Abstract: To investigate the anti-cancer and anti-inflammatory activities of volatile components in Pu-erh tea from Yunnan Daye variety, crude aroma was extracted by simultaneous distillation-extraction (SDE), and further isolated using chemical method and thin layer chromatography method (TLC), and gas chromatography-mass spectrometry (GC-MS) was applied to analyze aroma components. The CD values of the double-induced quinone reductase activity induced by murine hepatoma cell (Hepa1c1c7) and the IC₅₀ values of the inhibitory rate of nitric oxide (NO) by lipopolysaccharide (LPS) -stimulated mouse macrophage (RAW264.7) cell were used to evaluate and screen the anti-cancer and anti-inflammatory components. Results showed that, in the volatile components of Pu-erh tea, the crude aroma, neutral component, F6, and F6-2 exhibited strong QR inducing activities, and their CD values were 28.07, 45.31, 12.8 and 15.12 μg/mL, respectively. Furthermore, the crude aroma and neutral component possessed strong NO inhibitory activities, and the IC₅₀ values were 51.68 and 73.32 μg/mL, respectively. Additionally, among the main monomers, β-ionone, 1, 2, 3-trimethoxybenzene, 1, 2, 4-trimethoxybenzene, and 1, 2-dimethoxybenzene possessed anti-cancer activities and anti-inflammatory activities in the concentration range of 12.5~800.0 μg/mL, meanwhile. However, 2-pentadecanone, phytol, and α-terpineol displayed anti-cancer activities in the concentration range of 200~800 μg/mL. The above results showed that the volatile components of Pu-erh tea had anticancer and anti-inflammatory activities, and β-ionone and methoxybenzene components were their active components.