Chemicals and Drugs Commons^™

The Gating Charge Should Not Be Estimated By Fitting A Two-State Model To A Q-V Curve, Francisco Bezanilla, Carlos A. Villalba-Galea

School of Pharmacy Faculty Articles

The voltage dependence of charges in voltage-sensitive proteins, typically displayed as charge versus voltage (Q-V) curves, is often quantified by fitting it to a simple two-state Boltzmann function. This procedure overlooks the fact that the fitted parameters, including the total charge, may be incorrect if the charge is moving in multiple steps. We present here the derivation of a general formulation for Q-V curves from multistate sequential models, including the case of infinite number of states. We demonstrate that the commonly used method to estimate the charge per molecule using a simple Boltzmann fit is not only inadequate, but in …

Characterization Of Prophylactic Antiemetic Regimens In Pediatric Patients Receiving Moderately And Highly Emetogenic Chemotherapy, Jessica Degiacomo Pharmd, Kristin M. Held Pharmd, Bcop

Department of Pharmacy

No abstract provided.

Erg11-Mediated Azole Resistance In Candida Albicans, Stephanie Ann Flowers

Theses and Dissertations (ETD)

Although many medically important Candida species are commensal to the gut or colonizers of the skin, these organisms have the propensity to cause disease in the event of a waning immune system. Clinical manifestations of infections with Candida species can range from superficial mucosal infections to deep organ involvement usually resulting from haematogenous spread of infection. Despite significant progress made in the management of patients with fungal infections, the emergence of antifungal resistant clinical isolates creates significant problem in regards to antifungal prophylaxis and empirical treatment strategies. Antifungal resistance is associated with high mortality rates and hefty medical costs. The …

Synthesis Of Novel Ciprofloxacin Analogues And Evaluation Of Their Anti-Proliferative Effect On Human Cancer Cell Lines, Narva Suresh, Hunsur Nagendra Nagesh, Kondapalli Venkata Govri Chandra Sekhar, Anil Kumar, Amir Nasrolahi Shirazi, Keykavous Parang

Pharmacy Faculty Articles and Research

A series of twenty two novel 1-cyclopropyl-6-fluoro-4-oxo-7-(4-substitutedpiperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid analogues have been synthesized, characterized (1H NMR, 13C NMR and LCMS) and evaluated for their inhibitory activity on the proliferation of human caucasian acute lymphoblastic leukemiacells (CCRF-CEM), breast adenocarcinoma cells (MDA-MB-468) and human colon carcinoma cells (HCT-116). Among all the synthesized ciprofloxacin analogues 3t at 50 µM showed comparable potency to doxorubicin (10mol) in all three cell lines and 3j inhibited proliferation of MDA-MB-468 up to 35% selectively over other two cell lines. Cancer is a leading cause of death worldwide. It is a group of diseases characterized by uncontrolled growth. Cancer …

A Double-Blind, Randomized, Placebo-Controlled Trial Of Adjunctive Ramelteon For The Treatment Of Insomnia And Mood Stability In Patients With Euthymic Bipolar Disorder, Edward Norris, Karen Burke, Julia Correll, Ken Zemanek, Joel Lerman, Ralph Primelo, Michael Kaufmann

Edward R Norris MD, FAPA, FAPM

No abstract provided.

Sensing Charges Of The Ciona Intestinalis Voltage-Sensing Phosphatase, Carlos A. Villalba-Galea, Ludivine Frezza, Walter Sandtner, Francisco Bezanilla

School of Pharmacy Faculty Articles

Voltage control over enzymatic activity in voltage-sensitive phosphatases (VSPs) is conferred by a voltage-sensing domain (VSD) located in the N terminus. These VSDs are constituted by four putative transmembrane segments (S1 to S4) resembling those found in voltage-gated ion channels. The putative fourth segment (S4) of the VSD contains positive residues that likely function as voltage-sensing elements. To study in detail how these residues sense the plasma membrane potential, we have focused on five arginines in the S4 segment of the Ciona intestinalis VSP (Ci-VSP). After implementing a histidine scan, here we show that four arginine-to-histidine mutants, namely R223H to …

Local Tobacco Control: Application Of The Essential Public Health Services Model In A County Health Department’S Efforts To Put It Out Rockland, Lisa D. Lieberman, Una Diffley, Sandy King, Shelley Chanler, Maryanne Ferrera, Oscar Alleyne, Joan Facelle

Department of Public Health Scholarship and Creative Works

In 2000, Rockland County, a small suburban county north of New York City, dedicated $1 million of its Master Settlement Agreement funds to a comprehensive tobacco control program, Put It Out Rockland. Developed and implemented by the county health department, this program used an essential public health services model and an ongoing financial investment, within the context of strong statewide tobacco control efforts, to lower adult smoking rates to 9.7% and to reduce both smoking among youths and exposure to secondhand smoke over the ensuing decade. By combining state funds and local dollars for a total of $6.75 cost per …

Asthma Knowledge, Adherence, And Administration Techniques In Hispanic Caregivers Of Pediatrics, Joshua Arnold, Rachel Culp, Kyle Hultz, Benjamin Robertson, Jon Wilkie, Amy Wuobio, Marty L. Eng, Kelly J. Hiteshew

Kelly J. Wright, R.Ph., Pharm.D.

