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Articles 1 - 25 of 25
Full-Text Articles in Medicine and Health Sciences
Protein Aggregation Through Acoustic Cavitation, John A. Giarratano
Protein Aggregation Through Acoustic Cavitation, John A. Giarratano
Electronic Theses and Dissertations
Therapeutic proteins represent an essential piece of a health management plan for diseases such as diabetes, cancer, hemophilia, Crohn's Disease, and myocardial infarction. These proteins, however, must be maintained in their correct, biologically active conformation throughout processing, transportation, and delivery. This requirement poses serious engineering challenges because of a protein's susceptibility to thermodynamic instabilities resulting from the weak bonds driving the tertiary structure of the molecule. A particularly problematic type of protein degradation is aggregation. Administration of aggregated proteins, a particularly problematic degradation form, can have dire consequences, including blocking a patient's responsiveness to therapy, inducing immunogenicity, and even anaphylactic …
Approaches In The Treatment Of Parkinson's Disease : A Focus On Stem Cell-Based Therapies., Tareq Al-Maqtari 1979-
Approaches In The Treatment Of Parkinson's Disease : A Focus On Stem Cell-Based Therapies., Tareq Al-Maqtari 1979-
Electronic Theses and Dissertations
Parkinson's disease (PD) is a hypokinetic movement disorder resulting from the progressive neurodegeneration of the dopaminergic nigrostriatal system in the brain and the resulting imbalance between dopamine and acetylcholine in the basal ganglia motor circuitry. Although drug-based therapy approaches have shown dramatic symptomatic improvement in patients, they do not halt the progressive nature of the disease and their long-term use is associated with distressing adverse side effects. Consequently, several studies have aimed at discovering effective non-pharmacological strategies to reduce or to eliminate the need for drugs and possibly to halt or to reverse the neurodegenerative process in PD. Surgical deep …
Development Of Novel Thermosensitive Polymers For Bioresponsive Drug Delivery, Vivek Kumar Garripelli
Development Of Novel Thermosensitive Polymers For Bioresponsive Drug Delivery, Vivek Kumar Garripelli
Electronic Theses and Dissertations
Stimuli-responsive polymers have already shotremendous promise in controlled and self-regulated drug delivery. Successful construction of responsive polymers requires amalgamation of chemical, physical and biological principles. For careful therapy, a great deal of advantages offered by stimuli-responsive polymers is essential. A small or modest change in the environmental condition (e.g. temperature, pH, light) brings a sharp change in the properties of the responsive polymers. 'Smart' drug delivery systems utilize these principles to mimic the biological response behavior to a certain extent. Synthetic polymers incorporated with stimuli-responsive behavior would be amenable to overcome some of the systemic and intracellular delivery barriers. Development …
Effects Of Off-Label Prescribing On Patient Decision Making, Douglas Paul
Effects Of Off-Label Prescribing On Patient Decision Making, Douglas Paul
Electronic Theses and Dissertations
Objectives: Despite the comuse of off-label prescribing in the US, no research has been conducted to understand the impact of off-label prescribing on patient decision making. This study sought to measure the impact on trust in physicians, intentions of involvement in the decision making, beliefs about the drug, and initial compliance intentions in elderly and nonelderly populations. Methods. This study was designed to assess the effects of off-label prescribing using a 2 × 2 × 2 design. Using an online panel, 830 consumers were surveyed, 409 elderly and 421 nonelderly, using 8 different scenarios based on disease criticality, off-label use …
The Effect Of Exercise On Mechanical Pressure Pain Threshold In The Presence And Absence Of Delayed-Onset Muscle Soreness, Brandon Tynes
The Effect Of Exercise On Mechanical Pressure Pain Threshold In The Presence And Absence Of Delayed-Onset Muscle Soreness, Brandon Tynes
Electronic Theses and Dissertations
