Cousiniais one of the widespread genera of Asteraceae family. This study aims to evaluate the biological activities and phytochemical compositions ofC. iconicaextracts. The antioxidant effects of the extracts were investigated on DPPH center dot, ABTS(+center dot), and iron chelating methods, and the inhibition effects were tested on alpha-amylase,alpha-glucosidase, and tyrosinase, as well as AChE, and BChE enzymes. The quantitative and qualitative determinations of the compounds of the extracts were carried out by LC-MS/MS. As a result, the highest TPC (271.65 +/- 3.32 mg GAE/g(extract)), and TFC (4.79 +/- 0.06 mg QE/g(extract)) were found inC. iconicaethyl acetate (CIE) sub-extract. The highest antioxidant activity on DPPH center dot(IC50 = 90.397 +/- 0.575 mu g/mL) was shown inC. iconicamethanol (CIM) extract. The highest ABTS(+center dot), and iron chelating activities were found in CIE with IC50 = 70.70 +/- 0.38, and 615.10 +/- 2.47 mu g/mL, respectively. The highest alpha-amylase, and tyrosinase activities were found in CIE, andC. iconica n-butanol sub-extract (CIB) with 864.57 +/- 0.68, and 475.21 +/- 6.22 mu g/mL IC(50)values, respectively. AChE, and BChE activities were observed as the highest in CIB (IC50 = 426.50 +/- 3.78 mu g/mL), and CIM (IC50 = 330.54 +/- 0.79 mu g/mL), respectively. According to LC-MS/MS analyses, rutin, and cynarin were determined as the main constituents of CIM, and CIE. This is the first report that these biological activities and phytochemical compositions ofC. iconicawere investigated.