1. Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative.
- Author
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Gu T, Zhong Y, Lu YT, Sun Y, Dong ZX, Wu WY, Shi ZH, Li NG, Xue X, Fang F, Li HM, and Tang YP
- Subjects
- Animals, Antioxidants chemical synthesis, Antioxidants chemistry, Antioxidants pharmacology, Apigenin chemical synthesis, Apigenin chemistry, Apigenin pharmacology, Biphenyl Compounds metabolism, Brain Ischemia drug therapy, Cerebrovascular Disorders drug therapy, Chromans chemistry, Chromans pharmacology, Chromans therapeutic use, Erigeron chemistry, Fibrinolytic Agents pharmacology, Fibrinolytic Agents therapeutic use, Free Radical Scavengers chemical synthesis, Free Radical Scavengers chemistry, Free Radical Scavengers pharmacology, Glucuronates chemistry, Glucuronates pharmacology, Humans, Male, Picrates metabolism, Rabbits, Solubility, Chromans chemical synthesis, Fibrinolytic Agents chemical synthesis
- Abstract
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., Competing Interests: All authors declare no financial/commercial conflict of interests.
- Published
- 2017
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