Synthesis and Evaluation of a Series of Novel Asymmetrical Curcumin Analogs for the Treatment of Inflammation

Molecules

Yali Zhang¹  Leping Zhao³  Jianzhang Wu²  Xin Jiang²  Lili Dong⁴  Fengli Xu⁴  Peng Zou¹  Yuanrong Dai⁴  Xiaoou Shan⁴  Shulin Yang¹ 

[1] School of Environmental and Biological Engineering, Nanjing University of Science and Technology, Nanjing 210094, Jiangsu, China; E-Mails:;Chemical Biology Research Center at School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, Zhejiang, China; E-Mails:;Department of Pharmacy at the Affiliated Yueqing Hospital, Wenzhou Medical University, Wenzhou 325699, Zhejiang, China; E-Mail:;The 2nd Affiliated Hospital, Wenzhou Medical University, Wenzhou 325035, Zhejiang, China; E-Mails:

关键词: curcumin;    asymmetrical curcumin analogs;    anti-inflammation;    QSAR;    cytokines;   

DOI  :  10.3390/molecules19067287

来源: mdpi

【 摘 要 】

Curcumin 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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.