Open Access. Powered by Scholars. Published by Universities.®

Pharmacology Commons™

Open Access. Powered by Scholars. Published by Universities.®

Discipline
Institution
Keyword
Publication Year
Publication
Publication Type
File Type

Articles 631 - 660 of 3580

Full-Text Articles in Pharmacology

Impact Of Sodium Dichloroacetate Alone And In Combination Therapies On Lung Tumor Growth And Metastasis, Aya Mudhafar A. Al-Azawi Sep 2021

Impact Of Sodium Dichloroacetate Alone And In Combination Therapies On Lung Tumor Growth And Metastasis, Aya Mudhafar A. Al-Azawi

Theses

Lung cancer is the second most common form of cancer with the highest mortality rate worldwide in 2020 despite the advances in targeted- and immuno-therapies. Metabolic reprogramming has been recognized as an essential emerging cancer hallmark in which altered metabolic pathways represent an attractive therapeutic target. Sodium Dichloroacetate (DCA), a pyruvate dehydrogenase kinase (PDK) inhibitor, effect has been investigated in various tumors. Building on the already published data, this pre-clinical study aims to explore the anticancer potential of DCA in lung cancer alone and in combination with chemo- and targeted therapies using two non-small cell lung cancer (NSCLC) cell lines …

Go to article

Exploring Fused Deposition Modeling (Fdm) Three-Dimensional Printing Tablet Design Options For Pharmaceutical Dosage Forms, Guluzar Gorkem Buyukgoz Aug 2021

Exploring Fused Deposition Modeling (Fdm) Three-Dimensional Printing Tablet Design Options For Pharmaceutical Dosage Forms, Guluzar Gorkem Buyukgoz

Dissertations

This dissertation examines the use of Fused Deposition Modeling (FDM) based three-dimensional (3D) printing approach for developing patient-specific dosage forms and addressing related technical challenges in such drug delivery systems. The first main objective is to explore pharmaceutical tablet design options using novel FDM 3D printing technology as the drug delivery platform such that drug form and tablet properties are tailored by considering patient age-specific formulations and dissolution control. Of the five different design options, two proposed options meet the main objective of providing similar drug release, whereas the popular option of fixed drug concentration but differing tablet size could …

Go to article

In Vivo Antidiabetic Activities Of Polyherbal Extracts Against Streptozotocin-Nicotinamide Induced Type 2 Diabetic Mice Model, Pradnya Jagtap, Yashashri Nimbalkar, Vidya Patil, Ravindra Y. Patil Aug 2021

In Vivo Antidiabetic Activities Of Polyherbal Extracts Against Streptozotocin-Nicotinamide Induced Type 2 Diabetic Mice Model, Pradnya Jagtap, Yashashri Nimbalkar, Vidya Patil, Ravindra Y. Patil

Tanzania Journal of Science

Diabetes mellitus is a chronic metabolic disorder and rapidly increasing cases of diabetes throughout the world are major concerns in both developed and developing countries. Currently available oral antidiabetic medicines have limitations in efficacy and safety, which in conjunction with the emergence of diabetes mellitus as a global epidemic have aided the popularity of alternative therapies to manage the disease safely and more efficiently. Herbal medicines are accepted as alternative therapies for blood sugar control. Gymnema sylvestre, Boerhavia diffusa, Tinospora cordifolia, and Argyreia nervosa are some potent herbs used for the management of diabetes. Mixing of these plants in different …

Go to article

Prunus Africanus Herbal Extracts Reverse And Ameliorate The Histological And Histomorphometric Changes In Testosterone-Induced Benign Prostate Hyperplasia Rat Models, Felix P. William, Denis A. Russa Aug 2021

Prunus Africanus Herbal Extracts Reverse And Ameliorate The Histological And Histomorphometric Changes In Testosterone-Induced Benign Prostate Hyperplasia Rat Models, Felix P. William, Denis A. Russa

Tanzania Journal of Science

Benign prostatic hyperplasia (BPH) is the most common benign proliferative disease among men during aging. The herbal extract of P. africanus has been used for the treatment of BPH since time immemorial. However microstructural changes of this extract to the prostate of animal or human models are still elusive. Therefore, histological and histomorphometric changes in rats with testosterone-induced BPH due to P. africanus herbal extracts were investigated. Twenty-eight male Wistar rats (200 ± 50 g) were divided into four groups each with 7 rats. Group 1 (Negative control) was given 2 ml/day of olive oil subcutaneously and 2 ml/day of …

