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Medicinal Chemistry and Pharmaceutics Commons™
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Articles 1 - 30 of 32
Full-Text Articles in Medicinal Chemistry and Pharmaceutics
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
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
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 …
Anticancer Activity Of Some Boronic Acid Arylidene Heterocycles, Joy Kim
Anticancer Activity Of Some Boronic Acid Arylidene Heterocycles, Joy Kim
Honors Theses
This research was done in order to investigate the anticancer activity of boronic acid arylidene heterocycles. Boronic acid, heterocycles, and aryl compounds have all independently exhibited various anti-microbial properties and have shown potential to be used in pharmaceuticals for the treatment of viruses and cancers. Using a one-step protocol developed by Dr. Murray, several different arylheterocyclic compounds were combined with an arylboronic acid to synthesize novel compounds. These were then tested for their anti-cancer activity on glioblastoma brain cancer cells. Although varied in potency, all had some amount of anti-cellular effect on the cancer cells. This is only the start …
Lack Of Resistance Of Plasmodium Falciparum To Dihydroartemisinin In Uganda Based On Parasitogolgical And Molecular Assays, Roland A. Cooper, Melissa D. Conrad, Quentin D. Watson, Stephanie J. Huezo, Harriet Ninsiima, Patrick Tumwebaze, Samuel L. Nsobya, Philip J. Rosenthal
Lack Of Resistance Of Plasmodium Falciparum To Dihydroartemisinin In Uganda Based On Parasitogolgical And Molecular Assays, Roland A. Cooper, Melissa D. Conrad, Quentin D. Watson, Stephanie J. Huezo, Harriet Ninsiima, Patrick Tumwebaze, Samuel L. Nsobya, Philip J. Rosenthal
Collected Faculty Scholarship
- Artemisinin-‐based combination therapy is now standard treatment for falciparum malaria. However, this regimen is threatened by resistance to artemisinins, manifest as delayed clearance of parasitemia after therapy, in southeast Asia.
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Artemisinin resistance in southeast Asia is associated with increased parasitemias in culture, compared to those in sensi0ve parasites, 72 hours a=er a 6 hour pulse with 700 nM dihydroartemisinin (DHA), and with propeller domain polymorphisms in the Plasmodium falciparum kelch (K13; PF3D7_1343700) gene
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Given that artemether/lumefantrine has been adopted as standard therapy for malaria within the last decade in Uganda, we characterized artemisinin sensiBvity in fresh P. falciparum isolates from …
Mutations In The Plasmodium Falciparum Chloroquine Resistance Transporter, Pfcrt, Enlarge The Parasite's Food Vacuole And Alter Drug Sensitivities, Serena Pulcini, Henry M. Staines, Andrew H. Lee, Sarah H. Shafik, Guillaume Bouyer, Catherine M. Moore, Daniel A. Daley, Matthew J. Hoke, Lindsey M. Altenhofen, Heather J. Painter, Jianbing Mu, David J. P. Ferguson, Manuel Llinas, Rowen E. Martin, David A. Fidock, Roland Cooper, Sanjeev Krishna
Mutations In The Plasmodium Falciparum Chloroquine Resistance Transporter, Pfcrt, Enlarge The Parasite's Food Vacuole And Alter Drug Sensitivities, Serena Pulcini, Henry M. Staines, Andrew H. Lee, Sarah H. Shafik, Guillaume Bouyer, Catherine M. Moore, Daniel A. Daley, Matthew J. Hoke, Lindsey M. Altenhofen, Heather J. Painter, Jianbing Mu, David J. P. Ferguson, Manuel Llinas, Rowen E. Martin, David A. Fidock, Roland Cooper, Sanjeev Krishna
Collected Faculty Scholarship
Mutations in the Plasmodium falciparum chloroquine resistance transporter, PfCRT, are the major determinant of chloroquine resistance in this lethal human malaria parasite. Here, we describe P. falciparum lines subjected to selection by amantadine or blasticidin that carry PfCRT mutations (C101F or L272F), causing the development of enlarged food vacuoles. These parasites also have increased sensitivity to chloroquine and some other quinoline antimalarials, but exhibit no or minimal change in sensitivity to artemisinins, when compared with parental strains. A transgenic parasite line expressing the L272F variant of PfCRT confirmed this increased chloroquine sensitivity and enlarged food vacuole phenotype. Furthermore, the introduction …
