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787 full-text articles. Page 6 of 37.

Comparative Molecular Transporter Properties Of Cyclic Peptides Containing Tryptophan And Arginine Residues Formed Through Disulfide Cyclization, Eman H. M. Mohammed, Dindyal Mandal, Saghar Mozaffari, Magdy Abdel-Hamied Zahran, Amany Mostafa Osman, Rakesh Kumar Tiwari, Keykavous Parang 2020 Chapman University

Comparative Molecular Transporter Properties Of Cyclic Peptides Containing Tryptophan And Arginine Residues Formed Through Disulfide Cyclization, Eman H. M. Mohammed, Dindyal Mandal, Saghar Mozaffari, Magdy Abdel-Hamied Zahran, Amany Mostafa Osman, Rakesh Kumar Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

We have previously reported cyclic cell-penetrating peptides [WR]5 and [WR]4 as molecular transporters. To optimize further the utility of our developed peptides for targeted therapy in cancer cells using the redox condition, we designed a new generation of peptides and evaluated their cytotoxicity as well as uptake behavior against different cancer cell lines. Thus, cyclic [C(WR)xC] and linear counterparts (C(WR)xC), where x = 4–5, were synthesized using Fmoc/tBu solid-phase peptide synthesis, purified, and characterized. The compounds did not show any significant cytotoxicity (at 25 µM) against ovarian (SK-OV-3), leukemia (CCRF-CEM), gastric ...


Cancer Pain And The Risks Of Opioid Abuse, Yarelis Diaz 2020 Nova Southeastern University

Cancer Pain And The Risks Of Opioid Abuse, Yarelis Diaz

College of Pharmacy Student Articles

No abstract provided.


Recombinant Human Proteoglycan-4 Mediates Interleukin-6 Response In Both Human And Mouse Endothelial Cells Induced Into A Sepsis Phenotype, Holly A. Richendrfer, Mitchell M. Levy, Khaled A. Elsaid, Tannin A. Schmidt, Ling Zhang, Ralph Cabezas, Gregory D. Jay 2020 Brown University

Recombinant Human Proteoglycan-4 Mediates Interleukin-6 Response In Both Human And Mouse Endothelial Cells Induced Into A Sepsis Phenotype, Holly A. Richendrfer, Mitchell M. Levy, Khaled A. Elsaid, Tannin A. Schmidt, Ling Zhang, Ralph Cabezas, Gregory D. Jay

Pharmacy Faculty Articles and Research

Objectives:

Sepsis is a leading cause of death in the United States. Putative targets to prevent systemic inflammatory response syndrome include antagonism of toll-like receptors 2 and 4 and CD44 receptors in vascular endothelial cells. Proteoglycan-4 is a mucinous glycoprotein that interacts with CD44 and toll-like receptor 4 resulting in a blockade of the NOD-like receptor pyrin domain-containing-3 pathway. We hypothesized that endothelial cells induced into a sepsis phenotype would have less interleukin-6 expression after recombinant human proteoglycan 4 treatment in vitro.

Design:

Enzyme-linked immunosorbent assay and reverse transcriptase-quantitative polymerase chain reaction to measure interleukin-6 protein and gene expression.

Setting ...


Nanoparticle-Mediated Drug Delivery For The Treatment Of Cardiovascular Diseases, Rajasekharreddy Pala, VT Anju, Madhu Dyavaiah, Siddhardha Busi, Surya M. Nauli 2020 Chapman University

Nanoparticle-Mediated Drug Delivery For The Treatment Of Cardiovascular Diseases, Rajasekharreddy Pala, Vt Anju, Madhu Dyavaiah, Siddhardha Busi, Surya M. Nauli

Pharmacy Faculty Articles and Research

Cardiovascular diseases (CVDs) are one of the foremost causes of high morbidity and mortality globally. Preventive, diagnostic, and treatment measures available for CVDs are not very useful, which demands promising alternative methods. Nanoscience and nanotechnology open a new window in the area of CVDs with an opportunity to achieve effective treatment, better prognosis, and less adverse effects on non-target tissues. The application of nanoparticles and nanocarriers in the area of cardiology has gathered much attention due to the properties such as passive and active targeting to the cardiac tissues, improved target specificity, and sensitivity. It has reported that more than ...


