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  1. Article ; Online: Therapeutic potential of reserpine in metabolic syndrome: An evidence-based study.

    Verma, Kanika / Paliwal, Sarvesh / Sharma, Swapnil

    Pharmacological research

    2023  Volume 190, Page(s) 106728

    MeSH term(s) Humans ; Reserpine/therapeutic use ; Metabolic Syndrome/drug therapy
    Chemical Substances Reserpine (8B1QWR724A)
    Language English
    Publishing date 2023-03-13
    Publishing country Netherlands
    Document type Letter ; Comment
    ZDB-ID 1003347-6
    ISSN 1096-1186 ; 0031-6989 ; 1043-6618
    ISSN (online) 1096-1186
    ISSN 0031-6989 ; 1043-6618
    DOI 10.1016/j.phrs.2023.106728
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: N1-benzenesulfonyl-2-pyrazoline hybrids in neurological disorders: Syntheses, biological screening and computational studies.

    Tripathi, Avinash C / Upadhyay, Savita / Paliwal, Sarvesh / Saraf, Shailendra K

    EXCLI journal

    2018  Volume 17, Page(s) 126–148

    Abstract: A novel series of 1,3,5-trisubstituted-2- ... ...

    Abstract A novel series of 1,3,5-trisubstituted-2-pyrazolines
    Language English
    Publishing date 2018-01-19
    Publishing country Germany
    Document type Journal Article
    ISSN 1611-2156
    ISSN 1611-2156
    DOI 10.17179/excli2017-871
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Mitochondrial transfer restores impaired liver functions by AMPK/ mTOR/PI3K-AKT pathways in metabolic syndrome.

    Paliwal, Swati / Jain, Smita / Mudgal, Pallavi / Verma, Kanika / Paliwal, Sarvesh / Sharma, Swapnil

    Life sciences

    2023  Volume 332, Page(s) 122116

    Abstract: Aim: We investigated the effect of mitochondria transfer in high fat diet and streptozotocin (HFD + STZ) induced metabolic syndrome (MeS) in rats. The effect of mitochondria transfer in MeS with co-existing hypertension, hyperlipidaemia, diabetes and ... ...

    Abstract Aim: We investigated the effect of mitochondria transfer in high fat diet and streptozotocin (HFD + STZ) induced metabolic syndrome (MeS) in rats. The effect of mitochondria transfer in MeS with co-existing hypertension, hyperlipidaemia, diabetes and fatty liver together, has not been reported.
    Materials and methods: Heathy mitochondria was transferred intravenously and the effect on several physiological parameters and biochemical parameters were examined in HFD + STZ rats. In addition, RNA-sequencing of healthy liver tissues was performed to elucidate the molecular pathways affected by mitochondria transfer in restoring metabolic health.
    Key findings: We observed reduction in both systolic and diastolic blood pressure levels, reduced blood glucose levels, and a marked reduction in serum lipid profiles. The levels of alanine transaminase (ALT) and aspartate transaminase (AST) also improved along with evident restoration of liver morphology demonstrated by histopathological analysis. Enhanced mitochondrial biogenetics and reduction in oxidative stress and inflammatory markers was also observed. The pathway enrichment analysis revealed reduction in insulin resistance, inflammatory markers, regulation of mitochondrial bioenergetics, calcium ion homeostasis, fatty-acid β-oxidation, cytokine immune regulators, and enhanced lipid solubilisation. The significant effect of healthy mitochondria transfer in restoration of metabolic functions was observed by the activation of PI3K-AKT, AMPK/mTOR pathways and cytokine immune regulators, suggesting that inflammatory mediators were also significantly affected after mitochondria transfer.
    Significance: This study, provides insights on molecular processes triggered by mitochondria transfer in fatty liver regeneration and improvement of overall metabolic health.
    MeSH term(s) Rats ; Animals ; Metabolic Syndrome/metabolism ; Proto-Oncogene Proteins c-akt/metabolism ; AMP-Activated Protein Kinases/metabolism ; Phosphatidylinositol 3-Kinases/metabolism ; Liver/metabolism ; Mitochondria/metabolism ; Fatty Liver/metabolism ; Insulin Resistance ; TOR Serine-Threonine Kinases/metabolism ; Cytokines/metabolism ; Lipids/pharmacology ; Diet, High-Fat/adverse effects
    Chemical Substances Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; AMP-Activated Protein Kinases (EC 2.7.11.31) ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; TOR Serine-Threonine Kinases (EC 2.7.11.1) ; Cytokines ; Lipids ; mTOR protein, rat (EC 2.7.1.1)
    Language English
    Publishing date 2023-09-20
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 3378-9
    ISSN 1879-0631 ; 0024-3205
    ISSN (online) 1879-0631
    ISSN 0024-3205
    DOI 10.1016/j.lfs.2023.122116
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  4. Article ; Online: Simvastatin ameliorates oxidative stress levels in HepG2 cells and hyperlipidemic rats.

