Pharmacology Commons^™

Structural Characterization And Therapeutic Utility Of The Proton-Coupled Folate Transporter, Michael Roy Wilson

Wayne State University Dissertations

Folate is a B9 vitamin essential to DNA synthesis. The proton-coupled folate transporter (PCFT) is a newly discovered proton/folate symporter with an acidic pH optimum and broad expression across a variety of solid tumor types, with limited expression in normal tissues. Several antifolate molecules have been developed as cancer therapeutics, although these classical antifolates display numerous off-target effects due to transport by the ubiquitous reduced folate carrier (RFC). In this dissertation, we determine the roles of multiple PCFT structure/function domains, and develop PCFT-specific antifolates to target solid tumors. We utilize substituted cysteine accessibility methods (SCAM) to identify a novel reentrant …

Molecular Docking Study Of Tyrosinase Inhibitors Using Arguslab 4.0.1 : A Comparative Study, Prasan Tangyuenyongwatana, Nathjanan Jongkon

The Thai Journal of Pharmaceutical Sciences

We conducted a docking study with ArgusLab 4.0.1, a free molecular docking software, on tyrosinase inhibitors comparing with AutoDock 4 and AutoDock VINA. In this study, hydroxyl substituted 2-phenyl-naphthalenes (a group of modified structure based on o...

Tlc-Densitometric Method For Quantitation Of Lurasidone Hydrochloride In Nanoemulsion, Microemulsion, For Equilibrium Solubility And Ex Vivo Diffusion Studies., Rashmin B. Patel, Khyati B. Vekaria, Mrunali R. Patel

The Thai Journal of Pharmaceutical Sciences

A new TLC-densitometric method has been successfully developed for quantitation of Lurasidone hydrochloride (LURHA) in pharmaceutical formulations. LURHA was well separated from sample matrix and degradation product using TLC plate; precoated with silica...

Neuronal Insult Either By Exposure To Lead Or By Direct Neuronal Damage Cause Genome-Wide Changes In Dna Methylation And Histone 3 Lysine 36 Trimethylation, Arko Sen

Wayne State University Dissertations

Prenatal and postnatal exposure to pervasive neuro-toxicants such as Lead (Pb) has been reported to causes extensive and diverse changes in the epigenetic profile. Among epigenetic modification, DNA methylation (5mC) is perhaps the most widely studied and has been proposed to be potential early biomarkers for Pb toxicity. Several studies have demonstrated the association between Pb-exposure and 5mC. However most of these studies are restricted to looking at a specific set of target genes or repetitive elements. Therefore, one of the main objectives of our study was to use an unbiased genome-wide approach to look at Pb-exposure associated changes in …

Childhood Obesity, A Public Health Crisis: Narrative Review Of Public Health Interventions For Childhood Obesity, Sumera Aziz Ali, Savera Aziz Ali, Nadir Suhail, Shiyam Sunder Tikmani, Gulshan Bano

Community Health Sciences

Introduction: Child obesity is the major pediatric public health crisis of the current century and its trend is increasing in the developing countries due to nutrition and epidemiologic transition. Considering the burden of childhood obesity and its associated outcomes need for obesity prevention in children has become priority both for government and researchers.
Objective: The objective of this review is to provide the updated knowledge and evidence from various research studies, designed to provide interventions either in school or at home.
Methodology: Electronic databases like Google scholar, PubMed and Sciencedirect were used as search engines. Key terms used during the …

Compensatory Mechanisms And T Cell Migration In Mouse Models Of Dopaminergic Loss, Kristi M. Anderson

Theses & Dissertations

Parkinson’s disease (PD) is the most common neurodegenerative movement disorder and second most common neurodegenerative disorder. PD is characterized by the selective loss of dopaminergic neurons and dopamine neurotransmitter within the substantia nigra and termini in the striatum. Progressive loss of dopaminergic neurons occurs over many years in PD, and by the time movement disorder symptoms manifest, up to 50-70% of dopaminergic neurons have been lost. Several aspects of PD pathology have been described in detail, but a better understanding of PD progression is needed to develop more efficient treatments.

Motor symptoms associated with PD do not manifest until significant …

Is Dexamethasone 4mg A More Effective Anti-Emetic Than Dexamethasone 8mg For The Prevention Of Early Post-Operative Nausea And Vomiting In Women Undergoing Laparoscopic Gynecological Surgery?, Steven B. Doyle

Doctoral Projects

Postoperative nausea and vomiting (PONV) is a common problem in the surgical setting. It affects as much as 20 to 80 percent of patients undergoing surgery (D'souza, Swami, & Bhagwat, 2011). PONV can lead to increased patient costs and recovery time by causing the patient to stay in the healthcare facility for a longer period of time. A retrospective cohort study was completed to examine whether or not there was a significant difference between patients who received 4mg and 8mg of dexamethasone in the incidence of PONV. All patients studied received ondansetron intraoperatively as their primary anti-emetic. English speaking patients …

The Effectiveness Of A Preoperative Multimodal Antiemetic Regimen On Reducing Early Postoperative Nausea And Vomiting In Total Joint Arthroplasty Patients, Jerry Mosley