Research has shown decreased pain sensitivity (hypoalgesia) during and following maximal and sub-maximal isometric exercise (Koltyn, 2002). Research on fibromyalgia patients however has shown the same exercises increase pain sensitivity (hyperalgesia) (Staud, Robinson, & Price, 2005; Kosek, Ekholm, & Hansson, 1996). The purpose of the present study was to examine the effects of exercise on pressure pain thresholds (PPT) in the presence and absence of delayed-onset muscle soreness (DOMS) within the ipsilateral (contracting) and contralateral quadriceps muscle and plurisegmental finger. Data were collected using twenty-five male participants (aged 18-29) over five testing days: two days of familiarization, one day of …
Isolation, Structure Elucidation And Biological Evaluation Of Natural Products From Plants And Fungi, Xiaoning Wang
Isolation, Structure Elucidation And Biological Evaluation Of Natural Products From Plants And Fungi, Xiaoning Wang
Electronic Theses and Dissertations
Natural products have provided considerable value for drug discovery over the past half-century. Nearly four fifth of drugs were natural products or inspired by natural compounds. Bioactive secondary metabolites isolated from natural source, either fungal or terrestrial, are relatively safer for human health and the environment and can serve as drug or as drug leads for the development of synthetic or semi-synthetic analogs. Natural products have also been successfully used in agriculture as plant growth regulators, signal transductions, fungicides, herbicides and tranquilizers. In our continued efforts to identify bioactive compounds, seventy-seven plant and fungal extracts were evaluated using a direct-bioautography …
Anticancer And Antibiotic Leads From Marine Organis, Bin Wang
Anticancer And Antibiotic Leads From Marine Organis, Bin Wang
Electronic Theses and Dissertations
During the past three decades, the development of marine natural products as drug leads has become a promising avenue for research. As our efforts towards the discovery of anticancer and antibiotic drug leads from marine organisms, modifications of anticancer drug candidate kahalalide F, isolations of new peptides from the mollusk, Elysia rufescens and anticancer drug leads from the NCI repository, as well as chemical regulation of antibiotic production from marine Pseudomonas aeruginosa were investigated. Kahalalide F (KF) is a potent anticancer lead isolated from the herbivorous marine mollusk E. rufescens and its algal diet Bryopsis pennata. Our semisynthesis approach was …
Geographic And Host-Microbe Symbiotic Influence On Secondary Metabolism, Samuel Hamed Abbas
Geographic And Host-Microbe Symbiotic Influence On Secondary Metabolism, Samuel Hamed Abbas
Electronic Theses and Dissertations
This thesis is composed of studies that regard the advancement to the Arctic region and the importance of host-microbe interactions in natural product discovery. Bioactive metabolites have been reported from a myriad of marine and terrestrial organisms around the world including plants, insects, sponges, tunicates, bacteria, and fungi among others. Many macroorganisms, of which the metabolites are found, depend on the symbiotic relationship of microorganisms for metabolite production. The scope of this work is to investigate secondary metabolism of both marine and terrestrial organisms from different areas of the world as well as search for the importance of host-microbe symbiosis …
An Evaluation Of Medicaid Programs Using Medication Use-Related Quality Measures, Vennela Thumula
An Evaluation Of Medicaid Programs Using Medication Use-Related Quality Measures, Vennela Thumula
Electronic Theses and Dissertations
Objective: To assess quality of care provided to Medicaid beneficiaries using medication use-related quality indicators. Methods: This study is a retrospective analysis of 2006 & 2007 Medicaid administrative claims data from 45 states and DC. Eleven medication use-related measures (adherence/persistence and standard of care) from the AHRQ initial core set were included. A composite measure of medication use-related quality was also created. Patient case-mix adjusted measure scores were computed using hierarchical logistic regression models. States were ranked on both case-mix adjusted and unadjusted scores and categorized into top (?20%), medium (60%) and bottom (?20%) performers. Agreement in rankings and groups …
Design And Development Of Drug Delivery Systems For Immediate And Sustained Release Utilizing Hot Melt Extrusion, Abhilasha Singh
