中国中药杂志

2021, v.46(20) 5362-5371

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金花茶有效部位抑制表皮生长因子受体(EGFR)抗非小细胞肺癌的作用机制研究
Active fractions of Camellia nitidissima inhibit non-small cell lung cancer via suppressing epidermal growth factor receptor

王梓灵;郭瑜婕;朱芸芸;陈乐;吴婷;刘大会;黄必胜;杜鸿志;
WANG Zi-ling;GUO Yu-jie;ZHU Yun-yun;CHEN Le;WU Ting;LIU Da-hui;HUANG Bi-sheng;DU Hong-zhi;Traditional Chinese Medicine Resource Center, Hubei University of Chinese Medicine;Hubei Provincial Key Laboratory of Traditional Chinese Medicine Resource and Traditional Chinese Medicine Chemistry, Hubei University of Chinese Medicine;

摘要(Abstract):

探究金花茶4个有效部位(金花茶叶总皂苷、金花茶叶总多酚、金花茶花总皂苷、金花茶花总多酚)抑制表皮生长因子受体(epidermal growth factor receptor, EGFR)抗非细小细胞肺癌细胞增殖和迁移作用及其分子作用机制。采用MTT实验检测金花茶4个有效部位对非小细胞肺癌NCI-H1975与HCC827细胞活力的影响;通过细胞划痕实验与Transwell小室迁移实验考察金花茶4个有效部位给药后对非小细胞肺癌细胞迁移能力的影响;基于酶活检测,测定金花茶4个有效部位对EGFR酶活性的影响;采用药物分子对接实验,探究金花茶有效部位代表性成分与EGFR蛋白的直接作用能力与作用位点;利用Wes-tern blot检测金花茶4个有效部位对EGFR下游信号通路相关蛋白的表达水平的影响。结果发现金花茶4个有效部位在50、100、150、200μg·mL~(-1)均能显著性抑制人非小细胞肺癌NCI-H1975与HCC827细胞的活力并呈时间与浓度依赖性;划痕实验与Transwell小室迁移实验显示金花茶4个有效部位作用于NCI-H1975与HCC827细胞均能显著性抑制非小细胞肺癌细胞的迁移能力;蛋白激酶活力测定实验结果表明,EGFR的酶活被金花茶4个有效部位显著性抑制;分子对接实验结果证实,金花茶4个有效部位化合物中多种药效成分与EGFR酶有较强的结合作用;Western blot实验结果确证,金花茶4个有效部位能下调非小细胞肺癌细胞EGFR及其下游信号通路蛋白表达水平。结果表明,金花茶4个有效部位均能抑制非小细胞肺癌,且其作用机制可能与EGFR及其下游信号通路相关。该研究为金花茶有效成分治疗非小细胞肺癌提供科学依据,对金花茶抗肿瘤作用机制的深入研究具有一定的参考意义。
The present study explored the effects and its underlying mechanisms of four active fractions of Camellia nitidissima(leaf polyphenols, leaf saponins, flower polyphenols, and flower saponins in C. nitidissima) in inhibiting the proliferation and migration of non-small cell lung cancer(NSCLC) by suppressing the epidermal growth factor receptor(EGFR). MTT assay was used to detect the effect of four active fractions on the proliferation of NCI-H1975 and HCC827 cells. Wound healing assay and Transwell assay were adopted to evaluate the effect of four active fractions on the migration of NSCLC. The effect of four active fractions on the enzyme activity of EGFR was detected. Molecular docking was carried out to explore the direct action capacity and action sites between representative components of the four active fractions and EGPR. Western blot assay was employed to investigate the effect of four active fractions on the protein expression in EGFR downstream signaling pathways. The results of the MTT assay indicated that the cell viability of NCI-H1975 and HCC827 cells was significantly inhibited by four active fractions at 50, 100, 150, and 200 μg·mL~(-1) in a dose-dependent manner. Wound healing assay and Transwell assay revealed that the migration of NCI-H1975 and HCC827 cells was significantly suppressed by four active fractions. In addition, the results of the protein activity assay showed that the enzyme activity of EGFR was significantly inhibited by four active fractions. The molecular docking results confirmed that various components in four active fractions possessed strong binding activity to EGFR enzymes. Western blot assay revealed that four active fractions down-regulated the protein expression of EGFR and its downstream signaling pathways. It is concluded that the four active fractions of C. nitidissima can inhibit NSCLC. The mechanism may be related to EGFR and its downstream signaling pathways. This study provides a new scientific basis for the clinical treatment of NSCLC with active fractions of C. nitidissima, which is of reference significance for further research on the anti-tumor mechanism of C. nitidissima.

关键词(KeyWords): 金花茶;人非小细胞肺癌;增殖;迁移;EGFR通路
Camellia nitidissima;human non-small cell lung cancer;proliferation;migration;epidermal growth factor receptor pathway

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金项目(81903845)

作者(Author): 王梓灵;郭瑜婕;朱芸芸;陈乐;吴婷;刘大会;黄必胜;杜鸿志;
WANG Zi-ling;GUO Yu-jie;ZHU Yun-yun;CHEN Le;WU Ting;LIU Da-hui;HUANG Bi-sheng;DU Hong-zhi;Traditional Chinese Medicine Resource Center, Hubei University of Chinese Medicine;Hubei Provincial Key Laboratory of Traditional Chinese Medicine Resource and Traditional Chinese Medicine Chemistry, Hubei University of Chinese Medicine;

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