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The present study assessed two different plant parts (leaves and tubers) of Arum italicum species growing in Northeast Algeria for their phytochemical composition and pharmacological effects. The phytochemical content was determined using ultra-high-performance liquid chromatography coupled with a diode array detector and an electrospray mass spectrometer (UHPLC-DADESI/MS). The results revealed that the tuber extract was rich in lignans with a fraxiresinol glycoside as the major compound. In contrast, the leaf extract was rich in flavonoid glycosides, described for the first time in the aerial part of this species. The extract’s inhibitory activity against key enzymes was linked to hyperglycemia, α-glucosidase, and α-amylase, and their ability to inhibit the growth of human gastric carcinoma (AGS) and lung carcinoma (A549) cancer cell lines was also assessed. A cell line morphology study was also conducted with the most effective extract. The chromatin status of the cells was evaluated using DAPI, while the cytoplasmic morphology was evaluated using phalloidin. The tuber extract generally inhibited α-glucosidase and α-amylase enzymes more efficiently than the leaf extract. Its inhibition effect against the α-glucosidase was significantly higher when compared to the standard acarbose. The tuber extract also caused more viability loss of AGS and A549 cancer cells than the leaf extract in the cytotoxicity assay. In conclusion, our findings show that, compared to the leaf extract, the tuber extract exhibited more pronounced biological effects. The strong inhibitory potential of the tuber extract against the α-glucosidase enzyme should also be highlighted, which suggests it is a good candidate for discovering new antidiabetic agents. [ABSTRACT FROM AUTHOR]