2. Academic Validation
  3. Chemical Constituents from Apios americana and Their Inhibitory Activity on Tyrosinase

Chemical Constituents from Apios americana and Their Inhibitory Activity on Tyrosinase

  • Molecules. 2018 Jan 22;23(1):232. doi: 10.3390/molecules23010232.
Jang Hoon Kim 1,  Hyo Young Kim 2,  Si Yong Kang 3,  Jin-Baek Kim 4,  Young Ho Kim 5,  Chang Hyun Jin 6
Affiliations

Affiliations

  • 1 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. [email protected].
  • 2 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. [email protected].
  • 3 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. [email protected].
  • 4 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. [email protected].
  • 5 College of Pharmacy, Chungnam National University, Daejeon 34134, Korea. [email protected].
  • 6 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. [email protected].
PMID: 29361770 DOI: 10.3390/molecules23010232
Abstract

The goal of this study was to identify phytochemicals with inhibitory activity against Tyrosinase. Nine compounds 1-9 were isolated from the tubers of Apios americana. This is the first report of aromadendrin 5-methyl ether (1) being isolated from the Apios species. Among them, compounds 2 and 8 showed inhibitory activity toward Tyrosinase. Based on a Dixon plot, the potential Ki values of competitive inhibitors 2 and 8 were calculated as 10.3 ± 0.8 µM and 44.2 ± 1.7 µM, respectively. An IC50 value of 13.2 ± 1.0 µM was calculated for the slow-binding inhibitor 2 after preincubation with Tyrosinase. Additionally, the predicted binding sites between the receptor and ligand, as well as secondary structure changes, in the presence of 2 were examined by molecular simulation.

Keywords

Apios americana; Leguminosae; molecular simulation; slow binding inhibitor; tyrosinase.

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