In the present study, we investigated the potential anti-angiogenic mechanism and anti-tumour activity of β-eudesmol using in vitro and in vivo experimental models. Proliferation of human umbilical vein endothelial cells (HUVEC) stimulated with vascular endothelial growth factor (VEGF, 30 ng/ml) and basic fibroblast growth factor (bFGF, 30 ng/ml) was significantly inhibited by β-eudesmol (50-100 μM). β-Eudesmol (100 μM) also blocked the phosphorylation of cAMP response element binding protein (CREB) induced by VEGF (30 ng/ml) in HUVEC. β-Eudesmol (10-100 μM) inhibited proliferation of HeLa, SGC-7901, and BEL-7402 tumour cells in a time- and dose-dependent manner. Moreover, β-eudesmol treatment (2.5-5 mg/kg) significantly inhibited growth of H22 and S180 mouse tumour in vivo. These results indicated that β-eudesmol inhibited angiogenesis by suppressing CREB activation in growth factor signalling pathway. This is the first study to demonstrate that β-eudesmol is an inhibitor of tumour growth.