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Model-Based In-Vitro Pk/Pd Profiling Of Novel Synthetic Allosteric Effectors Of Hemoglobin (Aeh) As Potential Sickle Cell Disease (Scd) Therapeutics, Xiaomeng Xu 2020 VCU, School of Pharmacy

Model-Based In-Vitro Pk/Pd Profiling Of Novel Synthetic Allosteric Effectors Of Hemoglobin (Aeh) As Potential Sickle Cell Disease (Scd) Therapeutics, Xiaomeng Xu

Theses and Dissertations

Introduction: Allosteric effectors of hemoglobin (AEH) represent a class of synthetic aromatic aldehydes that transiently form covalent interactions (Schiff-base) with hemoglobin (Hb) to form Hb-AEH adduct, preventing the HbS polymerization and sickling of red blood cells (RBC). The overall objective of this research was to aid in the optimization of novel AEH by understanding their target-site disposition of AEH in relevant biological matrices, e.g., HbA solution, whole blood (WB) and human liver cytosol (HLC), a surrogate of aldehyde dehydrogenase (ALDH)-mediated oxidative metabolism.

Methods: A “universal” HPLC-UV/Vis assay method was developed for the quantitation of HbA-AEH adduct for chemically …


The Impact Of The Fda Warning On Post-Tonsillectomy Opioid Prescribing In Publicly And Privately Insured Children, Dianna J. Soelberg 2020 Virginia Commonwealth University

The Impact Of The Fda Warning On Post-Tonsillectomy Opioid Prescribing In Publicly And Privately Insured Children, Dianna J. Soelberg

Theses and Dissertations

Due to reports of significant adverse events, the U.S. FDA placed a Boxed Warning on the opioid codeine in February 2013 – contraindicating its use in pediatric patients undergoing tonsillectomy and/or adenoidectomy. Studies conducted in privately insured children showed a reduction in codeine prescribing and a slight increase in alterative opioid prescribing following the FDA warning, yet the extent to which the FDA warning impacted prescribing in publicly insured children is unknown. Using a quasi-experimental interrupted time series design, this study evaluated codeine and alternative opioid prescribing before and after the FDA warning in both publicly and privately insured children …


Development And Validation Of Predictive Risk And Multiple Criteria Decision Analysis Models To Evaluate Cardiovascular Outcomes Among Cancer Patients, Purva N. Parab 2020 Virginia Commonwealth University

Development And Validation Of Predictive Risk And Multiple Criteria Decision Analysis Models To Evaluate Cardiovascular Outcomes Among Cancer Patients, Purva N. Parab

Theses and Dissertations

Objective: The objectives of our study were to characterize the study population with cancer and cardiovascular diseases (CVD) both as compared to those without and to build a predictive model using machine learning (ML) algorithms that can predict the risk of CVD in cancer patients. In addition, our objective was also to evaluate characteristics associated with cardiotoxic adverse events of breast cancer therapies and develop a multiple criteria decision analysis (MCDA) model to conduct benefit-risk assessment of breast cancer therapy regimens. Methods: We used Medical Expenditure Panel Survey (MEPS) and FDA Adverse Events Reporting System (FAERS) 2005-2015 files along with …


Development Of A Screening Assay For Type Iii Secretion System Inhibitors And High Throughput Screening Campaign Of Inhibitors Of Prp Of Staphylococcus Aureus, Heather A. Pendergrass 2020 Virginia Commonwealth University

Development Of A Screening Assay For Type Iii Secretion System Inhibitors And High Throughput Screening Campaign Of Inhibitors Of Prp Of Staphylococcus Aureus, Heather A. Pendergrass

Theses and Dissertations

Antibiotics inhibit the growth or survival of bacteria by targeting their essential functions.1 Due to weaknesses in traditional antibiotics and the increasing prevalence of antibiotic resistance genes, virulence factors are being targeted for therapeutic treatment of bacterial infection.2 We have developed an assay to quantify and observe type III secretion system (T3SS) activity. The type III secretion system (T3SS) is a virulence factor present in some Gram-negative pathogens including enteropathogenic and enterohemorrhagic E. coli (EPEC and EHEC, respectively),3 and others.4–9 The T3SS between EPEC and EHEC are highly conserved and share over 90% sequence identity with …


