Synthesis and evaluation of multifunctional ferulic and caffeic acid dimers for Alzheimer’s disease
Xi-xin He, Xiao-hong Yang, Rui-ying Ou, Ying Ouyang, Sheng-nan Wang, Zi-Wei Chen, Shijun Wen, Rongbiao Pi · Natural Product Research · 2016
Xi-xin Hea*†, Xiao-hong Yangbc†, Rui-ying Oua, Ying Ouyangd, Sheng-nan Wangbc, Zi-wei Chenbc, Shi-jun Wenbc & Rong-biao Pibc*a College of Chinese Materia Media, Guangzhou University of Chinese Medicine, Guangzhou, Chinab Department of Pharmacology, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, Chinac International Joint Laboratory (SYSU-PolyU HK) of Novel Anti-dementia Drugs of Guangdong, Guangzhou, Chinad Department of Pediatrics, Sun Yat-Sen Memorial Hospital, Sun Yat-Sen University, Guangzhou, China† The first two authors contributed equally to this work.* Corresponding authors. Email: [email protected]** Email: [email protected] this study, a series of novel ferulic and caffeic acid dimers was designed and synthesised, and their multifunctional properties against Alzheimer’s disease (AD) were evaluated. Results showed that our multifunctional strategy was great supported by enhancing the inhibition of Aβ1–42 self-induced aggregation. Moreover, 7b also had potent protective effects against glutamate-induced cell death without significant cell toxicity in mouse hippocampal neuronal HT22 cells and 10c effectively scavenged diphenylpicrylhydrazyl free radicals. Collectively, these data strongly encourage further optimisation of 7b as a new hit to develop multifunctional agents for the treatment of AD.