Tyrosinase is involved in early stages of the pathway and is considered the target molecule in the development of skin-whitening cosmetics, which means that the key is how the product inhibits this enzymatic activity. Arbutin has been developed as a tyrosinase inhibitor and approved as an active ingredient of quasi-drugs. It is also a wellknown naturally occurring compound contained in bilberry ( Figure 2), pear, or the genus Arctostaphylos. Arbutin,-D-glucopyranoside of hydroquinone ( Figure 3), is effective in the topical treatment of various cutaneous hyperpigmentations characterized by hyperactive melanocyte function.