Amit Singh

Amit Singh
Banaras Hindu University | BHU · Department of Pharmacology

MBBS, MD, PhD, LL.B, PGDIPR, PDCR
Drug Development, Diabetes

About

80
Publications
19,622
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1,368
Citations
Additional affiliations
January 2015 - present
Institute of Medical Sciences (Banaras Hindu University)
Position
  • Head of Faculty
Description
  • Drug Development
Education
July 1992 - December 1997

Publications

Publications (80)
Article
The JAK2/STAT signaling cascades facilitates receptor signals which is responsible for cell growth, survival and homeostasis. Ligand binding to JAKs causes phosphorylation other proteins known as STATs, which translocate to the nucleus and regulate transcription of several important proteins. Growth hormone, prolactin and γ-interferon known agonist...
Article
Full-text available
The histone acetylation-deacetylation at lysine regulates the functions of many cellular proteins. An increased expression of HDAC6 can cause an increased amount of deacetylated histones, which leads to an inhibition of gene expression and has been associated with cancer cell proliferation. The present study screened the ZINC database to find novel...
Article
Tyrosine kinase (TK) is an important protein responsible for phosphorylation of variety of proteins that helps in signal transduction process in transferring signal to regulate various physiological and biochemical processes. Drugs inhibiting signal transduction pathways can be a very rational approach to inhibit cellular physiological and biochemi...
Article
Isoniazid is an important component of first-line antitubercular therapy. The drug at its therapeutic dose is known to cause hepatitis and peripheral neuropathy. The association of isoniazid with pure delirium is rare. Here, we present an interesting case of new-onset delirium associated with isoniazid in an elderly female with spinal tuberculosis....
Preprint
Neuroleptic malignant syndrome(NMS) is a lethal idiosyncratic reaction characterized by fever, rigidity, altered sensorium and autonomic disturbances. Antidopaminergic drugs such as haloperidol, dopamine depletors like reserpine and atypical antipsychotics such as risperidone, are the major drugs implicated in NMS. Levosulpiride belongs to the benz...
Preprint
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Phytochemicals are rich source of bioactive constituents and can be used as another alternative to currently used drugs for diseases like Diabetes mellitus. The potential of Isoliquiritigenin (a constituent of Pterocarpus marsupium) as PPAR𝛾 agonist was evaluated by in silico technique. Autodock results showed that Tyr327, and Tyr473 of the PPARγ f...
Article
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Background We provide the first post-approval safety analysis of COVISHIELD in health care workers (HCWs) in northern India. Methods This continuing prospective observational study (February 2021 to May 2022) enrolled participants ≥18 years receiving COVISHIELD vaccination. Primary outcome was safety and reactogenicity. Categories (FDA toxicity gr...
Article
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The present aim of this investigation was to evaluate the effect of catechin from faba beans on oxidative stress and glucose uptake in yeast cells. Flow cytometry approach indicated that 2-NBDG (1.98 ± 0.37) seed extract had a lower relative fluorescence signal than methanol (5.98 ± 0.67) and acetone seed extract (4.43 ± 0.55). In comparison to the...
Preprint
Full-text available
Vaccines are an important public health measure for tiding over the COVID-19 pandemic. Several vaccines have been approved in different countries for emergency use. In India, two vaccines have been currently approved- COVISHIELD (Serum Institute of India (SII)) which is a recombinant simian adenovirus-based vaccine and COVAXIN (Bharat Biotech) whic...
Article
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The motive of this article is to review the pharmacological and clinical aspects of esketamine (ESK), an NMDA-receptor antagonist approved recently by the FDA for treatment-resistant depression (TRD). PubMed/Medline database was searched using keywords ‘esketamine’ and ‘depression’, ‘S-ketamine’ and ‘depression’, and ‘NMDA antagonist’ and ‘depressi...
Article
Coronaviruses are RNA viruses that infect varied species including humans. TMPRSS2 is gateway for SARS CoV-2 entry into the host cell. It causes proteolytic activation of spike protein and discharge of the peptide into host cell. The TMPRSS2 inhibition could be one of the approaches to stop the viral entry, therefore, interaction pattern and bindin...
Article
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India has witnessed a high number of COVID-19 cases, but mortality has been quite low, and most cases have been asymptomatic or mild. In early April, we had hypothesized a low COVID-19 mortality in India, based on the concept of cross-immunity. The presence of cross-immunity is presumed to lead to a milder course of disease and allow the time neces...
Article
Plant derived product can be used as other alternatives to currently used drugs for controlling chronic diseases like Diabetes mellitus. The potential of Coagulin L (a constituent of Withania coagulans) as dipeptidyl peptidase-4 (DPP-4) inhibitor was evaluated by molecular modelling study. It was observed that amino acid residues such as Glu205, Gl...
