1. Academic Validation
  2. Isolindleyin exerts anti-melanogenic effects in human epidermal melanocytes via direct binding to tyrosinase

Isolindleyin exerts anti-melanogenic effects in human epidermal melanocytes via direct binding to tyrosinase

  • Biochem Biophys Res Commun. 2021 Jan 1;534:802-807. doi: 10.1016/j.bbrc.2020.10.105.
Ji Young Lee 1 Juewon Kim 2 Yeon Joo Nam 3 Hyoung-June Kim 4 Kyoung Tai No 5
Affiliations

Affiliations

  • 1 Amorepacific Corporation R&D Center, Yongin-si, 17074, Gyeonggi-do, Republic of Korea; Biomaterial Science and Engineering, Yonsei University, Seoul, 03722, Republic of Korea.
  • 2 Amorepacific Corporation R&D Center, Yongin-si, 17074, Gyeonggi-do, Republic of Korea.
  • 3 Biocenter, Gyeonggido Business & Science Acceleator, Suwon, 16229, Republic of Korea.
  • 4 Amorepacific Corporation R&D Center, Yongin-si, 17074, Gyeonggi-do, Republic of Korea. Electronic address: [email protected].
  • 5 Biomaterial Science and Engineering, Yonsei University, Seoul, 03722, Republic of Korea; Bioinformatics and Molecular Design Research Center (BMDRC), Yonsei University, Incheon, 21983, Republic of Korea. Electronic address: [email protected].
Abstract

To overcome dermatological concerns causing abnormally excessive melanin synthesis, highly effective and safe skin depigmentation compounds have been identified in the cosmetic and pharmaceutical industries. Among several methods used to achieve skin depigmentation, inhibition of Tyrosinase is one of the most effective, since Tyrosinase is a crucial Enzyme in melanogenesis. Herein, isolindleyin, a novel inhibitor of human Tyrosinase, was introduced and evaluated for its anti-melanogenic effects in human epidermal melanocytes. The results revealed that isolindleyin was directly bound to Tyrosinase and it suppressed melanin synthesis. The binding mode between isolindleyin and the active sites of human Tyrosinase was investigated using computational molecular docking at the atomic level. Isolindleyin binding was found to be stabilized by hydrophobic interactions between His 367 and Val 377 and by hydrogen bonds between Ser 380 and Asn 364. The results of this study revealed the anti-melanogenic effects of isolindleyin that could contribute toward overcoming dermatological concerns that cause abnormally excessive melanin synthesis.

Keywords

Anti-melanogenic effects; Human epidermal melanocytes; Isolindleyin; Tyrosinase.

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