Characterisation of naturally occurring isothiocyanates as glutathione reductase inhibitors.

ABSTRACT: Glutathione reductase (GR), an essential antioxidant enzyme against oxidative stress, has become an attractive drug target for the development of anticancer and antimalarial drugs. In this regard, we evaluated the naturally occurring isothiocyanates as promising GR inhibitors and elucidated the mechanism of action. It was found that benzyl isothiocyanate (BITC) and phenethyl isothiocyanate (PEITC) inhibited yeast GR (yGR) and human GR (hGR) in a time- and concentration-dependent manner. The K_i and k_inact of BITC against yGR were determined to be 259.87 µM and 0.0266 min^-1, respectively. The GR inhibition occurred only in the presence of NADPH and persisted after extensive dialysis. The tandem mass spectrometric analysis revealed that Cys⁶

SUBMITTER: Li X 

PROVIDER: S-EPMC7534374 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature