Ziziphora clinopodioides Lam. has been used in traditional Uyghur medicine for a long time. In order to illustrate the pharmaceutical activity of Z. clinopodioides as skin-whitening agents, The petroleum ether, chloroform, ethyl acetate, water extracts, and hydrodistilled essential oil from Z. clinopodioides were evaluated for their inhibitory effects on tyrosinase. The inhibitory effects on tyrosinase were weak but show a dose-dependent type. We also studied preliminary phytochemical and showed differences were exist between different extract. As rosmarinic acid is a major active compound in Z. clinopodioides, the result of tyrosinase activity indicated rosmarinic acid have both inhibit and activate effect at low and high does, respectively. A 3D model showed a good docking result between rosmarinic acid and tyrosinase. The weak effects may reveal that the concentration was too low to inhibit this enzyme or tyrosinase inhibitor and activator exist in Z. clinopodioides at the same time.