Go to article

Epidemiology, Pathogenesis, And Clinical Manifestations Of Acute Esophageal Necrosis In Adults, Obaid Rehman, Urooj Jaferi, Inderbir Padda, Nimrat Khehra, Harshan Atwal, Mayur Parmar Jul 2021

Epidemiology, Pathogenesis, And Clinical Manifestations Of Acute Esophageal Necrosis In Adults, Obaid Rehman, Urooj Jaferi, Inderbir Padda, Nimrat Khehra, Harshan Atwal, Mayur Parmar

HPD Articles

Acute esophageal necrosis (AEN), also termed "black esophagus," is a unique and uncommon occurrence observed in severely sick patients. Other terminologies include acute necrotizing esophagitis and Gurvits syndrome. This condition is described as a darkened distal third of the esophagus observed on endoscopy and presents as an upper gastrointestinal (GI) bleed, difficulty swallowing, abdominal pain, fever, syncope, nausea, and vomiting. The etiology of AEN has been linked to several possibilities, such as excessive gastric acid reflux, hypoperfusion, and ischemia due to impaired vascular supply and hemodynamic instability. Risk factors include increased age, sex (male), heart disease, hemodynamic insufficiency, alcohol use, …

Go to article

Genetic Testing For Antipsychotic Pharmacotherapy: Bench To Bedside, Mujeeb U. Shad Jun 2021

Genetic Testing For Antipsychotic Pharmacotherapy: Bench To Bedside, Mujeeb U. Shad

Psychiatry & Behavioral Health Faculty Research

There is growing research interest in learning the genetic basis of response and adverse effects with psychotropic medications, including antipsychotic drugs. However, the clinical utility of information from genetic studies is compromised by their controversial results, primarily due to relatively small effect and sample sizes. Clinical, demographic, and environmental differences in patient cohorts further explain the lack of consistent results from these genetic studies. Furthermore, the availability of psychopharmacological expertise in interpreting clinically meaningful results from genetic assays has been a challenge, one that often results in suboptimal use of genetic testing in clinical practice. These limitations explain the difficulties …

Go to article

A Study Of Trpa1 Activation Via Covalent Electrophilic Modification Of Cysteines, Thomas A. Parks Jun 2021

A Study Of Trpa1 Activation Via Covalent Electrophilic Modification Of Cysteines, Thomas A. Parks

USF Tampa Graduate Theses and Dissertations

A subset of sensory nerves called nociceptors are stimulated by noxious stimuli and evoke nocifensive responses in different organ systems. Transient Receptor Potential Ankyrin 1 (TRPA1) is a tetrameric, nonselective, cation channel that initiates the generator potential that evokes afferent signaling in nociceptive nerves. TRPA1 is activated many harmful irritants, such as food chemicals, environmental pollutants, reactive oxygen species and other endogenous mediators. Most TRPA1 agonists have electrophilic properties, which covalently modify cysteine residues on the cytosolic side of the channel. Biochemical studies in our lab have identified four cysteines (C273, C621, C665, C1085) that rapidly bound iodoacetamide (irreversible electrophile); …

Go to article

Corrigendum To “Novel Uplc-Ms/Ms Method For Standardization Of Niazimicin Content In Edible Seeds And Leaves Of Moringa Oleifera Lam” [J Food Drug Anal 29 (2021) 128-143] Jun 2021

Corrigendum To “Novel Uplc-Ms/Ms Method For Standardization Of Niazimicin Content In Edible Seeds And Leaves Of Moringa Oleifera Lam” [J Food Drug Anal 29 (2021) 128-143]

Journal of Food and Drug Analysis

none

Go to article

Corrigendum To “Determination Of Glycidyl Esters And 3-Mcpd Esters In Edible Oils By Sample Pretreatment With The Combination Of Lipase Hydrolysis And Modified Quechers For Gc-Ms Analysis” [J Food Drug Anal 29 (2021) 153-167] Jun 2021

Corrigendum To “Determination Of Glycidyl Esters And 3-Mcpd Esters In Edible Oils By Sample Pretreatment With The Combination Of Lipase Hydrolysis And Modified Quechers For Gc-Ms Analysis” [J Food Drug Anal 29 (2021) 153-167]

Journal of Food and Drug Analysis

none

Go to article

Pepsin-Digested Chicken-Liver Hydrolysate Attenuates Hepatosteatosis By Relieving Hepatic And Peripheral Insulin Resistance In Long-Term High-Fat Dietary Habit, Yi-Hsieng Samuel Wu, Yi-Ling Lin, Wen-Yuan Yang, Sheng-Yao Wang, Yi-Chen Chen Jun 2021

