Inhibitory mechanism of Penicillin V on mushroom tyrosinase.

Abstract:

:Penicillin V is a bacteriolytic β-lactam antibiotic drug. In the present work, we investigated the inhibitory effect of Penicillin V on the activity of mushroom tyrosinase for the first time. The molecular mechanism for the inhibition of tyrosinase by Penicillin V was investigated by means of kinetics analysis, fluorescence quenching and molecular docking techniques. The results showed that Penicillin V could inhibit both monophenolase and diphenolase activities with IC50 of 16.6 ± 0.5 and 11.0 ± 0.2 mmol/L, respectively. The inhibitory type of Penicillin V on mushroom was mixed type, and the values of KI and KIS were 13.46 and 17.26 mmol/L, respectively. The fluorescence quenching and molecular docking showed that Penicillin V could form static interaction near the catalytic pocket of the enzyme to hinder the transportation of substrate to the active site, as well as reduce the copper plasticity for catalysis. Our results contributed to the usage of Penicillin V as a novel tyrosinase inhibitor with dual effect in field of antimicrobial and food preservation and could also provide guidance for the design of novel tyrosinase inhibitors.

journal_name

Mol Biol Rep

authors

Dong X,Wang S,Xu L,Lin J,Xu X

doi

10.1007/s11033-019-05188-6

subject

Has Abstract

pub_date

2020-02-01 00:00:00

pages

967-975

issue

2

eissn

0301-4851

issn

1573-4978

pii

10.1007/s11033-019-05188-6

journal_volume

47

pub_type

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