Design And Development Of Drug Delivery Systems For Immediate And Sustained Release Utilizing Hot Melt Extrusion, Abhilasha Singh
Electronic Theses and Dissertations
Polymers have indispensable role in pharmaceutical formulation development. Polymer choice is a critical factor to obtain the desired drug-release profile during formulation development for HME (Hot melt extrusion). Many commercially available, pharmaceutical-grade polymers can be used in HME formulations. The suitable polymer choice facilitates processing in the extruder. When choosing a polymer to use in a formulation, processing conditions and processing attributes of the active pharmaceutical ingredients (APIs) should be considered. The physicochemical and the mechanisms of drug release from drug delivery systems prepared by utilizing HME with various polymeric carriers were investigated. Amorphous forms of API can have as …
Pharmaceutical Formulation Development Utilizing Hot Melt Extrusion And Other Techniques For Development Of Immediate And Controlled Release Dosage Forms, Noorullah Naqvi Mohammed
Pharmaceutical Formulation Development Utilizing Hot Melt Extrusion And Other Techniques For Development Of Immediate And Controlled Release Dosage Forms, Noorullah Naqvi Mohammed
Electronic Theses and Dissertations
Hot melt extrusion (HME) was evaluated as a processing technology for the manufacture of immediate as well as controlled release formulations for oral delivery of two model compounds. For immediate release applications lower molecular weight grades of Hydroxypropyl cellulose polymers, EF and ELF, were utilized as carrier matrices to form solid solutions of a poorly soluble compound, Ketoprofen (KPR). Thermal characterization techniques were used to confirm thermal stability, miscibility and setting up processing conditions for extrusion. Extruded matrices were pelletized to be filled into pellets or further milled and compressed into tablets. Pellets exhibited a carrier dependent release with ELF …
Preformulation Characterization And Formulation Development Of Δ9-Tetrahydrocannabinol Prodrugs For Potential Treatment Of Glacuoma, Tushar Hingorani
Preformulation Characterization And Formulation Development Of Δ9-Tetrahydrocannabinol Prodrugs For Potential Treatment Of Glacuoma, Tushar Hingorani
Electronic Theses and Dissertations
Relationship between smoking marihuana and a drop in intraocular pressure (IOP) was first reported in 1971. Research efforts since then have identified a number of constituents that could be linked to this observation. Delta-9-Tetrahydrocannabinol (THC) was one of the ingredients identified. However, four decades and numerous research efforts since the first observation, it has still not been concluded whether THC is effective in the treatment of glaucoma or not. Current therapy for IOP control in glaucoma, though effective, cannot prevent vision loss completely. Thus, identification of agents that can lower IOP as well as protect the retinal ganglion cells from …
Design Synthesis And Biological Evaluation Of Non-Peptide Neuropeptide Ff Ligands, Jessica Valentinas Mankus
Design Synthesis And Biological Evaluation Of Non-Peptide Neuropeptide Ff Ligands, Jessica Valentinas Mankus
Electronic Theses and Dissertations
Neuropeptide FF is an endogenous RF-amide with two receptor subtypes originally described as having anti-opioid characteristics. While peptide work helped to elucidate key features for targeting the subtypes of the neuropeptide FF receptor, non-peptide small molecules offer a more refined tool to discover features that affect selectivity and affinity. Improvements in small molecule ligands for neuropeptide FF support lead development and offer a clearer understanding of the binding pocket of each receptor subtype. Previous work on the lead 4–anilindopiperidine structure clarified a key feature between agonist and antagonist behavior. Early modifications of substituents of the piperidine nitrogen were tolerated and …
Antimalarials From Plant Pathogenic Fungi, Mallika Kumarihamy
Antimalarials From Plant Pathogenic Fungi, Mallika Kumarihamy
Electronic Theses and Dissertations
