Computational Design Of Β-Fluorinated Morphine Derivatives For Ph-Specific Binding,
2022
Chapman University
Computational Design Of Β-Fluorinated Morphine Derivatives For Ph-Specific Binding, Nayiri Alexander, Makena Augenstein, Matthew Gartner
Student Scholar Symposium Abstracts and Posters
The opioid epidemic impacted over 12 million Americans in 2019. Although they are effective pain-relieving medications, they carry addictive and dangerous side effects. Opioids, like morphine, bind non-selectively in both central and peripheral tissues; however, dangerous side effects result from central activation. Inflamed conditions of injured tissues have a lower pH (pH=6-6.5) environment than healthy central tissue (pH=7.4). We aim to design a morphine derivative that binds selectively within inflamed tissue using computationally-based molecular extension and dissection techniques. Binding to the mu-opioid receptor (MOR) is dependent on protonation of the biochemically active amine group of morphine. Fluorination of a carbon …
Challenge And Development Strategy For Colon-Targeted Drug Delivery System,
2022
Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia
Challenge And Development Strategy For Colon-Targeted Drug Delivery System, Raditya Iswandana, Kurnia Sari Setio Putri, Fathia Amalia Putri, Maxius Gunawan, Sekar Arum Larasati
Pharmaceutical Sciences and Research
Colon-Targeted Drug Delivery System (CTDDS) is able to improve local therapeutic effects in the treatment of colon-specific diseases, such as Crohn’s disease, Ulcerative Colitis (UC), and Irritable Bowel Syndrome (IBS). A colon can also be a suitable site for systemic delivery of drugs susceptible to extreme gastric pH, such as peptides and protein therapeutics. The physiological conditions of the gastrointestinal tract and the physicochemical properties of drugs are being considered to develop strategies and approaches to overcome emerging challenges. This review will discuss factors, challenges, strategies, and approaches to developing a colon-targeted drug delivery system.
Antihypertensive And Antioxidant Activity Of Herbal Medicine (Jamu) B On Rats Induced By 10% Fructose,
2022
Department of Pharmacy, Faculty of Health Sciences, Universitas Esa Unggul, Jakarta, Indonesia
Antihypertensive And Antioxidant Activity Of Herbal Medicine (Jamu) B On Rats Induced By 10% Fructose, Aprilita Rina Yanti Eff, Reza Ayu Pertiwi, Hermanus Ehe Hurit, Sri Teguh Rahayu, Yonatan Eden
Pharmaceutical Sciences and Research
Prolonged fructose intake can activate the renin-angiotensin-aldosterone system and enhance oxidative stress conditions, causing hypertension and hyperuricemia. This study aimed to determine the antihypertensive and antioxidant activity of Jamu B on the activity of superoxide dismutase (SOD), glutathione (GSH), and malondialdehyde (MDA) in the kidneys of Sprague Dawley rats induced by 10% fructose. Thirty rats were divided into six groups. Groups B1-B3 were Jamu groups at a dose of 0.12 g/kg BW (B1), 0.24 g/kg BW (B2), and 0.36 g/kg BW (B3); group C (positive control) was given captopril 0.1 g/kg BW, group D (negative control) was given only 10% …
Association Of Environmental Pollutants Exposure With Pulmonary Fibrosis: A Mini Review Of Molecular Mechanism Mediated,
2022
Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia
Association Of Environmental Pollutants Exposure With Pulmonary Fibrosis: A Mini Review Of Molecular Mechanism Mediated, Soni Siswanto, Bantari W.K. Wardhani
Pharmaceutical Sciences and Research
Pulmonary fibrosis is a specific form of chronic progressive interstitial lung disease. Deposition of extracellular matrix, mainly collagen, is the pathogenic characteristic of pulmonary fibrosis. Many reports show that environmental pollutants, particularly asbestos, silica, mercury, cadmium, and benzo(a)pyrene, are contributed in the etiology of lung injury and a risk factor in the development of idiopathic pulmonary fibrosis (IPF) in humans. Based on its physicochemical properties, environmental pollutant-induced pulmonary fibrosis can be developed after a particular type or dose of exposure. To date, some studies have focused on variant pollutants that are induced. However, the molecular mechanism of various pollutants to …
