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Journals / International Journal of Secondary Metabolite / 2020 / Cilt: 7 - Sayı: 2

Investigation of Some Corticosteroids as Glutathione Reductase Inhibitor

Esra ŞENTÜRK
Murat ŞENTÜRK
Pages
119–125
Publication Date
2022-10-19
DOI
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AI Summary & Key Takeaways

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

These corticosteroids exhibit very potent inhibitory activity against GR enzyme at low micromolar concentrations when compared to well-known GRIs.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:The detection of glutathione reductase inhibitors (GRIs) has recently become very popular due to their use as malarial and cancer drugs.
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Key Findings & Data:IC50 values were determined by drawing % activity-[I] graphs for these corticosteroids showing inhibition effects.
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Conclusion & Impact:These corticosteroids exhibit very potent inhibitory activity against GR enzyme at low micromolar concentrations when compared to well-known GRIs.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Steroid · Glutathione reductase · Inhibition

Abstract

The detection of glutathione reductase inhibitors (GRIs) has recently become very popular due to their use as malarial and cancer drugs. Today, steroidal compounds have several clinical roles due to their potent immunomodulating and anti-inflammatory properties. In this study, GR inhibitory capacity of some corticosteroids (dexamethasone, prednisolone and methylprednisolone) has been reported. Amongst these steroidal molecules dexamethasone showed the weakest inhibitory effect on GR enzyme. IC50 values were determined by drawing % activity-[I] graphs for these corticosteroids showing inhibition effects. These corticosteroids have inhibition ranging micromolar for GR with IC50 values. These corticosteroids exhibit very potent inhibitory activity against GR enzyme at low micromolar concentrations when compared to well-known GRIs.

Özet

The detection of glutathione reductase inhibitors (GRIs) has recently become very popular due to their use as malarial and cancer drugs. Today, steroidal compounds have several clinical roles due to their potent immunomodulating and anti-inflammatory properties. In this study, GR inhibitory capacity of some corticosteroids (dexamethasone, prednisolone and methylprednisolone) has been reported. Amongst these steroidal molecules dexamethasone showed the weakest inhibitory effect on GR enzyme. IC50 values were determined by drawing % activity-[I] graphs for these corticosteroids showing inhibition effects. These corticosteroids have inhibition ranging micromolar for GR with IC50 values. These corticosteroids exhibit very potent inhibitory activity against GR enzyme at low micromolar concentrations when compared to well-known GRIs.

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Cite This Article

ŞENTÜRK, E., ŞENTÜRK, M. (2022). Investigation of Some Corticosteroids as Glutathione Reductase Inhibitor. International Journal of Secondary Metabolite, Cilt: 7 - Sayı: 2, 119–125. https://ajindex.com/articles/541648

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References (8)

  1. Karplus, P.A., Schulz, G.E. (1987). Refined structure of glutathione reductase at 1.54 A resolution. J. Mol. Biol., 195, 701-729. doi:https://doi.org/10.1016/0022-2836(87)9019-4
  2. Karplus, P.A., Pai, E.F., Schulz, G.E. (1989). A crystallographic study of the glutathione binding site of glutathione reductase at 0.3 nm resolution. Eur. J. Biochem., 178, 693-703. doi:https://doi.org/10.1111/j.1432-1033.1989.tb14500.x
  3. Kocaoglu, E., Talaz, O., Cavdar, H., Senturk, M., Supuran, C.T., Ekinci, D. (2019). Determination of the inhibitory effects of N-methylpyrrole derivatives on glutathione reductase enzyme. J. Enzym. Inhib. Med. Chem., 34, 51 54. doi:https://doi.org/10.1080/14756366.2018.1520228
  4. Yu, J., Zhou, C.Z. (2007). Crystal structure of glutathione reductase Glr1 from the yeast Saccharomyces cerevisiae. Proteins, 68, 972-979. doi:https://doi.org/10.1002/prot.21354
  5. Balaydin, H.T., Ozil, M., Senturk, M. (2018). Synthesis and glutathione reductase inhibitory properties of 5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one’s aryl schiff base derivatives. Archive der Pharm., 351, e1800086. doi:10.1002/ardp.201800086 Couto, N., Wood, J., Barber, J. (2016). The role of glutathione reductase and related enzymes on cellular redox homoeostasis network. Free Rad. Biol. Med., 95, 27-42. doi:https://doi.org/10.1016/j.freeradbiomed.2016.02.028
  6. Balendiran, G.K., Dabur, R., Fraser, D. (2004). The role of glutathione in cancer. Cell Biochem. Funct., 22, 343-352. doi:10.1002/cbf.1149 Traverso, N., Ricciarelli, R., Nitti, M., Marengo, B., Furfaro, A.L., Pronzato, M.A., Marinari, U.M., Domenicotti, C. (2013). Role of glutathione in cancer progression and chemoresistance. Oxid. Med. Cell. Longev., 2013. doi:https://doi.org/10.1155/2013/972913
  7. Williams, D.M. (2018). Clinical pharmacology of corticosteroids. Respir Care, 63, 655-670. doi:https://doi.org/10.4187/respcare.06314
  8. Stewart, P.M., Krone, N.P. (2011). The adrenal cortex. In: Melmed, S., Polonsky, K., Larsen, P.R., Kronenberg, H. eds. Williams Textbook of Endocrinology. 12th ed. Philadelphia, PA: Saunders-USA. ISBN: 9781437703245. Beutler, E. (1984). Red Cell Metabolism. A Manual of Biochemical Methods. Grune and Stratton Inc, Orlando. ISBN: 0808916726 9780808916727. Boehme, C.C., Arscott, L.D., Becker, K., Schirmer, R.H., Williams, C.H. (2000). Kinetic characterization of glutathione reductase from the malarial parasite Plasmodium falciparum comparison with the human enzyme. J. Biol. Chem., 275, 37317-37323. doi:10.1074/jbc.M007695