Medicinal Chemistry and Pharmaceutics Commons^™

Assessment Of Lemon Juice Quality And Adulteration By Ultra-High Performance Liquid Chromatography/Triple Quadrupole Mass Spectrometry With Interactive And Interpretable Machine Learning, Weiting Lyu, Bo Yuan, Siyu Liu, James E. Simon, Qingli Wu

Journal of Food and Drug Analysis

A total of 81 lemon juices samples were detected using an optimized UHPLC-QqQ-MS/MS method and colorimetric assays. Concentration of 3 organic acids (ascorbic acid, malic acid and citric acid), 3 saccharides (glucose, fructose and sucrose) and 6 phenolic acids (trans-p-coumaric acid, 3-hydroxybenzoic acid, 4-hydroxybenzoic acid, 3,4-dihydroxybenzoic acid, caffeic acid) were quantified. Their total polyphenol, antioxidant activity and Ferric reducing antioxidant power were also measured. For the prediction of authentic and adulterated lemon juices and commercially sourced lemonade beverages based on the acquired metabolic profile, machine learning models including linear discriminant analysis, Gaussian naïve Bayes, lasso-regularized logistic regression, random forest (RF) …

Ursolic Acid Restores Sensitivity To Gemcitabine Through The Rage/Nf-Κb/Mdr1 Axis In Pancreatic Cancer Cells And In A Mouse Xenograft Model, Zih-Ying Lia, Sheng-Yi Chena, Gow-Chin Yen

Journal of Food and Drug Analysis

Gemcitabine (GEM) is a first-line drug for pancreatic cancer therapy, but GEM resistance is easily developed in patients. Growing evidence suggests that cancer chemoprevention and suppression are highly associated with dietary phytochemical and microbiota composition. Ursolic acid (UA) has anti-inflammatory and anticancer effects; however, its role in improving cancer drug resistance in vivo remains unclear. In this study, the aim was to explore the role of UA in managing drug resistance-associated molecular mechanisms and the influence of gut microbiota. The in vitro results showed that receptor for advanced glycation end products (RAGE), nuclear factor kappa B p65 (NF-κB/p65), and multidrug …

Determination Of Phytochemical Compounds In Chicken Breast By Gas Chromatography-Tandem Mass Spectrometry, Federico Cozzi, Irene Eder-Neuhauser, Klaus Teichmann, Mathias Zaunschirm

Journal of Food and Drug Analysis

A gas chromatography–tandem mass spectrometry (GC–MS/MS) method was developed for the simultaneous detection and quantification of five phytogenic compounds (carvone, menthol, thymol, carvacrol and methyl salicylate) in chicken breast. Chicken breast samples were analyzed using a QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) approach using acetonitrile as extraction solvent, followed by a d-SPE (dispersive-solid phase extraction) clean up step. The linearities for the 5 substances were studied in the range between 2 and 100 µg/L and the coefficients of determination (R2) were always > 0.995. Matrix effects were also assessed by comparing the slopes obtained in solvent and chicken breast …

Application Of A Comprehensive Metabolomics Approach For The Selection Of Flaxseed Varieties With The Highest Nutritional And Medicinal Attributes, Mohamed A. Salem, Shahira M. Ezzat, Patrick Giavalsico, Essam Abdel Sattar, Nebal El Tanbouly

Journal of Food and Drug Analysis

Flaxseed is considered an indispensable generally recognized as safe (GRAS) source of polyphenolic lignans, poly-unsaturated fatty acids (PUFA), fibers as well as minerals and vitamins. The metabolite content of flaxseed reflects its nutritional and medicinal value. Therefore, the selection of flaxseed variety for food industry is dependent on its metabolome. A metabolomics approach based on liquid or gas chromatography coupled to mass spectrometry, has been applied to discriminate different flaxseed cultivars that are commercially available in Egypt. The available Sakha cultivars were subjected to a comprehensive metabolomics and lipidomics approach for investigation of their metabolomes. Our results showed that among …

Human Breast Milk-Based Nutritherapy: A Blueprint For Pediatric Healthcare, Pravin Shende, Bhakti Khanolkar

