JPTRM Vol. 5 No. 2 (November 2017)
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Item Histone Deacetylase Inhibitors As Potential Therapeutic Agents For Various Disorders(Chitkara University Publications, 2017-11-02) Kajal Thapa; Savir Kumar; Anurag Sharma; Sandeep Arora; Amarjot Kaur Grewal; Thakur Gurjeet SinghEpigenetic modification acetylation or deacetylation of histone considered as an important element in various disorders. Histone acetyltransferases (HATs) and histone deacetylases (HDACs) are the enzymes which catalyse the acetylation and deacetylation of histone respectively. It helps in regulating the condensation of chromatin and transcription of genes. Lysine acetylation and deacetylation present on the nucleosomal array of histone is the key factor for gene expression and regulation in a normal working living cell. Modification in histone protein will lead to the development of cancer and can cause various neurodegenerative disorders. To safeguard the cells or histone proteins from these diseases histone deacetylase inhibitors are used. In this review, the main focus is upon the role of histone deacetylases inhibitors in various diseases.Item Ebola Hemorrhagic Fever: Recent Update On Disease Status, Current Therapies And Advances In Treatment(Chitkara University Publications, 2017-11-02) Jaskaran Singh; Thapa Komal; Sandeep Arora; Amarjot Kaur; Thakur Gurjeet SinghSwiftly growing viruses are a major intimidation to human health. Such viruses are extremely pathogenic like Ebola virus, influenza virus, HIV virus, Zika virus etc . Ebola virus, a type of Filovirus, is an extremely infectious, single-stranded ribonucleic acid virus that infects both humans and apes, prompting acute fever with hemorrhagic syndrome. The high infectivity, severity and mortality of Ebola has plagued the world for the past fifty years with its first outbreak in 1976 in Marburg, Germany, and Frankfurt along with Belgrade and Serbia. The world has perceived about 28,000 cases and over 11,000 losses. The high lethality of Ebola makes it a candidate for use in bioterrorism thereby arising more concern. New guidelines have been framed for providing best possible care to the patients suffering from Ebola virus i.e Grading of Recommendation Assessment, Development And Evaluation (GRADE) methodology to develop evidence-based strategy for the treatment in future outbreak of Ebola virus. No drugs have been approved, while many potent drugs like rVSV-EBOV, Favipiravir, ZMapp are on clinical test for human safety. In this review we will discover and discuss perspective aspects that lead to the evolution of different Ebola variants as well as advances in various drugs and vaccines for treatment of the disease.Item An Insight on Analytical Profile on Bisoprolol Fumarate – A Selective Beta-1 Adrenoreceptor Blocker(Chitkara University Publications, 2017-11-02) Ajinkya G. Dhandar; Suraj R. Chaudhari; Saurabh B. Ganorkar; Amod S. Patil; Sanjay J. Surana; Atul A. ShirkhedkarBF is Beta-adreno receptor antagonist and used as an AntiHypertensive Drug. BF gives the blocking action on β1-adrenergic receptors in the heart and vascular smooth muscle. The present review compiles the various approaches implemented for quantification of BF in bulk drug, pharmaceutical matrix and biological fluid. This review represents more than 50 analytical methods which include capillary electrophoresis, HPLC, HPTLC, UV-Spectroscopy, UPLC, impurity profiling and electrochemical methods implemented for estimation of BF as a single component as well as in multicomponent.Item Microneedle Mediated Vaccine Delivery: A Comprehensive Review(Chitkara University Publications, 2017-11-02) Anureet Arora; Manju Nagpal; Geeta AggarwalMicroneedles can be representative for paradigm shift of drug delivery from patient non-compliant parenteral injections to patient compliant drug delivery system, which can be utilized for administration of vaccines particularly along with macromolecular/micromolecular drugs. The concept of microneedles came into existence many decades ago but the use of microneedles to achieve efficient delivery of drugs into the skin became subject of research from mid of 1990’s. Various types of microneedles were utilized to enhance delivery of drugs and vaccines including solid microneedles for pre-treatment of skin to enhance drug permeability, dissolvable polymeric microneedles encapsulating drugs, microneedles coated with drugs and hollow microneedles for infusion of drugs through the skin. Microneedles have shown promising delivery of vaccines through skin in literature. But the successful utilization of this system for vaccine drug delivery mainly depends on design of device to facilitate microneedle infusion, vaccine stability and storage in system, recovery of skin on removal of microneedle and improved patient compliance. This