Objective: To optimize the synthetic process conditions of and study the antioxidation activity of orientin and orientin zinc complexes in vitro. Methods: Using elemental analyzer, plasma emission spectrometer, ultraviolet spectrometer, infrared spectrometer, thermogravimetric analyzer and nuclear magnetic resonance instrument, the structural characterization of orientin zinc complexes was observed, taking superoxide anion radicals, hydroxyl radicals, 1,1-Diphenyl-2-picrylhydrazyl radical 2,2-Diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl (DPPH)radical generation system as experimental system, to examine the antioxidant activity of orientin and orientin-zinc complexes. Results: The best coordination reaction optimum process of complexes formed by orientin and zinc acetate was shown as follows. Taking anhydrous ethanol as solvent, reaction pH was 8, reaction temperature was 65℃, and reaction time was 8 h. The orientin-zinc complexes maybe the chemical formula [Zn3(C21H15O11)2]?4H2O and chemical structural formula. Orientin and orientin-zinc complexes have clear ability of removing ·OH and ·DPPH, and the effect of orientin-zinc complexes in each dose group was more obvious than equivalent dose orientin at 1.0~8.0μg·mL-1. Conclusion: Orientin-zinc complexes is more superior than orientin on the activity of antioxidation.