Introduction. Several treatments are available for type 2 diabetes mellitus. However, more medications are needed to assist with the optimal management of the different stages of the disease. Teucrium polium L. (Tp) is a herb that has a folk reputation for its antidiabetic potential. Previous studies indicate that Tp extracts decrease blood glucose levels in vivo and induce insulin secretion from pancreatic β-cells in vitro. Although the constituent/s responsible for this action have not yet been elucidated, select flavonoids (namely, apigenin and quercetin) that are also constituents of this plant have been shown to have glucose-lowering potential when tested in vitro and in vivo. Aims. To examine the insulin secretagogue potential of apigenin and quercetin, and their human metabolites. Methods. Insulin secretagogue effect of Tp extract and selected flavonoids/metabolites was evaluated using pancreatic β-cell line INS-1 and BRIN-BD11. Insulin release was determined with the aid of the Insulin ELISA kits, and Glucose uptake assays. Results. Insulin release increased significantly in response to Tp extract compared to glucose alone. Apigenin and Quercetin showed an increase insulin secretion, however, insulin release was more evident with Apigenin-7-glucuronide and Quercetin-3-glucuronide and their combination revealed even higher insulin secretion. Discussion. Tp extract promoted insulin secretion from pancreatic beta cells. This result provides compelling evidence that constituents within the Tp extract promote insulin secretion. Insulin secretion in the presence of Apigenin-7-glucuronide and quercetin-3-glucuronide exceeds that in the presence of Apigenin and Quercetin and was more evident when tested in combination, suggesting a possible synergistic effect. Apigenin and Quercetin were specifically selected in this study as previous studies indicate potential insulin secretagogue ability when tested in vitro. Flavonoid human metabolites are essential in this study as they would give a more realistic assessment of their probable activity in vivo. This observation will pave the way for identifying the active compounds in Tp that might be valuable for developing new medication for type 2 diabetes.