Synthesis of 1,5-Anhydro-d-fructose derivatives and evaluation of their inflammasome inhibitors
| Autor: | Junko Amano, Kohtaro Goto, Hiroko Ideo, Takashi Shirai, Satoshi Noma, Akio Matsuda, Ikuro Maruyama, Akiko Tsuchida, Yuriko Hirose, Mamoru Mizuno |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Lipopolysaccharides Inflammasomes Dimer Clinical Biochemistry Interleukin-1beta Pharmaceutical Science Fructose 010402 general chemistry Inhibitory postsynaptic potential 01 natural sciences Biochemistry 03 medical and health sciences chemistry.chemical_compound Mice Structure-Activity Relationship Drug Discovery NLR Family Pyrin Domain-Containing 3 Protein medicine High activity Animals Humans Molecular Biology Cells Cultured Chemistry Macrophages Organic Chemistry D fructose Low activity Inflammasome 0104 chemical sciences Mice Inbred C57BL 030104 developmental biology Molecular Medicine medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry. 26(13) |
| ISSN: | 1464-3391 |
| Popis: | Synthesis of several 1,5-Anhydro-d-fructose (1,5-AF) derivatives to evaluate inhibitory activities of the inflammasome was carried out. Recently, 1,5-AF reported to suppress the inflammasome, although with only low activity. We focused on the hydration of 2-keto form of 1,5-AF and speculated that this hydration was the cause of low activity. Therefore, we synthesized some 1,5-AF derivatives that would not be able to form the dimer conformation and can be expected to have high activity against inflammasome, and then evaluated their inhibitory activities with respect to the NLRP3 inflammasome by using mouse bone marrow-derived macrophages and human THP-1 cells. As a result, some synthesized 2-keto form compounds had much higher inhibitory activities with respect to the NLRP3 inflammasome than did 1,5-AF. |
| Databáze: | OpenAIRE |
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