Pepsin-Digested Chicken-Liver Hydrolysate Attenuates Hepatosteatosis By Relieving Hepatic And Peripheral Insulin Resistance In Long-Term High-Fat Dietary Habit, Yi-Hsieng Samuel Wu, Yi-Ling Lin, Wen-Yuan Yang, Sheng-Yao Wang, Yi-Chen Chen

Journal of Food and Drug Analysis

This study aims to clarify the effects of chicken liver hydrolysates (CLHs) on long-term high-fat diet (HFD)-induced insulin resistance (IR) and hepatosteatosis in mice. In vitro, the 400 mM oleic acid (OA)-added medium successfully stimulated the cellular steatosis on FL83B cells, and the cellular steatosis was attenuated ( p < 0.05) by supplementing with CLHs (4 mg/L). In vivo, the effects of CLHs on IR and hepatosteatosis development were tested in 20-week HFD-fed mice. HFD-induced increases in final body weight, but body weight gains of mice were decreased ( p < 0.05) by supplementing CLHs. Elevated ( p < 0.05) serum aspartate aminotransferase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), free fatty acids (FFAs), triglyceride (TG), total cholesterol (TC), and fasted glucose values in HFD-fed mice decreased ( p < 0.05) by supplementing CLHs. Both results of hepatic steatosis and fibrotic scores also indicated the retardation ( p < 0.05) of the hepatosteatosis in cotreated groups. Moreover, the CLH supplementation sustained ( p < 0.05) hepatic and peripheral insulin signal sensitivity in HFD-fed mice. CLH supplementation could ameliorate hepatic lipid deposition, hepatic/peripheral IR in a long-term high-fat dietary habit, and also improve the universal glucose homeostasis by upregulating hepatic and peripheral insulin sensitivities.

Go to article

Adverse Effects On Birth Weight Of Parental Illegal Drug Use During Pregnancy And Within Two Years Before Pregnancy, Ching-Heng Lin, Wei-Szu Lin, I-An Wang, Jui Hsu, Shiow-Ing Wu, Chuan-Yu Chen Jun 2021

Adverse Effects On Birth Weight Of Parental Illegal Drug Use During Pregnancy And Within Two Years Before Pregnancy, Ching-Heng Lin, Wei-Szu Lin, I-An Wang, Jui Hsu, Shiow-Ing Wu, Chuan-Yu Chen

Journal of Food and Drug Analysis

This study investigates possible links between maternal illegal drug use during pregnancy and up to two years before pregnancy with birth weight (BW), and explores the potential role of paternal illegal drug use on low birth weight. A population-based retrospective cohort study was conducted that linked four national databases in Taiwan. A total of 1,698 subjects with a criminal record of schedule I or II illegal drug use within two years before pregnancy were enrolled as the drug-exposed group, and 16,980 matched subjects were enrolled as the unexposed group. Multivariate analysis of BW found a decrease of 108.63 g (95% …

Go to article

Simultaneously Qualitative And Quantitative Analysis Of The Representative Components In Kadsura Heteroclita Stem By Uhplc-Q-Orbitrap Hrms, Qian-Qian Liu, Bin Li, Kang Sun, Cai-Hong Li, Nuzhat Shehla, Yu-Pei Yang, Liang Cao, Wei Wang, Rong-Xia Liu Jun 2021

Simultaneously Qualitative And Quantitative Analysis Of The Representative Components In Kadsura Heteroclita Stem By Uhplc-Q-Orbitrap Hrms, Qian-Qian Liu, Bin Li, Kang Sun, Cai-Hong Li, Nuzhat Shehla, Yu-Pei Yang, Liang Cao, Wei Wang, Rong-Xia Liu

Journal of Food and Drug Analysis

Kadsura heteroclita (Roxb) Craib stem (KHS) is a medicinal plant used for the treatment of rheumatism arthritis diseases in Tujia ethnomedicine. Thus far, the complex chemical compositions in KHS are not clear, and the levels of the major compounds in KHS are not well understood. In this study, a novel UHPLC-Q-Orbitrap HRMS method was established for the simultaneous quali-quantitative analysis of KHS. A total of 204 compounds were identified, including triterpenoids, lignans, sesquiterpenes, fatty acids, phenolic acids, and flavonoids, more than 100 of which were first discovered in KHS. Using the same method, 12 representative bioactive components were successfully quantified. …

Go to article

Characterization Of L-Theanine In Tea Extracts And Synthetic Products Using Stable Isotope Ratio Analysis, Matteo Perini, Silvia Pianezze, Luca Ziller, Federica Camin Jun 2021

Characterization Of L-Theanine In Tea Extracts And Synthetic Products Using Stable Isotope Ratio Analysis, Matteo Perini, Silvia Pianezze, Luca Ziller, Federica Camin

