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Title of Journal: Sci China Chem

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Abbravation: Science China Chemistry

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SP Science China Press

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DOI

10.1007/11833529_104

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ISSN

1869-1870

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Synthesis and biological evaluation of 8substitut

Authors: Ping Yang XiangZhen Kong ChangMei Cheng ChangYan Li XiaoMing Yang Xing’E Zhao
Publish Date: 2011/08/25
Volume: 54, Issue: 10, Pages: 1565-
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Abstract

Flavonoids are important bioactive dietary compounds which are proved to be antioxidant responsive element ARE activators to defend against electrophilic toxicants and oxidative stress The activators induce ARE gene transcription through Nrf2 factor a major transcriptional stimulator of cytoprotective genes relieved from a Keap1 complex In this report based on the structures of two flavonoids scutellarin and baicalin which are extracted from two common Chinese plants Dengzhanhua Erigeron breviscapus vant HandMazz and Huangqin Scutellaria baicalensis Georigi respectively we synthesized several 8substituted and deglucuronidated analogues and identified the ARE activation effects of these flavonoids We found that the Baicalin deglucurnonidated Baicalin and diaza cyclopenta derivative were more active Their dosedependent upregulation activities of ARE and NQO1 and induction effects of Nrf2 were testified The results presented that these three analogues had good upregulation effects on ARE and they could be potentially utilized in relieving oxidative stress upon further neuroprotective tests

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