7.5% of Hispanics in the United States suffer from asthma-related diseases, and Latino children are not as likely to use preventative asthma medications as compared with Caucasians. Educational interventions may reduce the number of visits to emergency-care. The reasons for non-adherence are currently unknown, and discovering these reasons will help to address the problem.

Prostate Cancer Stem Cell-Targeted Efficacy Of A New-Generation Taxoid, Sbt-1214 And Novel Polyenolic Zinc-Binding Curcuminoid, Cmc2.24, Galina I. Botchkina, Edison S. Zuniga, Rebecca H. Rowehl, Rosa Park, Rahuldev Bhalla, Agnieszka B. Bialkowska, Francis Johnson, Lorne M. Golbu, Yu Zhang, Iwao Ojima, Kenneth R. Shroyer

Department of Biomedical Engineering Faculty Publications

Background

Prostate cancer is the second leading cause of cancer death among men. Multiple evidence suggests that a population of tumor-initiating, or cancer stem cells (CSCs) is responsible for cancer development and exceptional drug resistance, representing a highly important therapeutic target. The present study evaluated CSC-specific alterations induced by new-generation taxoid SBT-1214 and a novel polyenolic zinc-binding curcuminoid, CMC2.24, in prostate CSCs.

Principal Findings

The CD133high/CD44high phenotype was isolated from spontaneously immortalized patient-derived PPT2 cells and highly metastatic PC3MM2 cells. Weekly treatment of the NOD/SCID mice bearing PPT2- and PC3MM3-induced tumors with the SBT-1214 led to dramatic suppression of tumor …

Effects Of Short-Term Portacaval Anastomosis On The Peripheral And Brain Disposition Of The Blood-Brain Barrier Permeability Marker Sodium Fluorescein In Rats, Imam H. Shaik, M. K. Miah, Ulrich Bickel, Reza Mehvar

Pharmacy Faculty Articles and Research

Contradictory results have been reported with regard to the effects of various models of hepatic encephalopathy on the blood-brain barrier (BBB) permeability, which may be due partly to the use of brain concentrations of BBB markers without attention to their peripheral pharmacokinetics. The purpose of the current study was to investigate the effects of short-term portacaval anastomosis (PCA), a type B model of hepatic encephalopathy, on the peripheral pharmacokinetics and brain distribution of sodium fluorescein (FL), which is a small molecule marker of BBB passive permeability. A single 25 mg/kg dose of FL was administered intravenously to 10-day PCA and …

Single Step Synthesis Of Antibiotic Kanamycin Embedded Gold Nanoparticles For Efficient Antibacterial Activity, Shravan Gavva

Masters Theses & Specialist Projects

Nanotechnology has become the most advanced type of drug delivery system within the last decade. This advancement shifted the focus on small carriers to increase the efficiency of the drugs. Among these, gold nanoparticles (GNPs) were found to have profound biomedical applications. In current research, kanamycin embedded GNPs were prepared in a single step, single phase, and bio-friendly (green synthesis) procedure. The synthesized Kanamycin-GNPs (Kan-GNPs) were spherical in shape and had a size range of 15 ± 3 nm. The chosen kanamycin is an aminoglycosidic antibiotic that is isolated from Streptomyces kanamyceticus. These special antibiotic GNPs are further characterized using …

Random Mutagenesis Of The Aspergillus Oryzae Genome Results In Fungal Antibacterial Activity, Cory A. Leonard, Stacy D. Brown, James Russell Hayman

ETSU Faculty Works

Multidrug-resistant bacteria cause severe infections in hospitals and communities. Development of new drugs to combat resistant microorganisms is needed. Natural products of microbial origin are the source of most currently available antibiotics. We hypothesized that random mutagenesis of Aspergillus oryzae would result in secretion of antibacterial compounds. To address this hypothesis, we developed a screen to identify individual A. oryzae mutants that inhibit the growth of Methicillin-resistant Staphylococcus aureus (MRSA) in vitro. To randomly generate A. oryzae mutant strains, spores were treated with ethyl methanesulfonate (EMS). Over 3000 EMS-treated A. oryzae cultures were tested in the screen, and one isolate, …

