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Computational modeling studies on anti-HIV-1 non-nucleoside reverse transcriptase inhibition by dihydroalkoxybenzyloxopyrimidines analogues: an electrotopological atomistic approach

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Journal of Biophysical Chemistry 2011年第3期2卷 361-372页

作者： Nitin s. sapre Tarang Bhati swagata Gupta Nilanjana Pancholi Urmila Raghuvanshi Divya dubey Vandana Rajopadhyay Neelima sapre Department of Applied Chemistry SGSITS Indore MP INDIA

For the first time we report quantitative structure activity relationship (QsAR) studies based on Kier-Hall Electrotopological state (E-state) Indices for Dihydroalkoxybenzyloxopyrimidines (DABO) derivatives acting as NNRTIs of HIV-1. A dataset of 74 compounds was compiled from published studies and randomly subdivided into training and test sets. To understand the pharmacophoric effect, Kier-Hall Electrotopological state descriptors namely sN1, sN3, sF, sAr, ss, sO, sNO2, sCl, sY (Y = s-alkyl and NH-alkyl), sX (X = Me) and biological activity were used as independent and dependent variable respectively. statistical results were highly encouraging for the training set multiple linear regression [(MLR): r2 = 0.961, F = 100.41 and q2 = 0.926, neural networks (NN): r2 = 0.966, F = 115.594, degrees of freedom = 40 and k-nearest neighbour (k-NN): r2 = 0.770, q2 = 0.757, degrees of freedom = 40]. Results of validation using a test set showed the same trend as training set (NN > MLR > kNN). The above results suggest that of various functional groups present in DABO such as sN3, sO, sCl, sAr and sNO2 contribute more significantly towards activity. On the other hand sN1, ss, and sF do not play any role in enhancing the activity. The substitution of s-alkyl and NH-alkyl at C2 position is essential though it does not contribute much towards the activity. The substitution of methyl group at C5 position is unfavorable and exhibit negative impact on inhibitory activity. Therefore, it seems reasonable to choose E-state indices as suitable and significant descriptors for exploring the relationship between the pIC50 and the pharmacological properties of the compounds.

关键词： AIDs HIV-1 NNRTIs DABOs QsAR pIC50 Kier Hall E-state Indices MLR NN k-NN

A simple and Highly Efficient Enantioselective synthesis of (s)-Rivastigmine

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International Journal of Organic Chemistry 2011年第2期1卷 26-32页

作者： Veera R. Arava Laxminarasimhulu Gorentla Pramod K. dubey 不详

A highly efficient and convenient procedure for the enantioselective synthesis of (s)-Rivastigmine, a cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer’s type and dementia due to Parkinson’s disease, is accomplished by the treatment of versatile, readily accessible (s)-(-)-2-methyl-2-propanesulfinamide with 3-hydroxyacetophenone. This protocol provides high yield and excellent enantiomeric excess in short step synthesis.

关键词： Cholinergic Agent Enantioselective Highly Efficient (s)-(-)-2-Methyl-2-Propane sulfina-mide (s)-Rivastigmine

Prospected epigenetic moderators from natural sources and drug of class NsAIDs as effective treatment options to Prostate cancer

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Journal of Acute Disease 2017年第4期6卷 145-153页

作者： Vaibhav dubey Richard Owusu-Apenten shipra Tripathi Udaya Pratap singh Aloksemwal Volhart Health Care Pvt.Ltd. Department of Research and DevelopmentSitapur Road YojnaLucknowUPIndia Faculty of Life and Health sciences School of Biomedical SciencesUniversity of UlsterColeraineBT521SAUnited Kingdom Babu Banarasi Das Northern India Institute of Technology Department of PharmacyFaizabad RoadLucknowUPIndia sam Higginbottom University of Agriculture Technology and SciencesDepartment of Pharmaceutical SciencesAllahabadNainiUPIndia Department of Pharmacy Himachal Institute of PharmacyPaonta Sahib-173025H.P India

Prostate cancer (PC) is one of the most common and leading cancer amongst the males all around the world. Depending upon it long latency and cost involved in its management and treatment, there is extensive need for more personalized and economical therapeutic approach for its effective therapy. The current review here discusses agents from natural dietary sources and drug class Non-steroidal Antinflammatory (NsAIDs) that bears chemopreventive potential to regulate PC progression & tumour development and therefore could be devised into effective future treatment strategy against PC along with its metastatic castration-resistant form. Based on the literature search the therapeutic scope of selected agents are delineated, sighting their previous activity and prospects as epigenetic moderators in specific to particular PC causing biomarkers like over expression of AKR1C3, lost intracellular glutathione/glutathione-s-tranferases(GsH/GsT) expression, DNA hypermethylation, aberrant cell proliferation and other related factors that are thought to potentiate and aggravate the onset of PC like smoking and use of other narcotics products.