Rapamycin Treatment Correlates Changes In Primary Cilia Expression With Cell Cycle Regulation In Epithelial Cells, Maha Jamal, Ane C.F. Nunes, Nosratola D. Vaziri, Ramani Ramchandran, Robert L. Bacallao, Andromeda M. Nauli, Surya M. Nauli 2020 Chapman University

Rapamycin Treatment Correlates Changes In Primary Cilia Expression With Cell Cycle Regulation In Epithelial Cells, Maha Jamal, Ane C.F. Nunes, Nosratola D. Vaziri, Ramani Ramchandran, Robert L. Bacallao, Andromeda M. Nauli, Surya M. Nauli

Pharmacy Faculty Articles and Research

Primary cilia are sensory organelles that regulate cell cycle and signaling pathways. In addition to its association with cancer, dysfunction of primary cilia is responsible for the pathogenesis of polycystic kidney disease (PKD) and other ciliopathies. Because the association between cilia formation or length and cell cycle or division is poorly understood, we here evaluated their correlation in this study. Using Spectral Karyotyping (SKY) technique, we showed that PKD and the cancer/tumorigenic epithelial cells PC3, DU145, and NL20-TA were associated with abnormal ploidy. We also showed that PKD and the cancer epithelia were highly proliferative. Importantly, the cancer epithelial ...


Does Long-Term Proton Pump Inhibitor Use Pump Up Your Risk Of Adverse Effects?, Hindu Rao, Jelena Lewis 2020 Chapman University

Does Long-Term Proton Pump Inhibitor Use Pump Up Your Risk Of Adverse Effects?, Hindu Rao, Jelena Lewis

Pharmacy Faculty Articles and Research

"Many studies have linked proton pump inhibitor (PPI) use to several adverse effects including Clostridium difficile-associated diarrhea, community-acquired pneumonia, bone fractures, and nutritional deficiencies.1 Other reports have linked PPI use with chronic kidney disease, cognitive decline, myocardial infarction (MI), stroke, and even death.1,2,3 Many patients take PPIs chronically and may be concerned about the risk of these side effects. This poses a challenge for healthcare providers as safety data has been primarily based on retrospective and observational studies. Thus, the fears associated with long term PPI therapy can create confusion, result in extended patient visits, and ...


Understanding Elements Involved In Active Racial And Ethnic Minority Recruitment Practices For Biopharmaceutical-Sponsored Clinical Trials: A Socio-Ecological Qualitative Inquiry, Rebecca Rae Johnson 2020 Seton Hall University

Understanding Elements Involved In Active Racial And Ethnic Minority Recruitment Practices For Biopharmaceutical-Sponsored Clinical Trials: A Socio-Ecological Qualitative Inquiry, Rebecca Rae Johnson

Seton Hall University Dissertations and Theses (ETDs)

Inequitable participation in clinical trials continues to be a problem, and trial populations do not always reflect the demographics of the population that the investigational product will ultimately be treating. Because genetic differences between racial and ethnic groups affect the safety and efficacy of new treatments, it is important that standard of care decisions are made based on a representative population. The purpose of this study is to understand the socio-ecological elements that are involved in the active implementation of racial and ethnic minority recruitment practices for biopharmaceutical-funded trials in the United States. This general qualitative study was both descriptive ...


Comparative Antiviral Activity Of Remdesivir And Anti-Hiv Nucleoside Analogs Against Human Coronavirus 229e (Hcov-229e), Keykavous Parang, Naglaa Salem El-Sayed, Assad J. Kazeminy, Rakesh Tiwari 2020 Chapman University

Comparative Antiviral Activity Of Remdesivir And Anti-Hiv Nucleoside Analogs Against Human Coronavirus 229e (Hcov-229e), Keykavous Parang, Naglaa Salem El-Sayed, Assad J. Kazeminy, Rakesh Tiwari

Pharmacy Faculty Articles and Research

Remdesivir is a nucleotide prodrug that is currently undergoing extensive clinical trials for the treatment of COVID-19. The prodrug is metabolized to its active triphosphate form and interferes with the action of RNA-dependent RNA polymerase of SARS-COV-2. Herein, we report the antiviral activity of remdesivir against human coronavirus 229E (HCoV-229E) compared to known anti-HIV agents. These agents included tenofovir (TFV), 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA), alovudine (FLT), lamivudine (3TC), and emtricitabine (FTC), known as nucleoside reverse-transcriptase inhibitors (NRTIs), and a number of 5′-O-fatty acylated anti-HIV nucleoside conjugates. The anti-HIV nucleosides interfere with HIV RNA-dependent DNA polymerase and/or act ...


