Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease

被引：46

作者：

Qian, Li-Hua ^{[1
]}

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

Tang, Yu-Ping ^{[1
]}

Zhang, Li ^{[1
]}

Tang, Hao ^{[1
]}

Wang, Zhen-Jiang ^{[1
]}

Liu, Li ^{[1
]}

Song, Shu-Lin ^{[1
]}

Guo, Jian-Ming ^{[1
]}

Ding, An-Wei ^{[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：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2011年 / 12卷 / 11期

基金：

中国国家自然科学基金;

关键词：

scutellarein; scutellarin; synthesis; antioxidant activity; ischemic cerebrovascular disease; PC12; CELLS; PROTECTION; STROKE; RATS;

D O I：

10.3390/ijms12118208

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：

Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+center dot), (OH)-O-center dot free radicals and its protective effect on H2O2-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H2SO4 in 90% ethanol in N-2 atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease.

引用

页码：8208 / 8216

页数：9

共 25 条

[1]

Cao Feng, 2006, Yaoxue Xuebao, V41, P595

[2]

Che Q.-M, 2005, [No title captured], Patent No. 1683357

[3]

[车庆明 CHE Qingming], 2007, [中国药学杂志, Chinese Pharmaceutical Journal], V42, P1418

[4]

CHEN XX, 1998, J CHIN PHARM SCI, V7, P91

[5] Total synthesis of scutellarin-7-O-Glucuronide [J].

Cui, JM ;

Fang, G ;

Duan, YB ;

Liu, Q ;

Wu, LP ;

Zhang, GH ;

Wu, S .

JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH, 2005, 7 (04) :655-660

[6]

Cuzzocrea S, 2001, PHARMACOL REV, V53, P135

[7] Stroke [J].

Donnan, Geoffrey A. ;

Fisher, Marc ;

Macleod, Malcolm ;

Davis, Stephen M. .

LANCET, 2008, 371 (9624) :1612-1623

[8] SYNTHESIS OF GLUCURONIDES IN FLAVONOID SERIES .6. SYNTHESIS OF SCUTELLARIN, PLANTAGININ, SCUTELLAREIN-7-BETA-RUTINOSIDE AND FIRST PREPARATION OF ISOSCUTELLAREIN [J].

FARKAS, L ;

MEZEYVAN.G ;

NOGRADI, M .

CHEMISCHE BERICHTE-RECUEIL, 1974, 107 (12) :3878-3882

[9] Antioxidant actions of flavonoids: Thermodynamic and kinetic analysis [J].

Galleano, Monica ;

Verstraeten, Sandra V. ;

Oteiza, Patricia I. ;

Fraga, Cesar G. .

ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 2010, 501 (01) :23-30

[10]

[葛庆华 Ge Qinghua], 2003, [中国医药工业杂志, Chinese Journal of Pharmaceuticals], V34, P618

← 1 2 3 →