Journal of Food and Drug Analysis

Human Breast Milk (HBM) is a storehouse of micronutrients, macronutrients, immune factors, microbiota and numerous other bioactive macromolecules. Fulfilment of optimum nutritional requirements of more than 240 million malnourished infants worldwide is possible via adequate amount (570-900 mL/d) of breast milk administration to infants in first few years of life. Technological advancements enable study of multiple components of HBM like stem cells, bioactive proteins, micro RNAs, immunoglobulins and epithelial cells to understand their role in enhancement of nutritional value of HBM. Furthermore, immunological and protective functions of HBM against various illnesses like diabetes, anemia, respiratory and cardiovascular abnormalities, otitis media …

Current And Potential Applications Of Simultaneous Dsc-Ftir Microspectroscopy For Pharmaceutical Analysis, Shan-Yang Lin

Journal of Food and Drug Analysis

Quality control (QC) is the most important key issue in the pharmaceutical industry to ensure the quality of drug products. Many analytical instruments and techniques in pharmaceutical analysis are applied to assess the quality and quantity of the drugs. In the current and future trends, a combination of digitization, automation and hyphenation with high throughput on-line performance will be the topics for the future of pharmaceutical QC. The hyphenated analytical techniques have recently received great attention as unique means to solve complex analytical problems in a short period of time. This review article is an update on the recent potential …

Psychedelics Can Save: The Scientific And Social Case For Rescheduling Psychedelic Compounds, Galen M. Fader

Chancellor’s Honors Program Projects

No abstract provided.

Investigations Into The Cellular Target Of 4-Trifluoromethoxy Chalcone Via Darts Method, Jordan Stacy

Undergraduate Theses

Cellular drug target discovery is an important step in any drugs journey from bench to bedside. This is true for our lab's molecule of interest, the Chalcone. The Chalcone molecule and its derivatives have been identified as small, plant-derived secondary metabolites that, when interacting with human cancer cell lines, trigger apoptotic pathways leading to varying levels of cell death. One derivative, 4-Trifluoromethoxy Chalcone (4TFM), was identified through screenings as inducing the highest death rate in A549 cancer cells, in conjunction with having the lowest IC50, making it a good candidate to use in searching for the currently unknown cellular target …

Surface-Eroding Drug Delivery Films For Sequential And/Or Intermittent Release Of Psychoactive Drugs, Jason Price

Honors Theses

ABSTRACT JASON BLAKE PRICE: Surface-Eroding Drug Delivery Films for Sequential and/or

Intermittent Release of Psychoactive Drugs For patients with psychiatric diseases, adherence to medication schedules, medication

errors, and abuse are common issues. Promising new forms of therapy for these patients, such as micro-dosed lysergic acid diethylamide (LSD), where patients receive 10-20% of a full dose every third day, present further drug delivery challenges. Sequential or intermittent release of drugs from an implanted device could ensure long-term drug compliance, automate drug dosing during the life of the implant, and eliminate potential for abuse and medication errors. To this end, we generated …

Hyperoxia-Induced Cardiac Pathophysiology In Guinea Pig Hearts, Zain Ul Abidin

USF Tampa Graduate Theses and Dissertations

Hyperoxia, is regularly introduced to critically ill patients in ICU. Nevertheless, recent studies have shown the negative effects of this treatment on patients in critical care, including increased rates of lung and cardiac injury and thereby high in-hospital mortality. Large part of the literature related to hyperoxia was majorly focused on lung injury, with no or minimal investigations on cardiac injury. Our lab is the first to investigate the effect of hyperoxia on cardiac pathophysiology in mice and showed that mice exposed to hyperoxia for 3 days demonstrated brady-arrhythmia, cardiac hypertrophy, QTc prolongation along with other electrical remodeling and functional …

Development Of Continuous Flow Sonogashira Coupling Of Lead Anti-Cancer Small Molecule Inhibitors For Potential Treatment Of Acute Myeloid Leukemia, Yuta W. Moriuchi, Shruti A. Biyani, David H. Thompson

Discovery Undergraduate Interdisciplinary Research Internship

As the technology for science develops, the research strategy in medicines and therapeutics also improves. In this paper, I will cover the process of Sonogashira cross-coupling and Amide Coupling reaction for an anticancer agent in both batch and flow chemistry. Continuous Flow Chemistry has advantages such as being more efficient, safer, and faster. This paper studies the synthesis of HSNO608, an anticancer lead compound for Acute Myeloid Leukemia (AML), which has a specific potent activity to FTL3 Kinase. Inhibition of FLT3 Kinase leads to inhibition of downstream pathways such as MPK and P13K pathways. In this two-step experiment, the Sonogashira …

