Discovery and repurposing of artemisinin

Abstract

Malaria is an ancient infectious disease that threatens millions of lives globally even today. The discovery of artemisinin, inspired by traditional Chinese medicine (TCM), has brought in a paradigm shift and been recognized as the “best hope for the treatment of malaria” by World Health Organization. With its high potency and low toxicity, the wide use of artemisinin effectively treats the otherwise drug-resistant parasites and helps many countries, including China, to eventually eradicate malaria. Here, we will first review the initial discovery of artemisinin, an extraordinary journey that was in stark contrast with many drugs in western medicine. We will then discuss how artemisinin and its derivatives could be repurposed to treat cancer, inflammation, immunoregulation-related diseases, and COVID-19. Finally, we will discuss the implications of the “artemisinin story” and how that can better guide the development of TCM today. We believe that artemisinin is just a starting point and TCM will play an even bigger role in healthcare in the 21st century.

Keywords

artemisinin / drug repurposing / cancer / inflammation / COVID-19 / traditional Chinese medicine

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Acknowledgements

The authors gratefully acknowledge the financial support from the National Key R&D Program of China (No. 2020YFA0908000), the National Natural Science Foundation of China (Nos. 82074098 and 82104480), the Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine (No. ZYYCXTD-C-202002), the CACMS Innovation Fund (No. CI2021A05101), and the Fundamental Research Funds for the Central Public Welfare Research Institutes (Nos. ZZ14-YQ-050, ZZ14-YQ-051, ZZ14-YQ-059, ZZ14-YQ-060, ZZ14-ND-010, ZZ14-LFL-002, ZZ15-ND-10, ZXKT19018, and ZXKT19021).

Compliance with ethics guidelines

Qiaoli Shi, Fei Xia, Qixin Wang, Fulong Liao, Qiuyan Guo, Chengchao Xu, and Jigang Wang declare that they have no conflict of interest. This manuscript is a review article, and it does not involve a research protocol requiring approval by the relevant institutional review board or ethics committee.

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