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Tanshinone I (T1) and tanshinone II (T2) are the major diterpenes isolated from Danshen (Salvia miltiorrhiza Bunge). Three human lung adenocarcinoma cell lines, A549, CL1‐0, and CL1‐5, were treated with T1 and T2 for the in vitro antitumor test. Results showed that T1 was more effective than T2 in inhibiting the growth of lung cancer cells via suppressing the expression of VEGF, Cyclin A, and Cyclin B proteins in a dose‐dependent manner. Moreover, a transgenic mice model of the human vascular endothelial growth factor‐A₁₆₅ (hVEGF‐A₁₆₅) gene‐induced pulmonary tumor was further treated with T1 for the in vivo lung cancer therapy test. T1 significantly attenuated hVEGF‐A₁₆₅ overexpression to normal levels of the transgenic mice (Tg) that were pretreated with human monocytic leukemia THP‐1 cell‐derived conditioned medium (CM). It also suppressed the formation of lung adenocarcinoma tumors (16.7 …