Development Of Polymer Peptide Conjugates For Enhanced Pancreatic Cancer Imaging, Wen Shi
Development Of Polymer Peptide Conjugates For Enhanced Pancreatic Cancer Imaging, Wen Shi
Theses & Dissertations
Pancreatic ductal adenocarcinoma (PDAC) is the fourth leading cause of cancer-related deaths in the US with very poor prognosis. All clinically available biomarkers and diagnostic tools either fail to detect early stage PDAC or suffer from low specificity and sensitivity. There is an urgent need for diagnostic agents with greater efficacy for PDAC detection and staging. Nanomaterials such as N-(2-Hydroxypropyl) methacrylamide (HPMA) copolymers can effectively target tumors, and offer novel opportunities for the development of effective diagnostic agents for cancer. However, a major problem of many nanomaterials-based diagnostics is their opsonization and sequestration by the mononuclear phagocyte system (MPS), leading …
Macrophage Uptake And Cytotoxicity Of Paclitaxel Nanocrystals, Deborah Lee, Emeri Zhang, Wei Gao, Tonglei Li
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 …
Lack Of Artemisinin Resistance In Plasmodium Falciparum In Uganda Based On Parasitological And Molecular Assays, Roland A. Cooper, Melissa D. Conrad, Quentin D. Watson, Stephanie J. Huezo, Harriet Ninsiima, Patrick Tumwebaze, Samuel L. Nsobya, Philip J. Rosenthal
Lack Of Artemisinin Resistance In Plasmodium Falciparum In Uganda Based On Parasitological And Molecular Assays, Roland A. Cooper, Melissa D. Conrad, Quentin D. Watson, Stephanie J. Huezo, Harriet Ninsiima, Patrick Tumwebaze, Samuel L. Nsobya, Philip J. Rosenthal
Collected Faculty Scholarship
We evaluated markers of artemisinin resistance in Plasmodium falciparum isolated in Kampala in 2014. By standard in vitro assays, all isolates were highly sensitive to dihydroartemisinin (DHA). By the ring-stage survival assay, after a 6-h DHA pulse, parasitemia was undetectable in 40 of 43 cultures at 72 h. Two of 53 isolates had nonsynonymous K13-propeller gene polymorphisms but did not have the mutations associated with resistance in Asia. Thus, we did not see evidence for artemisinin resistance in Uganda.
Combating Infectious Diseases In Aquaculture With An Original Probiotic Product, Meagan Hamblin, Saebom Sohn, Christine Ahn Dao, Marta Gomez-Chiarri, David R. Nelson, David Worthen, David Rowley
Combating Infectious Diseases In Aquaculture With An Original Probiotic Product, Meagan Hamblin, Saebom Sohn, Christine Ahn Dao, Marta Gomez-Chiarri, David R. Nelson, David Worthen, David Rowley
Senior Honors Projects
Oyster production in Rhode Island accounts for over $2.5 million in annual revenue, making it the top aquaculture product in the state. However, larval tank infections significantly constrain production and create substantial economic losses for commercial hatcheries. In most cases antibiotics may not be used to prevent or treat larval tank infections. A probiotic, or beneficial microbe which competes with pathogens, is a safer and “green” approach to preventing infections. Vibriosis, a common cause of oyster larval mortality, is the result of Vibrio species infections. Previous studies have shown that a native Rhode Island microbe, Bacillus pumilus RI06-95, protects oyster …
Investigating The Bioactive Constituents Of The Edible Blue-Green Alga Spirulina Platensis, Georgette Appiah-Pippim
Investigating The Bioactive Constituents Of The Edible Blue-Green Alga Spirulina Platensis, Georgette Appiah-Pippim
Honors Scholar Theses
