This study investigates the industrial potential of Dendranthema zawadskii (DZ) by fractionating it to enhance material efficiency and economic feasibility. Evaluating functional substances and biological activities, we found that the butanol (Bu) and ethyl acetate (EtOAc) fractions exhibited significantly higher linarin contents, 77.360 mg/g and 70.603 mg/g, respectively—approximately 3.4 times greater than the methanol extract. In the EtOAc fraction, luteolin content (52.135 mg/g) and 3,5-DCQA content (184.704 mg/g) were 6.4 and 9.7 times higher than in the methanol extract, respectively. Cell viability for HaCaT cells (≤ 200 μg/mL) and B16F10 cells (≤ 25 μg/mL) was consistently 80% or higher, indicating negligible toxicity, except for hexane (He) and chloroform (Ch) fractions. The EtOAc fraction demonstrated the highest total polyphenol content (370.50 mg/g) and total flavonoid content (947.47 mg/g), significantly surpassing other fractions. Importantly, at 25 μg/mL, the EtOAc fraction exhibited antioxidant activity (92.47%), comparable to the control, while He and Bu fractions showed high antioxidant activity (> 90%) at 100 μg/mL. Furthermore, the EtOAc fraction displayed the highest tyrosinase inhibitory activity (33.33%) and reduced melanin formation by 37.12% compared to the α-MSH treatment group. Antibacterial activities of 100 mg/mL He, Ch, and EtOAc fractions against Staphylococcus aureus exceeded the positive control, and their activity against Pseudomonas aeruginosa surpassed the positive control for all fractions. The Ch fraction demonstrated superior activity against Candida albicans . In conclusion, the EtOAc fraction of DZ emerges as a promising industrial material, offering safety, high functionality, and remarkable polyphenol and flavonoid contents, making it versatile for applications in cosmetics, functional foods, and pharmaceuticals.