Synthesis Of 1-(4-Ethoxy-3-Methoxybenzyl)-1,10-Phenanthrolin-1-Ium Bromide And Its Evaluation As Antiplasmodium Through Heme Polymerization Inhibitory Activity (Hpia) Assay, Dhina Fitriastuti, Viny Alfiyah, Mustofa Mustofa, Jumina Jumina, Muhammad Idham Darussalam Mardjan

Makara Journal of Science

This study describes the development of N-benzyl-1,10-phenantrolinium salt as an antiplasmodium agent. The salt, that is, 1-(4-ethoxy-3-methoxybenzyl)-1,10-phenanthrolin-1-ium bromide, was prepared using vanillin as the starting material in four simple synthetic steps. First, the alkylation of vanillin using diethyl sulfate produced 4-ethoxy-3-methoxybenzaldehyde in 79% yield. Second, the reduction of the protected vanillin by NaBH₄ through the grinding method allowed us to obtain 4-ethoxy-3-methoxybenzyl alcohol in 96% yield. Next, the bromination of the benzyl alcohol under solvent-free condition led to the formation of the corresponding benzyl bromide, which in turn underwent bimolecular nucleophilic substitution with 1,10-phenanthroline to produce the desired …

Use Of A Zebrafish Model To Identify Anticonvulsant Properties Of Cannabinoid And Terpenoid Extracts And Mixtures, Courtney Murr

LSU Master's Theses

Epilepsy is a complex group of neurological disorders affecting approximately 65 million people worldwide. Animal models reveal the activation of cannabinoid receptor 1 and cannabinoid receptor 2 reduces the severity of seizures associated with epilepsy. Trials of phytocannabinoids in mammals demonstrate their efficacy of reducing the severity of epileptic seizures. Numerous terpenoid compounds are present in Cannabis plants but most have yet to be clinically investigated. The goal of this research was to use zebrafish (Danio rerio) to identify the potential anticonvulsive properties of phytocannabinoid and terpenoid compounds. During acute cannabinoid exposures, 7-days-post-fertilization (7 dpf) zebrafish larvae were …

Investigating The Novel Role Of Dextromethorphan In Mitigating Oxidative Stress Induced Changes In Retinal Pigment Epithelial Cells (Rpe), Zeinab A. Mohamed

USF Tampa Graduate Theses and Dissertations

Oxidative stress contributes to the degeneration of retinal pigment epithelial (RPE) cells and photoreceptors that lead to the dry form of age-related macular degeneration. Activation of N-Methyl-D-aspartate (NMDA) receptors contributes to the increase of free radicals that induce oxidative stress-induced changes. Our study investigates if Dextromethorphan, an NMDA receptor antagonist, reverses oxidative stress-induced changes in RPE. We used Paraquat and H2O2 as oxidative stress-inducing agents to induce oxidative damage in human ARPE-19 cells. To illustrate the change in cell viability and measure the apoptosis of ARPE-19 cells from oxidative damage, we performed MTT assay and Annexin V-DAPI flow cytometry analysis. …

Drug Candidates Targeting Hsp90/Cdc37 For The Treatment Of Neurodegenerative Disease, Ryan Martin

USF Tampa Graduate Theses and Dissertations

Neurodegenerative disease refers to the death of specific populations of neurons that canresult in dementia, loss of voluntary muscle motility, and other abnormalities. Two major neurodegenerative diseases are Alzheimer’s disease (AD) and Parkinson’s disease (PD), which are linked to abnormalities in Tau and a-synuclein proteins, respectively. Currently, there is no cure for these diseases. Our group and others have shown that chaperone proteins play a critical role in the processing of Tau and a-synuclein. The inhibition of the Hsp90/Cdc37 chaperone complex is shown to affect the levels of these two proteins. Hence, we hypothesized that a drug molecule, conglobatin (Cb), …

Glutathione-S-Transferase Mu 1 (Gstm1) Gene Augmentation Attenuated Oxidative Stress Induced Changes In Retinal Pigment Epithelium Cells (Rpe), Riddhi Sandeep Vichare

USF Tampa Graduate Theses and Dissertations

Purpose: Loss of Retinal Pigment Epithelial (RPE) cells and photoreceptors leads to Age-related macular degeneration (AMD), one of the leading causes of blindness in the elderly worldwide. Oxidative stress-mediated damage is one of the factors that impair the survival of RPE and photoreceptors in dry-AMD. We sought to determine the role of human Glutathione S-Transferase Mu-1 (GSTM1) in protecting RPE cells from oxidative stress-induced changes.