More people die annually from cardiovascular disease than from any other cause. Two risk factors for cardiovascular disease are hyperlipidemia and inflammation. Current drugs that are prescribed to regulate lipid levels often have adverse effects such as liver dysfunction. Blue-green algae (BGA), also known as cyanobacteria, have been consumed for years for their health benefits because they are believed to increase energy and prevent disease. One genus of edible blue-green algae is Spirulina plantesis (SP, Spirulina). Various studies have shown that Spirulina may have anti-cancer and anti-inflammation and anti-bacterial properties. In a previous study, Spirulina platensis lowered triglyceride and cholesterol …
The Impact Of Stress History Of Deformable Dry Granules On The Mechanical Properties Of Tablets, Biplob K Mitra
The Impact Of Stress History Of Deformable Dry Granules On The Mechanical Properties Of Tablets, Biplob K Mitra
Open Access Dissertations
A mechanistic understanding of the relationship among the granule composition, individual granule property, downstream robust processing, and the final tablet attributes is critical for rational development of a quality tablet. However, in the dry granulation literature, milled granules that are polydisperse in solid fraction, size, and shape are extensively used for compaction studies. Thus, the effect of an individual granule property or an individual component on the compaction properties of dry granules was not adequately separated. To advance the mechanistic understanding of the effect of dry granulation on tensile strength of tablets, individual granule properties such as size, solid fraction, …
Impact Of Antimalarial Treatment And Chemoprevention On The Drug Sensitivity Of Malaria Parasites Isolated From Ugandan Children, Patrick Tumwebaze, Melissa D. Conrad, Andrew Walakira, Norbert Leclair, Oswald Byaruhanga, Christine Nakazibwe, Benjamin Kozak, Jessica Bloome, Jaffer Okiring, Abel Kakuru, Victor Bigira, James Kapisi, Jennifer Legac, Jiri Gut, Roland A. Cooper, Moses R. Kamya, Diane V. Havlir, Grant Dorsey, Bryan Greenhouse, Samuel L. Nsobya, Philip J. Rosenthal
Impact Of Antimalarial Treatment And Chemoprevention On The Drug Sensitivity Of Malaria Parasites Isolated From Ugandan Children, Patrick Tumwebaze, Melissa D. Conrad, Andrew Walakira, Norbert Leclair, Oswald Byaruhanga, Christine Nakazibwe, Benjamin Kozak, Jessica Bloome, Jaffer Okiring, Abel Kakuru, Victor Bigira, James Kapisi, Jennifer Legac, Jiri Gut, Roland A. Cooper, Moses R. Kamya, Diane V. Havlir, Grant Dorsey, Bryan Greenhouse, Samuel L. Nsobya, Philip J. Rosenthal
Collected Faculty Scholarship
Changing treatment practices may be selecting for changes in the drug sensitivity of malaria parasites. We characterized ex vivo drug sensitivity and parasite polymorphisms associated with sensitivity in 459 Plasmodium falciparum samples obtained from subjects enrolled in two clinical trials in Tororo, Uganda, from 2010 to 2013. Sensitivities to chloroquine and monodesethylamodiaquine varied widely; sensitivities to quinine, dihydroartemisinin, lumefantrine, and piperaquine were generally good. Associations between ex vivo drug sensitivity and parasite polymorphisms included decreased chloroquine and monodesethylamodiaquine sensitivity and increased lumefantrine and piperaquine sensitivity with pfcrt 76T, as well as increased lumefantrine sensitivity with pfmdr1 86Y, Y184, and 1246Y. …
Increasing Expression Of Hepatitis B Surface Antigen In Maize Through Breeding, Erin Suzanne Miller
Increasing Expression Of Hepatitis B Surface Antigen In Maize Through Breeding, Erin Suzanne Miller
Master's Theses
The hepatitis B virus (HBV) is a common virus, with two billion people infected worldwide. It causes approximately 600,000 deaths each year, despite the availability of an effective vaccine since 1982. Maize as a platform for oral vaccination can supply a heat stable vaccine, which does not require syringes or trained personnel to administer. The Hepatitis B Surface antigen was transformed into maize and this seed was used to evaluate expression levels through the breeding process. The transgene was transferred into two elite maize inbreds by backcrossing. Highest expressing ears were selected each generation until approximately 99% commercial parent was …
