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7. Pharmacological evaluation of newly synthesized benzimidazole derivative for anti-Alzheimer potential.

Author

Ahmed, Aleeza, Khan, Arif-ullah, Nadeem, Humaira, Imran, Muhammad, and Irshad, Nadeem

Subjects
BENZIMIDAZOLES, BENZIMIDAZOLE derivatives, ENZYME-linked immunosorbent assay, WESTERN immunoblotting, BENZOIC acid, NEUROFIBRILLARY tangles, ATHEROSCLEROTIC plaque
Abstract

Backgound: Alzheimer disease (AD) is a disastrous disease characterized by accretion of amyloid-beta plaques, neurofibrillary tangles inducing oxidative stress, loss of neuronal functions and continuous progression of cognitive impairment leading to severe dementia. Material and Methods: The newly synthesized benzimidazole derivative 4-chloro-3-(2-phenyl-1H-benzimidazole-1-sulfonyl) benzoic acid (CB) was evaluated for its anti-Alzheimer activity using in silico, in vivo, in vitro and molecular techniques (ELISA, WB & IHC). Results:In-silico studies revealed that CB has atomic contact energy values of −3.9 to −8.9 kcal/mol against selected targets. In vitro assay showed that CB caused acetylcholinesterase (AChE) and diphenyl-1-picrylhydrazyl inhibition. In-vivo findings revealed improvement in dementia as observed in the morris water maze test and Ymaze test. Amyloid-beta disaggregation, increased level of anti-oxidants, decreased expressions of inflammatory markers and enhanced cellular architecture were found in the cortex and hippocampus of treated rats in the histopathological examination, immunohistochemistry analysis, enzyme-linked immunosorbent assay and western blot analysis. Conclusions: This study revealed that CB possess different binding affinities with the Alzheimer-related targets and it possess anti-Alzheimer activity, mediated via AChE and amyloid-beta inhibition, anti-oxidant and anti-inflammatory pathways. [ABSTRACT FROM AUTHOR]

Published
2024
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9. Effects of dapagliflozin against streptozotocin and isoproterenol-induced heart failure via investigating NLRP3 and PPAR-γ signaling.

Author

Ijaz, Khadija, Khan, Arif-Ullah, Kamal, Yousaf, and Irshad, Nadeem

Abstract

Heart failure is a condition in which the heart's one or both ventricles are unable to either receive an adequate amount of blood or eject an adequate amount of blood. Diabetes is considered one of the major risk factors for cardiovascular diseases. The current research is designed to evaluate the cardioprotective effects of dapagliflozin in streptozotocin and isoproterenol-induced comorbid rats. The COX-2, TNF-α, NF-Κ B, NLRP3, PPAR-γ, CKMB, TROP-I, AR, GP and SGLT were docked against dapagliflozin, propranolol and metformin. Dapagliflozin restored adequate blood flow and halted myofibril damage. Moreover, it's evident from this study that dapagliflozin significantly decreased serum concentration of various blood markers, decreased relative growth rate and QT interval prolongation, as compared to the negative control group. However, it improved the ventricular ejection fraction in rats of the treatment group. The GST, GSH and CAT levels were increased, as compared to normal. On the contrary, a decrease in LPO concentrations was observed. Evaluation of the coronal section of heart tissues showed the anti-inflammatory expressions evaluated through H & E staining and immunohistochemical techniques and with ELISA and PCR. In a nutshell, dapagliflozin reverses myocardial necrosis and apoptosis. [ABSTRACT FROM AUTHOR]

Published
2024
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10. Neuroprotective Effects of Melatonin and Celecoxib against Ethanol-Induced Neurodegeneration: A Computational and Pharmacological Approach [Corrigendum]

Author

Al Kury, Lina, primary, Zeb, Alam, additional, Abidin, Zain Ul, additional, Irshad, Nadeem, additional, Malik, Imran, additional, Mohsin Alvi, Arooj, additional, Khan Khalil, Atif Ali, additional, Ahmad, Sareer, additional, Faheem, Muhammad, additional, Khan, Arif-ullah, additional, Shah, Fawad Ali, additional, and Li, Shupeng, additional

