Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative.

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.