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.
Copyright © 2020 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Artemisinins / chemical synthesis
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Artemisinins / chemistry
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Artemisinins / pharmacology*
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Glycosides / chemical synthesis
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Glycosides / chemistry
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Glycosides / pharmacology*
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Humans
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Immunosuppressive Agents / chemical synthesis
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Immunosuppressive Agents / chemistry
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Immunosuppressive Agents / pharmacology*
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Interferon-gamma / antagonists & inhibitors*
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Molecular Conformation
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Stereoisomerism
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Structure-Activity Relationship
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T-Lymphocytes / drug effects*
Substances
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Artemisinins
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Glycosides
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Immunosuppressive Agents
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artenimol
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Interferon-gamma