Bioactive Indanes: Development And Validation Of An Lc-Ms/Ms Bioanalytical Method For The Determination Of Ph46a, A New Potential Anti-Inflammatory Agent, In Dog And Rat Plasma And Its Application To A Pharmacokinetic Study In Dog, Gaia Scalabrino, Tao Zhang, Neil Frankish, Helen Sheridan 2020 Trinity College Dublin

Bioactive Indanes: Development And Validation Of An Lc-Ms/Ms Bioanalytical Method For The Determination Of Ph46a, A New Potential Anti-Inflammatory Agent, In Dog And Rat Plasma And Its Application To A Pharmacokinetic Study In Dog, Gaia Scalabrino, Tao Zhang, Neil Frankish, Helen Sheridan

Articles

A new chemical entity, which is a chiral indane dimer, PH46A, has been developed by our research group. As a clinical candidate. PH46A has recently completed Phase I clinical studies in man. Previously, during its pre-clinical development, in in vivo pre-clinical studies PH46A showed potent anti-inflammatory properties, which can be targeted at a range of diseases, including inflammatory bowel disease (IBD). To support the pre-clinical development of this drug candidate, we developed a LC MS/MS method for determining PH46 (the acid form of PH46A salt) in both dog and rat plasma using Compound 1 as internal standard (IS). Those species …


Research News. Publications, 2019. Volume 4, University of Mississippi. School of Pharmacy, Soumyajit Majumdar 2019 University of Mississippi

Research News. Publications, 2019. Volume 4, University Of Mississippi. School Of Pharmacy, Soumyajit Majumdar

Publications (2015-)

Publications that appeared during the period October 1 through December 31, 2019


Research News. Grants, 2019. Volume 4, University of Mississippi. School of Pharmacy, Soumyajit Majumdar 2019 University of Mississippi

Research News. Grants, 2019. Volume 4, University Of Mississippi. School Of Pharmacy, Soumyajit Majumdar

Grants (2015-)

Grants and contracts awarded during October-December 2019


Effect Of 3d Printed Tablet Shape On Drug Release Profile, Christina Gedeon 2019 New Jersey Institute of Technology

Effect Of 3d Printed Tablet Shape On Drug Release Profile, Christina Gedeon

Theses

There is a growing interest in utilizing additive manufacturing (AM) as a manufacturing tool to develop oral tablets for personalized medicine. This ultimate goal in mind, this study explores the feasibility of extrusion-based fused deposition modeling (FDM) to 3D print oral tablets with tunable design to control drug release profile. Tablets are printed using poly(vinyl alcohol) (PVA) loaded with model drugs: acetaminophen and caffeine. Hot melt extrusion (HME) is used to fabricate PVA filaments loaded with acetaminophen and caffeine. These filaments are used to fabricate a range of tablets with varying designs to prepare immediate and delayed release tablets. Thermal …


Model Hewan Coba Pada Penelitian Diabetes, Fauzul Husna, Franciscus D. Suyatna, Wawaimuli Arozal, Erni H. Purwaningsih 2019 Department of Pharmacology, Faculty of Medicine, Universitas Syiah Kuala, Aceh, Indonesia

Model Hewan Coba Pada Penelitian Diabetes, Fauzul Husna, Franciscus D. Suyatna, Wawaimuli Arozal, Erni H. Purwaningsih

Pharmaceutical Sciences and Research

The animal model has been widely used and contributed vastly to the scientific research over the years. While it can be used as an alternate subject in a study, the selection of the animal is crucial to assess and investigate the influence of the environment and genes on the pathogenesis of a disease. Many factors contribute to the choosing of the animal. They can be ranged from the similarities with the modelled object, easily looked after with less expensive cost, good reproductive performance, ability to produce blood and tissue samples, well-known genetic composition, and the status of the disease can …


Identification And Evaluation Of Antibacterial Compounds From The Vibrio Sp. Associated With The Ascidian Pycnoclavella Diminuta, Abdurraafi’ Maududi Dermawan, Elin Julianti, Masteria Yunovilsa Putra 2019 School of Pharmacy, Bandung Institute of Technology, Bandung, West Java, Indonesia

Identification And Evaluation Of Antibacterial Compounds From The Vibrio Sp. Associated With The Ascidian Pycnoclavella Diminuta, Abdurraafi’ Maududi Dermawan, Elin Julianti, Masteria Yunovilsa Putra

