Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimer's Disease Candidates Based on Metabolic Mechanism
Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimer's Disease Candidates Based on Metabolic Mechanism
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DOI：
10.2174/157018012798192946
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发表时间：
2012-01-01
影响因子：
1
通讯作者：
Duan, Jin-Ao
中科院分区：
文献类型：
--
作者：
Song, Shu-Lin;Li, Nian-Guang;Duan, Jin-Ao
为了提高野黄芩苷的代谢稳定性和生物利用度，设计合成了其主要代谢产物野黄芩苷元的衍生物。通过测定目标产物清除DPPH自由基的能力和对H2O2诱导的PC12细胞毒性的保护作用来评价目标产物的抗氧化活性。结果表明，目标化合物7g的抗氧化活性高于野黄芩苷。因此，7g可能被认为是一种新的有效的抗阿尔茨海默病的候选药物。
In order to improve the metabolic stability and bioavailability of scutellarin, some derivatives of its main metabolite (scutellarein) were designed and synthesized. The antioxidant activities of these target products were assessed by measuring its scavenging capacities toward DPPH and the protective effects on H2O2-induced cytotoxicity in PC12 cells. The results showed that the target compound 7g had a higher antioxidant activity than scutellarin. Thus 7g may be considered as a novel potent anti-Alzheimer's Disease drug candidate.