Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimer's Disease Candidates Based on Metabolic Mechanism

被引：15

作者：

Song, Shu-Lin ^{[1
]}

Li, Nian-Guang ^{[1
,2
]}

Tang, Yu-Ping ^{[1
]}

Wang, Zhen-Jiang ^{[1
]}

Qian, Li-Hua ^{[1
]}

Tang, Hao ^{[1
]}

Duan, Jin-Ao ^{[1
]}

机构：

[1] Nanjing Univ Chinese Med, Jiangsu Key Lab High Technol Res TCM Formulae, Nanjing 210046, Jiangsu, Peoples R China

[2] Nanjing Univ Chinese Med, Dept Med Chem, Nanjing 210046, Jiangsu, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2012年 / 9卷 / 01期

基金：

中国国家自然科学基金; 高等学校博士学科点专项科研基金;

关键词：

Alzheimer's disease; Antioxidant; Derivative; Metabolism; Scutellarein; Scutellarin; Synthesize; CEREBRAL-ISCHEMIA; TACRINE; MELATONIN; HYBRIDS; RATS;

D O I：

10.2174/157018012798192946

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：78 / 83

页数：6

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