青蒿琥酯和其他青蒿素类药物的抗疟和抗癌特性:目前的发展情况。

IF 1.7 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY
Monatshefte Fur Chemie Pub Date : 2021-01-01 Epub Date: 2021-03-30 DOI:10.1007/s00706-021-02759-x
Pitambar Khanal
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引用次数: 0

摘要

本综述从最新角度介绍了青蒿琥酯和其他青蒿素类抗疟药物及其在癌症治疗中的应用。青蒿琥酯是一种青蒿素衍生物。青蒿素是从植物黄花蒿中提取的。青蒿素及其衍生物是人类历史上治疗疟疾最有用的药物。与其他青蒿素相比,青蒿琥酯具有亲水基团的优势,因此药效更强。在工业规模上,青蒿素是以半合成方式合成的。青蒿素的 1,2,4-内过氧桥是该药物具有抗疟活性的原因。恶性疟原虫对青蒿素产生了抗药性,有证据表明这主要是由于恶性疟原虫的 Kelch13 蛋白发生了突变。临床试验数据显示,青蒿琥酯比奎宁和其他青蒿素类药物更有利于治疗重症疟疾患者。一些证据表明,青蒿素类药物可以开发成抗癌药物。青蒿素类药物作为抗癌药物的作用机制涉及氧化应激、DNA损伤和修复以及各种类型的细胞死亡:
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Antimalarial and anticancer properties of artesunate and other artemisinins: current development.

Antimalarial and anticancer properties of artesunate and other artemisinins: current development.

Antimalarial and anticancer properties of artesunate and other artemisinins: current development.

Antimalarial and anticancer properties of artesunate and other artemisinins: current development.

This review provides a recent perspective of artesunate and other artemisinins as antimalarial drugs and their uses in cancer therapy. Artesunate is an artemisinin derivative. Artemisinin is extracted from the plant Artemisia annua. Artemisinin and its derivatives have been the most useful drug for malarial treatment in human history. The artesunate has an advantage of a hydrophilic group over other artemisinins which makes it a more potent drug. On the industrial scale, artemisinins are synthesized in semisynthetic ways. The 1,2,4-endoperoxide bridge of artemisinins is responsible for the drug's antimalarial activity. There is the emergence of artemisinin resistance on Plasmodium falciparum and pieces of evidence suggest that it is mainly due to the mutation at Kelch13 protein of P. falciparum. Clinical trial data show that the artesunate is more favorable than quinine and other artemisinins to treat patients with severe malaria. Pieces of evidence indicate that artemisinins can be developed as anticancer drugs. The mechanism of actions on how artemisinins act as an anticancer drug involves oxidative stress, DNA damage and repair, and various types of cell deaths.

Graphic abstract:

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来源期刊
Monatshefte Fur Chemie
Monatshefte Fur Chemie 化学-化学综合
CiteScore
3.70
自引率
5.60%
发文量
116
审稿时长
3.3 months
期刊介绍: "Monatshefte für Chemie/Chemical Monthly" was originally conceived as an Austrian journal of chemistry. It has evolved into an international journal covering all branches of chemistry. Featuring the most recent advances in research in analytical chemistry, biochemistry, inorganic, medicinal, organic, physical, structural, and theoretical chemistry, Chemical Monthly publishes refereed original papers and a section entitled "Short Communications". Reviews, symposia in print, and issues devoted to special fields will also be considered.
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