Non-small cell lung cancer (NSCLC) accounts for 85% of lung cancer cases, and is characterized by more insensitivity to chemotherapy and poor prognosis. Epidermal growth factor receptor (EGFR) has been confirmed as a tumorigenic driving factor of NSCLC. Taspine has been proved effective in the inhibition of malignant tumours. Here, we found TPD7, a novel taspine derivative, exerted most inhibitory effect on EGFR-dependent HCC827 cells and investigated the underling mechanism. In addition, TPD7 could block cell cycle at G0/G1 phase of HCC827 cells by regulating the expression of cyclin D1 and cyclin E. Furthermore, TPD7 induced HCC827 cell apoptosis by regulating the expression of BCL-2 family proteins. Further study revealed that TPD7 could down-regulate the phosphorylation of EGFR and downstream members. TPD7 might present a potential EGFR inhibitor in the treatment of NSCLC.
Keywords: EGFR; HCC827; TPD7; cell growth; lung cancer.