Medicinal Chemistry and Pharmaceutics Commons^™

Prevention Of Doxorubicin-Induced Cardiotoxicity By A Coumestan Analogue, Psoralidin, Mujtaba H. Shah, Myia Aiges, Kota V. Ramana

Annual Research Symposium

Natural phenolic compound Psoralidin limits cardiotoxicity associated with Doxorubicin

Development Of A Method For Identifying And Quantifying Epicatechin In Cinnamon Extract Supplement Capsules, Danielle Valls

Annual Research Symposium

No abstract provided.

Development Of An Lcms Method To Detect And Quantify Curcumin In A Novel Oral Formulation Of Turmeric, Brandon Renninger

Annual Research Symposium

No abstract provided.

A Review On The Impact Of Cannabis In Society And The Analytical Methodologies For Cannabinoids, Matt J. Vergne, Lindsey K. Reynolds, Alexus Brown, Grayson Pullias, Anna Froemming

Faculty Works

The use of plant-based medicine dates back centuries, and cannabis (Cannabis sativa) is one such plant that has been used medicinally and illicitly. Although cannabis contains hundreds of cannabinoids and other natural products, its potential medicinal use was largely ignored by modern researchers due to the legal restrictions and heavy regulations introduced in the 1930s. As restrictions on cannabis access have eased since the 1990s there is renewed interest in the research of cannabinoids and the other components in the cannabis plant. The focus of this review article is an overview of cannabis and the analytical challenges in the quality …

Leveraging Bio-Inspired Molecules For Cancer Theranostics, Douglas S. Macpherson

Dissertations, Theses, and Capstone Projects

A variety of molecules can be radiolabeled and delivered to a cancer site for the purposes of diagnostics and therapy. Among the most promising of tumor targeting molecules are peptides and antibodies. These bio-inspired molecules can be designed and synthesized to target and respond to cancer cells based on the properties of those cells. Matrix metalloproteinase (MMP) enzymes are over-expressed by some metastatic cancers, in which they are responsible for the degradation and remodeling of the extracellular matrix. In recent years, MMPs have emerged as promising targets for enzyme-responsive diagnostic probes because oligopeptides can be designed to be selectively hydrolyzed …

Phase 1a Clinical Study For Q-Griffithsin Intranasal Spray For Prevention Of Coronavirus, Megan Bezold, Kenneth Palmer, Nobuyuki Matoba, Elizabeth Cash

Posters-at-the-Capitol

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a highly transmissible virus that causes acute respiratory disease with possible long-term complications, known as coronavirus disease 2019 (COVID-19). Griffithsin (GRFT; including the oxidation-resistant variant Q-GRFT used in this study) is an algal carbohydrate-binding protein exhibiting antiviral effects against many enveloped viruses, including all major variants of SARS- CoV-2 reported to date. Q-GRFT has been recombinantly manufactured in Nicotiana benthamiana plants, thoroughly purified, and formulated as an intranasal spray designed to be developed as a non-vaccine broad-spectrum prophylactic product for acute use. This is the first-in-human, randomized, double-blind, placebo-controlled study. The …

Nsaids And Oral Drug Absorption: Ibuprofen Through A Pharmacokinetic Lens, Courtney Gant

Undergraduate Honors Theses

Human pharmacokinetics is the study of how administered medications move throughout and behave within the body. Absorption, distribution, metabolism, and excretion are four integral parts of this field of study and are commonly known as the ADME principles of pharmacokinetics, but other processes are studied within the field. For orally administered drugs, the absorption process lies within the small intestine and colon, two components of the gastrointestinal (GI) tract; this bodily system is associated with many variables––many of which must be considered in the study of oral drug absorption. Often administered orally, non-steroidal anti-inflammatory drugs (NSAIDs) make up a group …

The Impact Of Hiv-1 Tat And Morphine On Spatial Distribution Of Drugs In The Brain., Austin M. Jones

Theses and Dissertations

Despite combination antiretroviral therapy effectively suppressing HIV within the periphery, the central nervous system (CNS) remains affected by the virus. Approximately half of people living with HIV will experience HIV-associated neurocognitive disorders (HAND) or neuroHIV. Concurrent opioid use exacerbates neuroHIV by promoting neuroinflammation, viral replication, and potentially altering the antiretroviral concentrations within the brain.

Using a transgenic mouse that expresses the HIV-1 Tat protein, we examined the effects of Tat and morphine on antiretroviral accumulation and distribution and the effects of Tat on morphine accumulation within the brain using infrared matrix-assisted laser desorption electrospray ionization with mass spectrometry imaging (IR-MALDESI-MSI). …

Proposing An Rna Interference (Rnai)-Based Treatment For Human Immunodeficiency Virus (Hiv) By Analyzing The Post-Transcriptional Gene Targeting Of Sars-Cov-2, Hepatitis C Virus, And A549 Lung Cancer Cells, Arjun Jagdeesh

