Attempted Synthesis & Antibacterial Properties Of Apt-6k Against Ndm-1 K. Pneumoniae,
2022
Andrews Universty
Attempted Synthesis & Antibacterial Properties Of Apt-6k Against Ndm-1 K. Pneumoniae, Alec Bofetiado
Honors Theses
NDM-1 K. pneumoniae is a highly resistant bacterial organism that is capable of causing debilitating nosocomial infections in immunocompromised patients. Only "last-resort" antibiotics--such as colistin--work against this organism. Therefore, new antibiotics are needed to help fight against these types of infections. APT-6K is a novel compound that was demonstrated to be effective against MRSA with nanomolar concentrations in a prior study. Novel methods of APT-6K synthesis and its testing for antibiotic effects against NDM-1 K. pneumoniae were attempted in this research. APT-6K synthesis was unsuccessful. Commercially-prepared APT-6K also did not demonstrate growth inhibition against NDM-1 K. pneumoniae nor against a …
Targeting The Side-Chain Convergence Of Α-Helical Hot Spots To Design Small-Molecule Mimetics Disrupting Protein-Protein Interaction,
2022
University of South Florida
Targeting The Side-Chain Convergence Of Α-Helical Hot Spots To Design Small-Molecule Mimetics Disrupting Protein-Protein Interaction, Zhen Wang
USF Tampa Graduate Theses and Dissertations
α-Helix accounts for the largest class of protein secondary structures and plays a key role in mediating protein-protein interactions (PPIs). Small-molecule α-helix mimetics mimic the structural features of α-helical hot spots and offer a powerful tool to unravel complex signaling networks and mitigate aberrant PPIs. In this dissertation, the side-chain conformational convergence of α-helical hot spots was disclosed, and insights into the side-chain convergence were exploited to instruct the design of small-molecule α-helix mimetics. The first chapter of this dissertation provides an overview of the characteristics of α-helical hot spots and current strategies to design small-molecule α-helix mimetics. In chapter …
Efforts To Increase The Ketamine-Like Activity Of The Rapid-Acting Antidepressant Ro-25-6981 (Mi-4) By Increasing Ampa Potentiation,
2022
Roseman University of Health Sciences
Efforts To Increase The Ketamine-Like Activity Of The Rapid-Acting Antidepressant Ro-25-6981 (Mi-4) By Increasing Ampa Potentiation, Nathan Heger
Annual Research Symposium
The small molecule ketamine has generated much interest due to its rapid antidepressant effects. Despite having a rapid onset, ketamine has poor bioavailability, short duration of action, toxicities with long-term use, and a high potential for abuse. The molecule MI-4 (RO 25-6981) has also been shown to have both a rapid and sustained antidepressant effect. Most of the research into the mechanism of the rapid onset of MI-4 and ketamine has focused on their interaction with the NMDA receptor in addition to some monoamine transporters. Some recent publications have shown a significant role of AMPA receptors in the ketamine antidepressant …
Response To A Water Bolus In Long Term Oral Contraceptive Users,
2022
University of Arkansas, Fayetteville
Response To A Water Bolus In Long Term Oral Contraceptive Users, Whitley C. Atkins, Brendon P. Mcdermott, Abigail T. Colburn, Stavros A. Kavouras
Health, Human Performance and Recreation Faculty Publications and Presentations
The purpose of our study was to determine the responses to an acute water bolus in long-term oral contraception (OCP) users. Seventeen female volunteers (27 ± 5 y, 64.1 ± 13.7 kg, 39.6 ± 5.9 kg/LBM) provided consent and enrolled in our study. All were long-term OCP users and participated in two trials, one during the active pill (High Hormone, HH) dose of their prescribed OCP and one during the sham pill (Low Hormone, LH) dose. Participants reported to the laboratory euhydrated, were fed breakfast, remained seated for 60 min and were provided a bolus of room temperature water in …
Antimicrobial Activity Of Zinc Oxide Nanoparticles Compared To Silver Nanoparticles Administered Towards Methicillin-Resistant Staphylococcus Aureus Biofilms,
2022
