In Turkey, the genus Moltkia Lehm. is represented by two species, namely Moltkia aurea Boiss. and M. coerulea (Willd.) Lehm., which are used as both food and for medicinal purposes. This study aimed to evaluate the antidiabetic and antioxidant potential and phytochemical profiles of leaf, flower, and root extracts of Moltkia species. α-Glucosidase and α-amylase inhibitory activities, antioxidant effects, and total phenol and flavonoid contents of Moltkia extracts were evaluated. High-performance liquid chromatography was performed for identifying and quantifying phenolic compounds, which are responsible for various activities of these extracts. Among the investigated phenolic compounds, caffeic and rosmarinic acids and rutin were determined and quantified in methanol extracts. Rutin was the major compound in the flower extract of M. aurea. Rutin and rosmarinic acid were the major compounds in the leaf extract of M. aurea. The flowers, leaves and roots of M. coerulea were also rich in rosmarinic acid. The antioxidant and antidiabetic potential of these extracts may be attributable to their rutin and rosmarinic acid content. Moltkia species can be used as natural sources of antioxidants. Notably, M. aurea extracts can be used for the development of herbal products with antidiabetic potential.