Method: We cloned human GSTM1 cDNA with P2A tag into a lenti-plasmid vector and later made a lentivector to express GSTM1. After that, we infected human retinal pigment epithelial cells (ARPE-19), screened stable ARPE-19 cells …

New Psychoactive Substances In Taiwan: The Current Situation And Initiative For Rational Scheduling, Wen-Jing Yu, Linda B. Cottler, Jih-Heng Li

Journal of Food and Drug Analysis

Use of New Psychoactive Substances (NPS) has posed a global threat to public health and the security of the population. As of December 2019, the NPS items identified in total have outnumbered by three to one the controlled substances listed in the 1961 and 1971 UN Drug Conventions. However, most of these NPS have not been scheduled by the United Nations because of their easy modification on the chemical structures to shun control. Currently, the scheduling and control of NPS is mostly at the national level and a rational scheduling of NPS by objective assessments is essential but often lacking. …

A Convenient And Sensitive Colorimetric Iodide Assay Based On Directly Inducing Morphological Transformation Of Gold Nanostars, Rongju Zhou, Xiaohui Huang, Qingxiao An, Weizhen Xu, Yi Liu, Dong Xu, Suyan Wang, Qinlu Lin, Jianglin Zhang

Journal of Food and Drug Analysis

We propose a convenient and easy colorimetric assay for highly sensitive detection of iodide by using gold nanostars (GNSs) as probes. The assay relies on that iodide directly changes the morphology of GNSs and alters their longitudinal localized surface plasmon resonance (LSPR) without surface modifications and the use of other reagents. Upon increasing iodide concentration, GNSs gradually transformed to sphere gold nanoparticles, the absorbance at longitudinal LSPR decreased, and solution color varied from greenish blue to red, as confirmed by the UV-Vis absorption spectroscopy and transmission electron microscopy. With this strategy, as low as 0.005 μM of iodide can be …

Quercetin Blocks The Aggressive Phenotype Of Triple Negative Breast Cancer By Inhibiting Igf1/Igf1r-Mediated Emt Program, Wei-Jen Chen, Jie-Heng Tsai, Li-Sung Hsu, Chih-Li Lin, Hui-Mei Hong, Min-Hsiung Pan

Journal of Food and Drug Analysis

The cancer-preventive activities of quercetin have been extensively studied in invasive breast cancer; however, the role of quercetin on triple-negative breast cancer (TNBC) with overexpression of insulin-like growth factor-1 receptor (IGF1R) has not been resolved. In this article, we demonstrated that quercetin inhibited the activation of IGF1R and its downstream kinases Akt and Erk1/2 in a dose-dependent manner in human MDA-MB-231 breast cancer cells (TNBC cell line). Related to this, quercetin markedly suppressed the metastatic phenotype and epithelial–mesenchymal transition (EMT) of MDA-MB-231 cells by inhibiting the expression of EMT transcription factors Snail and Slug. Quercetin also increased the secretion of …

The Bioactivities Of Resveratrol And Its Naturally Occurring Derivatives On Skin, Ming-Hsien Lin, Chi-Feng Hung, Hsin-Ching Sung, Shih-Chun Yang, Huang-Ping Yu, Jia-You Fang

Journal of Food and Drug Analysis

Resveratrol has been extensively reported as a potential compound to treat some skin disorders, including skin cancer, photoaging, allergy, dermatitis, melanogenesis, and microbial infection. There has been an increasing interest in the discovery of cosmetic application using resveratrol as the active ingredient because of its anti-aging and skin lightening activities. The naturally occurring derivatives of resveratrol also exert a beneficial effect on the skin. There are four groups of resveratrol derivatives, including hydroxylated compounds, methoxylated compounds, glycosides, and oligomers. The major mechanism of resveratrol and its derivatives for attenuating cutaneous neoplasia, photoaging and inflammation, are related with its antioxidative activity …