 Jun;59(6):899-904. doi: 10.1211/jpp.59.6.0017.

Abstract

Increasing resistance of Plasmodium falciparum to commonly used antimalarial drugs has made the need for new agents increasingly urgent. In this paper, the potential of cryptolepine, an alkaloid from the West African shrub Cryptolepis sanguinolenta, as a lead towards new antimalarial agents is discussed. Several cryptolepine analogues have been synthesized that have promising in-vitro and in-vivo antimalarial activity. Studies on the antimalarial modes of action of these analogues indicate that they may have different or additional modes of action to the parent compound. Elucidation of the mode of action may facilitate the development of more potent antimalarial cryptolepine analogues.

摘要

恶性疟原虫对常用抗疟药物的耐药性不断增加,使得对新型抗疟药物的需求日益迫切。本文讨论了从西非灌木血叶藤中提取的生物碱隐丹参酮作为新型抗疟药物先导物的潜力。已经合成了几种具有良好体外和体内抗疟活性的隐丹参酮类似物。对这些类似物抗疟作用模式的研究表明,它们可能具有与母体化合物不同或额外的作用模式。阐明作用模式可能有助于开发更有效的抗疟隐丹参酮类似物。

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