To investigate the permeability of natural compounds through hairless mouse skin, compounds having a range of lipophilicity, i.e., ginsenoside-Re (1), baicalin (2), glycyrrhizin (3), baicalein (4), wogonin (5), honokiol (6), magnolol (7), bergapten (8), shikonin (9) and sinomenine (10) were used. These compounds permeated through the skin a little, however, they were generally accumulated into the skin. The uptake amount into the skin of each compound related to their lipophilicities in the in vitro experiment. Furthermore, Ligustici Chuanxiong Rhizoma (Senkyu) ether extract (SEE) enhanced their permeability into the skin; especially, it exhibited an effect on the skin permeability of moderately lipophilic compounds such as 4, 8. The effect of SEE in vivo was similar to that obtained in the in vitro experiment. From these results, it was clarified that natural compounds having high lipophilicity sufficiently permeated into the hairless mouse skin owing to their accumulative property, and SEE enhanced the permeability of the moderately lipophilic compounds into the skin.