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Hispolon decreases melanin production and induces apoptosis in melanoma cells through the downregulation of tyrosinase and microphthalmia-associated transcription factor (MITF) expressions and the activation of caspase-3, -8 and -9.

Abstract
Hispolon is one of the most important functional compounds that forms Phellinus linteus (Berkeley & Curtis) Teng. Hispolon has antioxidant, anti-inflammatory, antiproliferative and anticancer effects. In this study, we analyzed the functions of hispolon on melanogenesis and apoptosis in B16-F10 melanoma cells. The results demonstrated that hispolon is not an enzymatic inhibitor for tyrosinase; rather, it represses the expression of tyrosinase and the microphthalmia-associated transcription factor (MITF) to reduce the production of melanin in α-melanocyte-stimulating hormone (α-MSH)-stimulated B16-F10 cells at lower concentrations (less than 2 μM). In contrast, at higher concentration (greater than 10 μM), hispolon can induce activity of caspase-3, -8 and -9 to trigger apoptosis of B16-F10 cells but not of Detroit 551 normal fibroblast cells. Therefore, we suggest that hispolon has the potential to treat hyperpigmentation diseases and melanoma skin cancer in the future.
AuthorsYi-Shyan Chen, Shu-Mei Lee, Chih-Chien Lin, Chia-Yi Liu
JournalInternational journal of molecular sciences (Int J Mol Sci) Vol. 15 Issue 1 Pg. 1201-15 (Jan 17 2014) ISSN: 1422-0067 [Electronic] Switzerland
PMID24445257 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Catechols
  • MITF protein, human
  • Melanins
  • Microphthalmia-Associated Transcription Factor
  • hispolon
  • Monophenol Monooxygenase
  • Caspases
Topics
  • Apoptosis
  • Caspases (genetics, metabolism)
  • Catechols (pharmacology)
  • Cell Line, Tumor
  • Down-Regulation
  • Fibroblasts (drug effects, metabolism)
  • Humans
  • Melanins (biosynthesis)
  • Melanoma (metabolism)
  • Microphthalmia-Associated Transcription Factor (genetics, metabolism)
  • Monophenol Monooxygenase (genetics, metabolism)

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