Journal of Food and Drug Analysis

L-theanine involves a great number of health benefits and dietary supplements containing this molecule are becoming increasingly popular. There is, therefore, a growing need to find ways to discriminate between natural L-theanine extracted from tea leaves and the cheaper, synthetic one obtained using specific bacterial enzymes. A first attempt of stable isotope ratio analysis characterization of the possible synthetic adulterant L-theanine (δ13C of -14.3±1.5‰), obtained from vegetable substrates with C4 photosynthetic cycle, and of the more expensive natural L-theanine (δ13C of -24.4±1.3‰), extracted from Camellia sinensis plants with C3 photosynthetic cycle, is reported here .

Go to article

Development Of The Species-Specific Multiplex Pcr And Dna Sequencing Methods For Rapid Authentication Of Isatidis Folium And Its Adulterants, Yung-Chuan Hsieh, Ming-Sian Wu, Hui-Chun Lee, Chia-Yun Hsieh, Shih-Shan Huang, Chia-Fen Tsai, Ya-Tze Lin, Mei-Chih Lin, Su-Hsiang Tseng, Der-Yuan Wang Jun 2021

Development Of The Species-Specific Multiplex Pcr And Dna Sequencing Methods For Rapid Authentication Of Isatidis Folium And Its Adulterants, Yung-Chuan Hsieh, Ming-Sian Wu, Hui-Chun Lee, Chia-Yun Hsieh, Shih-Shan Huang, Chia-Fen Tsai, Ya-Tze Lin, Mei-Chih Lin, Su-Hsiang Tseng, Der-Yuan Wang

Journal of Food and Drug Analysis

Isatis indigotica Fort. (family Cruciferae), is an herb widely used in traditional herbal medicine and its dried leave was named “ISATIDIS FOLIUM”. Baphicacanthus cusia (Ness) Bremek. and Polygonum tinctorium Ait. are commonly misused as ISATIDIS FOLIUM in Chinese Medicine pharmacy. For the purpose of being not misused, specific primers based on the sequence difference of chloroplast trnH-psbA intergenic spacer were designed and Multiplex polymerase chain reaction method (Multiplex PCR) was developed. In this study, 29 original herbal materials were analyzed and our results show that DNA size after Multiplex PCR was able to distinguish variations between three herbs. DNA fragments …

Go to article

Rapid Determination Of Benzophenone Derivatives In Cereals Using Fapex Coupled With Ultra–High-Performance Liquid Chromatography–Tandem Mass Spectrometry, Yu-Fang Huang, Jui-Ting Chien, Hsin-Chang Chen, Xuan-Rui Liu, Jui-Pin Chang, Jun-Jie Huang Jun 2021

Rapid Determination Of Benzophenone Derivatives In Cereals Using Fapex Coupled With Ultra–High-Performance Liquid Chromatography–Tandem Mass Spectrometry, Yu-Fang Huang, Jui-Ting Chien, Hsin-Chang Chen, Xuan-Rui Liu, Jui-Pin Chang, Jun-Jie Huang

Journal of Food and Drug Analysis

A robust and sensitive analytical method was developed and validated for the simultaneous analysis of the levels of 10 benzophenone derivatives (BPs; BP, BP-1, BP-2, BP-3, BP-8, 2-hydroxybenzophenone [2-OHBP], 4-hydroxybenzophenone [4-OHBP], 4-methylbenzophenone [4-MBP], methyl-2-benzoylbenzoate [M2BB], and 4-benzoylbiphenyl [PBZ]) in 54 breakfast cereal samples. A fast pesticide extraction (FaPEx) technique coupled with isotope-labeled internal standards ultraehigh-performance liquid chromatographyetandem mass spectrometry was employed. The developed method exhibited satisfactory linearity (R2 > 0.998), high precision (intraday and interday relative standard deviations in the ranges of 1.4%e20.8% and 3.2%e23.9%, respectively), and a limit of detection ranging from 0.001 to 0.122 ng/g. BP and 4-MBP were …

Go to article

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 Jun 2021

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) …

Go to article

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 Jun 2021

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 …

Go to article

Determination Of Phytochemical Compounds In Chicken Breast By Gas Chromatography-Tandem Mass Spectrometry, Federico Cozzi, Irene Eder-Neuhauser, Klaus Teichmann, Mathias Zaunschirm Jun 2021

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 …

Go to article

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 Jun 2021

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 …

Go to article

Human Breast Milk-Based Nutritherapy: A Blueprint For Pediatric Healthcare, Pravin Shende, Bhakti Khanolkar Jun 2021

