Digambar Kumar Waiker, Akash Verma, Akhilesh Akhilesh, Gajendra T.A., Namrata Singh, Anima Roy, Hagera Dilnashin, Vinod Tiwari, Surendra Kumar Trigun, Surya Pratap Singh, Sairam Krishnamurthy, Prem Lama, V. Jo Davisson, Sushant K. Shrivastava,
Our present work demonstrates the successful design and synthesis of a new class of compounds based upon a multitargeted directed ligand design approach to discover new agents for use in Alzheimer's disease (AD). All the compounds were tested for their in vitro inhibitory potential against human acetylcholinesterase (hAChE), human butylcholinesterase (hBChE), β-secretase-1 (hBACE-1), and amyloid β (Aβ) aggregation. Compounds 5d and 5f have shown hAChE and hBACE-1 inhibition comparable to donepezil, while ...
Tópico(s): Alzheimer's disease research and treatments
2023 - American Chemical Society | ACS Chemical Neuroscience
Pidugu Venkata Ravi Kiran, Digambar Kumar Waiker, Akash Verma, Poorvi Saraf, Bhagwati Bhardwaj, Hansal Kumar, Abhinav Singh, Pradeep Kumar, Namrata Singh, Saripella Srikrishna, Surendra Kumar Trigun, Sushant K. Shrivastava,
Our present work demonstrates the molecular hybridization-assisted design, synthesis, and biological evaluation of 22 benzylpiperazine-linked 1,2,4-triazole compounds (PD1-22) as AD modifying agents. All the compounds were tested for their in vitro hChEs, hBACE-1, and Aβ-aggregation inhibition properties. Among them, compound PD-08 and PD-22 demonstrated good hChE and hBACE-1 inhibition as compared to standards donepezil and rivastigmine. Both compounds displaced PI from PAS at 50 µM concentration ...
Tópico(s): Tryptophan and brain disorders
2023 - Elsevier BV | Bioorganic Chemistry
Akanksha Pandey, Surendra Kumar Trigun,
Modulation of autophagy is evolving as a relevant strategy in cancer pathogenesis and therapeutic intervention and hence, needs to be examined as a target for the promising anticancer agents. Fisetin, a dietary flavanol, is emerging as a potent anticancer agent, however, its tumour-specific pharmacological targets remain largely unexplored. This article describes correlative profiles of autophagy and apoptotic markers versus nuclear factor erythroid 2-related factor 2 (Nrf2) and reactive oxygen species ( ...
Tópico(s): Ginseng Biological Effects and Applications
2023 - Wiley | Journal of Cellular Biochemistry
Anamika Anamika, Surendra Kumar Trigun,
Abstract The neurotoxic level of ammonia in the brain during liver cirrhosis causes a nervous system disorder, hepatic encephalopathy (HE), by affecting mitochondrial functions. Sirtuin‐3 (SIRT3) is emerging as a master regulator of mitochondrial integrity, which is currently being focused as a pathogenic hotspot for HE. This article describes SIRT3 level versus mitochondrial dysfunction markers in the hippocampus of the control, the moderate‐grade hepatic encephalopathy (MoHE), developed in thioacetamide‐ ...
Tópico(s): Neuroinflammation and Neurodegeneration Mechanisms
2021 - Wiley | Journal of Biochemical and Molecular Toxicology
Archita Khanna, Anamika Anamika, Suwarna Chakraborty, Sunil Jamuna Tripathi, Arup Acharjee, Shankaranarayana Rao Bs, Surendra Kumar Trigun,
A preliminary observation about resveratrol (RSV) dependent normalization of inflammatory and apoptotic factors in the cortex of hyperammonemic rat model of moderate grade hepatic encephalopathy (MoHE) led us to evaluate whether RSV is ultimately able to confer neuroprotection against MoHE pathogenesis and that it does so by activating its bonafide molecular target SIRT1. The present study compared the profile of relevant neurobehavioral pattern vs neuromorphometry of hippocampal CA1 neurons and SIRT1 ...
Tópico(s): Genomics, phytochemicals, and oxidative stress
2020 - Elsevier BV | Journal of Chemical Neuroanatomy
Neeta Kumar, Avika Dixit, Sanjiv Kumar, Vidyasagar Trigun,
Antimicrobial resistance (AMR) has emerged as a major threat to public health estimated to cause 10 million deaths annually by 2050. India carries one of the largest burdens of drug-resistant pathogens worldwide. NDM-1 reported in 2008, rapidly spread to other countries was named after India's capital. India is one of the largest consumers of antibiotics worldwide, and antibiotic sale is increasing rapidly. AMR develops when microbes develop mechanisms to evade the action of antimicrobials. The factors ...
