Constituents from the Formosan apple reduce tyrosinase activity in human epidermal melanocytes

Yi Pei Lin, Feng-Lin Hsu, Chien Shu Chen, Ji Wang Chern, Mei Hsien Lee

研究成果: 雜誌貢獻文章同行評審

77 引文 斯高帕斯(Scopus)


Tyrosinase is a copper-containing monooxygenase that catalyzes melanin synthesis in skin melanocytes. Herein, 13 compounds from the Formosan apple (Malus doumeri var. formosana), an indigenous Taiwanese plant, were isolated and identified. The active constituents were identified as 3-hydroxyphloretin (7) and catechol (9); they exhibited potent hydroxyl radical-scavenging (IC50 values, 0.6 and 1.1 μM) and cellular tyrosinase-reducing activities (IC50 values, 32 and 22 μM) in human epidermal melanocytes. In addition, we evaluated the level of several tyrosinase-related proteins by Western blot analysis. In contrast to 3-hydroxyphloretin (7), which showed no effect on the level of these proteins, catechol (9) reduced their activity and the expression of the respective genes, as determined by quantitative real-time PCR. In a kinetic analysis of mushroom tyrosinase, 3-hydroxyphloretin (7) was a competitive inhibitor. These two constituents exhibited metal-coordinating interactions with copper ions in a virtual model of molecular docking with human tyrosinase. Thus, 3-hydroxyphloretin (7) and catechol (9) were the most active constituents from the Formosan apple; they exhibited anti-oxidant and tyrosinase reducing activities, suggesting their possible use as cosmetic agents.

頁(從 - 到)1189-1199
出版狀態已發佈 - 4月 2007

ASJC Scopus subject areas

  • 植物科學
  • 生物化學
  • 分子生物學
  • 有機化學
  • 藥物發現


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