    Verma, Kanika / Makwana, Shikha / Paliwal, Sarvesh / Paliwal, Vartika / Jain, Smita / Paliwal, Swati / Sharma, Swapnil

    Current research in pharmacology and drug discovery

    2022  Volume 3, Page(s) 100088

    Abstract: Simvastatin is an established anti-hyperlipidemic drug and few studies have indicated its role in the mitigation of oxidative stress. However, a systematic study considering molecular binding/interaction of simvastatin with anti-oxidant enzymes followed ... ...

    Abstract Simvastatin is an established anti-hyperlipidemic drug and few studies have indicated its role in the mitigation of oxidative stress. However, a systematic study considering molecular binding/interaction of simvastatin with anti-oxidant enzymes followed by confirmational
    Language English
    Publishing date 2022-01-28
    Publishing country Netherlands
    Document type Journal Article
    ISSN 2590-2571
    ISSN (online) 2590-2571
    DOI 10.1016/j.crphar.2022.100088
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  5. Article ; Online: New insights on mode of action of vasorelaxant activity of simvastatin.

    Verma, Kanika / Shukla, Rahul / Dwivedi, Jaya / Paliwal, Sarvesh / Sharma, Swapnil

    Inflammopharmacology

    2023  Volume 31, Issue 3, Page(s) 1279–1288

    Abstract: Simvastatin is a semisynthetic inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and is used extensively to treat atherosclerotic cardiovascular disease. Apart from the lipid-lowering effect, simvastatin has been documented to offer ... ...

    Abstract Simvastatin is a semisynthetic inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and is used extensively to treat atherosclerotic cardiovascular disease. Apart from the lipid-lowering effect, simvastatin has been documented to offer impressive vasorelaxant activity. However, the mechanism associated with this vasorelaxant activity has yet not been substantially explored. Thus, the present study has aimed to elucidate the mechanism(s) associated with simvastatin-induced vasorelaxation using an established rat aortic ring model. The results from the study depicted that simvastatin caused significant relaxation in aortic rings pre-contracted with phenylephrine and potassium chloride (KCl). The vasorelaxant effect of simvastatin was attenuated by methylene blue (sGC-dependent cyclic guanosine monophosphate (cGMP) inhibitor), N
    MeSH term(s) Rats ; Animals ; Vasodilator Agents/pharmacology ; Calcium Channels/metabolism ; Aorta, Thoracic ; Calcium Signaling ; Enzyme Inhibitors ; Endothelium, Vascular
    Chemical Substances Vasodilator Agents ; Calcium Channels ; Enzyme Inhibitors
    Language English
    Publishing date 2023-04-10
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1080058-x
    ISSN 1568-5608 ; 0925-4692
    ISSN (online) 1568-5608
    ISSN 0925-4692
    DOI 10.1007/s10787-023-01219-8
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: An insight into PI3k/Akt pathway and associated protein-protein interactions in metabolic syndrome: A recent update.

    Verma, Kanika / Jaiswal, Ritika / Paliwal, Sarvesh / Dwivedi, Jaya / Sharma, Swapnil

    Journal of cellular biochemistry

    2023  Volume 124, Issue 7, Page(s) 923–942

    Abstract: Akt, a known serine/threonine-protein kinase B has been revealed to be an imperative protein of the PI3K/Akt pathway. Akt is available in three isoforms, Akt1, Akt2, and Akt3. Ubiquitously expressed Akt1 & Akt2 are essential for cell survival and are ... ...

