Abstract: OBJECTIVE This research intended to isolate and compare the antibacterial and antioxidant activities of Lo Han Kuo plant (Siraitia grosvenori Swingle) by extracting and purifying bioactive substances from the leaf/vine of Lo Han Kuo plant in large-scale purification. METHODS Extracts were prepared from Lo Han Kuo leaf/vine, and the extracts were further purified by large-scale amberlite column. The antibacterial, antioxidant, and insulin-stimulating activities of these extracts were tested and compared. RESULTS The Lo Han Kuo leaf/vine parts exhibited antibacterial, antioxidant, and insulin-stimulating activities. To further isolate the bioactive fractions, the extracts were purified with amberlite chromatography and the purified fractions were tested again for the bioactivities. These bioactive fractions are located in different amberlite fractions. CONCLUSION The experimental data demonstrated that extracts of Lo Han Kuo leaves and vines exhibited antibacterial, antioxidant and insulin-stimulating activities. Lo Han Kuo leaf/vine appears to have the potential to be used for pharmaceutical preparations and dietary supplements to treat various human ailments.