This is the first report to demonstrate the anti-cancer activity of newly isolated compound acetoxy-lup-5(6), 20(29)-diene (ALUP) in reducing the proliferation and differentiation on A549 human non-small cell lung cancer cell line via inhibition of mitotic phase, increased apoptosis, overexpression of Let-7-miRNA, Bax, CASP-8, CD-95 and down expression of miRNA-21, Bcl-2, KRAS, VEGF, and cyclin D1. This evidence concerns the gene VEGFA and cancer.