The Synthesis of Thiosemicarbazone-Based Aza-Ylides as Inhibitors of Rat Erythrocyte Glucose 6-Phosphate Dehydrogenase Enzyme

Abstract

Glucose 6-phosphate dehydrogenase (G6PD) enzyme plays an important role in various biochemical processes such as synthesis of cholesterol, fatty acids, sphingosine, steroid hormones, NADPH, some amino acids and ribose 5-phosphate. In this study, thiosemicarbazone-based aza-ylide (TSCAs) derivatives 3a-3e, which form the main framework of many drugs such as thioacetazone, ambazone, and perchlozone, were synthesized with a green approach and in vitro inhibitor or activator effects on G6PD enzyme activity was investigated. As a result of studies, TSCAs derivatives 3a-3d inhibited the G6PD enzyme activity with IC50 in the range of 40.77 µM to 58.0 µM for G6PD.

Purification and Characterization of 6-Phosphogluconate Dehydrogenase from Japanese Quail (Coturnix, coturnix japonica) Erythrocytes

“…The method used for the purification of the enzyme was 2ˈ, 5ˈ-ADP Sepharose 4B affinity gel chromatography, which is a very powerful, reliable, easy, economic and a single step purification method that gives very good purification yields with an ability to purify bulk amounts of the enzymes (Temel et al, 2017a,b;Temel and Kocyigit, 2017). These advantages of the method are some of the characteristics of it which make it by comparison to other purification methods to purify different enzymes (Temel et al, 2018;Temel and Bayındır, 2019).…”

In VitroEffects of Some Drugs on Glucose-6-Phosphate Dehydrogenase Enzyme Purified from Sheep Spleen Tissue

“…Çalışma sonuçları analiz edildiğinde iveral'ın 0,62 mM IC50 değeriyle enzim üzerinde en etkili inhibitör olduğu, linkomisin'in ise 231 mM IC50 değeriyle enzim üzerine inhibisyon etkisi en düşük ilaç olduğu tespit edildi. Literatürde G6PD enzimi farklı dokulardan çeşitli kromatografik teknikler yardımıyla saflaştırılarak karakterize edilmiş ve bazı ilaç ve organik bileşiklerin enzim aktivitesi üzerine etkileri incelenmiştir [6,46,47]. Çiftci ve ark.…”

“…Reaksiyon ürünlerinden D-ribuloz 5fosfat, ATP, CoA, NAD + , FAD, RNA ve DNA gibi hayati öneme sahip biyomoleküllerin bileşeni olan riboz 5-fosfata izomerize olur. Reaksiyon sırasında oluşan NADPH ise yağ asitleri, steroidler ve bazı amino asitlerin sentezinde kullanılan önemli bir koenzimdir [4][5][6]. Glutatyon ve tiyoredoksin sistemleri hücre içi iki ana antioksidan sistemidir.…”

Effects of Arbutin on Potassium Bromate-Induced Erythrocyte Toxicity in Rats: Biochemical Evaluation of Some Metabolic Enzyme Activities In Vivo and In Vitro

“…NADPH synthesis is critical for the defense of cells against oxidative stress since it functions as an electron donor for numerous enzymatic processes necessary in biosynthetic pathways. The pentose phosphate pathway’s initial step is catalyzed by the enzyme glucose-6-phosphate dehydrogenase (G6PD), supplying all cells with acts a reducing power in the form of NADPH. − 6-phosphogluconate dehydrogenase (6PGD), an essential enzyme for biological systems, catalyzes the conversion of 6-phosphogluconate into D-ribulose 5-phosphate, resulting in the production of NADPH in the presence of NADP + . − The glutathione reductase (GR) enzyme is required for glutathione disulfide (GSSG) to be converted to its reduced form (GSH). GSH is necessary for the protection of cells against oxidative stress as an antioxidant.…”