Oleyl Conjugated Histidine-Arginine Cell-Penetrating Peptides As Promising Agents For Sirna Delivery,
2022
Chapman University
Oleyl Conjugated Histidine-Arginine Cell-Penetrating Peptides As Promising Agents For Sirna Delivery, Muhammad Imran Sajid, Dindyal Mandal, Naglaa Salem El-Sayed, Sandeep Lohan, Jonathan Moreno, Rakesh Kumar Tiwari
Pharmacy Faculty Articles and Research
Recent approvals of siRNA-based products motivated the scientific community to explore siRNA as a treatment option for several intractable ailments, especially cancer. The success of approved siRNA therapy requires a suitable and safer drug delivery agent. Herein, we report a series of oleyl conjugated histidine–arginine peptides as a promising nonviral siRNA delivery tool. The conjugated peptides were found to bind with the siRNA at N/P ratio ≥ 2 and demonstrated complete protection for the siRNA from early enzymatic degradation at N/P ratio ≥ 20. Oleyl-conjugated peptide -siRNA complexes were found to be noncytotoxic in breast cancer cells (MCF-7 and MDA-MB-231) …
Acetaminophen, A Therapeutic Or An Extremely Toxic Remedy – A Review,
2022
Military Medical Research Center Bucharest
Acetaminophen, A Therapeutic Or An Extremely Toxic Remedy – A Review, Genica Caragea, Oana Avram, Andreea Pauna, Andreea Cristina Costea, Miruna Tudosie
Journal of Mind and Medical Sciences
When a new coronavirus appeared in the late 2019, identified as the cause of several cases of pneumonia in Wuhan, Paracetamol was initially reported to be the preferable antipyretic medication, choice which was detrimental to the use of other drugs. People have resorted to buying large stocks of Paracetamol and some have used it in large doses, regardless of the consequences. However, the Paracetamol (Acetaminophen) overdose remains the leading cause of death or transplantation due to acute liver failure in many parts of the world. This review aims at presenting the pharmacokinetics, the clinical signs, and the risk factors for …
Evaluation Of Protective Efficacy Of Viral Vector Based Swine Influenza Vaccine And A Method For B Cell Culture For Monoclonal Antibody Generation,
2022
University of Nebraska-Lincoln
Evaluation Of Protective Efficacy Of Viral Vector Based Swine Influenza Vaccine And A Method For B Cell Culture For Monoclonal Antibody Generation, Sushmita Kumari
School of Veterinary and Biomedical Sciences: Dissertations, Theses, and Student Research
Influenza A virus of the swine (IAV-S) is an economically important swine pathogen that has the potential to spread to humans, thus posing an ongoing public health concern due to its zoonotic potential. Hemagglutinin (HA), the most abundant viral envelope protein, is known to be the key protective antigen. Anti-HA antibodies alone, have been shown to prevent IAV infection. In this study we evaluated the feasibility of a recombinant tri segmented Pichinde virus (PICV) as a viral vector to deliver IAV-S hemagglutinin antigen in pigs. Four groups of weaned pigs (T01-04) were immunized twice with PBS, rPICV-GFP as a vector …
A Proposed Treatment Of Mixed Connective Tissue Disease By Competitive Inhibition Of Autoantibodies,
2022
Liberty University
A Proposed Treatment Of Mixed Connective Tissue Disease By Competitive Inhibition Of Autoantibodies, Thomas Russell
Senior Honors Theses
Mixed Connective Tissue Disease is an autoimmune disease characterized by Raynaud’s phenomenon and arthritis among other symptoms. It is primarily caused by antibodies that target the U1-RNP 70K peptide. The treatment proposed in this paper uses competitive inhibition to prevent the binding of the anti-U1-RNP 70K antibodies with the U1-RNP 70K peptide. A method for testing the designed treatment in silico is proposed using AutoDock Vina docking software.
