Medicinal Chemistry and Pharmaceutics Commons^™

Guilu Erxian Jiao Enhances Protein Synthesis, Glucose Homeostasis, Mitochondrial Biogenesis And Slow-Twitch Fibers In The Skeletal Muscle, Wei-Yu Fang, Wan-Hsuan Chang, Yi-Hong Tsai, Hung-Te Hsu, Fang-Rong Chang, Chih-Lung Lin, Yi-Ching Lo

Journal of Food and Drug Analysis

Guilu Erxian Jiao (GEJ) is a commonly used nutritional supplement due to its rich content of amino acids. It is also a traditional herbal medicine for improving degenerative joint. This study aimed to investigate the effect and mechanism of GEJ water extract (GEJ-WE) on skeletal muscle in C2C12 myotubes and C57BL/6J mice. Analysis of GEJ-WE were performed by high-performance liquid chromatography fingerprinting with chemical standards. Protein expression, mRNA level, glycogen content, mitochondria activity and ATP level were evaluated by western blots, real-time PCR, PAS staining, MTT and ATP bioluminescence assay, respectively. Skeletal muscle strength was evaluated by grip strength. Skeletal …

High-Resolution 1h Nmr Analysis Of Continuous And Discontinuous Thermo-Oxidative Susceptibility Of Culinary Oils During Frying At 180℃, Gilbert Ampem, Adam Le Gresley, Martin Grootveld, Declan P Naughton

Journal of Food and Drug Analysis

Lipid oxidations products (LOPs) are reactive mutagenic and carcinogenic species known to be generated in thermally stressed culinary oils. Mapping the evolution of LOPs in culinary oils exposed to standard frying practices – both continuous and discontinuous thermo-oxidation – at 180℃ is vital to our understanding of these processes, and to the development of scientific solutions for their effective suppression. Modifications in the chemical compositions of the thermo-oxidised oils were analysed using a high-resolution proton nuclear magnetic resonance (¹H NMR) technique. Research findings acquired showed that polyunsaturated fatty acid (PUFA)-rich culinary oils were the most susceptible to thermo-oxidation. …

Investigation Of Monacolin K, Yellow Pigments, And Citrinin Production Capabilities Of Monascus Purpureus And Monascus Ruber (Monascus Pilosus), Tzu-Shing Lin, Shih-Hau Chiu, Chien-Chi Chen, Chih-Hui Lin

Journal of Food and Drug Analysis

Red mold rice (RMR) is a traditional Chinese medicine prepared using Monascus fermentation. M. ruber (pilosus) and M. purpureus have a long history of use as food and medicine. As an economically important starter culture, the relationship between the taxonomy of Monascus and production capabilities of secondary metabolites is crucial for the Monascus food industry. In this study, monacolin K, monascin, ankaflavin, and citrinin production by M. purpureus and M. ruber were genomically and chemically investigated. Our findings suggest that M. purpureus can produce monascin and ankaflavin in a correlated manner, whereas M. ruber produces monascin with minimum …

Determination Of 24 Sulfonamide Antibiotics In Instant Pastries By Modified Quechers Coupled With Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry, Shuo Li, Can Zhang, Hui-Xin Tang, Yue Gu, Ai-Jing Guo, Ke Wang, Kao-Qi Lian

Journal of Food and Drug Analysis

There were few reports about antibiotic residues in egg-containing products. In the study, an effective method for the simultaneous determination of 24 sulfonamide antibiotics in two instant pastries based on a modified QuEChERS sample preparation technique coupled with ultra performance liquid chromatography-tandem mass spectrometry was developed. The results show that the average recoveries of the SAs at 5, 10, and 50 µg·kg^-1 levels were 67.6%-103.8%, with relative standard deviations (RSD) of 0.80-9.23%. The limit of detections (LODs) and limit of quantitations (LOQs) were 0.01-0.14 µg∙kg^-1 and 0.02-0.45 µg∙kg^-1, respectively. This method was suitable for analysis of …

Erinacine S From Hericium Erinaceus Mycelium Promotes Neuronal Regeneration By Inducing Neurosteroids Accumulation, Chun-Yu Lin, Yi-Ju Chen, Chih-Hsuan Hsu, Yu-Hsuan Lin, Peng-Tzu Chen, Ting-Han Kuo, Chris T. Ho, Hsin-Hua Chen, Sih-Jia Huang, Ho-Chieh Chiu, Chin-Chu Chen, Eric Hwang

Journal of Food and Drug Analysis

Erinacines derived from Hericium erinaceus have been shown to possess various health benefits including neuroprotective effect against neurodegenerative diseases, yet the underlying mechanism remains unknown. Here we found that erinacine S enhances neurite outgrowth in a cell autonomous fashion. It promotes post-injury axon regeneration of PNS neurons and enhances regeneration on inhibitory substrates of CNS neurons. Using RNA-seq and bioinformatic analyses, erinacine S was found to cause the accumulation of neurosteroids in neurons. ELISA and neurosteroidogenesis inhibitor assays were performed to validate this effect. This research uncovers a previously unknown effect of erinacine S on raising the level of neurosteroids.

Regulatory Considerations For Generic Products Of Non-Biological Complex Drugs, Yu-Hsuan Liu, Yi-Shuo Chen, Ting Tseng, Min-Lin Jiang, Churn-Shiouh Gau, Lin-Chau Chang

Journal of Food and Drug Analysis

The Non-Biological Complex Drug (NBCD) Working Group defines an NBCD as “a medicinal product, not being a biological medicine, where the active substance is not a homo-molecular structure, but consists of different (closely related and often nanoparticulate) structures that cannot be isolated and fully quantitated, characterized and/or described by physicochemical analytical means”. There are concerns about the potential clinical differences between the follow-on versions and the originator products and within the individual follow-on versions. In the present study, we compare the regulatory requirements for developing generic products of NBCDs in the European Union (EU) and the United States (US). The …

Recent Developments In Detection And Therapeutic Approaches For Antibiotic-Resistant Bacterial Infections, Kavya Moorthy, Kai-Chih Chang, Hsueh-Hui Yang, Wen-Min Su, Cheng-Kang Chiang, Zhiqin Yuan

Journal of Food and Drug Analysis

Owing to the widespread emergence and proliferation of antibiotic-resistant bacteria, the therapeutic benefits of antibiotics have been reduced. In addition, the ongoing evolution of multidrug-resistant pathogens poses a challenge for the scientific community to develop sensitive analytical methods and innovative antimicrobial agents for the detection and treatment of drug-resistant bacterial infections. In this review, we have described the antibiotic resistance mechanisms that occur in bacteria and summarized the recent developments in detection strategies for monitoring drug resistance using different diagnostic methods in three aspects, including electrostatic attraction, chemical reaction, and probe-free analysis. Additionally, to understand the effective inhibition of drug-resistant …

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 …

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 …

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). …

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 …