Journals / Iğdır Üniversitesi Fen Bilimleri Enstitüsü Dergisi / 2019 / Cilt: 9 - Sayı: 3

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

Sıçan Eritrosit Glukoz 6-Fosfat Dehidrogenaz Enzim İnhibitörleri Olarak Tiyosemikarbazon Temelli Aza-Ylidlerin Sentezi

Pages
1503–1512
Publication Date
2019-09-01
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

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.

📌 3 Key Takeaways

🎯
Objective & Hypothesis: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.
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Key Findings & Data: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.
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Conclusion & Impact: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.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Tiyosemikarbazon · aza-ylid · sıçan eritrosit

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.

Özet

Glukoz 6-fosfat dehidrogenaz (G6PD) enzimi NADPH, bazı amino asitler, sfingozin, steroid hormonları, kolesterol, yağ asitleri ve riboz 5-fosfat sentezi gibi pek çok biyokimyasal prosesin gerçekleşmesinde çok önemli bir role sahiptir. Bu çalışmada, tiyoasetazon, ambazon ve perklozon gibi birçok ilacın ana iskeletini oluşturan tiyosemikarbazon temelli aza-ylid (TSCAs) türevi 3a-3e moleküllerinin sentezi çevreci bir yaklaşımla gerçekleştirilerek, G6PD enzim aktivitesi üzerine in vitro şartlarda inhibisyon ve aktivasyon etkisi araştırılmıştır. Çalışmalar neticesinde, sentezlenen TSCAs türevleri 3a-3d moleküllerinin G6PD enzim aktivitesini 40.77 μM ile 58.0 μM aralığındaki IC50 değerlerinde inhibe ettiği belirlenmiştir.

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Cite This Article

TEMEL, Y., BAYINDIR, S. (2019). The Synthesis of Thiosemicarbazone-Based Aza-Ylides as Inhibitors of Rat Erythrocyte Glucose 6-Phosphate Dehydrogenase Enzyme. Iğdır Üniversitesi Fen Bilimleri Enstitüsü Dergisi, Cilt: 9 - Sayı: 3, 1503–1512. https://ajindex.com/articles/256793

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References (10)

  1. Aslan, H. E., Demir, Y., Özaslan, M. S., Türkan, F., Beydemir, Ş., Küfrevioğlu, Ö. I., (2018). The behavior of some chalcones on acetylcholinesterase and carbonic anhydrase activity. Drug Chem. Toxicol. 4: 1-7.
  2. Bayindir S., Toprak M., 2019, A novel pyrene-based selective colorimetric and ratiometric turn-on sensing for copper, Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 213: 6–11.
  3. Bayindir, S., Ayna, A., Temel, Y., Ciftci, M. 2018a. The synthesis of new oxindoles as analogs of natural product 3, 3'-bis (indolyl) oxindole and in vitro evaluation of the enzyme activity of G6PD and 6PGD. Turkish Journal of Chemistry, 42(2): 332-345.
  4. Bayindir, S., Temel, Y., Ayna, A., Ciftci, M. 2018b. The synthesis of N‐benzoylindoles as inhibitors of rat erythrocyte glucose‐6‐phosphate dehydrogenase and 6‐phosphogluconate dehydrogenase. Journal of biochemical and molecular toxicology, 32(9): e22193. Bayramoğlu Akkoyun, M., Bengü, A. Ş., Temel, Y., Akkoyun, H. T., Ekin, S., Ciftci, M. 2018. The effect of astaxanthin and cadmium on rat erythrocyte G6PD, 6PGD, GR, and TrxR enzymes activities in vivo and on rat erythrocyte 6PGD enzyme activity in vitro. Journal of biochemical and molecular toxicology, 32(8): e22170. Beutler, E., 1971. “Red cell metabolism manual of biochemical methods”, London Academic Press: 19-68,
  5. Beydemir, S., GüLCIN, I., Küfrevioğlu, O. I., Ciftçi, M. 2003. Glucose 6-phosphate dehydrogenase: in vitro and in vivo effects of dantrolene sodium. Polish journal of pharmacology, 55(5): 787-792.
  6. Bruinenberg, PM., Van Dijken, JP., Scheffers, WA., 1983. “A theoretical analysis of NADPH production and consumption in yeasts”, J. Gen. Microbiol. 129: 953-964,
  7. Çiftçi, M., Beydemir, Ş., Yılmaz, H., Altıkat, S. (2003). Purification of glucose 6-phosphate dehydrogenase from Buffalo (Bubalus bubalis) erythrocytes and investigation of some kinetic properties. Protein expression and purification, 29(2): 304-310.
  8. Çiftci, M., Özmen, İ., Büyükokuroğlu, M. E., Pençe, S., Küfrevioğlu, Ö. İ. (2001). Effects of metamizol and magnesium sulfate on enzyme activity of glucose 6-phosphate dehydrogenase from human erythrocyte in vitro and rat erythrocyte in vivo. Clinical biochemistry, 34(4): 297-302.
  9. Costello C., Karpanen T., Lambert P.A., Mistry P., Parker K.J., Rathbone D.L., Ren, Wheeldon L.J.M., Worthington T., 2008. Thiosemicarbazones active against Clostridium difficile, Bioorg. Med. Chem. Lett 18: 1708-1711.
  10. Cuperlovic-Culf, M., 2013. “NMR metabolomics in ca