Undergraduate Research Posters

Human Immunodeficiency Virus (HIV) is a retrovirus that infects CD4+ T cell lymphocytes in humans, leading to the development of Acquired Immunodeficiency Syndrome (AIDS) if left untreated. While current treatment methods, including antiretroviral combination treatments, effectively limit HIV replication, HIV can evade these treatments due to its high mutation rate. Long-term antiretroviral treatment can also be toxic to patients, meaning patients would benefit from a new mechanism of HIV treatment. RNA interference (RNAi) is an antiviral pathway found in mammals, plants, and insects that involves a small-interfering RNA that is incorporated into a protein complex called the RNA-induced Silencing Complex …

Development Of A Chemical Biology Approach To Uncover The Influence Of Sequence Variations On Ces1 Activity In Live Cells, Samuel James Knebel

Masters Theses

Drug metabolism is the biochemical process of modifying drugs to detoxify and remove them through enzymatic transformations. These biotransformation’s occur primarily in the liver and are critical to understanding how pharmaceutical compounds are chemically altered inside the human body. Human carboxylesterases (CESs) catalyze the hydrolysis of esters, amides, thioesters, and carbamates. CES-mediated hydrolysis plays an important role in the metabolism of many drugs including the first FDA approved antiviral treatment for COVID-19, remdesivir (Veklury), the seizure control medication rufinamide (Banzel), and the flu antiviral drug oseltamivir (Tamiflu). CES activity is known to be influenced by a variety of factors including …

Effectiveness And Safety Of Direct Oral Anticoagulants Among Patients With Non-Valvular Atrial Fibrillation And Multimorbidity, Amol Dhamane, Mauricio Ferri, Allison V. Keshishian, Cristina Russ, Nipun Atreja, Cynthia Gutierrez, Birol Emir, Huseyin Yuce, Manuela Di Fusco

Publications and Research

Introduction

In the USA, there is a steady rise of atrial fibrillation due to the aging population with increased morbidity. This study evaluated the risk of stroke/systemic embolism (S/SE) and major bleeding (MB) among elderly patients with non-valvular atrial fibrillation (NVAF) and multimorbidity prescribed direct oral anticoagulants (DOACs).

Methods

Using the CMS Medicare database, a retrospective observational study of adult patients with NVAF and multimorbidity who initiated apixaban, dabigatran, or rivaroxaban from January 1, 2012 to December 31, 2017 was conducted. High multimorbidity was classified as having ≥ 6 comorbidities. Cox proportional hazard models were used to evaluate the hazard …

Nanoparticle Conjugated Photosensitizer For Targeted Photodynamic Inactivation Of Cancer Cells, Symone D. Crowder

Honors College Theses

Photodynamic therapy (PDT) is considered to be a potential replacement for traditional methods of chemotherapy. It includes the administration of photosensitizing agents (PS), which generate reactive oxygen species (ROS) upon excitation at a specific wavelength. With new outlooks and techniques, cancer research is advancing each day. It has allowed the progress of several theranostic drug delivery systems (DDS) exploring the area of nanomedicine.2 In the present work, a Rhodamine derivative, Rhodamine 6G (R6G) was used as the PS. In general, rhodamine compounds undergo cytotoxic reactions on photoexcitation by electron transfer reactions with folic acid within cells, making them a favorable …

Designing And Synthesizing A Warhead-Fragment Inhibitory Ligand For Ivyp1 Through Fragment-Based Drug Discovery, Samuel Moore

Symposium of Student Scholars

Fragment-based drug discovery (FBDD) is a powerful tool for developing anticancer and antimicrobial agents. Within this, magnetic resonance spectroscopy (NMR) provides a comprehensive qualitative and quantitative approach to screening and validating weak and robust binders with targeted proteins, making NMR among the most attractive strategies in FBDD. Inhibitor of vertebrate lysozyme (Ivyp1) of P. aeruginosa serves as an excellent target because of its active cellular location and implications in clinical prognosis for cystic fibrosis and immunocompromised patients. This study uses current NMR and biophysical techniques to develop a covalent, fragment-linked warhead inhibitor for Ivyp1 through synthetic methods, warhead linking, and …

Understanding Effect Of Ionic Liquid On Metalloproteins: Laccase And Azurin, Aashka Y. Patel

Theses and Dissertations

Interactions between ionic liquids and biomolecules have been of great interest due to the intrinsic properties of ionic liquids and the flexibility to mix and match cations and anions to create unique ionic liquids. A number of ionic liquid-biomolecule studies have focused on the interactions with proteins, including industrially relevant enzymes. One of these, laccase from Trametes versicolor, is a naturally derived enzyme used in the breakdown of phenolic compounds in a wide variety of industries, especially useful in breakdown of lignocellulosic materials. Here, a combination of experiments and molecular dynamics (MD) simulations were used to investigate the interactions …

Acknowledgment Of Reviewers

Journal of Food and Drug Analysis

No abstract provided.