Article
Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has spread worldwide and caused widespread devastation. In the absence of definitive therapy, symptomatic management remains the standard of care. Repurposing of many existing drugs including several anti-viral drugs is being attempted to tackle the COVID-19 pandemic. However, most of the...
Article
The severe acute respiratory syndrome corona virus-2 (SARS-CoV-2) has resulted in almost 18 million cases of COVID-19 (Corona virus disease-2019) and more than 670000 deaths worldwide since December 2019. In the absence of effective antiviral therapy and vaccine, treatment of COVID-19 is largely symptomatic. By making use of its spike (S) protein,...
Article
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Sacubitril/Valsartan is a novel Angiotensin Receptor Blocker-Neprilysin Inhibitor (ARNI) approved for the treatment of patients with NYHA class II-IV Heart failure with reduced ejection fraction (HFrEF). Hypotension, renal dysfunction, upper respiratory tract infections and angioedema are the common adverse effects reported with sacubitril/valsarta...
Article
Leucoefdin an important constituent of various fruits such as banana, raspberry, etc. was explored to target MPro protease of SARS Co-V 2. Ligand was found to bind at active site of MPro with large negative binding energies in molecular docking and simulation study. The docking results showed that Leucoefdin interacted with the MPro by forming hydr...
Article
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Hypoglycemic potential and xanthine-oxidase (XO) activity of polyphenols from faba bean were evaluated in the 3T3-L1 cell line, and an interaction study in silico with XO was performed with considerable bioactive components of acetone extract of faba beans. The protonated and fragmented behavior of acetone seed extract revealed the presence of gall...
Article
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The present case study is of evaluation of Grade 3 obesity who visited the Arogyadhama (SVYASA University, Bangalore). Conversations with the patient uncovered that the patient was being treated for obesity and patient portrayed his capacity to deal with the mental pressure related with overweight. He credited it to the inspirational demeanor creat...
Article
The chemo-profiling of ethanolic extract of faba beans seeds was performed and explored as an a-glucosidase inhibitor. The inhibition of a-glucosidase is one of the alternatives approach to control postprandial hyperglycemia by, resulting in the delay of the carbohydrate digestion of absorbable monosaccharides. Ethanolic seed extract showed phenoli...
Article
Full-text available
The chemo-profiling of ethanolic extract of faba beans seeds was performed and explored as an a-glucosidase inhibitor. The inhibition of a-glucosidase is one of the alternatives approach to control postprandial hyperglycemia by, resulting in the delay of the carbohydrate digestion of absorbable monosaccharides. Ethanolic seed extract showed phenoli...
Article
Full-text available
To study the effect of methanolic extract of Phyllanthus niruri on animal model of Diabetes Mellitus. Diabetes Mellitus was induced in rats by injecting Streptozotocin (60mg/ kg) intraperitonealy. Blood glucose was measured on day 3by GOD-POD method. Rats having fasting blood glucose >250 mg/dl were further selected for study. Four groups were crea...
Article
Furosemide (FSM) is commonly used in the treatment of edema associated with congestive cardiac failure, cirrhosis of the liver, renal disease, including the nephrotic syndrome and hypertension. However, in ascites, it is clinically limited due to its frequent dosing and short biological half-life and its prolonged-release preparations are not avail...
Article
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Efficacy of Sahaj Vati containing Shilajeet, Guggul, Haridra and Chitrak has been evaluated at dose of 100, 200 and 400 mg/kg body weight after screening the appropriate diet induced obesity model (monosodium glutamate and cafeteria diet induced). It has been observed that both monosodium glutamate and cafeteria diet increases body weight but cafet...
Article
Full-text available
Efficacy of Sahaj Vati containing Shilajeet, Guggul, Haridra and Chitrak has been evaluated at dose of 100, 200 and 400 mg/kg body weight after screening the appropriate diet induced obesity model (monosodium glutamate and cafeteria diet induced). It has been observed that both monosodium glutamate and cafeteria diet increases body weight but cafet...
Article
Full-text available
Ciprofloxacin, a poorly soluble drug-loaded chitosan nanoparticle, was prepared for the treatment of microbial infections. Nanoformulation of ciprofloxacin was prepared using 85% deacetylated chitosan as a biodegradable polymer and tripolyphosphate (TPP) as a cross-linking agent by ionotropic gelation. It was further evaluated and characterized on...
Article
Full-text available
Objective: The present work incorporates the study of gastric antiulcer and ulcer healing effects of dried Punica granatum (PG) peel 50% ethanol extract (PGE) in rats.Methods: PGE (100 mg/kg) was administered orally once daily to rats either before or after induction of gastric ulcers (GU) for 7 d. Antiulcer effects of PGE were seen against acute G...
