Synthesis and Biological Evaluation of Novel Curcuminoid Derivatives

Molecules

Ya-Kun Cao²  Hui-Jing Li¹  Zhi-Fang Song²  Yang Li²  Qi-Yong Huai² 

[1]Department of Environmental Engineering, School of Marine Science and Technology, Harbin Institute of Technology, Weihai 264209, China

[2] E-Mail:

[3]Department of Applied Chemistry, Marine College, Shandong University, Weihai 264209, China

[4] E-Mails:

关键词: curcuminoids;    antibacterial;    antioxidant;    antiproliferative;   

DOI  :  10.3390/molecules191016349

来源: mdpi

【 摘 要 】

Curcuminoids have been reported to possess multiple bioactivities, such as antioxidant, anticancer and anti-inflammatory properties. Three novel series of curcuminoid derivatives (11a–h, 15a–h and 19a–d) with enhanced bioactivity have been synthesized. Among the synthesized compounds, 11b exhibited the most significant activity with an MIC of 0.5 µM /mL against selected medically important Gram-positive cocci (S. aureus and S. viridans) and Gram-negative bacilli (E. coli and E. cloacae). The derivatives exhibited remarkable results in an antioxidant test with an IC₅₀ 2.4- to 9.3-folder smaller than curcuminoids. With respect to antiproliferative activity against Hep-G2, LX-2, SMMC7221 and MDA-MB-231, the derivatives exhibited an effect stronger than curcuminoids with an IC₅₀ ranging from 0.18 to 4.25 µM.

【 授权许可】

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