2. Academic Validation
  3. Studies on the stereoselective synthesis and immunosuppressive activity of dihydroartemisinin-O-glycoside derivatives

Studies on the stereoselective synthesis and immunosuppressive activity of dihydroartemisinin-O-glycoside derivatives

  • Bioorg Med Chem Lett. 2020 Aug 15;30(16):127338. doi: 10.1016/j.bmcl.2020.127338.
Yu Yu 1,  Jingfeng Yu 1,  Xiaosu Zou 1,  Wei Xu 1,  Jinghua Zhang 2,  Hongzhu Bian 3,  Xun Dong 3,  Zhengwu Shen 4
Affiliations

Affiliations

  • 1 Shanghai University of Traditional Chinese Medicine, PR China.
  • 2 Shanghai Jiao Tong University School of Medicine, PR China.
  • 3 Yunnan Baiyao Group Co., Ltd., PR China.
  • 4 Shanghai Jiao Tong University School of Medicine, PR China; Shanghai University of Traditional Chinese Medicine, PR China. Electronic address: [email protected].
PMID: 32631539 DOI: 10.1016/j.bmcl.2020.127338
Abstract

Eight new dihydroartemisinin-O-glycosides were synthesized with their relative configurations were determined based on NMR spectrum. In vitro immunosuppressive assay showed that 10α-dihydroartemisinin-β-O-d-mannoside (19a) demonstrate 88% inhibition towards T cells proliferation and 98% reduction in IFN-γ levels in cell media. These results suggest that dihydroartemisinin-O-glycoside as a potential lead for further in vivo evaluation.

Keywords

Dihydroartemisinin; Glycoside; Immunosuppressive.

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