4-(6-Hydroxy-2-naphthyl)-1,3-bezendiol : A Potent, New Tyrosinase Inhibitor(Pharmacology)

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概要

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• Tyrosinase is a key enzyme for melanin biosynthesis and known to be sensitive to ultraviolet light in the presence of oxygen. Therefore, finding effective tyrosinase inhibitors, either from synthetic or natural sources, can be beneficial in the treatment of melanin-related disorders. We synthesized 4-(6-hydroxy-2-naphthyl)-1,3-bezendiol (HNB), a new family of hydroxyl substituted phenyl naphthalenes, as the isosteres of oxyresveratrol. This study investigated inhibitory effects of HNB on tyrosinase activity. HNB inhibited mushroom tyrosinase with an IC_<50> value of 0.07μM, which is more potent than the anti-tyrosinase activity of kojic acid (IC_<50>=38.24), a well-known tyrosinase inhibitor. The kinetic analysis of tyrosinase inhibition revealed that HNB is a competitiveinhibitor (K_i 4.78×10^<-9>M at 0.125μM and K_i 6.21×10^<-9>M at 0.25μM). We further found that HNB also inhibited melanin production in B16F10 melanoma cells (B16 cells). In addition to tyrosinase inhibiting activity, melanin biosynthesis was inhibited by HNB in the B16F10 cells. These data strongly suggest that HNB can suppress the production of melanin via the modulation of tyrosinase activity.

• 公益社団法人日本薬学会の論文
• 2007-09-01

著者

• SONG Suhee

  Department of Chemistry and Chemistry Institute for Functional Materials, Pusan National University

• SUH Hongsuk

  Department of Chemistry and Chemistry Institute for Functional Materials, Pusan National University

• Song Suhee

  Department Of Chemistry And Chemistry Institute For Functional Materials Pusan National University

• Suh Hongsuk

  Department Of Chemistry And Chemistry Institute For Functional Materials Pusan National University

• CHUNG Hae

  Department of Pharmacy, Pusan National University

• CHUNG SANG

  Department of Surgery, Chonnam University Medical School

• HA Young

  Department of Pharmacy, Pusan National University

• LEE Hyojin

  Department of Chemistry and Chemistry Institute for Functional Materials, Pusan National University

• Lee Hyojin

  Department Of Chemistry And Chemistry Institute For Functional Materials Pusan National University

• Chung Hae

  Department Of Pharmacy Pusan National University

• Chung Hae

  Department Of Pharmacy College Of Pharmacy:longevity Life Science And Technology Institutes Pusan Na

• Chung Sang

  Department Of Pharmacy Pusan National University

• Chung Sang

  Department Of Neurosurgery College Of Medicine Seoul National University

• Ha Young

  Department Of Animal Science And Biotechnology Kyungpook National University

• Ha Young

  Department Of Pharmacy Pusan National University

• Chung Hae

  Department Of Pediatrics Chonnam National University Medical School

• Chung Hae

  Department Of Kinesiology And Community Health University Of Illinois

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