University of South Florida
Antimicrobial Activity Of Zinc Oxide Nanoparticles Compared To Silver Nanoparticles Administered Towards Methicillin-Resistant Staphylococcus Aureus Biofilms, Kevin Núño
USF Tampa Graduate Theses and Dissertations
Zinc oxide nanoparticles (ZnO NPs), silver nanoparticles (AgNPs), and chitosan nanoparticles have strong antibacterial activity as a broad-spectrum antibiotic against multi-drug resistant (MDR) bacteria. MDR bacteria have a mechanism that increases antibiotic resistance through biofilm formations. MDR methicillin-resistant Staphylococcus aureus BAA-1720 was chosen for an in vitro assessment to calculate the biofilm reduction rate and the median effective dose (ED50) by performing biofilm quantification. Dynamic light scattering was chosen to determine the physiochemical characteristics of ZnO NPs, silver nanoparticles (AgNPs), and chitosan NPs. Transmission electron microscopy was conducted to verify each treatment’s physiochemical characteristics. Antimicrobial susceptibility testing of broad-spectrum and …
The Use Of Atmospheric-Pressure Chemical Ionization For Pesticide Analysis Using Liquid Chromatography Mass Spectrometry,
2022
Department of Chemistry, National Taiwan Normal University, Taipei, Taiwan
The Use Of Atmospheric-Pressure Chemical Ionization For Pesticide Analysis Using Liquid Chromatography Mass Spectrometry, Pei-Ting Jiang, Kuan-Lu Wu, Hsueh-Ting Wang, Sung-Fang Chen
Journal of Food and Drug Analysis
Based on the regulations of the Ministry of Health and Welfare (MOHW) of Taiwan in 2017, an analysis of 373 pesticides in food was conducted using the MOHW official method. The analyses involved the use of either liquid chromatography mass spectrometry (LC-MS) with electrospray ionization (ESI) or gas chromatography mass spectrometry (GC-MS) with electron ionization (EI). In this study, the applicability of detecting pesticides using atmospheric pressure chemical ionization (APCI) was investigated and evaluated. The pesticides were separated using an aqueous solution of ammonium formate with methanol as the mobile phase, and ionization efficiency was compared between APCI, ESI, and …
A Substructure-Based Screening Approach To Uncover N-Nitrosamines In Drug Substances,
2022
School of Pharmacy, National Defense Medical Center, Taipei City, Taiwan, Republic of China
A Substructure-Based Screening Approach To Uncover N-Nitrosamines In Drug Substances, Yu-Ting Kao, Shu-Fen Wang, Meng-Hsiu Wu, Shwu-Huey Her, Yi-Hsuan Yang, Chung-Hsien Lee, Hsiao-Feng Lee, An-Rong Lee, Li-Chien Chang, Li-Heng Pao
Journal of Food and Drug Analysis
Drug substances are at risk of contamination with N-nitrosamines (NAs), well-known carcinogenic agents, during synthesis processes and/or long-term storage. Therefore, in this study, we developed an efficient data-based screening approach to systemically assess marketed products and investigated its scalability for benefiting both regulatory agencies and pharmaceutical industries. A substructure-based screening method employing DataWarrior, an open-source software, was established to evaluate the risks of NA impurities in drug substances. Eight NA substructures containing susceptible amino sources for N-nitrosation have been identified as screening targets: dimethylamine (DMA), diethylamine, isopropylethylamine, diisopropylamine, N-methyl-2-pyrrolidone, dibutylamine, methylphenylamine, and tetrazoles. Our method detected 192 drug …
Repurposing Lansoprazole And Posaconazole To Treat Leishmaniasis: Integration Of In Vitro Testing, Pharmacological Corroboration, And Mechanisms Of Action,
2022
Infectious Diseases, Mayo Clinic, Jacksonville, Florida, USA
Repurposing Lansoprazole And Posaconazole To Treat Leishmaniasis: Integration Of In Vitro Testing, Pharmacological Corroboration, And Mechanisms Of Action, Yash Gupta, Steven Goicoechea, Jesus G. Romero, Raman Mathur, Thomas R. Caulfield, Daniel P. Becker, Ravi Durvasula, Prakasha Kempaiah
Journal of Food and Drug Analysis