Repeated Effects Of The Neurotensin Receptor Agonist Pd149163 In Three Animal Tests Of Antipsychotic Activity: Assessing For Tolerance And Cross-Tolerance To Clozapine, Shinnyi Chou, Collin Davis, Sean Jones, Ming Li
Repeated Effects Of The Neurotensin Receptor Agonist Pd149163 In Three Animal Tests Of Antipsychotic Activity: Assessing For Tolerance And Cross-Tolerance To Clozapine, Shinnyi Chou, Collin Davis, Sean Jones, Ming Li
Department of Psychology: Faculty Publications
Neurotensin is an endogenous neuropeptide closely associated with the mesolimbic dopaminergic system and shown to possess antipsychotic-like effects. In particular, acute neurotensin receptor activation can inhibit conditioned avoidance response (CAR), attenuate phencyclidine (PCP)-induced prepulse inhibition (PPI) disruptions, and reverse PCP-induced hyperlocomotion. However, few studies have examined the long term effects of repeated neurotensin receptor activation and results are inconsistent. Since clinical administration of antipsychotic therapy often requires a prolonged treatment schedule, here we assessed the effects of repeated activation of neurotensin receptors using an NTS1 receptor selective agonist, PD149163, in 3 behavioral tests of antipsychotic activity. We also investigated whether …
Development Of Non-Traditional Platinum Anticancer Agents: Trans-Platinum Planar Amine Compounds And Polynuclear Platinum Compounds, Daniel E. Lee
Development Of Non-Traditional Platinum Anticancer Agents: Trans-Platinum Planar Amine Compounds And Polynuclear Platinum Compounds, Daniel E. Lee
Theses and Dissertations
Development of Non-Traditional Platinum Anticancer Agents: trans-Platinum Planar Amine Compounds and Polynuclear Platinum Compounds
By Daniel E. Lee, Ph.D.
A dissertation submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy at Virginia Commonwealth University.
Virginia Commonwealth University, 2015
Major Director: Nicholas P Farrell, Ph.D., Professor, Department of Chemistry
Platinum anticancer compounds with cis geometry, similar to cisplatin, have been explored to circumvent the cisplatin resistance; however, they were not considered broadly active in cisplatin cells due to exhibiting similar or same cell death mechanism as cisplatin. Platinum compounds with trans geometry were less studied …
Elaboration And Design Of Α7 Nachr Negative Allosteric Modulators, Osama I. Alwassil
Elaboration And Design Of Α7 Nachr Negative Allosteric Modulators, Osama I. Alwassil
Theses and Dissertations
α7 Neuronal nicotinic acetylcholine receptors are one of two major classes of receptors responsible for cholinergic neurotransmission in the central nervous system. The existence of α7 neuronal nAChRs in different regions of the nervous system suggests their involvement in certain essential physiological functions as well as in disorders such as Alzheimer’s disease (AD), drug dependence, and depression. This project was aimed toward the discovery and development of small–molecule arylguanidines that modulate α7 nAChR function with improved subtype-selectivity through an allosteric approach. Identifying the required structural features of these small molecules allowed optimization of their negative allosteric modulator (NAM) actions at …
Development Of Irreversible Substrate Competitive Probes For Pka Activity, Robert A. Coover
Development Of Irreversible Substrate Competitive Probes For Pka Activity, Robert A. Coover
Theses and Dissertations
The current environment for drug discovery and disease treatment relies heavily on genomic analysis, structural biology and chemical biology techniques. With the enormous advances in genomic analysis and structural biology, the use of and desire for targeted therapies has increased. However, as more genomic data for cancer disease state pathology becomes available we must ask increasingly difficult questions and even produce new technologies, such as activity-based probes, to answer these questions.
