Zhai Peng, Xia Chun-Li, Tan Jia-Heng, Li Ding, Ou Tian-Miao, Huang Shi-Liang, Gu Lian-Quan, Huang Zhi-Shu
Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.
Curr Alzheimer Res. 2015;12(5):403-14. doi: 10.2174/1567205012666150504151120.
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).
合成了一系列新型不对称姜黄素类似物，并将其作为治疗阿尔茨海默病的潜在多功能药物进行评估。我们的结果表明，通过氧自由基吸收能力（ORAC）研究，与姜黄素相比，这些合成化合物中的大多数对Aβ聚集具有更好的抑制特性，与参比化合物Trolox相比具有更好的抗氧化特性。一些化合物在选择性螯合铜和铁等金属离子方面表现出良好的特性。此外，发现一些化合物能够解离已经聚集的Aβ蛋白。研究了这些合成化合物的构效关系（SAR）。目前的研究表明，我们合成的不对称姜黄素衍生物可能是治疗阿尔茨海默病（AD）的潜在多功能药物。
