In the present study, the substance that show anti-proliferation of cancer cells as well as anti-oxidant and anti-inflammatory effect was searched. As a results, the methanol extract of Pogostemon cablin (P. cablin), is a well-known herb for traditional medicine in Korea and China for treating the digestive disorders, less of appetite, vomiting and diarrhea, inhibited the growth of various cancer cells such as A549, HepG2, MCF7 and HT29 cells. Cytotoxic effect of methanol extraction of P. cablin was excellent in A549 cells. P. cablin extract induced cell cycle arrest at G1 phase of A549 in a dose dependent manner. And it induced phosphorylation of p38 and Cdc25A and reduced expression of Cdc25A, Cdks, Cyclins and phospho-Retinoblastoma (Rb) proteins. Therefore, P. cablin extract seems to act through the p38 -Cdc25A -Cdk -Cyclin -Rb pathway in A549 cells. In addition, P. cablin extract showed anti-oxidant effect by DPPH free radical scavenging assay and anti-inflammation effect by inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) in RAW 264.7 cells in a dose-dependent manner. Taken together, these results suggest that P. cablin may be used as not only candidate materials for anti-cancer, anti-inflammatory and anti-oxidant, moreover, it would be possible utilized in various health functional food materials.