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    Please use this identifier to cite or link to this item: http://asiair.asia.edu.tw/ir/handle/310904400/115155


    Title: Bioactivity Study of Tricyclic and Tetracyclic Genipin Derivatives as Anti-inflammatory Agents
    Authors: Li, Sin-Min;Li, Sin-Min;Chi, Chia-Yin;Chiang, Chia-Yin;Wei-ZhengZen;Wei-ZhengZeng;Cheng-YenChu;Cheng-YenChung;Ching-ChunTs;Ching-ChunTseng;Yu-PeiHu;Yu-PeiHu;Yu-ChingLin;Yu-ChingLin;黃冠中;Jhong, Huang Guan-;IchiroArai;IchiroArai;Der-YenLee;Der-YenLee;FuhWong, Fung;FuhWong, Fung
    Contributors: 醫學暨健康學院食品營養與保健生技學系
    Keywords: Genipin；Iridoids；Cyclopentaimidazopyridine；Cyclopentapyridopyrimidine；Anti-inflammation
    Date: 2022-05-01
    Issue Date: 2023-03-29
    Publisher: 亞洲大學
    Abstract: A series of genipin derivatives included tricyclic cyclopentaimidazopyridine, cyclopentapyridopyrimidine, octahydrocyclopentapyridodiazepine, and tetracyclic decahydrobenzoimidazocyclopentapyridine were synthesized and developed as anti-inflammatory agents. All of them were tested against NO production in LPS-induced RAW264.7 cells. Based on IC50 data and the SAR study, we found that tricyclic cyclopentaimidazopyridines 3d–f and 7–9 presented the better inhibitory activities (≦ 28.1 μM) in comparison with the reference standard Indomethacin (166 μM). On the other hand, all of them showed inactivity for in vitro cyclooxygenase COX-2 inhibition assays and compounds 8 and 9 possessed the cell toxity. To explore the further anti-inflammatory mechanism, Western blot analysis was carried out. Furthermore, compound 3d shown better bioactivity than Indomethacin. The suppression of NF-κB signal pathway by compound 3d was also determined. To sum-up, compound 3d would be the potential anti-inflammatory lead compound.
    Appears in Collections:[Department of Food Nutrition and Healthy Biotechnology] Journal Article

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