In particular, targeted kinase inhibitors for the treatment of cancer has become a mainstay for drug development for both industry and academia, but it is evident that the genomic …
A Retrospective Cohort Study Of High Prevalence Of St131 Among Extended Spectrum Β-Lactamase Producing E. Coli Among Inpatients In The Metropolitan Detroit Area, Pansy Awasthy
Wayne State University Theses
ABSTRACT
HIGH PREVALENCE OF ST131 AMONG EXTENDED SPECTRUM Β-LACTAMASE PRODUCING E. COLI AMONG INPATIENTS IN THE METROPOLITAN DETROIT AREA
by
PANSY AWSTHY
2015
Advisor: Dr. Emily T. Martin
Major: Pharmaceutical Sciences
Degree: Master of Science
Objectives: E.coli ST131 multi-locus sequence type (MLST) has been associated with extended spectrum β-lactamase (ESBL) production, conferring antimicrobial resistance, with increased virulence and with healthcare-associated infection. The high prevalence of multidrug antimicrobial resistance in ESBL-producing ST131 E.coli infections creates unique challenges in the studying patient outcomes and analysis are required to study ST131 E.coli amongst a large population of ESBL-producers. Our objective was to determine …
Protein Ubiquitination In Primary Human Skeletal Muscle Cells Under Hyperinsulinemic Hyperglycemic Conditions, Majed Abdullah Alharbi
Protein Ubiquitination In Primary Human Skeletal Muscle Cells Under Hyperinsulinemic Hyperglycemic Conditions, Majed Abdullah Alharbi
Wayne State University Theses
Ubiquitin proteasome system is a relatively newly discovered pathway for protein degradation. Many studies have successfully pointed out the critical functions that UPS plays in regulating many physiological processes. On the other hand, recent studies suggested that abnormal UPS activities might be involved in the pathophysiology of several disorders including type 2 diabetes. However, the specific changes in UPS during the development of insulin resistance and consequently T2D are still unclear.
UPS is composed of two major steps, a reversible ubiquitin conjugation to the targeted substrate followed by proteasomal degradation of the ubiquitinated proteins. In this study, we examined the …
Novel Protein Phosphatase 2a Complexes In Skeletal Muscle From Obese Insulin Resistant Human Participants, Divyasri Damacharla
Novel Protein Phosphatase 2a Complexes In Skeletal Muscle From Obese Insulin Resistant Human Participants, Divyasri Damacharla
Wayne State University Theses
Type 2 Diabetes is a metabolic disorder associated with insulin resistance and consequent high blood glucose levels. Maximum glucose disposal takes place in skeletal muscle and studying skeletal muscle insulin resistance is crucial. Protein Phosphatase 2A (PP2A) is one of the major serine/threonine phosphatases belonging to PhosphoProteinPhosphatase (PPP) family. It constitutes about 80% of all serine/threonine phosphatases. It is regulated by numerous regulatory subunits as well as other substrate molecules and post translational modifications. This alters their localization, activity and also its target molecules. Many evidences show the effect of insulin on PP2Ac and its abnormal regulation in conditions of …
The Role Of E3 Ligase Parkin In Trafficking Of Monoamine Storage Vesicles In Rat Model Of Methamphetamine Neurotoxicity, Heli Dineshchandra Chauhan
The Role Of E3 Ligase Parkin In Trafficking Of Monoamine Storage Vesicles In Rat Model Of Methamphetamine Neurotoxicity, Heli Dineshchandra Chauhan
Wayne State University Theses
Methamphetamine (METH), a psychostimulant, is a widely used drug of abuse. METH is toxic to dopaminergic (DAergic) and serotonergic (5-HT) nerve terminals in the striatum when administered at high doses. METH releases Dopamine (DA) from vesicular monoamine transporter 2 (VMAT2) containing synaptic vesicles and induces oxidative stress by auto-oxidation of DA. The VMAT2 plays a neurprotective role by sequestering cytoplasmic DA into vesicles for storage and protection from auto-oxidation. It has previously been shown that METH toxicity is associated with impaired VMAT2 trafficking and oxidative damage to the E3 ligase parkin. CDCrel1, a protein found to inhibit exocytosis, is regulated …