The purpose of this study was to discover antimalarial compounds from necrotropic plant pathogenic fungi. Various phytotoxins released by necrotropic plant pathogenic fungi may inhibit the plant-like metabolic pathways in the apicoplast, a chloroplast-like organelle, essential for the survival of apicomplexan parasites, such as Plasmodium which cause malaria in humans. This dissertation describes the isolation, characterization, and biological evaluation of secondary metabolites of eight fungal strains. In addition to the antiplasmodial assay, all the extracts were subjected to phytotoxic, antimicrobial, and cytotoxic bioassays. Isolation of metabolites was performed by chromatographic methods and identification was carried out by spectroscopic and spectrometric …
Discovery Of Novel Glycogen Synthase Kinase-3beta Inhibitors: Molecular Modeling, Virtual Screening, And Biological Evaluation, Gang Fu
Electronic Theses and Dissertations
Glycogen synthase kinase-3 (GSK-3) is a multifunctional serine/threonine protein kinase which is engaged in a variety of signaling pathways, regulating a wide range of cellular processes. Due to its distinct regulation mechanism and unique substrate specificity in the molecular pathogenesis of human diseases, GSK-3 is one of the most attractive therapeutic targets for the unmet treatment of pathologies, including type-II diabetes, cancers, inflammation, and neurodegenerative disease. Recent advances in drug discovery targeting GSK-3 involved extensive computational modeling techniques. Both ligand/structure-based approaches have been well explored to design ATP-competitive inhibitors. Molecular modeling plus dynamics simulations can provide insight into the protein-substrate …
Discovery Of Small-Molecule Natural Products That Target Cellular Bioenergetics, Sandipan Datta
Discovery Of Small-Molecule Natural Products That Target Cellular Bioenergetics, Sandipan Datta
Electronic Theses and Dissertations
Molecular-targeted antitumor therapy has found favor in antitumor drug discovery programs. Hypoxia (< 5% oxygen) is a comfeature of solid tumors and hypoxia-inducible factor-1 (HIF-1) represents an important antitumor target. Bioenergetic homeostasis is typically altered in tumor cells and HIF-1 plays an important role to produce a glycolytic phenotype. Glycolysis inhibitors are an emerging class of potential tumor-selective adjuvant therapeutic agents. Natural product aerobic glycolysis inhibitors may enhance the effectiveness of current therapies. Mitochondrial oxidative phosphorylation inhibitors in botanical dietary supplements (BDS) possess a potential health hazard which should be identified and appropriately regulated. Chapter one briefly reviews the molecular-targeted natural product antitumor drug discovery process. Descriptions of tumor hypoxia, HIF-1, HIF-1 regulatory pathways and the effect of HIF-1 on tumor cell bioenergetics are presented. Cellular bioenergetic pathways and natural products that inhibit HIF-1 by interfering with cellular bioenergetics are discussed. Mitochondriotoxic small-molecule natural products reported previously are further reviewed. Chapter two discusses the effect of chromatographic media on molecular-targeted antitumor drug discovery. A panel of crude extracts was eluted through columns of various chromatographic media using a step gradient method. Total recoveries from the various columns and various elution protocols were compared and statistically analyzed. The crude extracts and column eluates were evaluated for HIF-1 inhibitory activity. Chapter three discusses the development of a bioenergetics-based screening method to screen crude extracts for glycolysis inhibitors. Crude extracts (10,648) were screened and seven hits (hit rate 0.72%) were identified. Bioassay-guided isolation of Moronobea coccinea crude extract resulted in isolation of a protonophoric compound moronone (1) (false positive). The structure of 1 was determined by a combination of spectroscopic and spectrometric means. The protonophoric compounds must be rapidly dereplicated for successful discovery of glycolysis inhibitors. Chapter four discusses the screening of BDS products and pure compounds for mitochondrial uncouplers or electron transport chain inhibitors. The blue cohosh (Caulophyllum thalictroides) extract and three saponins cauloside A (3), saponin PE (4) and cauloside C (5) permeabilize the mitochondrial membrane. Sesamin (6) and guggulsterol III (7) and guggul (Commiphora wightii) extract inhibit mitochondrial complex I. These extracts and compounds are cytotoxic in nature.