Tópico(s): Antimicrobial Resistance in Staphylococcus
2019 - Medknow | Indian Journal of Community Medicine
Akanksha Mishra, Lalit P. Chandravanshi, Surendra Kumar Trigun, Sairam Krishnamurthy,
Reduced glucocerebrosidase (GCase) enzymatic activity is found in sporadic cases of Parkinson's disease making GCase a serious risk factor for PD. GCase gene mutations constitute a major risk factor in early-onset PD but only account for 5-10% cases. Having enough evidence for construct and face validity, 6-OHDA-induced hemiparkinson's model may be useful to assess the GCase-targeting drugs in order to have new leads for treatment of PD. Ambroxol (AMB) is reported to increase GCase activity in different ...
Tópico(s): Cellular transport and secretion
2018 - Elsevier BV | Biochemical Pharmacology
Divya Rawat, Saurabh Kumar Chhonker, Rayees Ahmad Naik, Aditi Mehrotra, Surendra Kumar Trigun, Raj Kumar Koiri,
Global metabolism of cancers exhibits a peculiar phenotype that is lactate acidosis (high lactate with acidic pH) in tumor microenvironment. Why tumor microenvironment becomes so responsive towards lactate is still not clear. In this review we have discussed lactate generation and recycling either exogenously, directly or indirectly by cancer cells via some transporters. Tumor cells in hypoxia use glucose rapidly and produce lactate while cells which have profuse oxygen supply take up lactate and ...
Tópico(s): ATP Synthase and ATPases Research
2018 - Frontiers in Bioscience | Frontiers in bioscience
Anamika Anamika, Archita Khanna, Papia Acharjee, Arup Acharjee, Surendra Kumar Trigun,
Sirtuins are highly conserved NAD+ dependent class III histone deacetylases and catalyze deacetylation and ADP ribosylation of a number of non-histone proteins. Since, they require NAD+ for their activity, the cellular level of Sirtuins represents redox status of the cells and thereby serves as bona fide metabolic stress sensors. Out of seven homologues of Sirtuins identified in mammals, SIRT3, 4 & 5 have been found to be localized and active in mitochondria. During recent past, clusters of protein ...
Tópico(s): Autophagy in Disease and Therapy
2017 - Elsevier BV | Journal of Chemical Neuroanatomy
Sahdeo Prasad, Subash C. Gupta, Manoj K. Pandey, Amit K. Tyagi, Lokesh Deb,
... hepatocellular carcinoma (B. K. Maurya and S. K. Trigun, Y.-Q. Hou et al.), pancreatic cancer (L. ...
Tópico(s): MicroRNA in disease regulation
2016 - Hindawi Publishing Corporation | Oxidative Medicine and Cellular Longevity
Amit Kumar, Ashish Kumar, Rakesh Kumar Gupta, Rajendra Prasad Paitandi, Krishna B. Singh, Surendra Kumar Trigun, M.S. Hundal, Daya Shankar Pandey,
Synthesis, characterization, DNA and protein binding as well as anticancer activity of the organometallic complexes [(η6-C6H6)RuCl(APBI)]Cl (1), [(η6-p-MeC6H4Pri)RuCl(APBI)]Cl (2), [(η6-C6Me6)RuCl(APBI)]Cl (3), [(η5-C5Me5)RhCl(APBI)]Cl·H2O (4) and [(η5-C5Me5)IrCl(APBI)]Cl·H2O (5) containing 2-aminophenyl benzimidazole (APBI) have been described. The complexes 1–5 exhibited strong DNA, protein binding and anticancer activity against cervical cancer (SiHa) cell line. Their binding with calf thymus DNA (CT-DNA) and ...
Tópico(s): Organometallic Compounds Synthesis and Characterization
2015 - Elsevier BV | Journal of Organometallic Chemistry
Raj Kumar Koiri, Surendra Kumar Trigun, Lallan Mishra,
There is a general agreement that most of the cancer cells switch over to aerobic glycolysis (Warburg effect) and upregulate antioxidant enzymes to prevent oxidative stress induced apoptosis. Thus, there is an evolving view to target these metabolic alterations by novel anticancer agents to restrict tumor progression in vivo. Previously we have reported that when a non toxic dose (10 mg/kg bw i.p.) of a novel anticancer ruthenium(II)-complex containing 4-carboxy N-ethylbenzamide; Ru(II)-CNEB, was ...
Tópico(s): DNA Repair Mechanisms
2015 - Elsevier BV | Biochimie
Brajesh Kumar Maurya, Surendra Kumar Trigun,
Fisetin, a known antioxidant, has been found to be cytotoxic against certain cell lines. However, the mechanism by which it inhibits tumor growth in vivo remains unexplored. Recently, we have demonstrated that Aflatoxin‐B1 (AFB1) induced hepatocarcinogenesis is associated with activation of oxidative stress‐inflammatory pathway in rat liver. The present paper describes the effect of in vivo treatment with 20 mg/kg b.w. Fisetin on antioxidant enzymes vis-a-vis oxidative stress level and on the profile ...