Leishmaniasis remains a serious public health problem in many tropical regions of the world. Among neglected tropical diseases, the mortality rate of leishmaniasis is second only to malaria. All currently approved therapeutics have toxic side effects and face rapidly increasing resistance. To identify existing drugs with antileishmanial activity and predict the mechanism of action, we designed a drug-discovery pipeline utilizing both in-silico and in-vitro methods. First, we screened compounds from the Selleckchem Bio-Active Compound Library containing ~1,622 FDA-approved drugs and narrowed these down to 96 candidates based on data mining for possible anti-parasitic properties. Next, we completed preliminary in-vitro testing …
Effect Of Repeated Shengmai-San Administration On Nifedipine Pharmacokinetics And The Risk/Benefit Under Co-Treatment,
2022
School of Pharmacy, National Defense Medical Center, Taipei, Taiwan
Effect Of Repeated Shengmai-San Administration On Nifedipine Pharmacokinetics And The Risk/Benefit Under Co-Treatment, Hong-Jaan Wang, Elise Chia-Hui Tan, Tzu-Yi Chiang, Wei-Ching Chen, Chien-Chang Shen, Yune-Fang Ueng
Journal of Food and Drug Analysis
Herbal interactions with nifedipine/felodipine through cytochrome P450 (CYP) 3A inhibition is significant in humans. Shengmai-San (SMS), a three-herbal formula of Chinese medicine, is commonly prescribed in Asia populations for cardiovascular disorders. This study aimed to elucidate the impact of SMS on nifedipine/felodipine treatment by the findings from rat pharmacokinetic study of nifedipine to the retrospective cohort study of patients with hypertension. The 3-week SMS treatment increased the systemic exposure to nifedipine by nearly two-fold and decreased nifedipine clearance by 39% in rats. Among the ingredients of SMS component herbs, schisandrin B, schisantherin A, and methylophiopogonanone A, inhibited the nifedipine oxidation …
Evaluation Of Opioid Consumption Trends For Pain In Taiwan And Comparison With Neighboring Asian Countries,
2022
Chi Mei Medical Center, Tainan, Taiwan
Evaluation Of Opioid Consumption Trends For Pain In Taiwan And Comparison With Neighboring Asian Countries, Jhi-Joung Wang, Shu-Fang Teng, Yu-Roo Chu, Chin-Chen Chu, Chung-Han Ho, Li-Ling Chu
Journal of Food and Drug Analysis
Opioids are effective analgesics for pain relief, however, inappropriate use may cause risks. The aims of the study were to evaluate trends of opioid consumption for pain management in Taiwan and compare them among neighboring Asian countries. Opioid consumption data, including fentanyl, morphine, oxycodone, hydromorphone, codeine, and pethidine, were collected from the Controlled Drugs Management Information System of Taiwan Food and Drug Administration from 2008 to 2018. Data of different continents and neighboring Asian countries were retrieved from the WHO website. The major findings include: (1) In Taiwan, the total annual opioid consumption has gradually increased from 2008 to 2018, …
A Three-Step Stacking Capillary Electrophoresis Of Field-Amplified Sample Injection, Sweeping, And Micellar Collapse For Determination Of Dabigatran And Its Active Metabolite In Human Plasma,
2022
College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan, ROC
A Three-Step Stacking Capillary Electrophoresis Of Field-Amplified Sample Injection, Sweeping, And Micellar Collapse For Determination Of Dabigatran And Its Active Metabolite In Human Plasma, Cheng-Wei Cheng, Wen-Han Feng, Wei-Hua Tang, Hwang-Shang Kou, Chun-Chi Wang, Shou-Mei Wu
Journal of Food and Drug Analysis
A three-step stacking capillary electrophoresis (CE) composed of field-amplified sample injection, sweeping, and analyte focusing by micellar collapse (FASI-sweeping-AFMC) was developed to determine dabigatran (D) and its major active metabolite, dabigatran acyl-beta-d-glucuronide (DAG), in human plasma. After optimization and validation, this novel approach was further applied to monitor 5 real samples, and the 25.2 to 186.8 ng mL-1 D could be observed among those. Based on these results, the novel CE stacking strategy was successfully applied for the analysis of D and DAG in human plasma and could be served as a tool for clinical assays.
