Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative

被引：6
作者：
Gu, Ting [1 ,2 ]
Zhong, Yue [1 ,2 ]
Lu, Yu-Ting [1 ,2 ]
Sun, Ying [1 ,2 ]
Dong, Ze-Xi [1 ,2 ]
Wu, Wen-Yu [1 ,2 ]
Shi, Zhi-Hao [3 ]
Li, Nian-Guang [1 ,2 ]
Xue, Xin [1 ,2 ]
Fang, Fang [1 ,2 ]
Li, He-Min [1 ,2 ]
Tang, Yu-Ping [1 ]
机构：
[1] Nanjing Univ Chinese Med, Natl & Local Collaborat Engn Ctr Chinese Med Reso, Nanjing 210023, Jiangsu, Peoples R China
[2] Nanjing Univ Chinese Med, Dept Med Chem, Nanjing 210023, Jiangsu, Peoples R China
[3] China Pharmaceut Univ, Dept Organ Chem, Nanjing 211198, Jiangsu, Peoples R China
来源：
MOLECULES | 2017年 / 22卷 / 06期
基金：
中国国家自然科学基金;
关键词：
scutellarin; scutellarein; sulfonated derivative; solubility; antioxidant; antithrombic; ORAL BIOAVAILABILITY; BIOLOGICAL-ACTIVITY; QUERCETIN; METABOLISM; MECHANISM; EXTRACT; DESIGN; STROKE;
D O I：
10.3390/molecules22061028
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：
Scutellarin (1) has been widely used to treat acute cerebral infarction in clinic, but poor aqueous solubility decreases its bioavailability. Interestingly, scutellarin (1) could be metabolized into scutellarein (2) in vivo. In this study, a sulfonic group was introduced at position C-8 of scutellarein (2) to enhance the aqueous solubility of the obtained derivative (3). DPPH (1,1-diphenyl-2-picrylhydrazyl)-radical scavenging ability and antithrombic activity were also conducted to determine its bioactivity. The result showed that scutellarein derivate (3) could be a better agent for ischemic cerebrovascular disease treatment.
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页数：8
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