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

J Pharm Biomed Anal. 2012 Mar 25:62:196-202. doi: 10.1016/j.jpba.2011.12.025. Epub 2011 Dec 30.

Abstract

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 MTT assay. In the dosage range of 0.40-50.0 μM, 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 × 10(-6), 2 × 10(-6), 10 × 10(-6) and 50 × 10(-6) molL(-1), respectively. These results showed that wogonin inhibited the growth of cells with high epidermal growth factor receptor expression in a dose-dependent manner.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Chromatography, High Pressure Liquid / methods*
  • Dose-Response Relationship, Drug
  • ErbB Receptors / drug effects*
  • Humans
  • Mass Spectrometry / methods*
  • Plant Extracts / pharmacology*
  • Reference Standards
  • Scutellaria baicalensis / chemistry*

Substances

  • Plant Extracts
  • ErbB Receptors