关键词： Prostate cancer NsAIDs AKR1C GsH/GsT DNA hypermethylation

Cope's sign and complete heart block secondary to acute cholecystitis: A case report

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Journal of Acute Disease 2020年第4期9卷 176-178页

作者： Neeraj Kumar Pankaj Kumar Prakash K dubey Abhyuday Kumar Amarjeet Kumar Department of Trauma and Emergency AIIMs Patna Bihar India Department of Emergency Medicine Paras Global HospitalDarbhangaBiharIndia Department of Anaesthesiology&Critical Care IGIMs Patna Bihar India Department of Anesthesiology AIIMs Patna Bihar India

Rationale: Cope's sign is reflex bradycardia seen in the patient presenting with symptoms of acute cholecystitis. This bradycardia may be due to vagally mediated cardio-biliary reflex. Many of these reflexes due to acute cholecystitis have similar clinical features (some electrocardiographic changes like bradycardia, complete heart block, and asystole) mimicking that of acute coronary syndrome. Patient's concern: A 60-year old male presented with symptoms of acute cholecystitis and referred to the emergency department with complete heart block and abdominal pain with hypotension requiring an emergency temporary pacemaker. Diagnosis: Cope's sign and complete heart block. Intervention: Emergency temporary cardiac pacemaker insertion. Outcomes: The patient was discharged after three days with regular follow-up and advice for laparoscopic cholecystectomy. Lessons: Complete heart block or any symptomatic bradycardia associated with abdominal pain should be under consideration of cholecystitis that may be associated with either presence or absence of gall stones due to cardio biliary reflex.

关键词： Cope sign Complete heart block Temporary pacemaker insertion

Tyrosine kinase receptor B isoforms alter APP and BACE1 endogenous levels independently of BDNF

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Advances in Alzheimer's Disease 2012年第3期1卷 93-101页

作者： sara Ansaloni Brian P. Leung Aditi dubey Aleister J. saunders Biology Department Drexel University Philadelphia USA

Brain derived neurotrophic factor (BDNF) levels and signaling via the tyrosine receptor kinase B (TrkB) have been shown to be altered in Alzheimer’s Disease. In addition, it has been reported that the isoforms of TrkB can differentially affect metabolism of amyloid precursor protein (APP). Conversely, Ab, a neurotoxic cleavage product of APP, has been shown to impair TrkB/ BDNF signaling. Therefore, we investigated whether the changes observed in APP metabolism were due to the isoform-specific effects of TrkB on either APP expression, and/or on the expression and activity of ADAM10 and BACE1. since BDNF levels are decreased in AD, we focused on BDNF independent effects of the TrkB isoforms. We found that TrkB FL increases endogenous APP levels in both HEK293 and sH-sY5Y naive cells. We did not find an increase in ADAM10 activity in HEK293 cells, but an increase in BACE1 levels. Additionally, we have found that TrkB FL is able to increase NFAT3 mediated transcriptional activity and we suggest that this causes transcriptional activation of the BACE1 promoter.

关键词： TrkB Alzheimer BACE1 sHC NFAT

Identification and Characterization of Heparan sulphate Binding Proteins of Entamoeba histolytica

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Journal of Biosciences and Medicines 2018年第8期6卷 60-71页

作者： Upninder Kaur sumeeta Khurana Uma Nahar saikia Mohan Lal dubey Rakesh sehgal Department of Medical Parasitology Postgraduate Institute of Medical Education and Research Chandigarh India Department of Histopathology Postgraduate Institute of Medical Education and Research Chandigarh India

A large number of microbial pathogens bind to heparan sulphate on eukaryotic cell surfaces. Heparan sulphate Binding Proteins (HsBPs) from Entamoeba histolytica culture lysates were obtained by sequential ammonium sulphate precipitation and Protein purify. sDs-PAGE and immunoblotting experiments indicated the presence of two major extracellular proteins in E. histolytica (51.2 kDa and 61.0 kDa). Characterization of HsBPs by 2D Gel electrophoresis of 40% (NH4)2sO4 precipitated lysate of E. histolytica revealed that the isoelectric point of 51.2 kDa HsBP was at pH3.0. The protein of 61.0 kDa HsBP showed three spots in 40% (NH4)2sO4 lysate which had isoelectric point between pH 4.0 - 7.0. While in 80% (NH4)2sO4 precipitated lysate, 51.2 kDa HsBP showed only one spot which had isoelectric point at pH 3. However, 61.0 kDa HsBP revealed 2 spots which had isoelectric point between pH 4 and 5. The result showed that this parasite has proteins which interact with heparan sulphate whose molecular formula is C14H23NO21s-23. These proteins may have a role in binding of parasite to heparan sulphate on host cells. Further characterization by MALDI-TOF analysis of HsBPs from E. histolytica demonstrated HsBPs to be novel protein in this parasite which has been isolated, purified and characterized first time by our group in the present study.