Tigecycline Induction Of Phenol-Soluble Modulins By Invasive Methicillin-Resistant Staphylococcus Aureus Strains, Jason Yamaki, Timothy Synold, Annie Wong-Beringer

Pharmacy Faculty Articles and Research

We examined the effects of tigecycline on three types of exoproteins, α-type phenol-soluble modulins (PSMα1 to PSMα4), α-hemolysin, and protein A, in 13 methicillin-resistant Staphylococcus aureus isolates compared to those of clindamycin and linezolid. Paradoxical increases in PSMαs occurred in 77% of the isolates with tigecycline at 1/4 and 1/8 MICs and clindamycin at 1/8 MIC compared to only 23% of the isolates with linezolid at 1/8 MIC. Induction was specific to PSMα₁ to PSMα₄, as protein A and α-hemolysin production was decreased under the same conditions by all of the antibiotics used.

Oral Contraceptives, Stephenie G. Fortier

Senior Honors Theses

Cyclic oral contraceptive and continuous oral contraceptives have many similarities yet a few distinct differences. One of the major differences between cyclic and continuous oral contraceptives is that cyclic oral contraceptive pills have twenty one active pills and seven inactive pills versus the new continuous oral contraceptive pills which have 28 active pills and no inactive pills. However, though cyclic and continuous oral contraceptives do have a few differences, both types of oral contraceptives affect a woman’s body in similar ways. When choosing between cyclic and continuous oral contraceptives, it is important for women to be informed about the advantages …

Effect Of Leaving Ligands Of Platinum(Ii) Diamine Complexes On Dna And Protein Residues, Ramya Kolli

Masters Theses & Specialist Projects

Platinum compounds are widely used drugs in cancer treatments. Although DNA is the biological target, reaction of platinum compounds with proteins is also potentially significant. Our objective is to study the effects of leaving ligands on the relative reactivity between 5'-GMP (guanosine 5' phosphate), a key DNA target, and N-Acetyl - L-Methionine (N-AcMet), a key protein target. We have used NMR spectroscopy to monitor reactions with N-AcMet and 5'-GMP added to a platinum complex to see which products are formed preferentially. Previous research showed that both a non-bulky complex such as [Pt(en)(D₂O)₂]²⁺ [en=ethylenediamine], and a …

Polypharmacy In Elderly: A Cautious Trail To Tread, Saniya Raghib Sabzwari, Waris Qidwai, Seema Bhanji

Department of Family Medicine

Polypharmacy has now increasingly come into focus as the recipient of healthcare in old age worldwide. In elderly it is associated with frequent adverse drug reactions (ADRs) and drug-drug interactions resulting in significant morbidity. Geriatrics is still an emerging specialty in South Asia, especially in Pakistan, where multiple reasons for polypharmacy exist. An extensive literature review of articles using key words like \'polypharmacy,\' \'elderly\' was conducted. The recently updated Beers Criteria of classification of inappropriate drugs in the elderly was reviewed in detail. Articles of relevance to polypharmacy and evaluation of guidelines for appropriate interventions to minimise inappropriate drug prescribing …

Reinforcing Effects Of Compounds Lacking Intrinsic Efficacy At Α1 Subunit-Containing Gabaa Receptor Subtypes In Midazolam- But Not Cocaine-Experienced Rhesus Monkeys, Nina M. Shinday, Eileen K. Sawyer, Bradford D. Fischer Phd, Donna M. Platt, Stephanie C. Licata, John R. Atack, Gerard R. Dawson, David S. Reynolds, James K. Rowlett

Bradford Fischer

Design, Synthesis And Evaluation Of Antimicrobial Activity Of N-Terminal Modified Leucocin A Analogues, Krishna Chaitanya Bodapati, Rania Soudy, Hashem Etayash, Michael Stiles, Kamaljit Kaur

Pharmacy Faculty Articles and Research

Class IIa bacteriocins are potent antimicrobial peptides produced by lactic acid bacteria to destroy competing microorganisms. The N-terminal domain of these peptides consists of a conserved YGNGV sequence and a disulphide bond. The YGNGV motif is essential for activity, whereas, the two cysteines involved in the disulphide bond can be replaced with hydrophobic residues. The C-terminal region has variable sequences, and folds into a conserved amphipathic α-helical structure. To elucidate the structure–activity relationship in the N-terminal domain of these peptides, three analogues (1–3) of a class IIa bacteriocin, Leucocin A (LeuA), were designed and synthesized by …

Synthesis And Polarographic Analysis Of A2e, Elise Rivett

Honors Program Projects

As humans age, fluorescent retinoid pigments accumulate in the retinal pigment epithelial (RPE) cells responsible for photoreceptor support. These fluorophores are of interest because they seem to contribute to diseases of the retina, particularly age-related macular degeneration, which is a leading cause of blindness in older adults in the United States and currently has no cure. One well-characterized fluorophore, A2E, can be oxidized by visible light and then generate harmful oxidative species capable of inducing programmed cell death in RPE cells. Further characterization of the redox behavior of A2E could ultimately aid the development of macular degeneration treatments designed to …

Design And Synthesis Of Hif-1 Inhibitors As Anti-Cancer Therapeutics, Zeus De Los Santos

Georgia State Undergraduate Research Conference

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Developing Pentamethine Cyanine Dyes For Photodynamic Therapy, Quoc Bao H. Nguyen

Georgia State Undergraduate Research Conference

No abstract provided.

