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Abstract The impact of heating treatments on antityrosinase capacities of polyphenols (quercetin, cinnamic acid, ferulic acid) and saponins (protodioscin and dioscin) from Asparagus was evaluated. Upon microwave heating (700 W for 20 min) with hot-air heating (120 °C for 30 min), the addition of protodioscin and dioscin significantly enhanced the antityrosinase capacities due to the deglycosylation. The analysis of fluorescence spectroscopy showed that combined heating increased the affinity between tyrosinase and inhibitors. Thermodynamic calculation indicated that randomness of molecules in the solution systems increased and hydrophobic force was the major force during interactions. In addition, two ester compounds (Est 1 and Est 2) were newly detected using UPLC-TOF/MS, which might be the major bioactive compounds of enhancing antityrosinase capacities. In particular, the addition of saponins induced the formation of Est 1 and Est 2. Taken together, the deglycosylation of saponins and the new compounds contributed to the enhancement of antityrosinase activity. These findings provide promising insight for increasing the antityrosinase abilities of polyphenols and saponins.