Inhibitory Effects of Esculetin on Melanin Biosynthesis (Pharmacology)

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概要

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• To investigate the structure-activity relationship of coumarins for the inhibitory activity on mushroom tyrosinase, the 50% inhibitory concentration (IC_<50> values) of 18 coumarins and four cinnamic acid derivatives were measured. Among these compounds, esculetin had the strongest inhibitory activity (IC_<50>=43μM) on mushroom tyrosinase. Introduction of a hydroxy group to the C6 and C7 positions of the coumarin ring and no substitution on the lactone ring played an important role in the expression of the strong inhibitory activity of esculetin. We performed further studies to estimate the in vitro inhibitory effects of esculetin on melanogenesis. Esculetin 5 μM significantly suppressed melanin production in murine B16 melanoma cells without affecting cell growth. Furthermore, the number of 3, 4-dihydroxyphenylalanine (DOPA) -positive melanocytes in the split-epidermal sheets treated with 0.05% or 0.1% esculetin was significantly lower than that in the control. From these results, it is suggested that esculetin has inhibitory effects on tyrosinase activity in vitro. However, further detailed studies are necessary to understand the inhibitory mechanism of esculetin.

• 公益社団法人日本薬学会の論文
• 2004-03-01

著者

• Murata Y

  Graduate School Of Natural Science And Technology Okayama University

• Miura Yoshie

  川崎医科大学 衛生学

• Miura Yoshie

  Dep. Of Biofunctional Chemistry Graduate School Of Natural Sci. And Technol. Okayama Univ.

• Baba K

  Faculty Of Phamacognosy Osaka University Of Pharmaceutical Sciences

• Baba Kenji

  Third Department Of Medicine Aichi Medical School School Of Medicine

• Baba K

  Division Of Pharmacognosy Osaka University Of Pharmaceutical Sciences

• Baba Kimiye

  Faculty Of Phamacognosy Osaka University Of Pharmaceutical Sciences

• TAKAHATA Kyoya

  Faculty of Agriculture, Okayama University

• TADA Mikiro

  Graduate School of National Science and Technology, Okayama University

• MURATA Yoshiyuki

  Faculty of Agriculture, Okayama University

• SHIMOISHI Yasuaki

  Faculty of Agriculture, Okayama University

• MASAMOTO Yukimitsu

  Graduate School of Natural Science and Technology, Okayama University

• Shimoishi Yasuaki

  Div. Of Bioscience Graduate School Of Natural Sci. And Technol. Okayama Univ.

• Masamoto Yukimitsu

  Graduate School Of Natural Science And Technology Okayama University

• Takahata K

  Faculty Of Agriculture Okayama University

• Tada M

  Department Of Biological Resources Chemistry Faculty Of Agriculture Okayama University

• Takahata Kyoya

  Faculty Of Agriculture Okayama University

• Murata Yoshiyuki

  Graduate School Of Natural Science And Technology Okayama University

• Tada Mikiro

  Fac. Of Agriculture Okayama Univ.

• Murata Yoshiyuki

  Okayama Univ. Okayama Jpn

• Shimoishi Yasuaki

  Graduate School Of Natural Science And Technology Okayama University

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