Bioactive Properties of Achillea biserrata M.Bieb. Extracts: Phytochemical Analysis, Antioxidant Activity, Target Enzyme Inhibition, and Cytotoxic Effects

In this study, the enzyme inhibition and antioxidant capacity of Achillea biserrata were determined, and their relationship with cytotoxic effects was investigated. Antiproliferative activity was evaluated by the MTT assay in L929, A549, B16F10, Hep-3B, PC-3, MCF-7, and CaCo-2 cell lines, and enzyme inhibition was assessed against tyrosinase, urease, PTP-1B, and DPP-4. Ethanol extracts showed the greatest bioactivity, whereas water extracts were the least active. The capitulum ethanol extract (CEE) exhibited the strongest inhibition of tyrosinase, urease, DPP-4, and PTP-1B (IC50: 72.83, 40.84, 70.12, and 302.42 µg/mL, respectively) and the highest cytotoxicity (IC50: 168.42–325.42 µg/mL). LC-MS/MS analysis identified quinic acid as the major constituent in the stem (44.614 mg/g extract) and capitulum (2.063 mg/g extract), and chlorogenic acid in the leaves (45.502 mg/g extract). Principal component analysis (PCA) integrating LC-MS/MS and bioactivity data supported the bioactive potential of A. biserrata, highlighting its promise as a pharmaceutical resource. © 2025 The Author(s). Chemistry & Biodiversity published by Wiley-VHCA AG.