This study selected the optimal conditions for enzyme treatment that can promote the extraction of functional components from Salvia plebeia (SP) and confirmed solubilization characteristics, functional component contents, and applicability evaluation in pilot-scale, antioxidative, and anti-inflammatory activity. The optimal conditions of pectinase, 1%, and 2 h (P) were determined through the enzyme treatment of SP. The water-soluble index and total polyphenol content were the highest in P compared to 100oC reflux condition for 2 h (CON). Component analysis performed using liquid chromatography-mass spectrometry revealed that flavonoid contents were increased 6.6-9.5 times in the P compared to CON. There was no difference in component content when comparing the measurement lab-scale and pilot scale. CON and P indicated cytoprotective effect against H2O2-induced RAW 264.7 cells. CON and P pre-treatment also reduced the production of nitric oxide and proinflammatory cytokines in LPS-induced RAW 264.7 cells. Furthermore, P showed higher antioxidant and anti-inflammation activities than CON. These results suggested that P has a higher concentration of bioactive compounds through enzyme treatment than that obtained from CON. Thus, it can be used as a primary material for industrial utilization, such as developing functional food materials using SP.