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• W2744203923 endingPage "47" @default.
• W2744203923 startingPage "41" @default.
• W2744203923 abstract "Malachite green (MG) has been widely used in aquaculture to treat a number of microbial and parasitic diseases. It is currently banned in the EU because of the high cytotoxicity and carcinogenic activity, which is also shared by leucomalachite green (LMG), a reduced MG metabolite that can persist in fish tissues for months. There is scant information about the ability of either compound to interact with drug metabolizing enzymes in fish. Therefore we evaluated the in vitro effects of MG and LMG (25, 50 and 100 μM) on some DMEs and glutathione (GSH) content in rainbow trout liver subfractions. LMG did not affect any of the examined parameters. In contrast, MG proved to deplete GSH and to depress to a various extent the activities of NAD(P)H cytochrome c reductase, 7-ethoxycoumarin O-deethylase, 1-naphthol uridindiphosphoglucuronyl-transferase and maximally those of 7-ethoxyresorufin O-deethylase (EROD) and glutathione S-transferase (GST) accepting 1-chloro2,4-dinitrobenzene (CDNB) as substrate. The inhibition mechanisms of EROD and GST were investigated by means of non-linear Michaelis-Menten kinetics and Lineweaver-Burk plots using 0.175–8 μM MG. The calculated IC50 for EROD was 7.1 μM, and the inhibition appeared to be competitive (Ki 2.78 ± 0.24 μM). In the case of GST, the calculated IC50 was 0.53 μM. The inhibition was best described as competitive toward GSH (Ki 0.39 ± 0.02 μM) and of mixed-type toward CDNB (Ki 0.64 ± 0.06 μM). Our findings indicate that, contrary to LMG, MG behaves as a relatively strong inhibitor of certain liver DMEs and can reversibly bind GSH." @default.
• W2744203923 created "2017-08-17" @default.
• W2744203923 creator A5022075992 @default.
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• W2744203923 date "2017-10-01" @default.
• W2744203923 modified "2023-09-27" @default.
• W2744203923 title "In vitro interactions of malachite green and leucomalachite green with hepatic drug-metabolizing enzyme systems in the rainbow trout (Onchorhyncus mykiss)" @default.
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• W2744203923 doi "https://doi.org/10.1016/j.toxlet.2017.07.900" @default.
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• W2744203923 hasPublicationYear "2017" @default.
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