Combination Of Photodynamic Therapy With Fenretinide And C6-Pyridinium Ceramide Enhances Killing Of Scc17b Human Head And Neck Squamous Cell Carcinoma Cells Via The De Novo Sphingolipid Biosynthesis And Mitochondrial Apoptosis, Nithin Bhargava Boppana
Wayne State University Theses
The ceramide generated via the de novo sphingolipid biosynthesis has been shown to regulate apoptosis and cell death. The de novo sphingolipid biosynthesis includes ceramide synthase (CERS)-dependent acylation of dihydrosphingosine, giving rise to dihydroceramide, which is then converted to ceramide by a desaturase-dependent reaction. The mitochondrial pathway of apoptosis, characterized by induction of Bax associated with mitochondria and cytochrome c release/redistribution. Bcl2, an anti-apoptotic protein blocks apoptosis by inhibiting Bax. Elucidating the role of de novo sphingolipid biosynthesis and mitochondrial apoptosis in PDT, PDT+4HPR and PDT+LCL29 could help in improving the effectiveness on these anti-cancer treatments. The objective of this …
Contaminants Of Emerging Concern: Effects Of Known Neuroactive Agents, Antibiotics, And Chemically Uncharacterized Photodegredates On Behavior And Physiology Of Daphnia Pulex, Vibhuti Matta
Wayne State University Theses
Emerging contaminants such as pharmaceuticals and personal care products (PPCPs), herbicides, pesticides, plasticizers, fire retardants, polycyclic aromatic hydrocarbons (PAHs), and other organic waste are increasingly being detected in surface water and ground water. These contaminants can enter into the environment through wastewater treatment plant effluent and agriculture runoff. Many of these emerging contaminants tend to be biologically active at very low concentrations, typically occur in water as part of complex mixtures, and may impact biota at concentrations not detected using traditional toxicity tests (e.g. LC 50 tests).
This study focuses on utilizing novel Daphnid optical bioassays to examine the toxicity …
Exploring Novel Daptomycin Combinations With Β-Lactam Against Susceptible & Non-Susceptible Enterococcus Species, Animesh Raut
Exploring Novel Daptomycin Combinations With Β-Lactam Against Susceptible & Non-Susceptible Enterococcus Species, Animesh Raut
Wayne State University Theses
EXPLORING DAPTOMYCIN COMBINATION WITH β-LACTAM SYNERGY AGAINST SUSCEPTIBLE AND NON-SUSCEPTIBLE ENTEROCOCCI SPECIES
by
ANIMESH RAUT
August 2015
Advisor: Dr. Michael J. Rybak
Major: Pharmaceutical sciences
Degree: Master of Science
Objective: Enterococcus faecalis and Enterococcus faecium are generally resistant to daptomycin and β-lactam antibiotics. However, documented in vitro data suggests synergy between several β-lactam antibiotics and daptomycin against resistant organisms. Primary goal of the study was to check various combinations of β-lactam antibiotics with daptomycin (DAP) and assess the potential of synergy and conclude which could be the superior combination. Study also evaluated potential of β-lactam antibiotics to enhance activity of …
Effect Of Metformin On Global Phosphorylation Profiles Of Primary Skeletal Muscle Cells Derived From Overweight/Obese Insulin Resistant Human Participants, Nishit Shah
Wayne State University Theses
Metformin is a drug from the biguanide class and it has been in use for the treatment of type 2 diabetes for a long time, and it can improve insulin sensitivity in skeletal muscle. However, the mechanism for metformin’s action is unclear. Phosphatases and kinases, and their subunits are the proteins required for dephosphorylation and phosphorylation of proteins in cells during various signaling pathways. Phosphorylation studies of proteins from primary cell culture derived from skeletal muscle tissue from obese/overweight insulin resistant participants will help to understand the regulation of phosphorylation in phosphatases and kinases by metformin.