关键词： Heparan sulphate Entamoeba histolytica Identification Characterization

PsIA与ONVIF：如何评估两种视频监控标准

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A&s（安全&自动化） 2010年第3期 140-142页

作者： Ajit dubey elnfochips公司

不同的网络视频标准相继出台，它们各有优劣。Ajit dubey是elnfochips公司嵌入式系统事业部的高级项目经理，elnfochips成立于1995年，是一家技术设计服务公司，以及软件产品及应用、嵌入式系统和AsIC／FPGA方案的提供商。在本文中，Aji... 详细信息

不同的网络视频标准相继出台，它们各有优劣。Ajit dubey是elnfochips公司嵌入式系统事业部的高级项目经理，elnfochips成立于1995年，是一家技术设计服务公司，以及软件产品及应用、嵌入式系统和AsIC／FPGA方案的提供商。在本文中，Ajit dubey将就各种网络视频标准作出分析比较。

关键词：视频标准视频监控嵌入式系统评估项目经理服务公司软件产品 FPGA

structural and Raman spectroscopic study of Antimony Doped Bi0.5Na0.5TiO3Electroceramic

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Journal of Materials science and Chemical Engineering 2015年第8期3卷 43-49页

作者： K. N. singh Versha sao P. Tamrakar s. soni V. K. dubey P. K. Bajpai Department of Physics Dr. C. V. Raman University Bilaspur India Department of Physics Government Science PG College Bilaspur India Advance Materials Research Laboratory Guru Ghasidas Vishwavidyalaya Bilaspur India

Pure and Antimony (sb, x = 0.01%, 0.02% and 0.03%) doped Bi0.5Na0.5TiO3 electro ceramics were successfully synthesized by a conventional solid state reaction route. X-ray diffraction analysis showed that a distinct 002/200 peak splitting appears when doping percentage changes from 0.02 to 0.03, referring to a hexagonal symmetry. The data show the Lorentzian deconvolution of the 002 and 200 peaks of the tetragonal phase and the 202 peak of the rhombohedral phase. There is no significant change in the Raman spectra for the prepared compositions while some additional peaks around 151, 281, 585 and 853 cm-1 compared to the peaks observed in BNT. It may be possible that a morphotrophic phase boundary (MPB) exists around x = 0.03. Analysis of peak positions, widths and intensities of Raman spectroscopy study also confirmed the existence of structural change around x = 0.03 composition.

关键词： Ceramics X-Ray Diffraction Raman spectroscopy

Application of Decision support system for Agro Technology Transfer (DssAT) to simulate Agronomic Practices for Cultivation of Maize in southern Highland of Tanzania

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Agricultural sciences 2018年第7期9卷 910-923页

作者： Lusajo Henry Mfwango sangharsh Kumar Tripathi Gogumalla Pranuthi sunil Kumar dubey Vijay Kumar Gubey Department of Water Resources and Irrigation Engineering Water Institute Dar es Salaam Tanzania

The southern highlands zone of Tanzania is the one of the most potential area for agriculture contributes up to 46% of the total country’s maize production. However, the rate of maize production tends to decrease with time due of poor agronomic practices. The aim of this study was to simulate the effect of nitrogen dose and plant spacing on grain yields from five selected maize varieties. Decision support system for Agrotechnology transfer crop model was used for this purpose. Based on the agroecological zones, six sites were selected which includes Ihumbu farm, Mwazye and Nyera Estate Mbozi, Lupa Tinga Tinga, santilya and Mbinga. Maize varieties H614, Kitumani Composite I, H511, H626 and H612;spacing (90 × 30 cm and 60 × 30 cm) and nitrogen dose (0, 50, 100, 150 and 200 kg/ha) were simulated. It was found that only H614 (4610.9 kg/ha) and Kitumani Composite I (3998.7 kg/ha) maize varieties performed well at the spacing of 60 × 30 cm and up to the nitrogen dose of 150 kg/ha. Therefore the two maize varieties H614 and Kitumani Composite I could be recommended for cultivation at the spacing of 60 × 30 cm and nitrogen dose of 150 kg/ha for improving production of maize in southern highland of Tanzania.

关键词： southern Highlands (Tanzania) DssAT Nitrogen Dose Plant spacing and Maize Varieties