    Abstract Akt, a known serine/threonine-protein kinase B has been revealed to be an imperative protein of the PI3K/Akt pathway. Akt is available in three isoforms, Akt1, Akt2, and Akt3. Ubiquitously expressed Akt1 & Akt2 are essential for cell survival and are believed to be involved in regulating glucose homeostasis. PI3K/Akt pathway has been evidenced to be associated with metabolic diseases viz. hypertension, dyslipidemia, and diabetes. Akt interacting proteins have been revealed to be scaffold proteins of the PI3K/Akt pathway. Notably, some protein-protein interactions are imperative for the inhibition or uncontrolled activation of these signaling pathways. For instance, Akt interacting protein binds with other protein namely, FOXO1 and mTOR, and play a key role in the onset and progression of metabolic syndrome (MS). The purpose of this review is to highlight the role of the PI3K/Akt pathway and associated protein-protein interactions which might serve as a valuable tool for investigators to develop some new promising therapeutic agents in the management of MS.
    MeSH term(s) Humans ; Proto-Oncogene Proteins c-akt/metabolism ; Phosphatidylinositol 3-Kinases/metabolism ; Metabolic Syndrome ; Signal Transduction ; Protein Isoforms/metabolism
    Chemical Substances Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; Protein Isoforms
    Language English
    Publishing date 2023-07-06
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 392402-6
    ISSN 1097-4644 ; 0730-2312
    ISSN (online) 1097-4644
    ISSN 0730-2312
    DOI 10.1002/jcb.30433
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  7. Article ; Online: Pharmacophore-driven identification of N-methyl-D-receptor antagonists as potent neuroprotective agents validated using

    Sharma, Mukta / Mittal, Anupama / Singh, Aarti / Jainarayanan, Ashwin K / Sharma, Swapnil / Paliwal, Sarvesh

    Biology methods & protocols

    2020  Volume 5, Issue 1, Page(s) bpaa013

    Abstract: Alzheimer's disease (AD), apparently the most widespread reason behind dementia, is delineated by a continuous cognitive weakening in the aged. During its progression, N-methyl-D-aspartate receptor (NMDAR) antagonists are known to play a pivotal part in ... ...

    Abstract Alzheimer's disease (AD), apparently the most widespread reason behind dementia, is delineated by a continuous cognitive weakening in the aged. During its progression, N-methyl-D-aspartate receptor (NMDAR) antagonists are known to play a pivotal part in the mechanisms of learning and memory. Since there is an unmet medical need for the treatment of AD, we aim to identify possible chemical compounds targeted toward N-methyl-D-aspartate receptors. Three-dimensional models are developed to unveil some of the essential characteristics of the N-methyl-D-aspartate receptors by using a collection of already discovered N-methyl-D-aspartate receptor inhibitors. This is followed by virtual screening, which results in novel chemical compounds having the potential to inhibit N-methyl-D-aspartate receptors. Molecular docking studies and analysis promulgated two lead compounds with a high LibDock score. The compounds are shortlisted based on high estimated activity, fit values, LibDock score, no violation of Lipinski's, and availability for procuring. Finally, the shortlisted compounds are tested by employing
    Language English
    Publishing date 2020-07-14
    Publishing country England
    Document type Journal Article
    ISSN 2396-8923
    ISSN (online) 2396-8923
    DOI 10.1093/biomethods/bpaa013
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  8. Article ; Online: Quantitative Structure-Activity Relationship Analysis of Selective Rho Kinase Inhibitors as Neuro-regenerator Agents.

    Kesar, Seema / Paliwal, Sarvesh K / Mishra, Pooja / Chauhan, Monika

    Turkish journal of pharmaceutical sciences

    2019  Volume 16, Issue 2, Page(s) 141–154

    Abstract: Objectives: To understand the role of Rho (serine/threonine) kinases in the treatment of neurological segments, attempts have been made to find potent inhibitors of Rho enzyme by a 2D quantitative structure-activity relationship (QSAR) model.: ... ...