Assessing The Effect Of Chronic Dopamine Receptor 2 Blockade As A Potential Model Of Secondary Negative Symptoms In Rats Using The Fr5/Chow Feeding Choice Task, Cyrene Nicholas 2020 University of Connecticut

Assessing The Effect Of Chronic Dopamine Receptor 2 Blockade As A Potential Model Of Secondary Negative Symptoms In Rats Using The Fr5/Chow Feeding Choice Task, Cyrene Nicholas

Honors Scholar Theses

Haloperidol, a dopamine (DA) D2 receptor antagonist, is an antipsychotic drug which is commonly used to treat schizophrenia and other psychiatric disorders. These disorders are often characterized by elevated striatal dopamine, which is speculated to have a role in producing positive symptoms such as hallucinations, delusions, and paranoia, as well as symptoms related to motivational salience and reward prediction. Individuals with schizophrenia also exhibit negative symptoms, such as amotivation, anergia, fatigue, and apathy among others. While some negative symptoms of schizophrenia are inherent to the pathophysiology, other negative symptoms are hypothesized to be partially induced by chronic exposure to antipsychotic ...


Proteoglycan-4 Regulates Fibroblast To Myofibroblast Transition And Expression Of Fibrotic Genes In The Synovium, Marwa Qadri, Gregory D. Jay, Ling X. Zhang, Holly Richendrfer, Tannin A. Schmidt, Khaled A. Elsaid 2020 Chapman University

Proteoglycan-4 Regulates Fibroblast To Myofibroblast Transition And Expression Of Fibrotic Genes In The Synovium, Marwa Qadri, Gregory D. Jay, Ling X. Zhang, Holly Richendrfer, Tannin A. Schmidt, Khaled A. Elsaid

Pharmacy Faculty Articles and Research

Background: Synovial tissue fibrosis is common in advanced OA with features including the presence of stress fiber-positive myofibroblasts and deposition of cross-linked collagen type-I. Proteoglycan-4 (PRG4) is a mucinous glycoprotein secreted by synovial fibroblasts and is a major component of synovial fluid. PRG4 is a ligand of the CD44 receptor. Our objective was to examine the role of PRG4-CD44 interaction in regulating synovial tissue fibrosis in vitro and in vivo.

Methods: OA synoviocytes were treated with TGF-β ± PRG4 for 24h and α-SMA content was determined using immunofluorescence. Rhodamine-labeled rhPRG4 was incubated with OA synoviocytes ± anti-CD44 or isotype control antibodies and ...


Ocular, Neural, And Cellular Biodistribution Of Multifunctional Antioxidants, Damian Daszynski 2020 University of Nebraska Medical Center

Ocular, Neural, And Cellular Biodistribution Of Multifunctional Antioxidants, Damian Daszynski

Theses & Dissertations

Aging is a complex biological process which stems from a growing imbalance between the regenerative capacity of an organism and endogenous as well as exogenous damaging factors. This imbalance leads to the slow deterioration of individual cells, organs, and eventually the entire organism. The free radical theory of aging combines the evolutionary and mechanistic aspects of aging, postulating that the innate process is caused by deleterious, irreversible, and inevitable changes in biological systems caused by oxidative damage that accumulates over the lifespan. Evidence of this phenomenon is supported by the pathogenesis of age-related diseases, such as age-related macular degeneration and ...


Regulating Neuronal Growth With Structurally Defined Glycans, Gabriella D. Hartman 2020 University of Mississippi

Regulating Neuronal Growth With Structurally Defined Glycans, Gabriella D. Hartman

Honors Theses

Chondroitin sulfate proteoglycans (CSPGs) and keratan sulfate proteoglycans (KSPGs) play an important role in neural development. Aggrecan, a CSPG, operates in the neural extracellular matrix where it negatively regulates neurite outgrowth to prevent aberrant process formation. Unfortunately, this aggrecan or CSPG-rich/KSPG-rich barrier can also prevent neuronal regeneration, which contributes to the inability to repair brain and spinal cord injuries. Removal of CSPGs and KSPGs has been shown to increase neurite outgrowth. We extend these findings by testing the ability of structurally-defined glycans to outcompete aggrecan and allow neurite outgrowth. Our overall goal is to determine if there is a ...