Inorganic Arsenic Speciation Analysis In Food Using Hplc/Icp-Ms: Method Development And Validation, Yu-Cheng Lai, Yi-Chen Tsai, Yu-Ning Shin, Ya-Chun Chou, Ying-Ru Shen, Nu-Ching Lin, Shu-Han Chang, Ya-Min Kao, Su-Hsiang Tseng, Der-Yuan Wang

Journal of Food and Drug Analysis

Arsenic (As) compounds can be classified as organic or inorganic, with inorganic arsenic (iAs) having significantly higher toxicity than organic As. As may accumulate in food materials that have been exposed to As-contaminated environments. Thus, the “Sanitation Standard for Contaminants and Toxins in Foods” published by the Ministry of Health and Welfare set the standard limits for iAs content in rice, seaweed, seafood, and marine oils to safeguard public health. Therefore, a robust analytical method must be developed to selectively and quantitatively determine iAs content in rice, seaweed, seafood, and marine oils. Herein, we reported and verified the method of …

Optimization Of Quechers And High Performance Liquid Chromatography-Fluorescence Detection Conditions To Assess The Impact Of Preparation Procedures On Eu Priority Pahs In Coffee Samples And Their Pahs Consumption Risk, Ying-Chun Wan, Zwe-Lin Kong, Yu-Hsuan Chao, Chia-Fang Teng, Deng-Jye Yang

Journal of Food and Drug Analysis

The good performance conditions for determination of EU priority PAHs in coffee samples were established to evaluate the effects of roasting degree on the PAHs in coffee beans and the brewing methods on the PAHs transfer from coffee beans to their brews. The consumption risk of the PAHs in coffee products was also assessed. The PAHs levels of the roasted coffee beans were in the order: 923.65 ng/g (dark roast) > 132.20 ng/g (medium roast) > 69.28 ng/g (light roast). Compared with general brewing with the drip bag (PAHs content, 0.30–0.62 ng/mL in coffee brews), the coffee machine brewing (set at 4 …

Effect Of Sterilization Conditions On The Formation Of Furan And Its Derivatives In Canned Foods With Different Substrates, Wen-Xuan Tsao, Bing-Huei Chen, Tsai-Hua Kao

Journal of Food and Drug Analysis

This study explored the effects of sterilization conditions on the formation of furan and its 10 derivatives in canned foods with a sterilizing value (F0) at 4. The contents of furans were determined by SPME arrow-GC-MS/MS, along with the furan precursors analyzed for elucidating the possible mechanism of furan formation. Results revealed that the total furan contents rose substantially in canned meat paste, tomato mackerel, chicken puree, tomato paste, pineapple slice, pineapple juice and carrot juice following sterilization. However, the total furan content did not change significantly ( p > 0.05) in canned oily mackerel, but decreased significantly ( p < 0.05) in canned apple puree after sterilization. With the exception of apple puree and pineapple slice, all the other canned foods showed a higher total furan content under low-temperature-long-time condition than that under high-temperature-short-time condition. Following heating, only the furan level showed a large increase in chicken puree, meat paste and tomato mackerel, whereas in canned fruit- and vegetable-based foods, the contents of furan and furfural showed a pronounced increase. The levels of alkylated furans were higher in sterilized samples containing high level of amino acid, while that of oxygenated furans were higher in sterilized samples containing high level of reducing sugar.

Optimum Synthesis Of Au@Ag Nanoparticle As Plasma Amplifier To Detect Trace Concentration Of Afb1 Via Object-Binder-Metal Sers Method, Wenwen Chen, Qiang Chen, Wei Zhang, De Zhang, Zhi Yu, Ying Song, Xiubing Zhang, Dejiang Ni, Pei Liang

Journal of Food and Drug Analysis

The problem of aflatoxin contamination emerged gradually in the field of food safety. Surface-enhanced Raman spectroscopy (SERS) is an ultra-sensitive and non-destructive spectroscopy technology with extensive application prospects in the detection field. In this paper, with the detection of AFB1 as the target, Au@Ag NPs substrate with uniform morphology and strong SERS effect was prepared. Furthermore, the intermediates formed by hydrogen bonding between AFB1 and melamine facilitate the binding of toxin molecules to the substrate. Moreover, the AFB1-melamine-Au@Ag NPs detection system was established by optimizing the melamine dosage, and the limit of detection can reach 10^-8 mol/L (M). In …

Simple And Rapid Detection Of Ractopamine In Pork With Comparison Of Lspr And Lfia Sensors, Min Ji Lee, Sheik Aliya, Eun-Seon Lee, Tae-Joon Jeon, Mi-Hwa Oh, Yun Suk Huh

Journal of Food and Drug Analysis

This study developed a simple and rapid strategic technique to detect ractopamine (chemical growth-promoting agent) in pork. Two highly sensitive and specific gold nanoparticle-based portable sensors, i.e., localized surface plasmon resonance (LSPR) sensors, and lateral flow immunoassay (LFIA) strips were developed to detect veterinary drug residues in food products, that have detrimental effects on humans. Optimization studies were conducted on several sensor devices to improve sensitivity. Each sensor comprised functionalized gold nanoparticles conjugated with ractopamine antibodies. The LSPR sensor chip achieved excellent detection sensitivity = 1.19 fg/mL and was advantageous for quantitative analysis due to its wide dynamic range. On …