Pharmaceutical Sciences and Research

This study aims to obtain secondary metabolites that have antibacterial activity from bacteria endophytic of ascidian Pycnoclavella diminuta collected from the coast of Bitung, North Sulawesi, Indonesia. The research was started with screening antibacterial activity of six bacteria isolated from P. diminuta. The active bacteria were selected for identification using standard biological molecular method and further fermentation to produce secondary metabolites. The isolation of secondary metabolites was conducted by various chromatography method and then selected fraction was based on the antibacterial activity from bioautography results. The result showed that the active isolate by coding M2.Tnk.Bt 5.10-3.2 was identified as Vibrio …


Chemical Components Of Ocimum Basilicum L. And Ocimum Tenuiflorum L. Stem Essential Oils And Evaluation Of Their Antioxidant Activities Using Dpph Method, Ni Putu Ermi Hikmawanti, Hariyanti, Nurkamalia, Sahera Nurhidayah 2019 Faculty of Pharmacy and Sciences, Universitas Muhammadiyah Prof. DR. HAMKA, Jakarta, Indonesia

Chemical Components Of Ocimum Basilicum L. And Ocimum Tenuiflorum L. Stem Essential Oils And Evaluation Of Their Antioxidant Activities Using Dpph Method, Ni Putu Ermi Hikmawanti, Hariyanti, Nurkamalia, Sahera Nurhidayah

Pharmaceutical Sciences and Research

Ocimum basilicum L. and Ocimum tenuiflorum L. are two types of plants from Ocimum (Lamiaceae). One of their chemical compounds is essential oil. Essential oil might have an antioxidant activities. The part of the plants which are often wasted and never used are stem. This study aimed to analyze the chemical components of O. basilicum L. and O. tenuiflorum L. stem essential oils and evaluate their antioxidant activities. Essential oils were obtained by steam-water distillation. Analysis of chemical component of essential oil was performed using Gas Chromatography-Mass Spectroscopy (GC-MS). Antioxidant activities were evaluated with DPPH method and then the IC50 …


Cytotoxic Activity Of Stem Of Pycnarrhena Cauliflora Through Apoptosis Induction On Human Breast Cancer Cell Line T47d, Masriani, Rudiyansyah, Rini Muharini, Eny Enawaty 2019 Chemistry Education Department, Faculty of Teaching and Education, Tanjungpura University, West Kalimantan, Indonesia

Cytotoxic Activity Of Stem Of Pycnarrhena Cauliflora Through Apoptosis Induction On Human Breast Cancer Cell Line T47d, Masriani, Rudiyansyah, Rini Muharini, Eny Enawaty

Pharmaceutical Sciences and Research

Cytotoxic activities of extracts of Pycnarrhena cauliflora leaves, stems and roots on some human cancer cells have been known. However, the cytotoxicity of stem of Pycnarrhena cauliflora on human breast cancer cell line T47D through an apoptosis induction has not been proven yet. This study was an effort in understanding the cytotoxic activity of stem of Pycnarrhena cauliflora through apoptosis induction. The crude ethanol extract was partitioned between n-hexane and dichloromethane at pH 3, 7 and 9, which was subsequently tested for their cytotoxic activity against human breast cancer cell line T47D by using 3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide (MTT). Flow cytometric …


Intervention For Cognitive Reserve Enhancement In Delaying The Onset Of Alzheimer's Symptomatic Expression (Increase), A Randomized Controlled Trial: Rationale, Study Design, And Protocol, Daniela C. Moga, Brooke F. Beech, Erin L. Abner, Frederick A. Schmitt, Riham H. El Khouli, Ashley I. Martinez, Lynne Eckmann, Mark Huffmyer, Rosmy George, Gregory A. Jicha 2019 University of Kentucky

Intervention For Cognitive Reserve Enhancement In Delaying The Onset Of Alzheimer's Symptomatic Expression (Increase), A Randomized Controlled Trial: Rationale, Study Design, And Protocol, Daniela C. Moga, Brooke F. Beech, Erin L. Abner, Frederick A. Schmitt, Riham H. El Khouli, Ashley I. Martinez, Lynne Eckmann, Mark Huffmyer, Rosmy George, Gregory A. Jicha

