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KMID : 0370220170610030178
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Yakhak Hoeji
2017 Volume.61 No. 3 p.178 ~ p.187
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(S)-(+)-Decursin and its Analogues as Inhibitors of Cytokines Secretion Induced by DpE in THP-1/EoL-1 Cell Line
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Lee Jee-Hyun
Cho Soo-Hyun
Yun Eun-Ju
O Yu-Seok
Kim Ji-Eun
Lee Ji-Sook
Yun Chi-Yong
Song Gyu-Yong
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Abstract
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(S)-(+)-Decursin and its analogues were synthesized and evaluated for their inhibitory effects on monocyte chemoattractant protein-1 (MCP-1), interleukin-8 (IL-8), and IL-6 secretion induced by Dermatophagoides pteronyssinus extract (DpE) in human acute monocytic leukemia (THP-1) cells and eosinophilic leukemia (EoL-1) cell lines. (S)-(+)-Decursin analogues with alkyl acryloyl groups, apart from (S)-(+)-decursin (1) and (S)-(+)-decursinol angelate (4a), did not influence the regulation of cytokine secretion. (S)-(+)-Decursin analogues (8d, 8f, 8g) with cinnamoyl groups carrying hydroxyl- and acetoxy-substitutes potently inhibited the secretion of MCP-1 and IL-6. The structure-activity relationship study revealed that increasing π-rich environment at the extensions from the eastern alcohol of (S)-(+)-decursin is a key element in building the pharmacophore for achieving the desired biological activity
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KEYWORD
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Decursin Analogues, Dermatophagoides Pteronyssinus, Anti-inflammation
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