Synthesis of scutellarein derivatives to increase biological activity and water solubility

被引：18

作者：

Shi, Zhi-Hao ^{[1
,2
,3
]}

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

Shi, Qian-Ping ^{[1
,2
]}

Zhang, Wei ^{[1
,2
]}

Dong, Ze-Xi ^{[1
,2
]}

Tang, Yu-Ping ^{[1
,2
]}

Zhang, Peng-Xuan ^{[1
,2
]}

Gu, Ting ^{[1
,2
]}

Wu, Wen-Yu ^{[1
,2
]}

Fang, Fang ^{[1
,2
]}

Xin-Xue ^{[1
,2
]}

Li, He-Min ^{[1
,2
]}

Yang, Jian-Ping ^{[1
,2
]}

Duan, Jin-Ao ^{[1
,2
]}

机构：

[1] Nanjing Univ Chinese Med, Jiangsu Collaborat Innovat Ctr Chinese Med Resour, Jiangsu Key Lab High Technol Res TCM Formulae, Nanjing 210023, Jiangsu, Peoples R China

[2] Nanjing Univ Chinese Med, Local Collaborat Engn Ctr Chinese Med Resources, Nanjing 210023, Jiangsu, Peoples R China

[3] China Pharmaceut Univ, Dept Organ Chem, Nanjing 211198, Jiangsu, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 21期

基金：

中国国家自然科学基金;

关键词：

Scutellarin; Scutellarein; Thrombin; Antioxidant; Solubility; METABOLIC MECHANISM; THROMBIN-INHIBITORS; NITRIC-OXIDE; DESIGN; ISCHEMIA/REPERFUSION; QUERCETIN; THERAPY; DISEASE; ANALOGS; STROKE;

D O I：

10.1016/j.bmc.2015.09.047

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In order to improve the biological activity and water solubility of scutellarin (1), some derivatives of its main metabolite (scutellarein) were designed and synthesized. All the compounds were tested for their thrombin inhibition activity through the analyzation of thrombin time (TT), activated partial thromboplastin time (APTT), prothrombin time (PT) and fibrinogen (FIB). Their antioxidant activities were assessed by measuring their scavenging capacities toward 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and the ability to protect PC12 cells against H2O2-induced cytotoxicity, their water solubility were also assessed by ultraviolet (UV) spectrophotometer. The results showed that compound 8b demonstrated stronger anticoagulant and antioxidant activity, better water solubility compared with scutellarein (2), which warrants it as a promising agent for the treatment of ischemic cerebrovascular disease. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：6875 / 6884

页数：10

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