A Multi-Biochemical and In Silico Study on Anti-Enzymatic Actions of Pyroglutamic Acid against PDE-5, ACE, and Urease Using Various Analytical Techniques: Unexplored Pharmacological Properties and Cytotoxicity Evaluation
Abstract
:1. Introduction
2. Materials and Methods
2.1. Anti-PDE5A1 Inhibitory Properties
2.1.1. Protein Expression and Purification
2.1.2. Anti-PDE5A1 Activity
2.2. Anti-Angiotensin-Converting Enzyme (ACE) Properties
2.3. Anti-Urease Properties
2.3.1. Enzyme, Substrate, Inhibitors, and Chemicals
2.3.2. Instrumentation: ESI-MS
2.3.3. Determination of Anti-Urease Activity
2.4. Cytotoxicity Study
2.4.1. Cell Lines, Medium and Reagents
2.4.2. Assessment of Cytotoxicity
2.5. Molecular Docking Studies
Protein-Ligand Preparation and Performance of Docking Studies
3. Results and Discussion
3.1. Assessment of Anti-PDE5A1 Activity
3.2. Assessment of Anti-ACE Activity
3.3. Evaluation of Anti-Urease Activity
3.4. Evaluation of Cytotoxicity Characteristics
3.5. Evaluation of Molecular Docking Analyses
3.5.1. Interaction of pGlu with Actice Site of PDE5A1
3.5.2. Interaction of pGlu with Actice Site of ACE
3.5.3. Interaction of pGlu with Actice Site of Urease
4. Conclusions
Author Contributions
Acknowledgments
Conflicts of Interest
References
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Inhibitor | IC50 (µM) |
---|---|
pGlu | 5.23 ± 1.33 |
Sildenafil citrate | 7.14 ± 1.52 |
Inhibitors | % Inhibition |
---|---|
pGlu | 98.2 ± 1.12 |
Captopril | 99.6 ± 1.64 |
ACE-catalyzed reaction (no inhibition) | Nd |
IC50 (µg/mL) | ||
---|---|---|
Compound | HeLa-R2 | MRC-5 |
pGlu | 96.42 ± 0.92 | 97.21 ± 0.61 |
Cisplatin | 6.32 ± 0.62 | 9.14 ± 0.42 |
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Šudomová, M.; Hassan, S.T.S.; Khan, H.; Rasekhian, M.; Nabavi, S.M. A Multi-Biochemical and In Silico Study on Anti-Enzymatic Actions of Pyroglutamic Acid against PDE-5, ACE, and Urease Using Various Analytical Techniques: Unexplored Pharmacological Properties and Cytotoxicity Evaluation. Biomolecules 2019, 9, 392. https://doi.org/10.3390/biom9090392
Šudomová M, Hassan STS, Khan H, Rasekhian M, Nabavi SM. A Multi-Biochemical and In Silico Study on Anti-Enzymatic Actions of Pyroglutamic Acid against PDE-5, ACE, and Urease Using Various Analytical Techniques: Unexplored Pharmacological Properties and Cytotoxicity Evaluation. Biomolecules. 2019; 9(9):392. https://doi.org/10.3390/biom9090392
Chicago/Turabian StyleŠudomová, Miroslava, Sherif T. S. Hassan, Haroon Khan, Mahsa Rasekhian, and Seyed Mohammad Nabavi. 2019. "A Multi-Biochemical and In Silico Study on Anti-Enzymatic Actions of Pyroglutamic Acid against PDE-5, ACE, and Urease Using Various Analytical Techniques: Unexplored Pharmacological Properties and Cytotoxicity Evaluation" Biomolecules 9, no. 9: 392. https://doi.org/10.3390/biom9090392