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Molecules 2017, 22(6), 1028; doi:10.3390/molecules22061028

Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative

1
National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China
2
Department of Medicinal Chemistry, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China
3
Department of Organic Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 211198, China
*
Authors to whom correspondence should be addressed.
Received: 27 May 2017 / Revised: 20 June 2017 / Accepted: 20 June 2017 / Published: 21 June 2017
(This article belongs to the Special Issue Synthesis and Modification of Natural Product)
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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. View Full-Text
Keywords: scutellarin; scutellarein; sulfonated derivative; solubility; antioxidant; antithrombic scutellarin; scutellarein; sulfonated derivative; solubility; antioxidant; antithrombic
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Gu, T.; Zhong, Y.; Lu, Y.-T.; Sun, Y.; Dong, Z.-X.; Wu, W.-Y.; Shi, Z.-H.; Li, N.-G.; Xue, X.; Fang, F.; Li, H.-M.; Tang, Y.-P. Synthesis and Bioactivity Characterization of Scutellarein Sulfonated Derivative. Molecules 2017, 22, 1028.

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