Article
Polymeric nanoparticles such as chitosan nanoparticles have been widely investigated in recent years as delivery systems for therapeutic molecules like amphotericin B. In this study antifungal drug like amphotericin B loaded chitosan nanoparticles were prepared via ionic gelation of tripolyphosphate (TPP) and chitosan. The optimum encapsulation eff...
Article
Abstract Apoptosis (programmed cell death) is a process by which cells died after completing physiological function, or after a severe genetic damage. Apoptosis is mainly regulated by the Bcl-2 family of proteins. Anti apoptotic protein Bcl-2 prevents the Bax activation/oligomerization to form heterodimer which is responsible for release of the cyt...
Article
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The study incorporates the wound healing potential of Aegle marmelos fruit pulp extract (AME) on excision, incision, and dead space wound models in rats. AME (200 mg/kg) was administered orally once daily for variable days depending on the type of wound ulcer study. AME was studied for its wound breaking strength (incision wound), rate of contracti...
Article
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Background: Aegle marmelos (AM) fruit has been advocated in indigenous system of medicine for the treatment of various gastrointestinal disorders, fever, asthma, inflammations, febrile delirium, acute bronchitis, snakebite, epilepsy, leprosy, myalgia, smallpox, leucoderma, mental illnesses, sores, swelling, thirst, thyroid disorders, tumours and u...
Article
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The present study evaluates the effects of extract of Musa sapientum fruit (MSE) on ulcer index, blood glucose level and gastric mucosal cytokines, TNF-alpha and IL-1beta and growth factor, TGF-alpha (affected in diabetes and chronic ulcer) in acetic acid (AA)-induced gastric ulcer (GU) in diabetic (DR) rat. MSE (100 mg/kg, oral), omeprazole (OMZ,...
Article
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Azadirachta indica leaves indicated the presence of active principles with proven antioxidants, antiinflammatory, immunomodulatory, free radical scavenging and healing properties. In the present study we evaluated the healing effects of 50% ethanol extract of dried leaves of Azadirachta indica on trinitrobenzene sulfonic acid-induced colitis in rat...
Article
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The present study aims to evaluate healing effect of 50% ethanolic extract of Terminalia chebula fruit pulp (TCE) on trinitrobenzene sulfonic acid (TNBS, intra-colonic route) induced colitis in rats. TCE (600 mg/kg, oral) was studied in TNBS-induced colitis for its effects on fecal output, food and water intake and body weight changes, histology, a...
Article
MLN4924 is an adenosine sulfamate analog that generates the inhibitory NEDD8-MLN4924 covalent complex. A single nucleotide transition that changes alanine 171 to threonine (A171T) of the NAE subunit UBA3 reduces the enzyme's sensitivity for MLN4924. Our molecular dynamics simulation study revealed that A171T transition brought remarkable conformati...
Article
Gallic acid, a predominant polyphenol, has been shown to inhibit carcinogenesis in animal models and in vitro cancerous cell lines. The inhibitory effect of gallic acid on cancer cell growth is mediated via the modulation of genes which encodes for cell cycle, metastasis, angiogenesis and apoptosis. Gallic acid inhibits activation of NF-κB and Akt...
Data
Full-text available
Graded doses of 50% ethanolic extract of dried fruit pulp of Aegle marmelos (AME) (100, 200 and 400 mg/kg) daily for 14 days in acetic acid (AA)-induced colitis in rats showed 200 mg/kg of AME as an optimal effective dose against AA-induced colonic damage score and weight. This dose (200 mg/kg; po) was further studied in AA-induced colitis for its...
Article
Full-text available
Graded doses of 50% ethanolic extract of dried fruit pulp of Aegle marmelos (AME) (100, 200 and 400 mg/kg) daily for 14 days in acetic acid (AA)-induced colitis in rats showed 200 mg/kg of AME as an optimal effective dose against AA-induced colonic damage score and weight. This dose (200 mg/kg; po) was further studied in AA-induced colitis for its...
Article
Inhibition of the MDM2‐p53 interaction has become a new therapeutic strategy to activate wild type p53 in tumors. Quercetin and taxifolin bind to p53 binding hydrophobic groove of MDM2, and alter the conformation of groove as evidenced by 65 ns molecular dynamics simulation. Quercetin showed hydrogen bonding with Gly 16, Ser 17, Phe 55 and Val 93 a...
Article
Full-text available
Objective To evaluate the healing effects of extract of dried leaves of Azadirachta indica (Neem) on acetic acid-induced colitis in rats. Neem tree is known as ‘arishtha’ in Sanskrit, meaning ‘reliever of sicknesses’.Methods50% ethanolic extract of Azadirachta indica leaves was administered orally, once daily for 14 days in rats after the induction...