The Antihyperlipidemic Equivalent Combinatorial Components From Peel Of Citrus Reticulata ‘Chachi’,
2022
State Key Laboratory of Natural Medicines, China Pharmaceutical University
The Antihyperlipidemic Equivalent Combinatorial Components From Peel Of Citrus Reticulata ‘Chachi’, Ping-Ting Xiao, Yu-Jia Kuang, Shi-Yu Liu, Zhi-Shen Xie, Jin-Hua Hao, E-Hu Liu
Journal of Food and Drug Analysis
Since the combinatorial components responsible for the antihyperlipidemic activity of Citrus reticulata‘Chachi’ (CRC) peels remains unclear, we herein developed a bioactive equivalence oriented feedback screening method to discover the bioactive equivalent combinatorial components (BECCs) from CRC peels. Using palmitic acid (PA)- stimulated hepatocyte model, a combination of five polymethoxyflavones (PMFs) including tangeretin, sinensetin, nobiletin, 5,7,8,4′-tetramethoxyflavone and 3,5,6,7,8,3',4'-heptamethoxyflavone was identified to be responsible for the antihyperlipidemic effect of CRC peels. Via evaluation of combination effect by combination index (CI), these 5 PMFs were found to take effect via a synergistic mode. Our data indicated that the antihyperlipidemic mechanism of PMF …
Food Glycomics: Dealing With Unexpected Degradation Of Oligosaccharides During Sample Preparation And Analysis,
2022
Department of Food Science and Technology, University of California-Davis, Davis, CA, USA
Food Glycomics: Dealing With Unexpected Degradation Of Oligosaccharides During Sample Preparation And Analysis, Yu-Ping Huang, Randall C. Robinson, Daniela Barile
Journal of Food and Drug Analysis
This study reveals that unexpected degradation of food oligosaccharides can occur during conventional glycomics workflows, including sample preparation and analysis by liquid chromatography-mass spectrometry (LC-MS). With the present investigation, we aim to alert the scientific community of the susceptibility of specific glycosidic linkages to degradation induced by heat and acid. Key standard oligosaccharides representing the major types found in foods (3’-sialyllactose and 6’-sialyl-N-acetyllactosamine for milk, raffinose and stachyose for legumes) were selected as model systems and underwent each of the following treatments independently: (1) labeled with the derivatizing agent 1-aminopyrene-3,6,8-trisulfonic (APTS) (followed by analysis with a capillary electrophoresis system coupled …
Ulva Prolifera Polysaccharide Exerts Anti-Obesity Effects Via Upregulation Of Adiponectin Expression And Gut Microbiota Modulation In High-Fat Diet-Fed C57bl/6 Mice,
2022
Institute of Food Sciences and Technology, National Taiwan University, Taipei, Taiwan
Ulva Prolifera Polysaccharide Exerts Anti-Obesity Effects Via Upregulation Of Adiponectin Expression And Gut Microbiota Modulation In High-Fat Diet-Fed C57bl/6 Mice, Hai-Ching Pung, Wei-Sheng Lin, Yi-Chen Lo, Cheng-Chih Hsu, Chi-Tang Ho, Min-Hsiung Pan
Journal of Food and Drug Analysis
