Arum maculatum, cuckoo‐pint in folk linguistics, is a poisonous but medicinal plant with tremendous properties that need investigation. This study subjected cuckoo‐pint's parts to in vitro antioxidant, enzyme inhibition, and antimicrobial susceptibility testing to investigate its biological activity. Further, phytochemistry was analyzed by both LC–MS/MS and total phenol, flavonoid, saponin, and reducing sugar content determination assays. Antioxidant activities were determined by Fe3+, Cu2+, Fe3+‐TPTZ metal‐reducing ability, 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) and 2,2ʹ‐azino‐bis‐3‐ethylbenzothiazoline‐6‐sulfonic acid (ABTS) radical scavenging assays. According to the results, seeds and berries have remarkable metal‐reducing and radical‐scavenging effects as natural and synthetic analogs such as ascorbic acid, butylated hydroxyanisole, butylated hydroxytoluene, trolox, and α‐tocopherol. Inhibition studies over human carbonic anhydrase II (hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α‐amylase were performed, and IC50 values were determined for each enzyme inhibition. According to the results, the cuckoo‐pint seeds inhibited the AChE, BChE, and hCA II activity with greater IC50 values than reference inhibitors. Antimicrobial activity over pan‐resistant strains was achieved for each strain with the extracts, at least 20 mm zone diameter was obtained with the lowest concentrations. LC–MS/MS results revealed 24 bioactive metabolites associated with the extracts’ biological activity. Notably, quinic acid and epicatechin correlated with cardioprotective, neuroprotective, antioxidant, and antidiabetic activity.