Dried-leaf Artemisia annua: A practical malaria therapeutic for developing countries?

查看全文 作　　者：Pamela J [1]Weathers;Melissa [1]Towler;Ahmed [2]Hassanali;Pierre [3]Lutgen;Patrick Ogwang [4]Engeu

机构地区：[1]Department of Biologyand Biotechnology, Worcester Polytechnic Institute, Worcester, MA 01609, United States;[2]School of Pure and Applied Sciences, Kenyatta University;[3]IFBV-BELHERB, PO Box 98, L-6908 Nieder-anven, Luxembourg;[4]Natural Chemotherapeutics Research Institute, Ministry of Health, PO Box 4864 Kampala, Uganda

出　　处：《World Journal of Pharmacology》索引2014年第3卷第4期,共17页

基　　金：Supported by Worcester Polytechnic Institute and University of Massachusetts Center for Clinical and Translational Science partially;partially by Award Number NIH-R15AT008277-01 from the National Center for Complementary and Alternative Medicine 摘　　要：Artemisinin from the plant Artemisia annua(A. annua) L., and used as artemisinin combination therapy(ACT), is the current best therapeutic for treating malaria, a disease that hits children and adults especially in developing countries. Traditionally, A. annua was used by the Chinese as a tea to treat 'fever'. More recently, investigators have shown that tea infusions and oral consumption of the dried leaves of the plant have prophylactic and therapeutic efficacy. The presence of a complex matrix of chemicals within the leaves seems to enhance both the bioavailability and efficacy of artemisinin. Although about 1000-fold less potent than artemisinin in their antiplasmodial activity, these plant chemicals are mainly small molecules that include other artemisinic compounds, terpenes(mainly mono and sesqui), flavonoids, and polyphenolic acids. In addition, polysaccharide constituents of A. annua may enhance bioavailability of artemisinin. Rodent pharmacokinetics showed longer T? and T max and greater C max and AUC in Plasmodium chabaudi-infected mice treated with A. annua dried leaves than in healthy mice. Pharmacokinetics of deoxyartemisinin, a liver metabolite of artemisinin, was more inhibited in infected than in healthy mice. In healthy mice, artemisinin serum levels were > 40-fold greater in dried leaf fed mice than those fed with pure artemisinin. Human trial data showed that when delivered as dried leaves, 40-fold less artemisinin was required to obtain a therapeutic response compared to pure artemisinin. ACTs are still unaffordable for many malaria patients, and cost estimates for A. annua dried leaf tablet production are orders of magnitude less than for ACT, despite improvements in the production capacity. Considering that for > 2000 years this plant was used in traditional Chinese medicine for treatment of fever with no apparent appearance of artemisinin drug resistance, the evidence argues for inclusion of affordable A. annua dried leaf tablets into the arsenal of drugs to combat malaria and other artemisinin-susceptible diseases. 关键词：青蒿素药代动力学治疗方法临床分析

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Dried-leaf Artemisia annua: A practical malaria therapeutic for developing countries?

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