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Molecules. 2018 Jan 22;23(1). pii: E232. doi: 10.3390/molecules23010232.

Chemical Constituents from Apios americana and Their Inhibitory Activity on Tyrosinase.

Author information

1
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. oasis5325@gmail.com.
2
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. thy5012@kaeri.re.kr.
3
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. sykang@kaeri.re.kr.
4
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. jbkim74@kaeri.re.kr.
5
College of Pharmacy, Chungnam National University, Daejeon 34134, Korea. yhk@cnu.ac.kr.
6
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk-do 56212, Korea. chjin@kaeri.re.kr.

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

PMID:
29361770
PMCID:
PMC6017567
DOI:
10.3390/molecules23010232
[Indexed for MEDLINE]
Free PMC Article

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