Obesity is characterized by metabolic disorder and accompanying an altered and less diverse gut microbiota composition during a fat-enriched diet. Recent studies indicated that sulphated polysaccharide prevents high-fat diet (HFD) induced obesity, reduces metabolic disorder, and restores the gut microbiota. However, there are few studies about Ulva prolifera polysaccharide (UPP) may induce anti-obesogenic effects. Therefore, the present study investigates the enzymatic extracted UPP effects in HFD-fed mice. The results showed that UPP considerably slowed down the HFD-induced weight gain and improved metabolic disorders in HFD-fed mice. Notably, the effects were associated with lower body weight gain, reduced adipose tissue hypertrophy, …
Stable Carbon Isotopic Characterization Of Rice Vinegar Protein As An Intrinsic Reference For Discriminating The Authenticity Of Brewed Rice Vinegar,
2022
Department of Agricultural Chemistry, National Taiwan University, Taipei City, Taiwan
Stable Carbon Isotopic Characterization Of Rice Vinegar Protein As An Intrinsic Reference For Discriminating The Authenticity Of Brewed Rice Vinegar, Chun-Jen Fang, Hsin-Cheng You, Zih-Ling Huang, Che-Lun Hsu, Chia-Fen Tsai, Ya-Tze Lin, Ya-Min Kao, Su-Hsiang Tseng, Der-Yuan Wang, Nan-Wei Su
Journal of Food and Drug Analysis
Rice vinegar plays an important role in daily life. However, some unscrupulous manufacturers may deliberately add synthetic acetic acid in vinegar products to reduce fermentation time and save production costs. To protect the rights and health of consumers, vinegar authenticity must be controlled. The rice vinegar protein was used as an intrinsic reference and its stable carbon isotope ratio (δ13Cprotein) was analyzed by elemental analyzer-isotope ratio mass spectrometry. The stable carbon isotope ratio difference between the acetic acid and the rice vinegar protein (Δδ13Cacetic acid-protein) was calculated to evaluate vinegar authenticity. Sixteen …
Direct Immersion Solid-Phase Microextraction Combined With Ambient Ionization Tandem Mass Spectrometry To Rapidly Distinguish Pesticides In Serum For Emergency Diagnostics,
2022
Department of Chemistry, National Sun Yat-Sen University, Kaohsiung, Taiwan
Direct Immersion Solid-Phase Microextraction Combined With Ambient Ionization Tandem Mass Spectrometry To Rapidly Distinguish Pesticides In Serum For Emergency Diagnostics, Hung Su, Hsin-Hua Lin, Lin-Jhen Su, Chia-Chen Lin, Zong-Han Jiang, Shiang-Jin Chen, Jentaie Shiea, Chi-Wei Lee
Journal of Food and Drug Analysis
Despite the fact that carbamates and organophosphates cause acute poisoning via different mechanisms and require disparate management, they are indistinguishable by current clinical assays. Herein, direct immersion solid-phase microextraction (DI-SPME) plus thermal desorption-electrospray ionization tandem mass spectrometry (TD-ESI/MS/MS) was developed to discern them. Both pesticides spiked in human serum were extracted by SPME and analyzed by TD-ESI/MS/MS. This is a promising emergency care platform as rapid analyses could be done in tiny sample volumes with satisfactory recovery (89.46%–116.32%), precision (covariance < 20%), sensitivity (LOD < 0.1 µg/mL), turnaround time (< 5 minutes), and linearity (R2 = 0.9827–0.9992) within 0.1–100 µg/mL.