The Development Of Inhibitors For Sars-Cov-2 Orf8,
2022
College of Saint Benedict/Saint John's University
The Development Of Inhibitors For Sars-Cov-2 Orf8, My Thanh Thao Nguyen
CSB and SJU Distinguished Thesis
An unexpected outbreak of SARS-CoV-2 caused a worldwide pandemic in 2020. Many repurposed drugs were tested, but there are currently only three FDA approved antivirals (Merck’s antiviral Molnupiravir, Pfizer’s antiviral Paxlovid, and Remdisivir).1 Most of the antiviral drugs tested SARS-CoV-2 main protease and RNA-dependent RNA polymerase. However, it is important to explore different drug targets of SARS-CoV-2 to prepare for the virus mutations of the future. This research looks at an alternative approach in which SARSCoV- 2 Open Reading Frame 8 (ORF8), which has been shown to be a rapidly evolving hypervariable gene, was chosen to be the protein of …
Sars-Cov-2 Main Protease Inhibitors Repurposed For Hiv-1 Protease Binding,
2022
College of Saint Benedict/Saint John's University
Sars-Cov-2 Main Protease Inhibitors Repurposed For Hiv-1 Protease Binding, Jacob Minkkinen
CSB and SJU Distinguished Thesis
Severe acute respiratory syndrome (SARS-CoV-2) led to the COVID-19 global pandemic, with over 460 million cases of infection and over 6 million deaths since the start of the pandemic. SARS-CoV-2 is a retrovirus that utilizes a main protease (Mpro). Mpro is a catalytic cys/his protease. Several treatments were proposed to stop the pandemic including repurposing drugs to inhibit the Mpro. Another retrovirus that uses a protease is human immunodeficiency virus (HIV-1) which has been a global epidemic for 40 years and is a devastating disease that attacks the immune system. HIV-1 has infected 79.5 million people and has killed an …
Targeting Protein Degradation To Uncover Novel Oncoprotein Drivers Of Acute Leukemia,
2022
University of Tennessee Health Science Center
Targeting Protein Degradation To Uncover Novel Oncoprotein Drivers Of Acute Leukemia, Fatemeh Keramatnia
Theses and Dissertations (ETD)
Acute Lymphoblastic Leukemia (ALL), the most common childhood cancer and the second most common acute leukemia in adults, arises from clonal expansion of undifferentiated lymphoid precursor cells in bone marrow. Despite the extensive knowledge on its cytogenetic and molecular biology, ALL treatment remains highly challenging especially after relapse. Conventional chemotherapy has shown significant improvement in overall survival rates of pediatric patients up to 90%, however, treatment failure due to ALL relapse occurs in 15-20% of the cases. On the other hand, adults and elderly patients with ALL are considered difficult to treat populations with the 5-year overall survival of 30–40%. …
Chloroquine-Susceptible And -Resistant Plasmodium Falciparum Strains Survive High Chloroquine Concentrations By Becoming Dormant But Are Eliminated By Prolonged Exposure,
2022
Projecto de Saúde de Bandim, Indepth Network, Bissau, Guinea-Bissau
Chloroquine-Susceptible And -Resistant Plasmodium Falciparum Strains Survive High Chloroquine Concentrations By Becoming Dormant But Are Eliminated By Prolonged Exposure, Johan Ursing, Rasmus Johns, Berit Aydin-Schmidt, Carla Calçada, Poul-Erik Kofoed, Najia Karim Ghanchi, Maria Isabel Veiga, Lars Rombo
Department of Pathology and Laboratory Medicine
Background: Plasmodium falciparum strains that are resistant to standard-dose chloroquine can be treated by higher chloroquine concentrations maintained for a longer time in vivo.
Objectives: To determine the relative importance of chloroquine concentrations versus exposure time for elimination of chloroquine-susceptible and -resistant P. falciparum in vitro.
Methods: Chloroquine-susceptible (3D7) and -resistant (FCR3) strains were exposed in vitro to 1, 2, 4, 8, 16 or 32 times their respective 90% inhibitory chloroquine concentrations for 3, 5, 7 or 14 days and then followed until recrudescence, or not, by 42 days after the end of exposure.
