Alpinetin is a phytochemical isolated from a variety of plants including those of the genus Alpinia. It is going through tests to see if it is a vasorelaxant. Alpinetin is a type of novel plant flavonoid derived from Alpinia katsumadai Hayata, found to possess strong anti-hepatoma effects. Alpinetin suppressed HepG2 cell proliferation and arrested cells in the G0/G1 phase by up-regulating the expression levels of p-MKK7. On the contrary, inhibiting the expression of MKK7 reversed the antitumor effect of alpinetin. Moreover, alpinetin enhanced the sensitivity of HepG2 hepatoma cells to the chemotherapeutic agent CDDP. Activation of MKK7 mediates the anti-hepatoma effect of alpinetin. MKK7 may be a putative target for molecular therapy against hepatoma and alpinetin could serve as a potential agent for the development of hepatoma therapy.