This study was designed to determine optimal extraction conditions of Chrysanthemum zawadskii (CZ) with high yield of bioactive compounds (linarin, polyphenols, and flavonoids) and improved in vitro activities. Ethanol extracts were examined at different concentrations (0, 30, 50, 70, and 95%) and temperatures (50 and 70°C). The recommended extraction conditions were 50% ethanol at 70°C for 4 h, which gave the highest yield of linarin, polyphenols, and flavonoids. This extract appeared to have the greatest ABTS and DPPH radical scavenging activities (87.81% and 51.42% at 500 μg/mL, respectively) and α-glucosidase (74.59%) and pancreatic lipase inhibitory activities (90.44%). As contents of linarin increased, antioxidative activity, inhibitory effects of carbohydrates and lipid absorption of CZ extracts increased as well. From these results, CZ extracts can be used in functional food industries.