Results: Exposure to chloroquine appeared to …
An Evaluation Of The Effect Of The Oxycontin® Reformulation On Unintentional Fatal And Non-Fatal Overdose,
2022
HealthCore
An Evaluation Of The Effect Of The Oxycontin® Reformulation On Unintentional Fatal And Non-Fatal Overdose, Daniel C. Beachler, Kelsey Hall, Renu Garg, Geetanjoli Banerjee, Ling Li, Luke Boulanger, Huseyin Yuce, Alexander M. Walker
Publications and Research
Objectives: OxyContin® was reformulated with a polyethylene oxide matrix in August 2010 to reduce the potential for intravenous abuse and for abuse by insufflation. The objective of this study was to evaluate the impact of OxyContin’s reformulation on overdose risk for individuals dispensed OxyContin in comparison to those dispensed other opioids under regular care. Methods: Three national insurance databases with National Death Index linkage identified OD in individuals with any dispensing of OxyContin or a primary comparator opioid (ER morphine, transdermal fentanyl, or methadone) between July 2008 through September 2015. A difference-in-differences design was used to compare the pre-post reformulation …
Comparison Of Liposomal Bupivacaine Versus Bupivacaine With Epinephrine Versus The Combination In Postoperative Pain Management Following Spinal Surgery,
2022
Valley Hospital Medical Center
Comparison Of Liposomal Bupivacaine Versus Bupivacaine With Epinephrine Versus The Combination In Postoperative Pain Management Following Spinal Surgery, Arianne Dagdag
Annual Research Symposium
No abstract provided.
Emerging Drug Targets And New Drugs In The Treatment Of Psoriatic Arthritis,
2022
Ohio Northern University
Emerging Drug Targets And New Drugs In The Treatment Of Psoriatic Arthritis, Carmen Lariccia, Natalie Lennartz, Jessica Lewe, Jeffery Allison
Pharmacy and Wellness Review
Psoriasis is an autoimmune disease characterized by painful skin lesions. When joints and connective tissue also become involved, the condition is referred to as psoriatic arthritis (PsA). Current treatments for moderate to severe PsA include therapies used to treat rheumatoid arthritis (RA) despite differences in disease presentation which includes factors such as peripheral disease, sacroiliitis, stiffness, presence of rheumatoid factor and psoriasis. Treatment out-comes for PsA are measured by the American College of Rheumatology (ACR) Responder Index (ACR20) and the Dis-ease Activity Score for 28 joints (DAS28). First-line treatment includes disease-modifying antirheumatic drugs (DMARDs) such as methotrexate, sulfasalazine or leflunomide …
Management Of Hyperkalemia To Prevent Cardiac Arrest,
2022
Ohio Northern University
Management Of Hyperkalemia To Prevent Cardiac Arrest, Jennifer Harklerode, Amber Paul, Crystal Zheng, Olivia Vanscoy, Olivia Henton, Mark Olah
Pharmacy and Wellness Review
Hyperkalemia is a metabolic problem that may be life threatening if left untreated. Cardiac arrhythmias may develop with the potential to lead to cardiac arrest and death. Hyperkalemia can oftentimes be undiagnosed due to the lack of clear, specific symptoms and inconclusive variations in electrocardiogram (ECG) readings and lab values. Therefore, it is important to recognize risk factors that can potentially in-crease serum potassium levels. Screening for medications that increase serum potassium levels and educating patients are steps that both inpatient and outpatient health care professionals can take to increase early detection and prevention of a hyperkalemic episode. It is …
Daclizumab (Zinbryta®): An Emerging Therapy For The Treatment Of Relapsing-Remitting Multiple Sclerosis,
2022
Ohio Northern University
Daclizumab (Zinbryta®): An Emerging Therapy For The Treatment Of Relapsing-Remitting Multiple Sclerosis, Morgan Homan, Sunitha Jones, Michaela Louden, Molly Wheeler, Anh Dao Le, Lindsey Peters
Pharmacy and Wellness Review
