Diabetes mellitus, a syndrome affecting many people in all countries over the world, is commonly treated with blood glucose lowering agents. On-going research seeks to develop anti-hyperglycaemic novel agents with less undesirable effects. More recently, the hyperglycaemic activity of vanadium compounds has received attention, particularly inorganic vanadium salts such as sodium orthovanadate and vanadyl sulphates which have been shown to lower blood glucose and increase glycogen synthesis in experimental diabetes. Accordingly this study, investigated the effects of novel oxidovanadium formulations on glucose utilization in liver and muscle cell lines. The oxidovanadium complexes, cis-[VO2(Hpybz)(pybz)] (1), (µ-O)[VO(Hpybz)(pybz).VO(Hpybz)(acac)] (2) and [VO(Hpbyz)2SO4] (3).H2O were synthesized from the 2:1 molar ratio reactions of the ligand, 2-pyridylbenzimidazole (Hpbyz) with the respective metal precursors, ammonium vanadate, vanadyl(IV) acetylacetone and vanadyl(IV) sulphate. The octahedral vanadium (IV) complex, [VO(Hpbyz)2SO4] (3).H2O was characterized by means of conductance measurements, UV/Vis, ESR and IR spectroscopy as well as single crystal X-ray diffraction. Each of the oxidovanadium complexes was evaluated for its effect on glucose uptake in C2C12 muscle and Chang cell lines. Insulin was used as a positive control. Vanadium compounds 1, 2 and 3 at various doses (12.5, 25 and 50 µg/mL) significantly increased glucose utilization in the liver and muscle cells mediated via glycogen synthesis with the lowest dose of cis-[VO2(Hpybz)(pybz)] decreasing glucose concentrations in Chang cells from 18.87 ± 0.16 to 6.08±0.33 mmol and skeletal muscle from 27.99 ± 0.15 to 4.88 ± 0.14 mmol. Despite their anti-diabetic properties, some vanadium complexes such as vanadyl sulphates are associated with toxic effects. The present observations, however, indicate that oxidovanadium 2-pyridylbenzimidazole (Hpybz) compounds improve glucose utilization in skeletal muscle and liver without evoking toxicity. These results show that oxidovanadium 2-pyridylbenzimidazole (Hpybz) complexes have high anti-diabetic properties and hence can provide novel approaches in diabetes management.