In the frame of this paper, the enzyme-assisted hydrolysis coupled with ultrasound and Soxhlet extraction was applied in order to get extracts of chamomile ligulate flowers (CLF). Obtained extracts were characterized in terms to their apigenin and apigenin glucoside composition, as well as antiproliferative potential against tumour cells. Antioxidant activity was determined by two different assays based on different mechanisms showing that autofermented extracts have higher reduction potential. Autofermented extracts prepared by ultrasound and Soxhlet extraction had a stronger impact on the treated carcinoma (HeLa and NCI-H358) and leukemia (K562) cells' growth reduction in comparison to the native extracts, 30-35% greater inhibition at the lowest concentration (0.01 mg/mL), in two observed time points (48 and 72 h). Leukemia cells are more sensitive to all tested extracts. The autofermented CLF extracts with highest antiproliferative efficacy induced morphological changes and apoptosis in the HeLa cells. Obtained results clearly showed that the combination of enzymatic hydrolysis with cavitation phenomenon results in extracts with higher apigenin content and increased biological potential.