Multiple sclerosis (MS) is an autoimmune disorder of the central nervous system characterized by the deterioration of the myelin sheath, causing axonal damage which leads to debilitating symptoms. Most therapies for the treatment of MS, including daclizumab, primarily target relapsing-remitting multiple sclerosis (RRMS), a form of MS where patients experience periods of exacerbated symptoms as well as intermittent periods of remission. Daclizumab is a humanized monoclonal antibody that is administered as a once monthly subcutaneous injection. The SELECT trilogy of trials have been instrumental in providing safety and efficacy data for daclizumab. The DECIDE study was the first randomized controlled …
Lipid Based Nanoparticles As A Novel Treatment Modality For Hepatocellular Carcinoma: A Comprehensive Review On Targeting And Recent Advances,
2022
The British University in Egypt
Lipid Based Nanoparticles As A Novel Treatment Modality For Hepatocellular Carcinoma: A Comprehensive Review On Targeting And Recent Advances, Khaled Mahmoud, Shady Swidan, Mohamed A. El-Nabarawi, Mahmoud H. Teaima
Pharmacy
Liver cancer is considered one of the deadliest diseases with one of the highest disease burdens worldwide. Among the different types of liver cancer, hepatocellular carcinoma is considered to be the most common type. Multiple conventional approaches are being used in treating hepatocellular carcinoma. Focusing on drug treatment, regular agents in conventional forms fail to achieve the intended clinical outcomes. In order to improve the treatment outcomes, utilizing nanoparticles—specifically lipid based nanoparticles—are considered to be one of the most promising approaches being set in motion. Multiple forms of lipid based nanoparticles exist including liposomes, solid lipid nanoparticles, nanostructured lipid carriers, …
Variants Associated With Bedaquiline (Bdq) Resistance Identified In Rv0678 And Efflux Pump Genes In Mycobacterium Tuberculosis Isolates From Bdq Naïve Tb Patients In Pakistan,
2022
Aga Khan University
Variants Associated With Bedaquiline (Bdq) Resistance Identified In Rv0678 And Efflux Pump Genes In Mycobacterium Tuberculosis Isolates From Bdq Naïve Tb Patients In Pakistan, Dania Khalid Saeed, Sadia Shakoor, Safina Abdul Razzak, Zahra Hasan, Saba Faraz Sabzwari, Zahida Azizullah, Akber Kanji, Asghar Nasir, Samreen Shafiq, Najia Karim Ghanchi, Rumina Hasan
Department of Pathology and Laboratory Medicine
Background: Mutations in the Rv0678, pepQ and atpE genes of Mycobacterium tuberculosis (MTB) have been reported to be associated with reduced antimycobacterial susceptibility to bedaquiline (BDQ). Resistance conferring mutations in treatment naïve MTB strains is likely to have implications for BDQ based new drug regimen that aim to shorten treatment duration. We therefore investigated the genetic basis of resistance to BDQ in MTB clinical isolates from BDQ naïve TB patients from Pakistan. In addition, mutations in genes associated with efflux pumps were investigated as an alternate mechanism of resistance.
Methods: Based on convenience sampling, we studied 48 MTB clinical isolates …
The Use Of Advanced Spectral Imaging To Reveal Nanoparticle Identity In Biological Samples,
2022
Chapman University
The Use Of Advanced Spectral Imaging To Reveal Nanoparticle Identity In Biological Samples, Qamar A. Alshammari, Rajasekharreddy Pala, Ayan K. Barui, Saud O. Alshammari, Andromeda M. Nauli, Nir Katzir, Ashraf M. Mohieldin, Surya M. Nauli
Pharmacy Faculty Articles and Research
Nanoparticles (NPs) have been used in drug delivery therapies, medical diagnostic strategies, and as current Covid-19 vaccine carriers. Many microscope-based imaging systems have been introduced to facilitate detection and visualization of NPs. Unfortunately, none can differentiate the core and the shell of NPs. Spectral imaging has been used to distinguish a drug molecule and its metabolite. We have recently integrated this technology to a resolution of 9 nm by using artificial intelligence-driven analyses. Such a resolution allowed us to collect many robust datapoints for each pixel of an image. Our analyses could recognize 45 spectral points within a pixel to …
