The synthesis, characterization, anti-hyperglycemic activity, oxidative DNA damage capacity, and acute toxicity of chromium(III) malate complex [Cr2(LMA)3] were described. [Cr2(LMA)3] was synthesized in a single-step reaction by chelating chromium(III) with L-malic acid in aqueous solution. Based on elemental analysis, thermodynamic analysis, and spectroscopy studies, the molecular formula of [Cr2(LMA)3] was inferred as Cr2(C4H4O5)3·5H2O. Daily treatment with 2.85-17.10 mg/kg body mass of [Cr2(LMA)3] in alloxan-induced diabetic rats for 2 weeks indicated that low-molecular-weight organic chromium complex [Cr2(LMA)3] had better bioavailability and more beneficial influences on the improvement of controlling blood glucose, serum lipid, and liver glycogen levels compared with CrCl3·6H2O. [Cr2(LMA)3] did not cause oxidative DNA damage under physiologically relevant conditions. Acute toxicity studies revealed no-measurable toxicity of the [Cr2(LMA)3]. Collectively, these results suggest that [Cr2(LMA)3] may represent a novel, proper chromium supplement with potential therapeutic value to control blood glucose and serum lipid in diabetes.