This invention discloses method for inhibiting inflammation and reducing melanophilin expression with glycine derivatives and the composition thereof. The mentioned glycine derivatives can not only efficiently inhibit skin inflammation, but also can present significant melanophilin expression reduction. This mentioned composition of this invention comprises the glycine derivatives, and shows melanophilin expression reduction and anti-inflammatory effect. The mentioned composition can be applied in topical cosmetic or pharmaceutical compositions as skin care preparations, or functional preparations.