Studies Of Salvinorin-Based Antagonists To Elucidate Pertinent Interactions For Kappa Opioid Receptor Antagonism, Madeline Keane 2020 University of Mississippi

Studies Of Salvinorin-Based Antagonists To Elucidate Pertinent Interactions For Kappa Opioid Receptor Antagonism, Madeline Keane

Honors Theses

Opioid abuse, leading to addiction and related deaths, has created a chronic epidemic in the United States for the past 30 years. This crisis has sprung from reliance on the prescription of opioid analgesics as the primary method for the management of pain in the 1990s. At that time, these drugs, specifically Purdue Pharma’s OxyContin, were marketed as non-addictive. Due to this systemic minimization of the addictive properties of opioid analgesics, as prescription rates increased, opioid-related mortality rates climbed. This epidemic continues to be pervasive, as opioid-related overdose resulted in 47,600 deaths in 2017. In addition to the ...


In-Vitro Assessment Of Cb1/Cb2 Receptor Binding And Function, Joey M. Davis 2020 University of Mississippi

In-Vitro Assessment Of Cb1/Cb2 Receptor Binding And Function, Joey M. Davis

Honors Theses

Cannabinoid receptors CB1 and CB2 are G protein-coupled receptors that have a variety of physiological effects on the human body. Many natural product agonists and antagonists are presumed to interact with the cannabinoid receptors and are therefore heavily studied in drug discovery. Assays are used to study the binding of compounds to these receptors. However, a limited number of these assays are efficient in determining the functional activity of ligands associated with CB1 and CB2. Of those, many use radioactivity which is both expensive and potentially dangerous to the researcher. In this study, we first validated the assays already found ...


Gene Delivery To The Blood-Brain Barrier For Ischemic Stroke Therapy, Wanzhu Zhao 2020 Duquesne University

Gene Delivery To The Blood-Brain Barrier For Ischemic Stroke Therapy, Wanzhu Zhao

Electronic Theses and Dissertations

Stroke is a major cause of death in the United States. We aim to develop safe and efficient approaches for the treatment of stroke. Regenerative therapies have been identified as the major need for curing stroke [1]. We explored two different carriers (poly (ethylene glycol)5k-poly (L-aspartate-diethylenetriamine)48 (PEG-DET) / Pluronic P84 (P84) and exosomes (EXOs) / microvesicles (MVs)) to deliver brain-derived neurotrophic factor (BDNF) plasmid DNA (pDNA), a functional gene encoding a neurotrophin. In the first project, our data showed that DNA nanoparticles (NPs) with 0.03% P84 was a promising formulation to deliver Luciferase pDNA into immortalized human cerebral ...


Phenylpyrazalopyrimidines As Tyrosine Kinase Inhibitors: Synthesis, Antiproliferative Activity, And Molecular Simulations, Bhupender S. Chhikara, Sajda Ashraf, Saghar Mozaffari, Nicole St. Jeans, Dindyal Mandal, Rakesh Kumar Tiwari, Zaheer Ul-Haq, Keykavous Parang 2020 University of Delhi

Phenylpyrazalopyrimidines As Tyrosine Kinase Inhibitors: Synthesis, Antiproliferative Activity, And Molecular Simulations, Bhupender S. Chhikara, Sajda Ashraf, Saghar Mozaffari, Nicole St. Jeans, Dindyal Mandal, Rakesh Kumar Tiwari, Zaheer Ul-Haq, Keykavous Parang

Pharmacy Faculty Articles and Research

N1-(α,β-Alkene)-substituted phenylpyrazolopyrimidine derivatives with acetyl and functionalized phenyl groups at α- and β-positions, respectively, were synthesized by the reaction of 3-phenylpyrazolopyrimidine (PhPP) with bromoacetone, followed by a chalcone reaction with differently substituted aromatic aldehydes. The Src kinase enzyme assay revealed modest inhibitory activity (half maximal inhibitory concentration, IC50 = 21.7–192.1 µM) by a number of PhPP derivatives. Antiproliferative activity of the compounds was evaluated on human leukemia (CCRF-CEM), human ovarian adenocarcinoma (SK-OV-3), breast carcinoma (MDA-MB-231), and colon adenocarcinoma (HT-29) cells in vitro. 4-Chlorophenyl carbo-enyl substituted 3-phenylpyrazolopyrimidine (10) inhibited the cell proliferation of HT-29 and ...


