Anti-H1N1 virus, cytotoxic and Nrf2 activation activities of chemical constituents from Scutellaria baicalensis
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. Various column chromatography t...
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| Published in | Journal of ethnopharmacology Vol. 176; pp. 475 - 484 |
|---|---|
| Main Authors | , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Ireland
Elsevier Ireland Ltd
24.12.2015
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| Subjects | |
| Online Access | Get full text |
| ISSN | 0378-8741 1872-7573 1872-7573 |
| DOI | 10.1016/j.jep.2015.11.018 |
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| Abstract | 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.
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.
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 12.8μM, respectively, which were remarkably more potent than the positive drug Osv-P (oseltamivir phosphate, IC50 45.6μM). Most free flavones (26–28 and 30) showed significant cytotoxic activities at 10μM (up to 61.2% inhibition rate). Furthermore, 30 could activate Nrf2 transcription by 3.8-fold of the control at 10μM. UPLC analysis indicated the 12 major compounds (including the bioactive ones) accounted for 195.93±43.9mgg−1 of the herbal materials.
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.
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| AbstractList | 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.
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.
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 12.8μM, respectively, which were remarkably more potent than the positive drug Osv-P (oseltamivir phosphate, IC50 45.6μM). Most free flavones (26–28 and 30) showed significant cytotoxic activities at 10μM (up to 61.2% inhibition rate). Furthermore, 30 could activate Nrf2 transcription by 3.8-fold of the control at 10μM. UPLC analysis indicated the 12 major compounds (including the bioactive ones) accounted for 195.93±43.9mgg−1 of the herbal materials.
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.
[Display omitted] 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.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.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 12.8μM, respectively, which were remarkably more potent than the positive drug Osv-P (oseltamivir phosphate, IC50 45.6μM). Most free flavones (26–28 and 30) showed significant cytotoxic activities at 10μM (up to 61.2% inhibition rate). Furthermore, 30 could activate Nrf2 transcription by 3.8-fold of the control at 10μM. UPLC analysis indicated the 12 major compounds (including the bioactive ones) accounted for 195.93±43.9mgg⁻¹ of the herbal materials.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. 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. 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. 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 μM, respectively, which were remarkably more potent than the positive drug Osv-P (oseltamivir phosphate, IC50 45.6 μM). Most free flavones (26-28 and 30) showed significant cytotoxic activities at 10 μM (up to 61.2% inhibition rate). Furthermore, 30 could activate Nrf2 transcription by 3.8-fold of the control at 10 μM. UPLC analysis indicated the 12 major compounds (including the bioactive ones) accounted for 195.93 ± 43.9 mg g(-)(1) of the herbal materials. 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. 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.ETHNOPHARMACOLOGICAL RELEVANCEHuang-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.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.MATERIALS AND METHODSVarious 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.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 μM, respectively, which were remarkably more potent than the positive drug Osv-P (oseltamivir phosphate, IC50 45.6 μM). Most free flavones (26-28 and 30) showed significant cytotoxic activities at 10 μM (up to 61.2% inhibition rate). Furthermore, 30 could activate Nrf2 transcription by 3.8-fold of the control at 10 μM. UPLC analysis indicated the 12 major compounds (including the bioactive ones) accounted for 195.93 ± 43.9 mg g(-)(1) of the herbal materials.RESULTSA 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 μM, respectively, which were remarkably more potent than the positive drug Osv-P (oseltamivir phosphate, IC50 45.6 μM). Most free flavones (26-28 and 30) showed significant cytotoxic activities at 10 μM (up to 61.2% inhibition rate). Furthermore, 30 could activate Nrf2 transcription by 3.8-fold of the control at 10 μM. UPLC analysis indicated the 12 major compounds (including the bioactive ones) accounted for 195.93 ± 43.9 mg g(-)(1) of the herbal materials.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.CONCLUSIONThis 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. |
| Author | Li, Zi-wei Miao, Wen-juan Yu, Si-wang Ji, Shuai Si, Long-long Li, Ru Wang, Qi Qiao, Xue Zhou, De-min Ye, Min |
| Author_xml | – sequence: 1 givenname: Shuai surname: Ji fullname: Ji, Shuai – sequence: 2 givenname: Ru surname: Li fullname: Li, Ru – sequence: 3 givenname: Qi surname: Wang fullname: Wang, Qi – sequence: 4 givenname: Wen-juan surname: Miao fullname: Miao, Wen-juan – sequence: 5 givenname: Zi-wei surname: Li fullname: Li, Zi-wei – sequence: 6 givenname: Long-long surname: Si fullname: Si, Long-long – sequence: 7 givenname: Xue surname: Qiao fullname: Qiao, Xue – sequence: 8 givenname: Si-wang surname: Yu fullname: Yu, Si-wang – sequence: 9 givenname: De-min surname: Zhou fullname: Zhou, De-min email: deminzhou@bjmu.edu.cn – sequence: 10 givenname: Min surname: Ye fullname: Ye, Min email: yemin@bjmu.edu.cn |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/26578185$$D View this record in MEDLINE/PubMed |
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| Keywords | oroxylin A (PubChem CID: 5320315) Nrf2 activation baicalein (PubChem CID: 5281605) chrysin (PubChem CID: 5281607) Effective components Baicalin (PubChem CID: 64982) wogonin (PubChem CID: 5281703) Cytotoxicity Scutellaria baicalensis Anti-H1N1 virus |
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| Snippet | 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... |
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| SubjectTerms | Animals Anti-H1N1 virus antioxidant activity Antioxidants - chemistry Antioxidants - pharmacology Antiviral Agents - chemistry Antiviral Agents - pharmacology baicalin Cell Line, Tumor Cell Survival - drug effects chemical composition chrysin Cytotoxicity Dogs Effective components herbal medicines high performance liquid chromatography Humans influenza Influenza A virus Influenza A Virus, H1N1 Subtype - drug effects Influenza A Virus, H1N1 Subtype - pathogenicity inhibitory concentration 50 luciferase Madin Darby Canine Kidney Cells neoplasm cells neoplasms NF-E2-Related Factor 2 - genetics Nrf2 activation nuclear magnetic resonance spectroscopy oseltamivir Phytochemicals - isolation & purification Phytochemicals - pharmacology Plant Extracts - chemistry Plant Extracts - pharmacology quality control roots Scutellaria baicalensis Scutellaria baicalensis - chemistry spectral analysis traditional medicine viruses |
| Title | Anti-H1N1 virus, cytotoxic and Nrf2 activation activities of chemical constituents from Scutellaria baicalensis |
| URI | https://dx.doi.org/10.1016/j.jep.2015.11.018 https://www.ncbi.nlm.nih.gov/pubmed/26578185 https://www.proquest.com/docview/1749620768 https://www.proquest.com/docview/2116887798 |
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