Published
2023
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16. Additional file 1 of Pharmacological evaluation of newly synthesized organotin IV complex for antiulcer potential

Author

Azmatullah, Syed, Khan, Arif-ullah, Qazi, Neelam Gul, Nadeem, Humaira, and Irshad, Nadeem

Abstract

Additional file 1: Figure S1. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and omeprazole with hydrogen potassium atipase pump (H+/K+-ATPase) evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S2. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and phenoxy benzamine with muscarinic receptor (M1) respectively, evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S3. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4- nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and ranitidine with histamine receptor (H2) respectively, evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S4. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4- nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and aspirin with cyclooxiginase-1 (COX1) respectively, evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S5. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and meclofenamate with cyclooxiginase-2 (COX2) respectively, evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S6. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and dinopristone with prostaglandin-E2 (PGE2) respectively, evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S7. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4- nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and curcumin with nuclear factor kappa B (NFĸB) respectively, evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S8. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and aspirin with tumor necrosis factor alpha (TNF- α) respectively, evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S1A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and Omeprazole with hydrogen potassium ATPase (H+/K+-ATPase) evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S2A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and Phenoxy-benzamine with Muscarinic receptor (M1) evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S3A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and Ranitidine with histaminergic receptor (H2), evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S4A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and Aspirin with cyclooxygenase-1 (COX1), evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S5A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and Meclofinamate with cyclooxygenase-2 (COX2) evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S6A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl) amino)-4-oxobut-2-enoate (DTN) and Dinopristone with prostaglandin-E2 (PGE2), evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S7A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl)amino)-4-oxobut-2-enoate (DTN) and Curcumin with Nuclear Factor kappa-B (NFκB) evaluated through Biovia Discovery Studio Visualizer (DSV) 2016. Figure S8A. (A) and (B) represents 2D-interactions of 2E,2′E) dibutylstannanediyl bis(4-(4-nitrophenyl) amino)-4-oxobut-2-enoate (DTN) and aspirin with Tumor necrosis factor alpha (TNF-α) evaluated through Biovia Discovery Studio Visualizer (DSV) 2016.

Published
2022
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17. Blood pressure lowering effect of selected pyrimidine derivatives mediated through inhibition of calcium channel: A computational approach.

Author

Irshad, Nadeem, Khan, Arif-ullah, Kamal, Yousaf, and Iqbal, Muhammad Nasir

Abstract

Pyrimidine 2, 4, 6-trione derivatives are known to have L-type calcium channel blockade activity due to which they are quite effective in cardiovascular diseases along with cancer, epilepsy and inflammatory disorders. The chemoinformatics prediction for test compounds: 5-(3-Hydroxybenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-5), 5-(4-Hydroxybenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-8), 5-(3-Chlorobenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-9) and 5-(4-Chlorobenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-10) was investigated. The druglikeliness and pharmacokinetic properties (PKs) of test compounds calculated using Molinspiration & Swiss ADME online servers. These test drugs subjected to molecular docking analysis and molecular dynamic (MD) simulation to calculate their binding energies with hypertensive and platelet aggregatory proteinaceous targets and their stability against calcium channel. The druggability and PKs of selected compounds exhibited that these compounds could be represented as potential candidates for further development into antihypertensive-like agents. The docking results indicated that binding energies ranged between -5 and -8.8 kcal/mol. Compounds showed good binding energies against calcium channels (CC) and subjected to molecular dynamic simulation to assess the stability of proteinligand complex. The results showed that all the ligands form stable complexes with the CC, though SR-9 and SR-10 had enhanced stability when compared to SR-5 and SR-8. [ABSTRACT FROM AUTHOR]

Published
2022
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20. Neuroprotective effects of melatonin and celecoxib against ethanol-induced neurodegeneration: a computational and pharmacological approach

Author

Al Kury,Lina, Zeb,Alam, Abidin,Zain Ul, Irshad,Nadeem, Malik,Imran, Mohsin Alvi,Arooj, Khan Khalil,Atif Ali, Ahmad,Sareer, Faheem,Muhammad, Khan,Arif-ullah, Shah,Fawad Ali, and Li,Shupeng