In the current research, …
Target-Directed Biosynthetic Evolution: Redirecting Plant Evolution To Genomically Optimize A Plant’S Pharmacological Profile, Dustin Paul Brown
Target-Directed Biosynthetic Evolution: Redirecting Plant Evolution To Genomically Optimize A Plant’S Pharmacological Profile, Dustin Paul Brown
Theses and Dissertations--Neuroscience
The dissertation describes a novel method for plant drug discovery based on mutation and selection of plant cells. Despite the industry focus on chemical synthesis, plants remain a source of potent and complex bioactive metabolites. Many of these have evolved as defensive compounds targeted on key proteins in the CNS of herbivorous insects, for example the insect dopamine transporter (DAT). Because of homology with the human DAT protein some of these metabolites have high abuse potential, but others may be valuable in treating drug dependence. This dissertation redirects the evolution of a native Lobelia species toward metabolites with greater activity …
Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen
Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen
Theses and Dissertations--Pharmacy
Natural products provide some of the most potent anticancer agents and offer a template for new drug design or improvement with the advantage of an enormous chemical space. The overall goal of this thesis research is to enhance the chemical space of two natural products in order to generate novel drugs with better in vivo bioactivities than the original natural products.
Polycarcin V (PV) is a gilvocarcin-type antitumor agent with similar structure and comparable bioactivity with the principle compound of this group, gilvocarcin V (GV). Modest modifications of the polyketide-derived tetracyclic core of GV had been accomplished, but the most …
Utilization Of Placebo Response In Double-Blind Psychopharmacological Studies, Contextual Perspective, Margarita Olegovna Ashirova
Utilization Of Placebo Response In Double-Blind Psychopharmacological Studies, Contextual Perspective, Margarita Olegovna Ashirova
Antioch University Dissertations & Theses
Placebo response has been an elusive phenomenon in the fields of medicine, medical research, and psychology. Even though it has been heavily utilized as a comparator treatment in double-blind psychopharmacological studies, the reliable definition and consistent understanding of placebo response are missing. In this contextual exploration, I outlined the state of current placebo response research and variable rates of placebo response reported in double-blind studies. I identified the gap in the literature—lack of consistent understanding of placebo response—that has led to a waste of resources by the psychopharmacological research industry. Further, I compared and contrasted the current inconsistent Western medical …
Bioethanol: Feedstock Alternatives, Pretreatments,Lignin Chemistry, And The Potential For Green Value-Added Lignin Co-Products, Ruben Michael Ceballos, N. A. Batchenkova, M.K. Y. Chan, A. X. Duffing-Romero, A. E. Nelson, S. Man
Bioethanol: Feedstock Alternatives, Pretreatments,Lignin Chemistry, And The Potential For Green Value-Added Lignin Co-Products, Ruben Michael Ceballos, N. A. Batchenkova, M.K. Y. Chan, A. X. Duffing-Romero, A. E. Nelson, S. Man
Biological Sciences Faculty Publications and Presentations
Major challenges still exist in the cost-competitive production of cellulosic ethanol. Lignocellulose deconstruction using physiochemical pretreatments continues to be the most efficient way to remove lignin and expose cellulose for enzyme-mediated sugar reduction. Recent interest in the development of “value-added” lignin co-products and the desire to reduce the use of hazardous materials has prompted a resurgence of interest in alternative lignocellulosic feedstock and research into environment-friendly biological pretreatments. This article provides an overview of bioethanol processes and economics, standard and alternative feedstocks, physiochemical and biological pretreatments, and lignin chemistry. The chemistry and mode of action of ligninolytic and cellulolytic enzymes …