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

• Published in: Biochimica et biophysica acta Vol. 1850; no. 7; pp. 1389 - 1396
• Main Authors: Kim, Ik-Soo, Yoon, Sung-Jin, Park, Young-Jun, Lee, Hee-Bong
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.07.2015
• Subjects: alpha-melanocyte-stimulating hormone; Animals; Anti-melanogenesis; Biocatalysis - drug effects; bleaching agents; Blotting, Western; Cell Line; Cell Line, Tumor; cell proliferation; Cell Survival - drug effects; Competitive inhibition; Dose-Response Relationship, Drug; Epehdra sinica; Ephedra sinica; Ephedra sinica - chemistry; Ephedrannin A; Ephedrannin B; eyes; Gene Expression Regulation, Enzymologic - drug effects; Humans; Keratinocytes - cytology; Keratinocytes - drug effects; Kinetics; melanin; Melanins - biosynthesis; melanogenesis; melanoma; Mice; Molecular Structure; Monophenol Monooxygenase - genetics; Monophenol Monooxygenase - metabolism; mushrooms; oxidation; physiological response; Plant Extracts - pharmacology; Plant Roots - chemistry; polymerase chain reaction; polyphenols; Proanthocyanidins - chemistry; Proanthocyanidins - pharmacology; Reverse Transcriptase Polymerase Chain Reaction; roots; spectral analysis; Substrate Specificity; Tyrosinase activity; tyrosine; Tyrosine - metabolism; ultraviolet radiation; PBS; Anti-melanogenesis; SDS; DMSO; EGCG; Tyrosinase activity; ECG; GCG; MITF; MTT; Ephedrannin A; Competitive inhibition; ECL; Ephedrannin B; DMEM; LDH; OD; FBS; l-DOPA; α-MSH; MAP; Epehdra sinica
• ISSN: 0304-4165; 0006-3002; 1872-8006
• DOI: 10.1016/j.bbagen.2015.04.001

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. 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. 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. 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. This is the first report that describes effective inhibition of melanin production by ephedrannins A and B isolated from Ephedra roots. [Display omitted] •Two polyphenols, ephedrannins A and B, were isolated from roots of Ephedra sinica.•Both ephedrannins were competitive inhibitors of mushroom tyrosinase.•Both compounds showed inhibitory effects on melanin productions in melanoma cells.•This anti-melanogenesis was caused by suppressing tyrosinase mRNA transcription.