2. Academic Validation
  3. The Luteolinidin and Petunidin 3- O-Glucoside: A Competitive Inhibitor of Tyrosinase

The Luteolinidin and Petunidin 3- O-Glucoside: A Competitive Inhibitor of Tyrosinase

  • Molecules. 2022 Sep 4;27(17):5703. doi: 10.3390/molecules27175703.
Seo Young Yang 1,  Jang Hoon Kim 2,  Xiangdong Su 3,  Jeong Ah Kim 4 5
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Engineering, Sangji University, 83 Sangjidae-gil, Wonju 26339, Korea.
  • 2 Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Korea.
  • 3 School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, No. 66, Gongchang Road, Guangming District, Shenzhen 518107, China.
  • 4 Vessel-Organ Interaction Research Center, VOICE (MRC), College of Pharmacy, Kyungpook National University, Daegu 41566, Korea.
  • 5 BK21 FOUR Community-Based Intelligent Novel Drug Discovery Education Unit, College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea.
PMID: 36080469 DOI: 10.3390/molecules27175703
Abstract

The enzyme Tyrosinase plays a key role in the early stages of melanin biosynthesis. This study evaluated the inhibitory activity of anthocyanidin (1) and anthocyanins (2-6) on the catalytic reaction. Of the six derivatives examined, 1-3 showed inhibitory activity with IC50 values of 3.7 ± 0.1, 10.3 ± 1.0, and 41.3 ± 3.2 μM, respectively. Based on Enzyme kinetics, 1-3 were confirmed to be competitive inhibitors with Ki values of 2.8, 9.0, and 51.9 μM, respectively. Molecular docking analysis revealed the formation of a binary encounter complex between 1-3 and the Tyrosinase catalytic site. Luteolinidin (1) and petunidin 3-O-glucoside (2) may serve as Tyrosinase inhibitors to block melanin production.

Keywords

anthocyanins; competitive inhibitor; melanin; molecular docking; tyrosinase.

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