Tópico(s): Phytochemistry and Biological Activities
2015 - Hindawi Publishing Corporation | Oxidative Medicine and Cellular Longevity
Papia Mondal, Surendra Kumar Trigun,
Hepatic encephalopathy (HE), characterized by impaired cerebellar functions during chronic liver failure (CLF), involves N-methyl-D-aspartate receptor (NMDAR) overactivation in the brain cells. Bacopa monnieri (BM) extract is a known neuroprotectant. The present paper evaluates whether BM extract is able to modulate the two NMDAR subunits (NR2A and NR2B) and its downstream mediators in cerebellum of rats with chronic liver failure (CLF), induced by administration of 50 mg/kg bw thioacetamide (TAA) i.p. ...
Tópico(s): Neuroscience and Neuropharmacology Research
2015 - Hindawi Publishing Corporation | Evidence-based Complementary and Alternative Medicine
Santosh Singh, Papia Mondal, Surendra Kumar Trigun,
Liver dysfunction led hyperammonemia (HA) causes a nervous system disorder; hepatic encephalopathy (HE). In the brain, ammonia induced glutamate-excitotoxicity and oxidative stress are considered to play important roles in the pathogenesis of HE. The brain ammonia metabolism and antioxidant enzymes constitute the main components of this mechanism; however, need to be defined in a suitable animal model. This study was aimed to examine this aspect in the rats with acute liver failure (ALF).ALF in the ...
Tópico(s): Alcoholism and Thiamine Deficiency
2014 - Public Library of Science | PLoS ONE
Krishna B. Singh, Brajesh Kumar Maurya, Surendra Kumar Trigun,
Tópico(s): Selenium in Biological Systems
2014 - Springer Science+Business Media | Molecular and Cellular Biochemistry
Santosh Singh, Surendra Kumar Trigun,
Hepatic encephalopathy (HE) is a nervous system disorder developed in the patients with liver cirrhosis. The low grade cirrhosis is of common occurrence, however, whether and the extent to which it affects brain function is not clearly understood. The present article examines certain neurobehavioral parameters in the rats with low grade chronic liver failure (CLF) induced by intraperitoneal administration of 50mg/kgb.w. thioacetamide up to 14 days. During Morris Water Maze tasks, the CLF rats, as ...
Tópico(s): Epilepsy research and treatment
2013 - Elsevier BV | Neuroscience Letters
Aditi Mehrotra, Surendra Kumar Trigun,
Tópico(s): Diet and metabolism studies
2011 - Springer Science+Business Media | Neurochemical Research
Niraj Kumari, Brajesh Kumar Maurya, Raj Kumar Koiri, Surendra Kumar Trigun, Saripella Srikrishna, Michael P. Coogan, Lallan Mishra,
A PtII complex [{Pt(en)L}2]·4PF6 (Ptcyp) (LH2 = N,N′-bis(salicylidene)-p-phenylenediamine, en = 1,2-diamino ethane) shows high cytotoxicity against HeLa cells (IC50—11.5 μM) and against Dalton's lymphoma (DL) cells (IC50—0.65 nM); UV-vis titration of Ptcyp with calf thymus DNA (CT-DNA) demonstrated its DNA binding, which could be further quantified by competitive fluorescence titration of DNA, Ptcyp and ethidium bromide. Circular dichroism studies suggest that Ptcyp interacts with CT-DNA by intercalation in ...
Tópico(s): Ferrocene Chemistry and Applications
2011 - Royal Society of Chemistry | MedChemComm
Raj Kumar Koiri, Surendra Kumar Trigun,
Dimethyl sulfoxide (DMSO) is evident to induce apoptosis in certain tumor cells in vitro. However, its apoptotic mechanism remains unexplored in in vivo tumors. This article describes that DMSO, being non-toxic to the normal lymphocytes, up regulated TNFα and p53, declined Bcl-2/Bax ratio, activated caspase 9 and PARP-1 cleavage and produced apoptotic pattern of DNA ladder in Dalton's lymphoma (DL) in vivo. This was consistent with the declined expressions of tumor growth supportive glycolytic enzymes; ...
