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Anti-H1N1 virus, cytotoxic and Nrf2 activation activities of chemical constituents from Scutellaria baicalensis
Ji, Shuai; Li, Ru; Wang, Qi; Miao, Wen-juan; Li, Zi-wei; Si, Long-long; Qiao, Xue; Yu, Si-wang; Zhou, De-min; Ye, Min
关键词Scutellaria Baicalensis Effective Components Anti-h1n1 Virus Cytotoxicity Nrf2 Activation
刊名JOURNAL OF ETHNOPHARMACOLOGY
2015-12-24
DOI10.1016/j.jep.2015.11.018
176页:475-484
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Plant Sciences ; Chemistry, Medicinal ; Integrative & Complementary Medicine ; Pharmacology & Pharmacy
研究领域[WOS]Plant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
关键词[WOS]C-GLYCOSIDES ; FLAVONOIDS ; BAICALIN ; ROOTS ; ANTIOXIDANT ; INFECTION ; GEORGI ; CELLS
英文摘要

Ethnopharmacological relevance: Huang-Qin, derived from the roots of Scutellaria baicalensis Georgi, is a popular Chinese herbal medicine mainly used to treat influenza and cancer. This study aims to elucidate the anti-influenza, anti-cancer and anti-oxidation effective components of S. baicalensis.

Materials and methods: Various column chromatography techniques and semi-preparative HPLC were used to isolate Scutellaria compounds, and their structures were identified by HRESIMS and NMR spectroscopic analysis. The pure compounds were evaluated for anti-influenza activities against A/WSN/33 (H1N1) virus in MDCK cells, cytotoxic activities against HepG2, SW480 and MCF7 human cancer cells by MTS assay, and antioxidant activities by Nrf2 luciferase reporter assay. In addition, the contents of 12 major compounds in 27 batches of S. baicalensis were simultaneously determined by a fully validated UPLC/UV method.

Results: A total of thirty compounds (1-30), including four new ones (3, 7, 11 and 23), were isolated from S. baicalensis. Baicalin (15), baicalein (26), wogonin (27), chrysin (28) and oroxylin A (30) showed potent anti-H1N1 activities, with IC50 values of 7.4, 7.5, 2.1, 7.7 and 12.8 mu M, respectively, which were remarkably more potent than the positive drug Osv-P (oseltamivir phosphate, IC50 45.6 mu M). Most free flavones (26-28 and 30) showed significant cytotoxic activities at 10 mu M (up to 61.2% inhibition rate). Furthermore, 30 could activate Nrf2 transcription by 3.8-fold of the control at 10 mu M. UPLC analysis indicated the 12 major compounds (including the bioactive ones) accounted for 195.93 +/- 43.9 mg g(-1) of the herbal materials.

Conclusion: This study demonstrated that free flavones showed potent anti-influenza, anti-cancer and anti-oxidative activities. They are important effective components of S. baicalensis, and can be used as chemical markers for quality control of this herbal medicine. (C) 2015 Elsevier Ireland Ltd. All rights reserved.

语种英语
WOS记录号WOS:000367106600044
项目编号81222054 ; 81470172 ; NCET-11-0019 ; 2014ZX09304307-001-011
资助机构National Natural Science Foundation of China ; Program for New Century Excellent Talents in University from Chinese Ministry of Education ; National Science and Technology Mega Project for Primary Drug Innovation of China
引用统计
被引频次:18[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/50193
专题北京大学药学院
北京大学药学院_化学生物学系
北京大学药学院_天然药物学系
北京大学药学院_药学院
北京大学公共卫生学院_公共卫生学院
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Ji, Shuai,Li, Ru,Wang, Qi,et al. Anti-H1N1 virus, cytotoxic and Nrf2 activation activities of chemical constituents from Scutellaria baicalensis[J]. JOURNAL OF ETHNOPHARMACOLOGY,2015,176:475-484.
APA Ji, Shuai.,Li, Ru.,Wang, Qi.,Miao, Wen-juan.,Li, Zi-wei.,...&Ye, Min.(2015).Anti-H1N1 virus, cytotoxic and Nrf2 activation activities of chemical constituents from Scutellaria baicalensis.JOURNAL OF ETHNOPHARMACOLOGY,176,475-484.
MLA Ji, Shuai,et al."Anti-H1N1 virus, cytotoxic and Nrf2 activation activities of chemical constituents from Scutellaria baicalensis".JOURNAL OF ETHNOPHARMACOLOGY 176(2015):475-484.
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