摘要
合成和评估一系列新的不对称姜黄素类似物作为治疗阿尔茨海默氏病的潜在性多功能因子。我们的研究结果显示,大多数的这些合成化合物比姜黄素有更好的抑制β-淀粉样蛋白聚合物的性能, 氧自由基吸收能力的研究(ORAC)也显示其具有较参照物抗氧化剂更好的抗氧化性能。一些化合物如铜和铁表现出良好的选择性螯合金属离子的性能。此外, 我们发现一些化合物能够分离已聚合的淀粉样β-蛋白。人们对这些合成化合物的构效关系(SAR)进行了研究。目前的调查研究表明,我们合成的不对称姜黄素衍生品可能成为治疗阿尔茨海默病(AD)的潜在性多功能制剂。
关键词: β-淀粉样蛋白聚合物;防治阿尔茨海默氏病制剂;姜黄素类似物;金属离子螯合;多功能缓蚀剂
Current Alzheimer Research
Title:Syntheses and Evaluation of Asymmetric Curcumin Analogues as Potential Multifunctional Agents for the Treatment of Alzheimer’s Disease
Volume: 12 Issue: 5
Author(s): Peng Zhai, Chun-Li Xia, Jia-Heng Tan, Ding Li, Tian-Miao Ou, Shi-Liang Huang, Lian-Quan Gu and Zhi-Shu Huang
Affiliation:
关键词: β-淀粉样蛋白聚合物;防治阿尔茨海默氏病制剂;姜黄素类似物;金属离子螯合;多功能缓蚀剂
摘要: 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).
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Peng Zhai, Chun-Li Xia, Jia-Heng Tan, Ding Li, Tian-Miao Ou, Shi-Liang Huang, Lian-Quan Gu and Zhi-Shu Huang , Syntheses and Evaluation of Asymmetric Curcumin Analogues as Potential Multifunctional Agents for the Treatment of Alzheimer’s Disease, Current Alzheimer Research 2015; 12 (5) . https://dx.doi.org/10.2174/1567205012666150504151120
DOI https://dx.doi.org/10.2174/1567205012666150504151120 |
Print ISSN 1567-2050 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5828 |
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Neuroinflammation is an invariable hallmark of chronic and acute neurodegenerative disorders and has long been considered a potential drug target for Alzheimer?s disease (AD) and dementia. Significant evidence of inflammatory processes as a feature of AD is provided by the presence of inflammatory markers in plasma, CSF and postmortem brain ...read more
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