This dissertation aimed to screen the beneficial health effects of a hydromethanolic extract (GTE) obtained from the golden thistle (S. hispanicus L.) on different health conditions, including type 2 diabetes, inflammation, cancer, and wound healing. First, 1 mg/mL GTE resulted in 6.94% chlorogenic acid (CGA) bioavailability with (1.82±0.07)x10-6 cm/s apparent permeability on differentiated CaCo-2 cells. Then, 1 mg/mL GTE prompted 39.4-42.6% less glucose efflux and 49-66% less GLUT2 mRNA expressions on CaCo-2 cells. In the systemic inflammation model, pre-treatments of 50-500 μg/mL GTE reduced some inflammatory markers after 0.5 μg/mL lipopolysaccharide (LPS) inflammation induction for 12 h on RAW 264.7 cells. Reductions in 30-53%, 32-45% and 16-36% ranges for nitric oxide, tumor necrosis factor-α, and interleukin-6 (IL-6) were determined, respectively. Additionally, same GTE concentrations were pre-treated with the CaCo-2 cells in the colonic inflammation model. 15.5-19.5% and 8.7-17.3% less IL-6 and IL-8 cytokine releases were detected from CaCo-2 cells, respectively. The wound healing model of 3T3-L1 mouse fibroblasts revealed that 40-80 μg/mL root bark extract resulted in enhanced wound closures with significant differences in the cell cycle distributions. As the most significant result, G2 phase distributions were 1.8% and 12.5% in the negative and positive control samples, respectively. The root bark extract treatments of 10, 40, and 80 μg/mL resulted in 6.6%, 7.1%, and 9.1% in increasing concentrations. Finally, 4 mg/mL GTE application to CaCo-2 human adenocarcinoma cells caused 78.4% reduced cell viability, a cell cycle arrest, and increased early and late apoptotic properties. Overall results suggest that S. hispanicus L. has functional molecules that influence cellular regulations and have potential beneficial health effects.