Synthesis and Evaluation of a Series of Novel Asymmetrical Curcumin Analogs for the Treatment of Inflammation
AbstractCurcumin has been reported to possess multiple bioactivities, such as antioxidant, anticancer, and anti-inflammatory properties, however the clinical application of curcumin has been significantly limited by its instability and poor metabolism. Modification of curcumin has led to discovery and development of lots of novel therapeutic candidates. In recent years acute and chronic inflammation has been the focus of numerous studies in various diseases. Here, we synthesized a series of asymmetrical curcumin analogs with high in vitro chemical stability, and their anti-inflammatory activity was evaluated in LPS-stimulated macrophages. According to the bio-screening results and QSAR analysis, these analogs exhibited potent activities against LPS-induced TNF-α and IL-6 release. Among the analogs of the potent anti-inflammatory activity, compounds 3b8 and 3b9 exhibited significant protection and possess enhanced anti-inflammatory activity thereby attenuated the LPS-induced septic death in mice. View Full-Text
- Supplementary File 1:
Supplementary Materials (PDF, 499 KB)
Scifeed alert for new publicationsNever miss any articles matching your research from any publisher
- Get alerts for new papers matching your research
- Find out the new papers from selected authors
- Updated daily for 49'000+ journals and 6000+ publishers
- Define your Scifeed now
Zhang, Y.; Zhao, L.; Wu, J.; Jiang, X.; Dong, L.; Xu, F.; Zou, P.; Dai, Y.; Shan, X.; Yang, S.; Liang, G. Synthesis and Evaluation of a Series of Novel Asymmetrical Curcumin Analogs for the Treatment of Inflammation. Molecules 2014, 19, 7287-7307.
Zhang Y, Zhao L, Wu J, Jiang X, Dong L, Xu F, Zou P, Dai Y, Shan X, Yang S, Liang G. Synthesis and Evaluation of a Series of Novel Asymmetrical Curcumin Analogs for the Treatment of Inflammation. Molecules. 2014; 19(6):7287-7307.Chicago/Turabian Style
Zhang, Yali; Zhao, Leping; Wu, Jianzhang; Jiang, Xin; Dong, Lili; Xu, Fengli; Zou, Peng; Dai, Yuanrong; Shan, Xiaoou; Yang, Shulin; Liang, Guang. 2014. "Synthesis and Evaluation of a Series of Novel Asymmetrical Curcumin Analogs for the Treatment of Inflammation." Molecules 19, no. 6: 7287-7307.