Caffeic acid is a kind of phytochemicals occurred in coffee, which is worked as a carcinogenesis restrainer and antioxidants on the human body. In this study, as one type of caffeic acid derivatives, methoxypolyethylene glycol caffeate(MPC) was synthesized by the esterification between caffeic acid and methoxypolyethylene glycol with N,N'-dicyclohexyl carbodiimide, 4-dimethylamino pyridine. The synthesized product was confirmed by using FT-IR and 1H-NMR, thin-layer chromatography. And these compound was investigated as antioxidant, Tyrosinase hindrance and skin moisturizers. In the free radical scavenging study, antioxidant effect of MPC was averagely high than the red ginseng extract that be used as a natural antioxidants. The result of Tyrosinase anti-activity test was better than embryo bud of rice extract at low concentration. At the iNOS anti-activity tested by using Raw 264.7 cell, and confirmed anti-inflammatory function. For the MPC handled with sodium lauryl sulfate, was tested for the skin moisture content and skin moisture loss.