Review Article

Artemisinin derivative SM934 in the treatment of autoimmune and inflammatory diseases: therapeutic effects and molecular mechanisms

Xiao Tong1,2, Li Chen1,2, Shi-jun He1,2, Jian-ping Zuo1,2
1 Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
2 University of Chinese Academy of Sciences, Beijing 100049, China
Correspondence to: Shi-jun He:, Jian-ping Zuo:,
DOI: 10.1038/s41401-022-00978-4
Received: 31 May 2022
Accepted: 7 August 2022
Advance online: 1 September 2022


Artemisinin and its derivatives are the well-known anti-malarial drugs derived from a traditional Chinese medicine. In addition to antimalarial, artemisinin and its derivatives possess distinguished anti-cancer, anti-oxidant, anti-inflammatory and anti-viral activities, but the poor solubility and low bioavailability hinder their clinical application. In the last decades a series of new water- soluble and oil-soluble derivatives were synthesized. Among them, we have found a water-soluble derivative β-aminoarteether maleate (SM934) that exhibits outstanding suppression on lymphocytes proliferation in immunosuppressive capacity and cytotoxicity screening assays with 35-fold higher potency than dihydroartemisinin. SM934 displays significant therapeutic effects on various autoimmune and inflammatory diseases, including systemic lupus erythematosus, antiphospholipid syndrome nephropathy, membranous nephropathy, rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease, and dry eye disease. Here, we summarize the immunomodulatory effects, anti-inflammatory, anti-oxidative and anti-fibrosis activities of SM934 in disease-relevant animal models and present the probable pharmacological mechanisms involved in its therapeutic efficacy. This review also delineates a typical example of natural product-based drug discovery, which might further vitalize natural product exploration and development in pharmacotherapy.
Keywords: artemisinin derivative; β-aminoarteether maleate (SM934); autoimmune and inflammatory diseases; T helper cells; macrophages; inflammatory cytokines

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