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青蒿素最新研究进展:作用机制与提高全球产量的策略分析

Updates on artemisinin: an insight to mode of actions and strategies for enhanced global production.

机构信息

Laboratory of Morphogenesis, Department of Botany, Banaras Hindu University, Varanasi, India.

出版信息

Protoplasma. 2016 Jan;253(1):15-30. doi: 10.1007/s00709-015-0805-6. Epub 2015 Mar 27.

Abstract

Application of traditional Chinese drug, artemisinin, originally derived from Artemisia annua L., in malaria therapy has now been globally accepted. Artemisinin and its derivatives, with their established safety records, form the first line of malaria treatment via artemisinin combination therapies (ACTs). In addition to its antimalarial effects, artemisinin has recently been evaluated in terms of its antitumour, antibacterial, antiviral, antileishmanial, antischistosomiatic, herbicidal and other properties. However, low levels of artemisinin in plants have emerged various conventional, transgenic and nontransgenic approaches for enhanced production of the drug. According to WHO (2014), approximately 3.2 billion people are at risk of this disease. However, unfortunately, artemisinin availability is still facing its short supply. To fulfil artemisinin's global demand, no single method alone is reliable, and there is a need to collectively use conventional and advanced approaches for its higher production. Further, it is the unique structure of artemisinin that makes it a potential drug not only against malaria but to other diseases as well. Execution of its action through multiple mechanisms is probably the reason behind its wide spectrum of action. Unfortunately, due to clues for developing artemisinin resistance in malaria parasites, it has become desirable to explore all possible modes of action of artemisinin so that new generation antimalarial drugs can be developed in future. The present review provides a comprehensive updates on artemisinin modes of action and strategies for enhanced artemisinin production at global level.

摘要

中药青蒿素最初源自青蒿(Artemisia annua L.),其在疟疾治疗中的应用现已得到全球认可。青蒿素及其衍生物具有明确的安全性记录,通过青蒿素联合疗法(ACT)成为抗疟治疗的一线药物。除了抗疟作用外,青蒿素在抗肿瘤、抗菌、抗病毒、抗利什曼原虫、抗血吸虫、除草等方面的作用也得到了评估。然而,植物中青蒿素含量低,因此人们采用了各种常规、转基因和非转基因方法来提高药物产量。根据世界卫生组织(WHO)(2014 年)的数据,约有 32 亿人面临这种疾病的风险。然而,不幸的是,青蒿素的供应仍然存在短缺。为了满足全球对青蒿素的需求,单凭单一方法是不可靠的,需要综合采用常规和先进方法来提高其产量。此外,青蒿素独特的结构使其不仅成为抗疟药物的潜在选择,也可能成为治疗其他疾病的潜在药物。其通过多种机制发挥作用可能是其广谱作用的原因。不幸的是,由于疟原虫对青蒿素产生耐药性的线索,人们希望探索青蒿素的所有可能作用模式,以便未来开发新一代抗疟药物。本综述提供了青蒿素作用模式的全面更新,并介绍了全球范围内提高青蒿素产量的策略。

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