Doctoral Projects

Postoperative nausea and vomiting (PONV) occurs frequently in all types of surgeries including after total joint orthopedic procedures. The resulting PONV can lead to many unwanted occurrences including immobilization, distress, and many serious adverse health complications. These unwanted occurrences may then lead to increased cost to the patient and healthcare facility. Administration of a preoperative multimodal regimen known to reduce PONV has the potential to reduce such unwanted anesthetic side effects influencing a reduction in overall healthcare cost. The purpose of this study is to determine the effectiveness of the preoperative kit which includes the administration of metoclopramide, famotidine, ondansetron, …

Street Drug Markets Beyond Favelas In Belo Horizonte, Brazil, Elenice De Souza Oliveira, Braulio Figueiredo Alves Silva, Marcos Oliveira Prates

Department of Justice Studies Faculty Scholarship and Creative Works

This study examines whether social disorganization mechanisms that explain clusters of street drug markets in socially disorganized neighborhoods in developed countries can also help explain geographical patterns of drug dealing across neighborhoods in Belo Horizonte, Brazil. Data for this study includes drug arrests from 2007 to 2011 and socio demographic data from the 2010 Census. To examine the influence of exploratory variables on drug market locations, the Negative Binominal regression model was used at two levels of analysis—the Belo Horizonte city center and other neighborhoods including favelas. The findings show that a high hot spot of street drug markets located …

Normal Glycolytic Enzyme Activity Is Critical For Hypoxia Inducible Factor-1a Activity And Provides Novel Targets For Inhibiting Tumor Growth, Geoffrey Grandjean Phd

Dissertations and Theses (Open Access)

Normal Glycolytic Enzyme Activity is Critical for Hypoxia Inducible Factor-1α Activity and Provides Novel Targets for Inhibiting Tumor Growth

By Geoffrey Grandjean

Advisory Professor: Garth Powis, D. Phil

Unique to proliferating cancer cells is the observation that their increased need for energy is provided by a high rate of glycolysis followed by lactic acid fermentation in a process known as the Warburg Effect, a process many times less efficient than oxidative phosphorylation employed by normal cells to satisfy a similar energy demand ^[1]. This high rate of glycolysis occurs regardless of the concentration of oxygen in the cell and …

Mechanisms And Intervention Strategies For Alcohol And Hiv-Antiretroviral Therapy-Induced Liver Injury., Hridgandh Donde

Electronic Theses and Dissertations

Chronic alcohol consumption is a leading cause of liver disease and liver-related death worldwide. Alcoholic liver disease includes, hepatic steatosis, steatohepatitis and ultimately fibrosis and cirrhosis. Emerging evidence has established the important role of the “gut-liver” axis in the development of alcoholic liver disease (ALD). Our recent work indicated that chronic alcohol induced perturbations in the gut microbiome and consequent changes in fatty acids have a major impact on the development of intestinal barrier dysfunction and ALD. The aim of this study was to investigate whether treatment with tributyrin - a butyrate prodrug results in protection against ALD in terms …

A Plant-Made Cholera Toxin B Subunit Enhances Mucosal Wound Healing And Protects Against Ulcerative Colitis And Colon Cancer., Keegan J Baldauf

Electronic Theses and Dissertations

This dissertation describes the previously unidentified effects of a plant-produced recombinant cholera toxin B subunit (CTBp) on the gastrointestinal (GI) tract and its ability to protect against inflammation in a mouse model of colonic injury and ulcerative colitis (UC). To comprehensively analyze CTBp’s impacts on the GI tract, we employed global analysis methodologies based on multi-color flow cytometry to analyze immune cell populations in GI and systemic lymphatic compartments, gene expression microarray to decipher transcript-level changes in the colon and small intestine, and 16S rRNA sequencing to characterize fecal microbiota. Based on a drastic shift observed in the immune cell …

Eicosapentaenoic Acid (Epa) From Porphyridium Cruentum: Increasing Growth And Productivity Of The Microalgae For Pharmaceutical Products, Maryam Asgharpour

Graduate Theses and Dissertations

One of the major nutritional requirements in our diet is an adequate intake of omega-3 specially eicosapentaenoic acid (EPA). In the present study, the effects of two temperatures (16°C & 20˚C) and light intensities (140 & 180µE/M2.S) and four nitrate levels (0.075, 0.3, 0.5 and 0.7g/L) on the cell growth and lipid productivity of Porphyridium cruentum, one of the most promising oil-rich species of microalgae, were investigated. A growth comparison was carried out using pure CO2 and 5% CO2/air. Additionally, the ratio of the fatty acids with omega-3 and omega-6 groups at various growth conditions were compared, since an appropriate …

An Animal Model Of Differential Genetic Risk For Methamphetamine Intake, Tamara J. Phillips, Shkelzen Shabani