Metabolism And Pharmacokinetics In The Development Of New Therapeutics For Cocaine And Opioid Abuse, Pradeep Kumar Vuppala
Metabolism And Pharmacokinetics In The Development Of New Therapeutics For Cocaine And Opioid Abuse, Pradeep Kumar Vuppala
Electronic Theses and Dissertations
Cocaine and opioid abuse are a major public health concern and the cause of significant morbidity and mortality worldwide. The development of effective medication for cocaine and opioid abuse is necessary to reduce the impact of this issue upon the individual and society. The pharmacologic treatment for drug abuse has been based on one of the following strategies: agonist substitution, antagonist treatment, or symptomatic treatment. This dissertation is focused on the role of metabolism and pharmacokinetics in the development of new pharmacotherapies, CM304 (sigma-1 receptor antagonist), mitragynine and 7-hydroxymitragynine (μ-opioid receptor agonists), for the treatment of drug abuse. The affinity …
The Potential For Screening For Interpersonal Violence In Community Pharmacies: An Exploratory Study, Marie Barnard
The Potential For Screening For Interpersonal Violence In Community Pharmacies: An Exploratory Study, Marie Barnard
Electronic Theses and Dissertations
Intimate partner violence (IPV) is a public health problem of epidemic proportion; the only known effective health care intervention is routine screening for IPV exposure. Despite professional guidelines for routine screening, this intervention has been poorly adopted. Expansion of screening efforts to the community pharmacy setting provides an opportunity to have a substantial impact on the health, well-being of pharmacy patients. This investigation is the first to examine IPV screening related to the pharmacy environment. An existing measure of physicians' readiness to manage IPV (PREMIS) was adapted for the community pharmacy environment and validated in a national random sample of …
Design And Synthesis Of Hiv-1 Integrase Inhibitors, Sarah Chajkowski Scarry
Design And Synthesis Of Hiv-1 Integrase Inhibitors, Sarah Chajkowski Scarry
Electronic Theses and Dissertations
In recent years, HIV-1 integrase (IN) has emerged as an attractive target for the treatment of human immunodeficiency virus type 1 (HIV-1), the causative pathogen of acquired immuno-deficiency syndrome (AIDS). Several classes of IN inhibitors are known but many of these compounds are toxic, do not show antiviral activity or display decreased potency. Therefore, new classes of potent IN inhibitors are desperately needed. The b-diketo (b-DK) class of compounds has emerged as one of the most successful classes of IN inhibitors. Although several b-DK inhibitors with potent antiviral activity are known, compounds containing b-DK motifs have limitations in drug development. …
Functional Studies Of Novel Bioactives From Complex Host-Microbiomes As Drug Leads For Cancer, Infectious Disease, Depression And Pain, John Jason Bowling
Functional Studies Of Novel Bioactives From Complex Host-Microbiomes As Drug Leads For Cancer, Infectious Disease, Depression And Pain, John Jason Bowling
Electronic Theses and Dissertations
The drug discovery process has become increasingly complex in comparison to early efforts particularly those involving diseases or conditions that affect large numbers of the human population. It is difficult to point directly to one factor leading evolution of the process but the definition of a mechanism of pharmacological action for a drug lead has noticeably become a higher priority. This evolution has helped diminish the stigma of natural products and compound supply issues. The issue of compound supply has also been addressed to some extent with the emergence of recombinant technologies and new synthetic methodology. With approximately 60 years …
Development And Comparative Predictive Validity Of An Outpatient Medication Exposure Measure For Risk Adjustment Using Retrospective Claims Data, Kyle Dennis Null
Development And Comparative Predictive Validity Of An Outpatient Medication Exposure Measure For Risk Adjustment Using Retrospective Claims Data, Kyle Dennis Null
Electronic Theses and Dissertations
