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青蒿素类抗疟药的研究进展:最新情况

Progress in the research of artemisinin-related antimalarials: an update.

作者信息

Woerdenbag H J, Pras N, van Uden W, Wallaart T E, Beekman A C, Lugt C B

机构信息

Department of Pharmaceutical Biology, University of Groningen, The Netherlands.

出版信息

Pharm World Sci. 1994 Aug 5;16(4):169-80. doi: 10.1007/BF01872865.

Abstract

Artemisinin, a sesquiterpene lactone endoperoxide isolated from Artemisia annua L., and a number of its semisynthetic derivatives have shown to possess antimalarial properties. They are all effective against Plasmodium parasites that are resistant to the newest and commonly used antimalarial drugs. This article gives a survey of the literature dealing with artemisinin-related antimalarial issues that have appeared from the end of 1989 up to the beginning of 1994. A broad range of medical and pharmaceutical disciplines is covered, including phytochemical aspects like the selection of high-producing plants, analytical procedures, and plant biotechnology. Furthermore, the organic synthesis of artemisinin derivatives is discussed, as well as their mechanism of action and antimalarial activity, metabolism and pharmacokinetics, clinical studies, side-effects and toxicology, and biological activities other than antimalarial activity.

摘要

青蒿素是从黄花蒿中分离出的一种倍半萜内酯过氧化物,其多种半合成衍生物均显示出抗疟特性。它们对耐最新常用抗疟药物的疟原虫均有效。本文综述了1989年末至1994年初出现的有关青蒿素相关抗疟问题的文献。涵盖了广泛的医学和药学学科,包括植物化学方面,如高产植物的选择、分析方法和植物生物技术。此外,还讨论了青蒿素衍生物的有机合成、作用机制和抗疟活性、代谢和药代动力学、临床研究、副作用和毒理学以及除抗疟活性以外的生物活性。

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