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Studies on the stereoselective synthesis and immunosuppressive activity of dihydroartemisinin-O-glycoside derivatives.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-06-10 , 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
中文翻译：
双氢青蒿素-O-糖苷衍生物立体选择性合成及免疫抑制活性的研究。
更新日期：2020-06-10
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-06-10 , 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
Affiliation
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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.
中文翻译：
双氢青蒿素-O-糖苷衍生物立体选择性合成及免疫抑制活性的研究。
合成了八种新的双氢青蒿素-O-糖苷，并基于核磁共振谱确定了它们的相对构型。体外免疫抑制试验表明，10α-二氢青蒿素-β-O- d-甘露糖苷 ( 19a)对 T 细胞增殖有 88% 的抑制作用，细胞培养基中 IFN-γ 水平降低 98%。这些结果表明双氢青蒿素-O-糖苷可作为进一步体内评估的潜在先导物。
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