The invention discloses an esculin hydrate thioctic ester compound with antioxidant activity, and a preparation method thereof. According to the preparation method, esculin hydrate and thioctic acid are taken as raw materials, in an organic solvent, esterification reaction is adopted so as to synthesize an esculin hydrate thioctic ester compound with a novel structure. The esculin hydrate thiocticester compound can be taken as a food anti-oxidant, is capable of preventing influences of oxidation deterioration of food especially grease or food rich in grease on food local flavor and editable quality, and at the same time, the esculin hydrate thioctic ester compound can be added into cosmetic to inhibit skin aging and cosmetic self oxidation deactivation as an anti-oxidant. The raw materials are easily available; the steps are simple; and the preparation method is suitable for industrialized production.