Bioactivity Study of Tricyclic and Tetracyclic Genipin Derivatives as Anti-inflammatory Agents

ASIA unversity > 醫學暨健康學院 > 食品營養與保健生技學系 > 期刊論文 > Item 310904400/115155

請使用永久網址來引用或連結此文件: http://asiair.asia.edu.tw/ir/handle/310904400/115155

題名:	Bioactivity Study of Tricyclic and Tetracyclic Genipin Derivatives as Anti-inflammatory Agents
作者:	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
貢獻者:	醫學暨健康學院食品營養與保健生技學系
關鍵詞:	Genipin；Iridoids；Cyclopentaimidazopyridine；Cyclopentapyridopyrimidine；Anti-inflammation
日期:	2022-05-01
上傳時間:	2023-03-29
出版者:	亞洲大學
摘要:	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.
顯示於類別:	[食品營養與保健生技學系] 期刊論文

文件中的檔案:

檔案	描述	大小	格式	瀏覽次數
index.html		0Kb	HTML	102	檢視/開啟

在ASIAIR中所有的資料項目都受到原著作權保護.

資料載入中.....