Background Achillea arabica is a perennial aromatic herb widely used in folk medicine for the treatment of the stomachache and abdominal pain, wound healing, gout, cancer, diabetes and such. The aim of this study was to determine the photochemical content of the ethanolic lyophilized extract of A. arabica flower by LC-MS/MS and NMR and to reveal the antidiabetic and antioxidant effects of this extract against streptozotosine (STZ)-induced in diabetic rats.Methods and Results After toxicity test, 35 female rats were divided into 5 groups. Control, Diabetes mellitus (DM), A.arabica (400 mg/kg) extract, DM +A.arabica (400 mg/kg) extract and DM+Glibenclamide (2 mg/kg). According to LC–MS/MS results of A. arabica flower extract, quinic acid (2439.9 μg/g), cyranoside (858.4 μg/g), chlorogenic acid (698.7 μg/g) and cosmosin (347.8 μg/g) were determined as major compounds, respectively. In addition, two new compounds were determined in this plant according to NMR analyzes and these compounds were named edremitine and achillosine, respectively. It was determined that while diabetic rats fed A. arabica plant extract significantly decreased blood glucose level, serum glucose, HbA1c, liver and kidney damage biomarker levels, and malondialdehyde (MDA) content compared to the DM group, it caused fluctuations in antioxidant enzyme levels.Conclusion We conclude that A. arabica flower plant extract may be a good addition to the well established pharmacological approach of DM by contributing to the reduction of overall oxidative load.