The purpose of this study was to develop and test a measure of outpatient prescription utilization (medication exposure measure, or MEM) that may be coupled with the CMS-HCC and CMS-RxHCC methodologies to improve risk-adjusted payments to Medicare Part C and Part D plans. Studies have identified prescription measures that predict future expenditures; however, many are easily manipulable by health plans or practitioners, thus limiting their utility as risk-adjusters. The addition of a non-manipulable prescription utilization measure to existing risk-adjustment models may improve prediction, reducing adverse risk selection incentives by health plans. A secondary objective of this study was to evaluate …
Discovery, Isolation, And Identification Of Antimalarials From Fungal Endophytes, Andrekeus Lee
Discovery, Isolation, And Identification Of Antimalarials From Fungal Endophytes, Andrekeus Lee
Electronic Theses and Dissertations
We examined fungal endophytes for their ability to inhibit bacterial, fungal and protozoal pathogens. Once antimalarial activity was discovered and confirmed, we sought to isolate and identify the active constituent(s) of our extracts. Bioassay-guided fractionation techniques were used to isolate our active compound, the structure of which was elucidated using 1H- and 13C-NMR. 2D-NMR and LC-MS analyses helped confirm that our endophytes were indeed producing artemisinin. Growth versus production studies were conducted to optimize our growth and extraction conditions while several other variables, like temperature and culture medium, were evaluated in an effort to improve our yields. Artemisinin production under …
Phytochemical Studies On The Medicinal Plant Sutherlandia Frutescens, Xiang Fu
Phytochemical Studies On The Medicinal Plant Sutherlandia Frutescens, Xiang Fu
Electronic Theses and Dissertations
Sutherlandia frutescens (L.) R. Br (Fabaceae) is a multipurpose medicinal plant with diverse biological activities, and has been widely used for the treatment of cancer, AIDS, diabetes, and infectious diseases in southern Africa. The primary goal of this study was to investigate the chemical constituents of S. frutescens and develop an analytical method to analyze this plant and the dietary supplements derived from this plant. The dissertation is composed of six chapters. Chapter 1 introduces the general background of S. frutescens, including traditional uses and chemical and biological studies on the plant. Chapter 2 describes the phytochemical studies that have …
Antileishmania Compounds From An Unidentified Endophytic Fungus And Biotransformation Of 5,7,2`,4`,5`-Pentahydroxyflavonol, Ahmed Idris
Electronic Theses and Dissertations
Leishmaniasis is a parasitic disease remaining a major public health problem. It causes illness and death especially in developing countries. Comchemotherapeutic agents currently used are often inadequate, requiring long courses of parenteral administration, having toxic side effects or becoming less effective due to the emergence of resistant strains. Thus, there is an urgent need for new, effective, and inexpensive drugs. In the fight against leishmaniasis, natural products are important sources of novel therapeutic agents. The goal of our research is to study secondary metabolites from endophytic fungi as a source of effective antileishmanial agents. Many crude extracts from endophytic fungi …
The Effects Of A Multi-Component Wellness Program On Employee Biometrics, Jennifer Erin Patrick
The Effects Of A Multi-Component Wellness Program On Employee Biometrics, Jennifer Erin Patrick
Electronic Theses and Dissertations
Corporate wellness initiatives are gaining momentum as a critical indicator of business performance. Metabolic Syndrome is commonly used within corporations to assess the health of their employees and estimate potential healthcare costs. Using five risk factors (blood pressure, high density lipoprotein (HDL-C), triglycerides (TG), fasting blood glucose, and waist circumference) individuals with three or more risk factors are classified as having Metabolic Syndrome. Voluntary pre and post health screenings were conducted at a rural manufacturing plant. A multi-component wellness program was conducted over six months to determine if the program would have significant beneficial effects on employee biometrics and Metabolic …