4.6 Article

Screening active compounds acting on the epidermal growth factor receptor from Radix scutellariae via cell membrane chromatography online coupled with HPLC/MS

Journal

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Volume 62, Issue -, Pages 196-202

Publisher

ELSEVIER
DOI: 10.1016/j.jpba.2011.12.025

Keywords

Radix scutellariae; Epidermal growth factor receptor; Cell membrane chromatography; High performance liquid chromatography/mass spectrometry; Wogonin

Funding

  1. National Natural Science Foundation of China [81073038]
  2. Program for New Century Excellent Talents in University [NCET-08-0437]
  3. Fundamental Research Funds for Central Universities of China

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Radix scutellariae is a traditional Chinese medicine (TCM) and has many pharmacological effects, including antiviral, antibacterial, antifungal, antipyretic, hypotensive, anti-inflammatory and anti-anaphylaxis effects. However, few studies have screened the active compounds in this complex product for tumor therapy. In this study, a two-dimensional online method was developed to screen the active compounds from Radix scutellariae acting on the epidermal growth factor receptor. The screening results showed that wogonin from Radix scutellariae was the targeted component which acted on epidermal growth factor receptor specificity. The in vitro inhibitory activity of wogonin on the viability of cells with high epidermal growth factor receptor expression was tested using the MIT assay. In the dosage range of 0.40-50.0 mu M, inhibition of HEK293/EGFR by wogonin was 8.94 +/- 0.2, 20.64 +/- 5.10, 34.16 +/- 5.90 and 69.03 +/- 7.80 at the concentrations of 0.4 x 10(-6), 2 x 10(-6), 10 x 10(-6) and 50 x 10(-6) mol L-1, respectively. These results showed that wogonin inhibited the growth of cells with high epidermal growth factor receptor expression in a dose-dependent manner. (C) 2012 Elsevier B.V. All rights reserved.

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