Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative

• Main Authors: Ting Gu, Yue Zhong, Yu-Ting Lu, Ying Sun, Ze-Xi Dong, Wen-Yu Wu, Zhi-Hao Shi, Nian-Guang Li, Xin Xue, Fang Fang, He-Min Li, Yu-Ping Tang
• Format: Article
• Language: English
• Published: MDPI AG 2017-06-01
• Series: Molecules
• Subjects: scutellarin; scutellarein; sulfonated derivative; solubility; antioxidant; antithrombic
• Online Access: http://www.mdpi.com/1420-3049/22/6/1028

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.