Pharmacy Practice and Science Faculty Publications

BACKGROUND: The course of Alzheimer's disease (AD) includes a 10-20-year preclinical period with progressive accumulation of amyloid β (Aβ) plaques and neurofibrillary tangles in the absence of symptomatic cognitive or functional decline. The duration of this preclinical stage in part depends on the rate of pathologic progression, which is offset by compensatory mechanisms, referred to as cognitive reserve (CR). Comorbid medical conditions, psychosocial stressors, and inappropriate medication use may lower CR, hastening the onset of symptomatic AD. Here, we describe a randomized controlled trial (RCT) designed to test the efficacy of a medication therapy management (MTM) intervention to reduce inappropriate …


Chemical Composition And Behavioural Responses Of Male And Female Bactrocera Dorsalis To Their Volatile Emissions, Fikira Kimbokota 2019 University of Dar es Salaam

Chemical Composition And Behavioural Responses Of Male And Female Bactrocera Dorsalis To Their Volatile Emissions, Fikira Kimbokota

Journal of Humanities and Social Sciences

Bactrocera dorsalis, (Tephritidae) presented a grave threat to a broad range of fruit and vegetables in the tropics, including Tanzania. Bactrocera dorsalis is among the most destructive tephritid fruit fly, causing devastating loss of fruits especially mango. Insects use olfactory cues to locate hosts, oviposition sites and mating, in which pheromones are believed to be a strong cue used by insect to locate their mates. However, due to their high ability to adapt and occupy different ecological niches into various agroecological zones, there is a need to evaluate pheromonal composition from time to time to improve their control strategies. Therefore, …


Glucocorticoids Rapidly Activate Camp Production Via GΑs To Initiate Non-Genomic Signaling That Contributes To One-Third Of Their Canonical Genomic Effects, Francisco J. Nuñez, Timothy B. Johnstone, Maia L. Corpuz, Austin G. Kazarian, Nicole N. Mohajer, Omar Tliba, Reynold A. Pannettieri Jr., Cynthia J. Koziol-White, Moom Roosan, Rennolds S. Ostrom 2019 Chapman University

Glucocorticoids Rapidly Activate Camp Production Via GΑs To Initiate Non-Genomic Signaling That Contributes To One-Third Of Their Canonical Genomic Effects, Francisco J. Nuñez, Timothy B. Johnstone, Maia L. Corpuz, Austin G. Kazarian, Nicole N. Mohajer, Omar Tliba, Reynold A. Pannettieri Jr., Cynthia J. Koziol-White, Moom Roosan, Rennolds S. Ostrom

Pharmacy Faculty Articles and Research

Glucocorticoids are widely used for the suppression of inflammation, but evidence is growing that they can have rapid, non-genomic actions that have been unappreciated. Diverse cell signaling effects have been reported for glucocorticoids, leading us to hypothesize that glucocorticoids alone can swiftly increase the 3′,5′-cyclic adenosine monophosphate (cAMP) production. We found that prednisone, fluticasone, budesonide, and progesterone each increased cAMP levels within 3 minutes without phosphodiesterase inhibitors by measuring real-time cAMP dynamics using the cAMP difference detector in situ assay in a variety of immortalized cell lines and primary human airway smooth muscle (HASM) cells. A membrane- impermeable glucocorticoid showed …


Molecular Serotype-Specific Identification Of Non-Type B Haemophilus Influenzae By Loop-Mediated Isothermal Amplification, Chika Takano, Yoko Kuramochi, Mitsuko Seki, Dong Wook Kim, Daisuke Omagari, Mari Sasano, Bin Chang, Makoto Ohnishi, Eun Jin Kim, Kazumasa Fuwa, Paul E. Kilgore, Tomonori Hoshino, Satoshi Hayakawa 2019 Nihon University

Molecular Serotype-Specific Identification Of Non-Type B Haemophilus Influenzae By Loop-Mediated Isothermal Amplification, Chika Takano, Yoko Kuramochi, Mitsuko Seki, Dong Wook Kim, Daisuke Omagari, Mari Sasano, Bin Chang, Makoto Ohnishi, Eun Jin Kim, Kazumasa Fuwa, Paul E. Kilgore, Tomonori Hoshino, Satoshi Hayakawa

Department of Pharmacy Practice

In children, the incidence of pneumococcal meningitis has decreased since the introduction of pneumococcal conjugate vaccine (PCV7 and PCV13). However, since the introduction of the vaccine, developed countries have seen the emergence of non-PCV13 serotypes. However, invasive pneumococcal disease (IPD) caused by PCV13-targeted serotypes still represents an important public health problem in resource-limited countries. To develop a rapid, simple, and cost-effective assay to detect serotypes of Streptococcus pneumoniae, we developed a novel loop-mediated isothermal amplification (LAMP) assay based on the sequences available for the 13 capsular types that are included in PCV13: 1, 3, 4, 5, 6 A, 6B, …