Subjects
Drug Design, Development and Therapy
Abstract

Lina T Al Kury,1 Alam Zeb,2 Zain Ul Abidin,2 Nadeem Irshad,3 Imran Malik,2 Arooj Mohsin Alvi,2 Atif Ali Khan Khalil,4 Sareer Ahmad,4 Muhammad Faheem,2 Arif-Ullah Khan,2 Fawad Ali Shah,2 Shupeng Li51College of Natural and Health Sciences, Zayed University, Abu Dhabi, United Arab Emirates; 2Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, Pakistan; 3Department of Pharmacy, Quaid-I-Azam University, Islamabad, Pakistan; 4Rehman Medical Institute, Peshawar, Pakistan; 5State Key Laboratory of Oncogenomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, People’s Republic of ChinaPurpose: Melatonin and celecoxib are antioxidants and anti-inflammatory agents that exert protective effects in different experimental models. In this study, the neuroprotective effects of melatonin and celecoxib were demonstrated against ethanol-induced neuronal injury by in silico, morphological, and biochemical approaches.Methods: For the in silico study, 3-D structures were constructed and docking analysis performed. For in vivo studies, rats were treated with ethanol, melatonin, and celecoxib. Brain samples were collected for biochemical and morphological analysis.Results: Homology modeling was performed to build 3-D structures for IL1β), TNFα, TLR4, and inducible nitric oxide synthase. Structural refinement was achieved via molecular dynamic simulation and processed for docking and postdocking analysis. Further in vivo experiments showed that ethanol induced marked neuronal injury characterized by downregulated glutathione, glutathione S-transferase, and upregulated inducible nitric oxide synthase. Additionally, ethanol increased the expression of TNFα and IL1β. Finally, neuronal apoptosis was demonstrated in ethanol-intoxicated animals using caspase 3 and activated JNK staining. On the other hand, melatonin and celecoxib treatment ameliorated the biochemical and immunohistochemical alterations induced by ethanol.Conclusion: These results demonstrated that ethanol induced neurodegeneration by activating inflammatory and apoptotic proteins in rat brain, while melatonin and celecoxib may protect rat brain by downregulating inflammatory and apoptotic markers.Keywords: simulation, docking, cortex, hippocampus, ethanol, neurodegeneration

Published
2019

25. Hypoglycaemic effects of Methanolic extract of Canscora decussata (Schult) whole-plant in normal and alloxan-induced diabetic rabbits.

Author

Irshad, Nadeem, Akhtar, Muhammad Shoaib, Bashir, Sajid, Hussain, Azhar, Shafiq, Muhammad, Iqbal, Javeid, and Malik, Abdul

Abstract

In present study hypoglycaemic effects of the crude powdered C. decussata and its methanolic extract (ME) in alloxan diabetic rabbits were evaluated. The hypoglycaemic effect was measured by blood glucose, insulin level, HbA1c and his to pathology of pancreas. Glucose lowering effect of the ME was studied in diabetic rabbits. The effects of extract on blood glucose, body weight, food in take, fluid intake, OGTT were also evaluated. The results showed that 0.5,1 and 2g/kg of the powder significantly decreased blood glucose levels in normal rabbits and diabetic rabbits at the intervals checked. Oral intake of pioglitazone also reduced the levels in these rabbits. Synergistic hypoglycaemic effect of 600mg/kg of ME with different doses of insulin (2 & 3unit/kg, s/c) further reduced blood glucose levels of treated alloxan-diabetic rabbits. The oral glucose tolerance test revealed lowered area under curve values in ME treated rabbits. Treatment with ME (400 and 600 mg/kg) for 30 days showed highly significant decrease in blood glucose level by augmenting insulin secretion, HbA1cand significant increase in body weight, serum insulin levels in treated diabetic rabbits. Histopathology study showed regeneration of β-cells. These studies have, therefore, supported the traditional use of this herb in diabetic patients. [ABSTRACT FROM AUTHOR]

Published
2015

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