中文摘要：

目的：探讨葛根素对Lewis肺癌细胞中表皮生长因子受体酪氨酸激酶（EGFR-TK）特异性抑制机理。方法：不同浓度葛根素组加入到EGFR-TK、Lewis肺癌细胞株中,利用ELISA法研究葛根素对EGFR-TK的抑制作用机理,利用MTT法测定葛根素对Lewis肺癌细胞株生长的抑制作用,利用CD光谱法监测葛根素对EGFR-TK二级结构的影响,流式细胞术检测细胞凋亡率,采用Transwell小室法检测细胞侵袭率。结果：葛根素是可逆的竞争性EGFR-TK抑制剂（半抑制率IC50和抑制常数Ki分别为4.18±0.34μg/ml和2.12±0.21μg/ml）,此外葛根素对Lewis肺癌细胞生长和侵袭具有良好的抑制能力,并能够明显的诱导Lewis肺癌细胞的凋亡;CD光谱分析表明葛根素诱导EGFR-TK的构象发生部分改变,α-螺旋含量逐渐增加,无规则卷曲逐渐减少。结论：葛根素能够特异性的抑制EGFR-TK的活性,表现出来良好的抗Lewis肺癌细胞生长、侵袭和诱导细胞凋亡的药理活性。

英文摘要：

Objective： Study the specific effect mechanism of epidermal growth factor receptor tyrosine kinase （EGFR-TK） inhibitor puerarin on Lewis cancer cell, and to establish an HPLC method for determination of erlotinib concentration in rats plasma. Methods： The inhibitory effect of puerarin on EGFR-TK was using the ELISA method, the inhibition rate of puerarin on Lewis cancer cell was using the MTr method, and CD assay was used to detect the change of secondary structure of EGFR-TK induced by puerarin. Results： Puerarin was a competitive in-hibitor （ the value of half inhibition rate （ IC50 ） and inhibition constant （Ki） was obtained to be 4.18 ± 0.34 μg/ml and 2.12 ± 0.21 μg/ml, respectively）. CD analysis showed that or-helical content increased gradually, and the conformation of EGFR-TK induced by puerarin was changed. Conclusion： Puerarin as a specific EGFR-TK inhibitor, showed a good pharmacological effects.