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采用细胞膜色谱在线耦联 HPLC/MS 技术筛选黄芩中作用于表皮生长因子受体的活性成分

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

机构信息

School of Medicine, Xi'an Jiaotong University, Xi'an 710061, China.

出版信息

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.

摘要

黄芩是一种中药,具有多种药理作用,包括抗病毒、抗菌、抗真菌、解热、降压、抗炎和抗过敏作用。然而,很少有研究从黄芩中筛选出用于肿瘤治疗的活性化合物。本研究采用二维在线方法筛选作用于表皮生长因子受体的黄芩中的活性化合物。筛选结果表明,黄芩中的汉黄芩素是作用于表皮生长因子受体特异性的靶向成分。采用 MTT 法测定汉黄芩素对高表皮生长因子受体表达细胞活力的体外抑制活性。在 0.40-50.0 μM 的剂量范围内,0.4×10(-6)、2×10(-6)、10×10(-6)和 50×10(-6)molL(-1)浓度的汉黄芩素对 HEK293/EGFR 的抑制率分别为 8.94±0.2、20.64±5.10、34.16±5.90和 69.03±7.80。结果表明,汉黄芩素呈剂量依赖性抑制高表皮生长因子受体表达细胞的生长。

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