T2DM is a multifaceted endocrine disorder arises due to insulin resistance coupled with insufficient secretion of insulin from the pancreatic β-cells. Its prevalence is increasing alarmingly worldwide due to genetic and environmental factors. Among the various oral antidiabetic drugs widely used for the treatment of T2DM, metformin is considered as the first line of treatment to T2DM and backbone for combination therapy. However, at higher doses metformin induced lactic acidosis in addition to vitamin B12 deficiency. In order to circumvent the toxicity of metformin at high doses, an attempt has been made to synthesize a new metformin-3-hydroxyflavone complex. The Schiff base complex synthesized was characterized by various spectral studies such as FT-IR, Mass, 1H NMR and 13C NMR. The effect of oral administration of metformin-3-hydroxyflavone complex at a concentration of 20 mg/kg.b.w./rat/day to high fat diet fed-low dose STZ induced type 2 diabetes in rats was evaluated. The biochemical alterations such as fasting blood glucose, hemoglobin, glycosylated hemoglobin, plasma insulin and c-peptide observed in the diabetic rats were restored to near normal after treatment with the Schiff base complex. Additionally, the complex treatment regulates the activity of carbohydrate and glycogen metabolizing enzymes. The efficacy of the complex was comparable with metformin which was administration at a relatively high dose of 50 mg/kg.b.w./rat/day. The data obtained evidenced the regulatory properties of metformin-3-hydroxyflavone complex in maintaining normoglycemia in experimental type 2 diabetes.