Peer Reviewed Articles

The question of whether genetic factors contribute to risk for methamphetamine (MA) use and dependence has not been intensively investigated. Compared to human populations, genetic animal models offer the advantages of control over genetic family history and drug exposure. Using selective breeding, we created lines of mice that differ in genetic risk for voluntary MA intake and identified the chromosomal addresses of contributory genes. A quantitative trait locus was identified on chromosome 10 that accounts for more than 50% of the genetic variance in MA intake in the selected mouse lines. In addition, behavioral and physiological screening identified differences corresponding …

Effects Of Nicotine On A Translational Model Of Working Memory, David Alderson Macqueen

USF Tampa Graduate Theses and Dissertations

Cognitive research with human non-smokers has demonstrated that nicotine generally enhances performance on tasks of attention but, working memory does not appear to be affected. In contrast, nicotine has been shown to produce robust enhancements of working memory in non-human animals. To address this disparity, the present study investigated the effects of nicotine (2mg, 4mg nicotine gum, and placebo) on the performance of 30 non-smokers (15 male) completing a working memory task developed for rodents (the odor span task, OST). Nicotine has been reported to enhance OST performance in rodents and the present study sought to determine whether the effect …

Macrophage Uptake And Cytotoxicity Of Paclitaxel Nanocrystals, Deborah Lee, Emeri Zhang, Wei Gao, Tonglei Li

The Summer Undergraduate Research Fellowship (SURF) Symposium

Effective drug delivery remains one of the most challenging tasks in combatting cancer cells. Anti-cancer drugs such as Paclitaxel (PTX) often struggle in having a high drug effect because they are often phagocytized by macrophages in Reticuloendothelial System (RES) before reaching the cancer cells. To combat this problem, PTX was inserted in a nanocrystal, coated with non-ionic surfactant F68; it is speculated that this formulation will minimize the particle aggregation and decrease the cellular uptake in the RES, which will increase the overall efficacy of the drug in the target areas. The aim of this project was to compare the …

An Analysis Of The Interaction Of Methylphenidate And Nicotine In Adolescent Rats: Effects On Bdnf, Elizabeth D. Freeman

Electronic Theses and Dissertations

This investigation was an analysis of the interaction of adolescent exposure to methylphenidate (MPH; trade name: Ritalin) on nicotine sensitization and conditioned place preference (CPP) in a rodent model and underlying mechanisms of this effect. Animals were treated IP with 1 mg/kg MPH or saline using a ―school day‖ regimen of five days on, two days off, from postnatal day (P) 28-50. During the final two weeks of MPH treatment, animals were either behaviorally sensitized to nicotine (0.5 mg/kg free base) or saline for 10 days, or conditioned to nicotine or saline using the CPP behavioral paradigm. In addition, three …

Removal Of Heavy Metal Ions From Aqueous Solution Using Rice Husks-Based Adsorbents, Fanuel J Ligate, James E.G Mdoe

Tanzania Journal of Science

This study reports on the preparation and characterization of rice husks-based adsorbents and their application in the removal of heavy metal ions from aqueous solution. Three different adsorbents were developed: rice husks ash (RHA), rice husks ash-derived silica (RHS) and triaminopropyl-silica hybrid (TSH-R). The prepared materials were characterized by acid titration, Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR) spectroscopy, Scanning Electron Microscopy-Energy Dispersive X-ray (SEM-EDX) spectroscopy and nitrogen physisorption analysis. Results from the ATR-FTIR analysis indicated that pure silica was obtained from RHA and that after surface modification the triaminopropyl group was successfully attached onto the silica framework with a …

Assessment Of Heavy Metal Concentration In Water Around The Proposed Mkuju River Uranium Project In Tanzania, Firmi P. Banzi, Peter K. Msaki, Najat K. Mohammed

Tanzania Journal of Science

Effective verification for compliance with water quality standards in uranium mining in Tanzania requires data sensitive to monitor heavy metal concentration in water around the Mkuju River Uranium Project before mining commences. The area susceptible for pollution by the project was estimated using AERMOD dispersion model and found to cover about 1300 km2. Thirty one surface and groundwater samples were collected and analysed for heavy metals and physicochemical properties using ICP-MS and standards techniques, respectively. The physicochemical properties for water samples analysed ranges from 5.7 to 7.8 for pH, 2.8 to 80.2 mg/L for TDS and 15 to 534.5 mS/cm …

The Cognition-Enhancing Effects Of Psychostimulants Involve Direct Action In The Prefrontal Cortex, Robert C. Spencer, David M. Devilbiss, Craig Berridge

Rowan-Virtua School of Osteopathic Medicine Departmental Research

Psychostimulants are highly effective in the treatment of attention-deficit/hyperactivity disorder. The clinical efficacy of these drugs is strongly linked to their ability to improve cognition dependent on the prefrontal cortex (PFC) and extended frontostriatal circuit. The procognitive actions of psychostimulants are only associated with low doses. Surprisingly, despite nearly 80 years of clinical use, the neurobiology of the procognitive actions of psychostimulants has only recently been systematically investigated. Findings from this research unambiguously demonstrate that the cognition-enhancing effects of psychostimulants involve the preferential elevation of catecholamines in the PFC and the subsequent activation of norepinephrine α2 and dopamine D1 receptors. …