Inhibitory effect of ephedrannins A and B from roots of Ephedra sinica STAPF on melanogenesis.

ABSTRACT

BACKGROUND: Melanogenesis, a process producing the pigment melanin in human skin, eyes and hair, is a major physiological response against various environmental stresses, in particular exposure to ultraviolet radiation, and its pathway is regulated by a key enzyme, tyrosinase. In this study, we evaluated the effects of ephedrannins A and B, which are polyphenols from the roots of Ephedra sinica, commonly used in herbalism in oriental countries, on mushroom tyrosinase and melanogenesis in B16F10 melanoma cells. METHODS: Their effects on mushroom tyrosinase were determined via kinetic studies using a spectrophotometric analysis and those on melanin and tyrosinase production in melanoma cells treated with α-MSH (melanin stimulating hormone) were examined using PCR and ELISA. RESULTS: Both ephedrannins A and B exhibited concentration-dependent inhibitory effects on L-tyrosine oxidation by mushroom tyrosinase, and the inhibition mechanism was competitive and reversible with L-tyrosine as the substrate. In addition, melanin production in melanoma cells was also suppressed in a concentration-dependent manner by ephedrannins A and B without significant effects on cell proliferation at the concentrations tested. Both compounds showed inhibitory effects on melanin production by suppressing the transcription of tyrosinase in the cells. CONCLUSION: Both compounds exhibited significant inhibitory effects, but the inhibition by ephedrannin B was much more effective than that by ephedrannin A. Both ephedrannins A and B may be good candidates for a whitening agent for skin. GENERAL SIGNIFICANCE: This is the first report that describes effective inhibition of melanin production by ephedrannins A and B isolated from Ephedra roots.