Pyruvate　kinase　M2　(PKM2)　plays　a　pivotal　role　in　the　growth,　survival　and　metabolic　reprogramming　of　cancer　cells.　Here,　we　presented　for　the　first　time　that　tanshinone　IIA　inhibited　human　esophagus　cancer　cell　growth　through　miR-122-mediated　PKM2　down-regulation　pathway.　Tanshinone　IIA　inhibited　cell　proliferation　and　induced　cell　cycle　arrest　in　S　phase　in　human　Ec109　cells.　As　expected,　tanshinone　IIA　down-regulated　PKM2　mRNA　and　protein　expression　in　Ec109　cells.　Given　these　findings,　we　further　investigated　microRNAs　regulation　of　PKM2　and　confirmed　miR-122　for　targeting　PKM2.　Moreover,　we　found　that　tanshinone　IIA-induced　up-regulation　of　miR-122　expression　inhibited　PKM2　expression　in　Ec109　cells.　Meanwhile,　tanshinone　IIA　inhibited　proliferation　through　miR122-medated　PKM2　down　regulation.　It　was　demonstrated　that　the　anticancer　activity　of　tanshinone　HA　was　targeted　at　metabolic　regulation　of　miR-122/PKM2　in　human　esophagus　cancer　cells.　Taken　together,　our　results　revealed　tanshinone　HA　targeting　at　PKM2-mediated　metabolic　reprogramming　play　an　important　role　in　inhibition　of　esophageal　cancer　cell　growth.　(C)　2016　Elsevier　Inc.　All　rights　reserved.