Determination Of Perfluoroalkyl Substances In Food Packaging In Taiwan Using Ultrasonic Extraction And Ultra-Performance Liquid Chromatography/Tandem Mass Spectrometry,
2022
Institute of Food Safety and Health, College of Public Health, National Taiwan University, Taipei, Taiwan
Determination Of Perfluoroalkyl Substances In Food Packaging In Taiwan Using Ultrasonic Extraction And Ultra-Performance Liquid Chromatography/Tandem Mass Spectrometry, Peng Siao, Su-Hsiang Tseng, Chia-Yang Chen
Journal of Food and Drug Analysis
Perfluoroalkyl substances (PFASs), as coating materials, possess oil-resistant and waterproof properties. However, their persistency and toxicity have caused concerns. This study developed a method for determining five types of 20 PFASs with ultra-performance liquid chromatography/tandem mass spectrometry, and measured seven categories of 32 commercial samples of oil-resistant food packaging in Taiwan. The assay was validated according to the specification of Taiwan Food and Drug Administration (TFDA). Samples of 100 cm2 were cut into pieces and were ultra-sonicated in 20-mL methanol at 50℃ for 45 minutes. The extracts were concentrated to 1 mL for instrumental analysis. Most matrix effect factors …
The Next Generation Beneficial Actions Of Novel Probiotics As Potential Therapeutic Targets And Prediction Tool For Metabolic Diseases,
2022
Department of Nutrition, Chung Shan Medical University, Taichung, Taiwan
The Next Generation Beneficial Actions Of Novel Probiotics As Potential Therapeutic Targets And Prediction Tool For Metabolic Diseases, Hsin-Lin Cheng, Gow-Chin Yen, Shih-Chien Huang, Shiuan-Chih Chen, Chin-Lin Hsu
Journal of Food and Drug Analysis
The prevalence of metabolic disease has rising and affected over 1,000 million populations globally. Since the metabolic disease and its related complication are board, it has become the major health hazard of modern world. However, Long term medication of metabolic disease may cause serious side effects and risk for adverse health problems. Recently, emerging studies focus on exploring the mechanistic details of metabolic state in disease development and progression. Gut bacteria ecosystem was considered to play a pivotal role in regulating energy homeostasis and great associated with the development of metabolic disease. Accumulated evidences indicated that Akkermansia muciniphila, Faecalibacterium prausnitzii, …
Effects Of Acid Hydrolyzed Chitosan Derivatives On Mhv Infection,
2022
University of South Florida
Effects Of Acid Hydrolyzed Chitosan Derivatives On Mhv Infection, Krishna Sharma
USF Tampa Graduate Theses and Dissertations
Coronaviruses have recently been under significant scrutiny due to the ongoing covid-19 pandemic that began in Wuhan, China, and subsequently spread to the rest of the world. Chitosan is a common chemical from crustaceans that has several desirable properties due to being biodegradable, non-toxic, and, most importantly, cheap. It also exhibits anti-viral properties, which is the focus of these experiments. We tested the toxicity of the chitosan on cell lines to see how much chitosan the cells can tolerate. We hydrolyzed the chitosan in acid, and the chitosan fibrils added cell lines to see if the anti-viral properties increased in …
Repurposing Lansoprazole And Posaconazole To Treat Leishmaniasis: Integration Of In Vitro Testing, Pharmacological Corroboration, And Mechanisms Of Action,
2022
Mayo Clinic
Repurposing Lansoprazole And Posaconazole To Treat Leishmaniasis: Integration Of In Vitro Testing, Pharmacological Corroboration, And Mechanisms Of Action, Yash Gupta, Steven Goicoechea, Jesus G. Romero, Raman Mathur, Thomas R. Caulfield, Daniel P. Becker, Ravi Durvasula, Prakasha Kempaiah
Chemistry: Faculty Publications and Other Works
Leishmaniasis remains a serious public health problem in many tropical regions of the world. Among neglected tropical diseases, the mortality rate of leishmaniasis is second only to malaria. All currently approved therapeutics have toxic side effects and face rapidly increasing resistance. To identify existing drugs with antileishmanial activity and predict the mechanism of action, we designed a drug-discovery pipeline utilizing both in-silico and in-vitro methods. First, we screened compounds from the Selleckchem Bio-Active Compound Library containing ~1622 FDA-approved drugs and narrowed these down to 96 candidates based on data mining for possible anti-parasitic properties. Next, we completed preliminary in-vitro testing …
