Abstract
Glutathione reductase inhibitors are very popular antimalarial and anticancer agents. In this study, in vitro inhibition effects of β-sitosterol, stigmasterol, diosgenin and jervine which containing steroidal structure were determined against glutathione reductase enzyme. β-sitosterol, diosgenin and jervine were isolated from Veratrum album and stigmasterol was isolated from Artemisia dracunculus L. by chromatographic methods. According to the results obtained, IC50 values of β-sitosterol, stigmasterol, diosgenin and jervine were found as 1.2580, 5.2116, 0.1916 and 0.7701 µM, respectively. Among test compounds, diosgenin showed the strongest inhibitory effect against glutathione reductase with Swissdock docking figure. In current study first time, β-sitosterol, stigmasterol, diosgenin and jervine were found to be much more glutathione reductase inhibitors.
Highlights
Glutathione reductase (GR, EC 1.8.1.7), found in most organism is an important homodimeric flavoprotein and an antioxidant enzyme in protection a critical intracellular reducing environment against oxidative stress
We report in vitro inhibitory effects of the steroidal natural compounds β-sitosterol, stigmasterol, diosgenin and jervine on GR enzyme
The most widely used anticancer drug N,N-bis(2-chloroethyl)-N-nitrosourea in the literature has an 647 μM IC50 value against the GR enzyme. This drug which is used as a GR inhibitor, leads to toxicity and inhibition of DNA synthesis [22]
Summary
Glutathione reductase (GR, EC 1.8.1.7), found in most organism is an important homodimeric flavoprotein and an antioxidant enzyme in protection a critical intracellular reducing environment against oxidative stress. It catalyzes the reduced glutathione (GSH) generation from oxidized glutathione using nicotinamide ademine dinucleotide phosphate (NADPH). Antimalarial drugs target GR enzyme inhibition and host cells in the malaria parasites. The steroidal compounds β-sitosterol (1), stigmasterol (2), diosgenin (3) and jervine (4) are important bioactive natural products that are quite common in plants and animals (Figure 1) [8, 9]. Diosgenin, which is used as a starting material for the synthesis of hormones cortisone and progesterone, is a very important natural steroidal sapogenin using in synthesize of new synthetic drugs. The inhibitory effects of β-sitosterol, stigmasterol, diosgenin and jervine were investigated on the GR enzyme
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