Effects Of Lisdexamfetamine And Haloperidol On A Binge-Like Eating Model & Preliminary Investigations Of The Dopaminergic Mechanism Underlying Binge Eating Disorder (Bed), Maxime Braun 2020 University of Connecticut

Effects Of Lisdexamfetamine And Haloperidol On A Binge-Like Eating Model & Preliminary Investigations Of The Dopaminergic Mechanism Underlying Binge Eating Disorder (Bed), Maxime Braun

Honors Scholar Theses

Binge eating disorder (BED) is a psychophysiological disorder defined as the excessive intake of high-caloric, palatable foods within a short span of time, accompanied by feelings of distress. Animal models of binge-like eating behavior have been developed that give intermittent, limited access to a highly palatable food. Presby et al. (2020) used chocolate as the highly palatable food to induce binge-like eating behavior in rats. Lisdexamfetamine (LDX), a d-amphetamine prodrug and dopamine (DA) uptake inhibitor, is currently used to treat BED in humand. In rats, binge-like eating of chocolate was induced by exposure to unpredictable and limited chocolate access over ...


Role Of Protein Phosphatase-2a In Regulating Monocyte Activation By Soluble And Crystalline Uric Acid In Gout, Sandy ElSayed 2020 Chapman University

Role Of Protein Phosphatase-2a In Regulating Monocyte Activation By Soluble And Crystalline Uric Acid In Gout, Sandy Elsayed

Pharmaceutical Sciences (MS) Theses

Gout is a chronic inflammatory disease caused by the phagocytosis of monosodium urate monohydrate (MSU) crystals by monocytes/macrophages resulting in downstream expression and production of interleukin-1 beta (IL-1β) and chemokines. The activation of monocytes by MSU crystals involves the priming of monocytes with danger signals e.g. lipopolysaccharide (LPS) or soluble uric acid (UA), crystal phagocytosis and subsequent NLRP3 inflammasome activation and conversion of pro-IL-1β to active IL-1β. Protein-phosphatase-2A (PP2A) is a serine/threonine phosphatase that plays an important role in cell growth and inflammation. The prodrug Fingolimod (FTY720) and its phosphorylated active metabolite (p-FTY720) activate intracellular PP2A. We ...


Sulforaphane Protects Against Ethanol-Induced Apoptosis And Teratogenesis Through Epigenetic Modulation Of Anti-Apoptotic Genes., Yihong Li 2020 University of Louisville

Sulforaphane Protects Against Ethanol-Induced Apoptosis And Teratogenesis Through Epigenetic Modulation Of Anti-Apoptotic Genes., Yihong Li

Electronic Theses and Dissertations

Background. Ethanol-induced excessive apoptosis in neural crest cells (NCCs), a multipotent progenitor cell population, is one of the major mechanisms underlying the pathogenesis of Fetal Alcohol Spectrum Disorders (FASD). However, the molecular mechanisms underlying FASD that results from maternal alcohol exposure during pregnancy are poorly understood. The overall goals of this study are to examine the mechanisms by which ethanol induces apoptosis and malformations in vitro and in vivo, and to develop a nutritional-based approach by using SFN and SFN-rich BSE to prevent FASD through epigenetic modulation. Results. This study demonstrates that ethanol exposure resulted in a significant increase in ...


Profil Terapi Antihipertensi Dan Antihiperlipidemia Terhadap Fungsi Ginjal Pasien Diabetes Melitus Tipe 2 Dengan Komplikasi Penyakit Ginjal Kronis Di Rsup Dr. Hasan Sadikin, Fitri Rachmaini, Lia Amalia, Cherry Rahayu 2020 Fakultas Farmasi Universitas Andalas, Sumatera Barat, Indonesia

Profil Terapi Antihipertensi Dan Antihiperlipidemia Terhadap Fungsi Ginjal Pasien Diabetes Melitus Tipe 2 Dengan Komplikasi Penyakit Ginjal Kronis Di Rsup Dr. Hasan Sadikin, Fitri Rachmaini, Lia Amalia, Cherry Rahayu

Pharmaceutical Sciences and Research

Chronic Kidney Disease (CKD) complication increases the risk of morbidity and mortality in type 2 diabetes mellitus (DMT2) patients. The presence of hypertension and dyslipidemia as comorbidity increases the risk of macrovascular and microvascular complications and further adding to the list of drugs used. Management of this comorbidity is essential to prevent cardiovascular events and minimize kidney damage. This study aimed to evaluate therapeutic profile of antihypertensive and antihyperlipidemia drugs towards kidney function in DMT2 patients with CKD complication at Dr. Hasan Sadikin Hospital. Study was done by using a prospective single cohort design with consecutive sampling technique and obtained ...


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