Design And Biological Evaluation Of Colchicine-Cd44-Targeted Peptide Conjugate In An In Vitro Model Of Crystal Induced Inflammation, Khalid A. Zoghebi, Emira Bousoik, Keykavous Parang, Khaled A. Elsaid 2019 Chapman University

Design And Biological Evaluation Of Colchicine-Cd44-Targeted Peptide Conjugate In An In Vitro Model Of Crystal Induced Inflammation, Khalid A. Zoghebi, Emira Bousoik, Keykavous Parang, Khaled A. Elsaid

Pharmacy Faculty Articles and Research

Gout is an inflammatory arthritis due to the joint deposition of monosodium urate (MSU) crystals. Phagocytosis of MSU crystals by tissue macrophages results in the generation of reactive oxygen species (ROS) and production of inflammatory cytokines and chemokines. Colchicine use in gout is limited by severe toxicity. CD44 is a transmembrane glycoprotein that is highly expressed in tissue macrophages and may be involved in gout pathogenesis. The P6 peptide is a 20-amino acid residue peptide that binds to CD44. We hypothesized that the conjugation of colchicine to the P6 peptide would reduce its off-target cytotoxicity while preserving its anti-inflammatory effect. …


Design, Synthesis, & Biological Evaluation Of Novel Het-Aromatic/Aromatic Analogs For The Treatment Of Hiv, Cancer, & Cognitive Dysfunctions, MOHIT GUPTA 2019 Duquesne University

Design, Synthesis, & Biological Evaluation Of Novel Het-Aromatic/Aromatic Analogs For The Treatment Of Hiv, Cancer, & Cognitive Dysfunctions, Mohit Gupta

Electronic Theses and Dissertations

Cyclophilin A are a class of peptidyl-prolyl isomerases that catalyzes isomerization of the proline residue within a protein. Cyclophilin A plays an instrumental role in the pathogenesis of HIV and HCV virus. Using structure-based drug we designed and synthesized small molecule inhibitors of cyclophilin A. These inhibitors were biologically evaluated for their ability to inhibit WT HIV-1 inhibition.

Mitogen-Activated Protein Kinase signaling cascades plays a critical role in cancer cell survival, metastasis, and chemo-resistance. The MEK5/ERK5 pathway, which is a member of MAPK signaling cascade, is involved in cell survival, anti-apoptotic signaling, angiogenesis, and cell motility. It is found to …


Patient Satisfaction With Substance Use Disorder Rehabilitation Services, Trupti Dhumal 2019 Duquesne University

Patient Satisfaction With Substance Use Disorder Rehabilitation Services, Trupti Dhumal

Electronic Theses and Dissertations

Background: Patient satisfaction is considered as an important indicator in the evaluation of healthcare quality across an array of treatments and services. It is deemed vital especially in the field of substance use disorder (SUD) research due to an increased emphasis on understanding patients’ perceptions regarding their treatment and the attributes that drive their progress towards recovery. Despite the potential value, gaps have been recognized in the exploration of these satisfaction-related assessments among patients undergoing SUD treatment in residential rehabilitative settings. Thus, there is a need for understanding the dimensions contributing to satisfaction which would facilitate the development of …


Delivery Of Small Molecule And Rna Using Synthetic Polymeric Micelles And Multifunctional Exosomes For The Treatment Of Type 1 Diabetes, Yang Peng 2019 University of Nebraska Medical Center

Delivery Of Small Molecule And Rna Using Synthetic Polymeric Micelles And Multifunctional Exosomes For The Treatment Of Type 1 Diabetes, Yang Peng

Theses & Dissertations

Type 1 diabetes is one of the most challenging chronic autoimmune diseases. The destruction and dysfunction of insulin-secreting β cells are the results of inflammatory infiltration and the synergistic effect of multiple immune cells. The aim of this dissertation is to develop novel and reliable therapeutic approaches to advance the treatment of T1D: including chemical modification of a broad-spectrum immunosuppressant, co-application of small molecule based immune intervention and siRNA based β cell preservative therapy, and administration of a PI3K-δ/γ dual inhibitor to specifically target immune cells, utilizing synthetic polymeric micelles or natural produced multi-functional exosomes derived from human bone marrow …


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