Endocrine Imaging Using Near-Infrared Fluorescent Pentamethine Cyanine Dyes, Tyler Dost

Georgia State Undergraduate Research Conference

No abstract provided.

A Thousand Tiny Pieces: The Federal Circuit’S Fractured Myriad Ruling, Lessons To Be Learned, And The Way Forward, Jonathan R. K. Stroud

Jonathan R. K. Stroud

No abstract provided.

Rescuing Acetylcholinesterase From Nerve Agent Inhibition: Protein Dynamics Driven Drug Discovery, Aiyana M. Emigh, Brian Bennion

STAR Program Research Presentations

Severe morbidity and mortality consequences result from irreversible inhibition of human acetylcholinesterase by organophosphates (OPs). Oxime-based reactivators are currently the only available treatments but lack efficacy in the central nervous system (CNS) where the most damage occurs. Computational docking and molecular dynamics (MD) simulations reveal complex structural barriers that may reduce oxime efficacy. These results may guide future drug designs of more effective countermeasures.

Environmental And Behavioral Controls Of The Expression Of Clozapine Tolerance: Evidence From A Novel Across-Model Transfer Paradigm, Min Feng, Nan Sui, Ming Li

Department of Psychology: Faculty Publications

Repeated administration of antipsychotic drugs induces a sensitization-like or tolerance-like effect in many behavioral tasks, including the conditioned avoidance response (CAR) and the phencyclidine (PCP)-induced hyperlocomotion, two rodent models with high predictive validity for antipsychotic activity. This study investigated the impacts of contextual and behavioral variables on the expression of clozapine tolerance using a recently validated across-model transfer paradigm (Zhang and Li, 2012). Male Sprague-Dawley rats were first repeatedly treated with clozapine (2.5–10.0 mg/kg, sc) in the CAR model or PCP (1.6 mg/kg, sc)-induced hyperlocomotion model for five consecutive days. They were then tested for the expression of clozapine tolerance …

Medical Marijuana Legislation: What We Know - And Don't, Linda Simoni-Wastila, Francis B. Palumbo

Journal of Health Care Law and Policy

No abstract provided.

Avoidance Disruptive Effect Of Clozapine And Olanzapine Is Potentiated By Increasing The Test Trials: Further Test Of The Motivational Salience Hypothesis, Min Feng, Nan Sui, Ming Li

Department of Psychology: Faculty Publications

Antipsychotic drugs suppress animals’ ability to avoid an aversive stimulus in the conditioned avoidance response model (CAR). This behavioral effect is thought to reflect antipsychotic activity and is suggested to be mediated by a drug’s action in attenuating the motivational salience of a conditioned stimulus (CS). In the present study, we tested whether atypical antipsychotic drugs clozapine and olanzapine act through this behavioral mechanism by manipulating the number of avoidance test trials. We reasoned that more CS trials in the present of clozapine or olanzapine would afford the drug more opportunities to decrease the motivational salience of the CS, thus …

The Best Of Both Worlds: Applying Federal Commerce And State Police Powers To Reduce Prescription Drug Abuse, Michael C. Barnes, Gretchen Arndt

Journal of Health Care Law and Policy

No abstract provided.

Evaluation Of Vancomycin Dosing And Corresponding Drug Concentrations In Neonatal Intensive Care Unit (Nicu) Patients, Christine Lam Pharmd, Jenny Boucher Bs, Pharmd, Jd, Bcps

Department of Pharmacy

No abstract provided.

Turning Stealth Liposomes Into Cationic Liposomes For Anticancer Drug Delivery, Vijay Gyanani

University of the Pacific Theses and Dissertations

Targeting the anticancer agents selectively to cancer cells is desirable to improve the efficacy and to reduce the side effects of anticancer therapy. Previously reported passive tumor targeting by PEGylated liposomes (stealth liposomes) have resulted in their higher tumor accumulation. However their interaction with cancer cells has been minimal due to the steric hindrance of the PEG coating. This dissertation reports two approaches to enhance the interaction of stealth liposomes with cancer cells. First, we designed a lipid-hydrazone-PEG conjugate that removes the PEG coating at acidic pH as in the tumor interstitium. However, such a conjugate was highly unstable on …