4-(Phenylsulfanyl)butan-2-One Suppresses Melanin Synthesis and Melanosome Maturation In Vitro and In Vivo

International Journal of Molecular Sciences

Shing-Yi Sean Wu⁴  Hui-Min David Wang⁴  Yi-Shan Wen⁴  Wangta Liu¹  Pin-Hui Li⁵  Chien-Chih Chiu¹  Pei-Chin Chen²  Chiung-Yao Huang⁴  Jyh-Horng Sheu⁴  Zhi-Hong Wen⁴  Vassilios Roussis³ 

[1] Department of Biotechnology, Kaohsiung Medical University, Kaohsiung 807, Taiwan, ROC; E-Mails:;Doctoral Degree Program in Marine Biotechnology, National Sun Yat-sen University and Academia Sinica, Kaohsiung 804, Taiwan, ROC; E-Mail:Department of Marine Biotechnology and Resources, National Sun Yat-Sen University, Kaohsiung 804, Taiwan, ROC;;Department of Marine Biotechnology and Resources, National Sun Yat-Sen University, Kaohsiung 804, Taiwan, ROC; E-Mails:;Department of Fragrance and Cosmetic Science, Kaohsiung Medical University, Kaohsiung 807, Taiwan, ROC; E-Mail:

关键词: 4-(phenylsulfanyl)butan-2-one;    melanogenesis;    tyrosinase;    melanosome maturation;    zebrafish;   

DOI  :  10.3390/ijms160920240

来源: mdpi

【 摘 要 】

In this study, we screened compounds with skin whitening properties and favorable safety profiles from a series of marine related natural products, which were isolated from Formosan soft coral Cladiella australis. Our results indicated that 4-(phenylsulfanyl)butan-2-one could successfully inhibit pigment generation processes in mushroom tyrosinase platform assay, probably through the suppression of tyrosinase activity to be a non-competitive inhibitor of tyrosinase. In cell-based viability examinations, it demonstrated low cytotoxicity on melanoma cells and other normal human cells. It exhibited stronger inhibitions of melanin production and tyrosinase activity than arbutin or 1-phenyl-2-thiourea (PTU). Also, we discovered that 4-(phenylsulfanyl)butan-2-one reduces the protein expressions of melanin synthesis-related proteins, including the microphthalmia-associated transcription factor (MITF), tyrosinase-related protein-1 (Trp-1), dopachrome tautomerase (DCT, Trp-2), and glycoprotein 100 (GP100). In an in vivo zebrafish model, it presented a remarkable suppression in melanogenesis after 48 h. In summary, our in vitro and in vivo biological assays showed that 4-(phenylsulfanyl)butan-2-one possesses anti-melanogenic properties that are significant in medical cosmetology.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.