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.
Hispolon is one of the most important functional compounds that forms Phellinus linteus (Berkeley &amp; 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.
Department of Cosmetic Science, Providence University, 200 Chung-Chi Road, Shalu, Taichung 43301, Taiwan. yishyan@gm.pu.edu.tw.
Yi-Shyan
YS
Chen
Department of Cosmetic Science, Providence University, 200 Chung-Chi Road, Shalu, Taichung 43301, Taiwan. s107@eip.mkc.edu.tw.
Shu-Mei
SM
Lee
Department of Cosmetic Science, Providence University, 200 Chung-Chi Road, Shalu, Taichung 43301, Taiwan. chchlin@pu.edu.tw.
Chih-Chien
CC
Lin
Department of Cosmetic Science, Providence University, 200 Chung-Chi Road, Shalu, Taichung 43301, Taiwan. g1000203@pu.edu.tw.
Chia-Yi
CY
Liu
D017209:Apoptosis; D020169:Caspases / Q000235:genetics / Q000378:metabolism; D002396:Catechols / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015536:Down-Regulation; D005347:Fibroblasts / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D008543:Melanins / Q000096:biosynthesis*; D008545:Melanoma / Q000378:metabolism*; D051739:Microphthalmia-Associated Transcription Factor / Q000235:genetics / Q000378:metabolism*; D014442:Monophenol Monooxygenase / Q000235:genetics / Q000378:metabolism*
D002396:Catechols; C497234:MITF protein, human; D008543:Melanins; D051739:Microphthalmia-Associated Transcription Factor; C103442:hispolon; D014442:Monophenol Monooxygenase; D020169:Caspases