Tópico(s): Cell death mechanisms and regulation
2011 - Elsevier BV | Leukemia Research
Krishna B. Singh, Surendra Kumar Trigun,
Tópico(s): Biological and pharmacological studies of plants
2011 - Springer Science+Business Media | Cell Biochemistry and Biophysics
Namrata Dixit, Raj Kumar Koiri, Brajesh Kumar Maurya, Surendra Kumar Trigun, Claudia Höbartner, Lallan Mishra,
A barbiturate derivative [1,5-dihydro-5-[5-pyrimidine-2,4(1H,3H)-dionyl]-2H-chromeno[2,3-d] pyrimidine-2,4(3H)-dione] (LH4) was allowed to react with 2,2′-bipyridyl-dinitrato-Copper(II)-dihydrate which provides two complexes, characterized as [Cu(bpy)(L1)]·3H2O (1) and [Cu(bpy)(L2)]·H2O (2), where bpy = 2,2′-bipyridine, L1 = 5-hydroxy-hydurilic acid and L2 = alloxanic acid. In a separate reaction of LH4 with Cu(NO3)2·H2O another type of complex [Cu(LH3)2·(H2O)2]·4H2O (3) is formed. The complexes were characterized ...
Tópico(s): Synthesis and biological activity
2010 - Elsevier BV | Journal of Inorganic Biochemistry
Santosh Singh, Surendra Kumar Trigun,
Tópico(s): Liver Disease Diagnosis and Treatment
2010 - Springer Science+Business Media | The Cerebellum
Rishikesh Prajapati, Santosh Kumar Dubey, Ruchi Gaur, Raj Kumar Koiri, Brajesh Kumar Maurya, Surendra Kumar Trigun, Lallan Mishra,
A synthetic precursor cis-[RuIICl2(dmso)4] is complexed separately with 3-(4-benzyloxyphenyl)-1-(2-hydroxylphenyl)-prop-2-en-1-one (L1H) and 2-(4-benzyloxyphenyl)-3hydroxy-chromen-4-one (L2H). The resulting complexes are assigned the composition fac-[RuCl(S-dmso)3(L1)] 1 and fac-[RuCl(S-dmso)3(L2)] 2 using elemental analyses, FAB mass data and spectroscopic (IR, 1H NMR, UV–Vis, emission) spectral properties. The X-ray diffraction analysis shows that complexes self-associate through non-covalent interactions ...
Tópico(s): Synthesis of Organic Compounds
2009 - Elsevier BV | Polyhedron
Raj Kumar Koiri, Surendra Kumar Trigun, Lallan Mishra, Kiran Pandey, Deobrat Dixit, Santosh Kumar Dubey,
Tópico(s): Radiopharmaceutical Chemistry and Applications
2008 - Springer Science+Business Media | Investigational New Drugs
Santosh Singh, Raj Kumar Koiri, Surendra Kumar Trigun,
Tópico(s): Alcoholism and Thiamine Deficiency
2007 - Springer Science+Business Media | Neurochemical Research
Raj Kumar Koiri, Surendra Kumar Trigun, Santosh Kumar Dubey, Santosh Kumar Singh, Lallan Mishra,
Tópico(s): Trace Elements in Health
2007 - Springer Science+Business Media | BioMetals
Teruya Tamaru, Surendra Kumar Trigun, Masato Okada, Hachiro Nakagawa,
The multiple cyclins and their catalytic subunit, cdc2-related kinase, play essential roles in the eucaryotic cell cycle. To examine their potential roles in highly differentiated nervous system, we determined their activity and localization in rat brain. pl3sucl associated histone H1 kinase activity was dramatically increased at the onset of brain maturation. The increased kinase activity was coprecipitated with cyclin D1, a type of G1 cyclin, which also increased with brain maturation. Immunohistochemical ...
Tópico(s): Pancreatic function and diabetes
1993 - Elsevier BV | Neuroscience Letters
B. Pałosz, S. Gierlotka, B. Wiktorowska, D. Dziąg,
... Chand & Trigunayat (1975a,b, 1976), Chadha (1976), Chaudhary & Trigun- ayat (1983). Tens of multilayer polytypes occurring in ...
Tópico(s): X-ray Diffraction in Crystallography
1985 - Wiley | Acta Crystallographica Section C Crystal Structure Communications
Surendra Kumar Trigun, Raj Kumar Koiri, Lallan Mishra, Santosh Kumar Dubey, Santosh Kumar Singh,
Ruthenium complex-protein interaction, particularly with respect to modulation of the enzymes associated to tumor development, is an evolving concept in understanding the mechanism of action of these complexes as anticancer agent. Lactate dehydrogenase (LDH; EC: 1.1.1.27) is critically implicated in maintaining tumor growth via ‘Warburg effect’ in cancerous cells. This article presents current status of Rucomplexes as enzyme inhibitors in general and a state of art on a novel ruthenium(II) complex ...
Tópico(s): Lanthanide and Transition Metal Complexes
2007 - Bentham Science Publishers | Current Enzyme Inhibition