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(S)-(+)-Decursin and its Analogues as Inhibitors of Cytokines Secretion Induced by DpE in THP-1/EoL-1 Cell Line

약학회지 2017년 61권 3호 p.178 ~ 187
이지현, 조수현, Yun Eun-Ju, O Yu-Seok, 김지은, 이지숙, Yun Chi-Yong, 송규용,
소속 상세정보
이지현 ( Lee Jee-Hyun ) - Chungnam National University College of Pharmacy
조수현 ( Cho Soo-Hyun ) - PCPIA BIT
 ( Yun Eun-Ju ) - Chungnam National University College of Pharmacy
 ( O Yu-Seok ) - Chungnam National University College of Pharmacy
김지은 ( Kim Ji-Eun ) - Chungnam National University College of Pharmacy
이지숙 ( Lee Ji-Sook ) - Wonkwang health Science University Department of Clinical Pathology
 ( Yun Chi-Yong ) - Daejeon University Department of Life Science and Biotechnology
송규용 ( Song Gyu-Yong ) - Chungnam National University College of Pharmacy

Abstract


(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

키워드

Decursin Analogues; Dermatophagoides Pteronyssinus; Anti-inflammation

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