    Abstract Objectives: To understand the role of Rho (serine/threonine) kinases in the treatment of neurological segments, attempts have been made to find potent inhibitors of Rho enzyme by a 2D quantitative structure-activity relationship (QSAR) model.
    Materials and methods: QSAR studies were executed on urea-based scaffolds from aniline and benzylamine analogues, which were aligned for generation of a chemometric-based model. Multivariate statistical approaches were applied including linear and nonlinear analysis such as multiple linear regression, partial least square and artificial neural network for the generation of model, and also an application of (
    Results: Ligand based analysis was implemented and showed excellent statistical relevance such as S value=0.38, F value=48.41, r=0.95, r²=0.91, and r²
    Conclusion: The values of standard statistical parameters reveal the predictive power and robustness of this model and also provide valuable insight into the significance of five descriptors. The acquired physicochemical properties (electronic, topological, and steric) show the important structural features required for activity against Rho kinase. After performing Lipinski's rule of five on urea-based derivatives no molecule was violating the rule. Therefore, these features can be effectively employed for the modeling and screening of active neurological agents as novel Rho kinase inhibitors.
    Language English
    Publishing date 2019-03-27
    Publishing country Turkey
    Document type Journal Article
    ZDB-ID 2238484-4
    ISSN 2148-6247 ; 2148-6247
    ISSN (online) 2148-6247
    ISSN 2148-6247
    DOI 10.4274/tjps.galenos.2018.70288
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  9. Article ; Online: Therapeutic potential of reserpine in metabolic syndrome: An evidence based study.

    Verma, Kanika / Paliwal, Sarvesh / Sharma, Swapnil

    Pharmacological research

    2022  Volume 186, Page(s) 106531

    Abstract: Reserpine is as old as the scientific diagnosis of hypertension. For many years' clinicians have used it for the treatment of high blood pressure, but with the passage of time and introduction of new anti-hypertensive drugs, the usage of reserpine has ... ...

    Abstract Reserpine is as old as the scientific diagnosis of hypertension. For many years' clinicians have used it for the treatment of high blood pressure, but with the passage of time and introduction of new anti-hypertensive drugs, the usage of reserpine has gone down drastically most probably due to poorly understood mechanism of action and multiple misleading adverse effects precisely due to high dosing of reserpine. With an aim to elucidate the specific mechanism of action, we screened reserpine against various targets associated with regulation of blood pressure. Surprisingly reserpine showed remarkable inhibitory potential for soluble epoxide hydrolase an enzyme responsible for pathophysiology of not only hypertension but also hyperlipidemia, diabetes and inflammation collectively known as metabolic syndrome. The in-silico, in-vitro and in-vivo results showed that reserpine has the ability to treat metabolic syndrome effectively by inhibiting soluble epoxide hydrolase.
    MeSH term(s) Humans ; Reserpine/therapeutic use ; Reserpine/pharmacology ; Epoxide Hydrolases/metabolism ; Epoxide Hydrolases/pharmacology ; Metabolic Syndrome/drug therapy ; Blood Pressure ; Hypertension/drug therapy
    Chemical Substances Reserpine (8B1QWR724A) ; Epoxide Hydrolases (EC 3.3.2.-)
    Language English
    Publishing date 2022-11-03
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1003347-6
    ISSN 1096-1186 ; 0031-6989 ; 1043-6618
    ISSN (online) 1096-1186
    ISSN 0031-6989 ; 1043-6618
    DOI 10.1016/j.phrs.2022.106531
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article: 2-pyrazoline derivatives in neuropharmacology: Synthesis, ADME prediction, molecular docking and in vivo biological evaluation.

    Upadhyay, Savita / Tripathi, Avinash C / Paliwal, Sarvesh / Saraf, Shailendra K

    EXCLI journal

    2017  Volume 16, Page(s) 628–649

    Abstract: A novel series of 1,3,5-trisubstituted-2-pyrazoline ... ...

    Abstract A novel series of 1,3,5-trisubstituted-2-pyrazoline derivatives
    Language English
    Publishing date 2017-05-08
    Publishing country Germany
    Document type Journal Article
    ISSN 1611-2156
    ISSN 1611-2156
    DOI 10.17179/excli2017-250
    Database MEDical Literature Analysis and Retrieval System OnLINE

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