Peng Zhai, Chun-Li Xia, Jia-Heng Tan, Ding Li, Tian-Miao Ou, Shi-Liang Huang, Lian-Quan Gu and Zhi-Shu Huang Pages 403 - 414 ( 12 )
A series of new asymmetric curcumin analogues were synthesized and evaluated as potential multifunctional agents for the treatment of Alzheimer’s disease. Our results showed that most of these synthetic compounds had better inhibitory properties against Aβ aggregation compared with curcumin, and better anti-oxidative properties compared with the reference compound Trolox through the study of oxygen radical absorbance capacity (ORAC). Some compounds showed good properties in selectively chelating metal ions such as copper and iron. Besides, some compounds were found to be able to dissociate Aβ protein which had already aggregated. The structure-activity relationships (SAR) of these synthetic compounds were studied. The present investigation indicated that our synthetic asymmetric curcumin derivatives could be potential multifunctional agents for the treatment of Alzheimer’s disease (AD).
Amyloid-beta aggregation, anti-Alzheimer’s agent, curcumin analogues, metal chelation, multifunctional inhibitor.
Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People’s Republic of China.