Article
Full-text available
The present study has evaluated the healing effects of extract of dried fruit pulp of Terminalia chebula (TCE) on acetic acid (AA)-induced colitis in rats. TCE (600 mg/kg) showed healing effects against AA-induced colonic damage score and weight when administered orally daily for 14 days. TCE was further studied for its effects on various physical...
Article
Alzheimer's disease (AD), a neurodegenerative disorder, is directly related to the aggregation of Aβ peptides. These peptides can self-assemble from monomers to higher oligomeric or fibrillar structures in a highly ordered and efficient manner. This self-assembly process is accompanied by a structural transition of the aggregated proteins from thei...
Chapter
Dried powder of pulp of unripe plantain banana (Musa sapientum var. paradisiaca, MS) have shown both anti-ulcerogenic and ulcer healing activities by increasing the defensive mucosal factors rather than affecting the offensive acid-pepsin secretions. Proinflammatory cytokines, tumour necrosis factor-á (TNF-á) and interleukin-1â (IL-1â) and transfor...
Article
Full-text available
A great number of aromatic, spicy, medicinal and other plants contain chemical compounds exhibiting antioxidant properties. Numerous studies were carried out on some of these plants, e.g. rosemary, sage and oregano, which resulted in a development of natural antioxidant formulations for food, cosmetic and other applications. In this study, the anti...
Article
INTRODUCTION Antioxidantsarevitalsubstanceswhichhavetheabilityto defend the body from damage caused by free radical induced oxidative stress. [1] Oxidative stress, induced by oxygenradicals,isaprimaryfactorinvariousdegenerative diseases, such as cancer, atherosclerosis, gastric ulcer, diabetes and other disease conditions. Human body has numerous m...
Article
Inhibition of the MDM2–p53 interaction has been becomes a new therapeutic strategy to activate wild-type p53 in tumors. Molecular dynamics (MD) simulations were used to study the effects of quercetin and taxifolin on MDM2–p53 complex. We found that binding of ligands (quercetin and taxifolin) led to the dissociation of MDM2–p53 complex. Analyses of...
Article
Hsp90 (heat shock protein 90), a molecular chaperone, stabilizes more than 200 mutated and over expressed oncogenic proteins in cancer development. Cdc37 (cell division cycle protein 37), a co-chaperone of Hsp90, has been found to facilitate the maturation of protein kinases by acting as an adaptor and load these kinases onto the Hsp90 complex. Tax...
Article
Full-text available
Problem statement: Present study was aimed to explore the acute and sub-acute toxicities studies with orally administered 50% ethanolic leaves extract of Murraya paniculata. Approach: Acute toxicity (oral single dose, 50-2000 mg kg −1) includes any mortality and CNS and ANS toxicities in mice while, sub-acute toxicity (100, 200 and 400 mg kg −1 , o...
Article
The VEGFR-2 kinase specific intracellular signalling cascades leading to proliferation, migration, survival of endothelial cells and increased permeability of vessels which contributes to angiogenesis. ATP is essentially required by VEGFR-2 to perform phosphorylation of specific proteins and to maintain cascad e downstream. Taxifolin (plant polyphe...
Conference Paper
Objective: To study wound healing effects of 50% ethanolic extract of fruit pulp of T. chebula (TCWE) in rats. Materials and Methods: TCWE (600 mg/kg), suspended in 1% CMC, was administered orally once daily to C-F rats (150-200 g) for variable days depending on the type of wound ulcer study (10 days both for Incisional and Dead space wound and 24...
Article
Full-text available
Objectives: Study of ulcer healing effects of 50% ethanolic extract of dried fruit pulp of Aegle marmelos (AMWE) on acetic acid (AA)- induced colitis in rats. Materials and Methods: Experimental colitis was produced in rats by intracolonic administration of AA (10%, 0.2 ml). AMWE (200 mg/kg) and sulfasalazine (SS, 100 mg/ kg) were orally administer...
Article
Full-text available
Series of pyrazole ester prodrugs analogues have been synthesized and found to contain highly potent inhibitors of the cyclooxygenase-2 (COX-2) enzyme. The paper describes synthesis of the target pyrazole analogues. The structure of the synthesized mutual ester prodrugs (6-8c) were confirmed by (1)H-, (13)C-NMR mass spectroscopy (MS) and their puri...
Article
Haptoglobin (Hp) is a plasma glycoprotein, the main biological function of which is to bind free hemoglobin (Hb) and prevents the loss of iron and subsequent kidney damage following hemolysis. In human, the Hp locus is polymorphic with two co-dominant alleles (Hp1 & Hp2) that yield three distinct genotype/ phenotype (Hp 1-1, Hp 2-1, Hp 2-2).The hap...