The level of UV radiation emitted by the sun is increasing due to the destruction of the ozone layer. Our skin is more exposed to UV radiation and often suffers from various harmful effects of UV. Melanin prodcution in human skin is an important defense mechanism against UV and a major determinant of skin color.1,2) Melanocytes residing within the basal layer of the epidermis synthesize melanin in specialized organelles, designated as melanosomes, by coordinated action of various melanogenic enzymes such as tyrosinase, tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2).3-8) Then, melanin-containing melanosomes are transferred to keratinocytes, providing protection against UV radiation and eventually disappear with desquamation of the skin.9,10) Despite the protective role of melanins, abnormal hyperpigmentation such as freckles, chloasma, and other forms of melanin hyperpigmentation sometimes can be serious aesthetic problems. Therefore potent active agents for the improvement of hyperpigmentation have been sought for cosmetic use. Many chemicals such as hydroquinone, arbutin, kojic acid, and ascorbic acid are well known for their melanogenic-inhibitory functions. [11][12][13][14] Even though these chemicals are often used in many skin-lightening, cosmetic formulations, they have some disadvantages such as poor safety and limited effectiveness. [15][16][17] In this study, we screened more than 200 medicinal herbal extracts that have been known for their skin-lightening effects to develop a skin-lightening agent from traditional medicinal plants and found that Atractylodis Rhizoma Alba, which has been used in the treatment and prevention of diabetes and ulceration, has strong melanogenic-inhibitory activity.18) Its active compound was purified using bioactivityguided fractionation and identified as selina-4(14),7(11)-dien-8-one (compound 1) by spectroscopic methods.The effects of compound 1 were evaluated on melan-a cells. Compound 1 markedly inhibited melanogenesis of melan-a cells by regulating the expression of melanogenic enzymes. Isolation of Compound 1 (Selina-4(14),7(11)-dien-8-one) Atractylodis Rhizoma Alba (2 kg) was extracted with methanol (three times, each 5 l) at 60°C. The concentrated methanol extract (350 g) was added to water and then partitioned successively with n-hexane, ethyl acetate (EtOAc), and 1-butanol. The n-hexane layer (35 g), which showed significant melanogenic-inhibitory activity (IC 50 ϭ100 mg/ml), was fractionated using silica gel column chromatography with n-hexane-ethyl acetate stepwise elution (n-hexane : EtOAcϭ80 : 1-2 : 1). Five fractions were obtained and fraction III showed the strongest activity (IC 50 ϭ20 mg/ml). This fraction was subjected to silica gel column chromatography with n-hexane-ethyl acetate (40 : 1-1 : 1). Compound 1 was further purified by HPLC with n-hexane-ethyl acetate (90 : 1) as eluting solvents (Chart 1). The molecular formula of compound 1 was determined on the basis of the spectral data ( LG Household & Healthcare Ltd.; K...