article reviews the conventional and advanced methods of vaccine drug deliver, microneedles for drug delivery, types of microneedles, advantages of microneedles and potential of microneedles for vaccine drug delivery.Item In Silico Designing of Novel Thiazolidine-2-one Derivatives as Dual PDE4/7 Inhibitors for Inflammatory Disorders(Chitkara University Publications, 2017-11-02) Ajmer Singh Grewal; Neelam Sharma; Sukhbir Singh; Sandeep AroraPhosphodiesterase 4 (PDE4) and phosphodiesterase 7 (PDE7), members of PDE super family, catalyse metabolism of secondary messenger cyclic adenosine monophosphate leading to augmented inflammatory processes in pro-inflammatory and immune-modulatory cells. Dual inhibitors of PDE4/7 are a novel class of drug candidates which can regulate pro-inflammatory as well as function of immune T-cell and are particularly beneficial for the treatment of various inflammatory diseases devoid of unwanted actions. Intense efforts have been directed towards the development of effective dual inhibitors of both PDE4 and PDE7, but not much success has been reported till yet. The aim of present study was to design some newer substituted thiazolidine-2-one derivatives as dual inhibitors of PDE4/7 using structure based rational drug design approach. A new series of thiazolidine-2-one analogues were designed and molecular docking was performed using AutoDock Vina to explore the bonding interactions of the designed molecules with the amino acid residues in the active site of target proteins. The docking study indicated that all the substituted thiazolidine-2-one derivatives have appreciable binding interactions with protein residues of both PDE4 and PDE7. The newly designed compounds could be used as lead molecules for development potent and non-toxic dual inhibitors of PDE4/7 for the management of various inflammatory conditions.Item Molecular Docking Evaluation of Some Natural Phenolic Compounds as Aldose Reductase Inhibitors for Diabetic Complications(Chitkara University Publications, 2017-11-02) Ajmer Singh Grewal; Neelam Sharma; Sukhbir Singh; Sandeep AroraThe enzyme aldose reductase (AR) is a member of aldoketoreductase super-family which catalyzes the formation of sorbitol from glucose through polyol pathway of glucose catabolism. Reduced sorbitol production via polyol pathway due to AR inhibition is a target of choice for controlling major complications of diabetes. Epalrestat is the only commercially available inhibitor of AR till date,thus, there is a great need to search for more economical, nontoxic and safer inhibitors of AR enzyme. Flavonoids, the polyphenol compounds in plants have been reported for inhibitory effects against AR. The objective of this study is to explore the binding modes of natural phenolic compounds with AR to design safer natural drugs as alternatives to synthetic drugs. We conducted a molecular docking study on some natural phenolic compounds with AR enzyme in complex with the synthetic inhibitor. The overlay of the docked pose of the selected natural phenols with the ARreference inhibitor complex showed that the selected natural compounds have the similar binding pattern with the active site residues of the enzyme as that of co-crystallized inhibitor. The results of docking study showed the best binding affinity of AR with that of 2-(4-hydroxy-3-methoxyphenyl) ethanoic acid and butein, having the lowest binding free energy of –9.8 kcal/mol and–9.7 kcal/mol, respectively. This information can be utilized to design potent, economical and non-toxic natural AR inhibitors from natural phenols for the therapeutics of diabetic complications.Item Ameliorative Potential of Aminophylline In Restrain Stress Induced Behavioural and Biochemical Alterations(Chitkara University Publications, 2017-11-02) Rajneet Kaur; Manjinder Kaur; Poonam AroraThis study is designed to investigate the attenuating prospective of aminophylline in immobilization stress generated behavioural changes in rats. Animals were exposed to restrain stress before being subjected to varying doses of aminophylline (1mg/kg, 2mg/kg and 4mg/kg). Behavioural changes were analyzed to assess the intensity and the degree of the stress, by estimating the changes in the exploratory behaviour, spontaneous activity and social behaviour using various paradigms. As a consequence of stress, the behavioral patterns so changed were assessed in the terms of changes in the locomotor activity, number of head dips and increased avoidance behaviour. Aminophylline (4mg/kg) modulated the stress produced changes in the behaviour and oxidative stress generated biochemical alterations in a significant manner (p<0.001). The results so obtained suggest that upon exposure to stress, animal behavioural patterns, biochemical markers levels changed and these changes wereefficiently modulated by aminophylline at therapeutic doses.