Baicalin and its aglycon, baicalein, are flavonoids present from Scutellaria baicalensis Georgi. Baicalin generally inhibits tumor cells by inducing apoptosis and arresting growth, while baicalein suppresses by regulating autophagy. Certain signaling pathways and regulating factors are involved among the induced-apoptosis and autophagy progress. In suppressing growth, baicalin and baicaein inhibit angiogenesis or induce cell cycle arrest at S phase against proliferation, migration and differentiation. The present agents against tumor still have related side effects. Therefore, the natural and nontoxic flavonoids are promising in present even future tumor treatment.