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 …

Go to article

Current And Potential Applications Of Simultaneous Dsc-Ftir Microspectroscopy For Pharmaceutical Analysis, Shan-Yang Lin Jun 2021

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 …

Go to article

Structural Recognition Of The Myc Promoter G-Quadruplex By A Quinoline Derivative: Insights Into Molecular Targeting Of Parallel G-Quadruplexes, Jonathan Dickerhoff, Jixun Dai, Danzhou Yang Jun 2021

Structural Recognition Of The Myc Promoter G-Quadruplex By A Quinoline Derivative: Insights Into Molecular Targeting Of Parallel G-Quadruplexes, Jonathan Dickerhoff, Jixun Dai, Danzhou Yang

Purdue University Libraries Open Access Publishing Fund

DNA G-Quadruplexes (G4s) formed in oncogene promoters regulate transcription. The oncogene MYC promoter G4 (MycG4) is the most prevalent G4 in human cancers. However, the most studied MycG4 sequence bears a mutated 3′-residue crucial for ligand recognition. Here, we report a new drug-like small molecule PEQ without a large aromatic moiety that specifically binds MycG4. We determined the NMR solution structures of the wild-type MycG4 and its 2:1 PEQ complex, as well as the structure of the 2:1 PEQ complex of the widely used mutant MycG4. Comparison of the two complex structures demonstrates specific molecular recognition of MycG4 and shows …

Go to article

Developmental Ethanol Exposure Causes Central Nervous System Dysfunction And May Slow The Aging Process In A Drosophila Model Of Fetal Alcohol Spectrum Disorder, Khaoula Belhorma, Nahed Darwish, Elizabeth Benn-Hirsch, Annalisa Duenas, Hillary Gates, Navneet Sanghera, Jodie Wu, Rachael L. French Jun 2021

Developmental Ethanol Exposure Causes Central Nervous System Dysfunction And May Slow The Aging Process In A Drosophila Model Of Fetal Alcohol Spectrum Disorder, Khaoula Belhorma, Nahed Darwish, Elizabeth Benn-Hirsch, Annalisa Duenas, Hillary Gates, Navneet Sanghera, Jodie Wu, Rachael L. French

Faculty Research, Scholarly, and Creative Activity

Alcohol is a known teratogen, and developmental exposure to ethanol results in fetal alcohol spectrum disorder (FASD). Children born with FASD can exhibit a range of symptoms including low birth weight, microcephaly, and neurobehavioral problems. Treatment of patients with FASD is estimated to cost 4 billion dollars per year in the United States alone, and 2 million dollars per affected individual's lifetime. We have established Drosophila melanogaster as a model organism for the study of FASD. Here we report that mutations in Dementin (Dmtn), the Drosophila ortholog of the Alzheimer's disease-associated protein TMCC2, convey sensitivity to developmental ethanol exposure, …

Go to article

Alzheimer’S Disease Drug Development Pipeline: 2021, Jeffrey Cummings, Garam Lee, Kate Zhong, Jorge Fonseca, Kazem Taghva May 2021

Alzheimer’S Disease Drug Development Pipeline: 2021, Jeffrey Cummings, Garam Lee, Kate Zhong, Jorge Fonseca, Kazem Taghva

Brain Health Faculty Research

Introduction The number of individuals worldwide with Alzheimer's disease (AD) is growing at a rapid rate. New treatments are urgently needed. We review the current pipeline of drugs in clinical trials for the treatment of AD. Methods We interrogated ClinicalTrials.gov, the federal registry of clinical trials to identify drugs in trials. Results There are 126 agents in 152 trials assessing new therapies for AD: 28 treatments in Phase 3 trials, 74 in Phase 2, and 24 in Phase 1. The majority of drugs in trials (82.5%) target the underlying biology of AD with the intent of disease modification; 10.3% are …

Go to article

Contemporary Brazilian Catholicism And Healing Practices: Notes On Environmentalism And Medicalization, Juliano F. Almeida May 2021

Contemporary Brazilian Catholicism And Healing Practices: Notes On Environmentalism And Medicalization, Juliano F. Almeida

Journal of Global Catholicism

Anthropological studies on Brazilian Catholicism traditionally focused on popular variants of this religious practice and their relationship with the official Catholicism. Encouraged by recent anthropological perspectives, which highlight the relevance of devoting researches not only on the margins, but also on the center of social practices, this paper analyzes contemporary practices of Brazilian Catholic friars and priests on health promotion. The analysis of their publications (books that include practices and tips on health and that became best sellers etc.), as well as interviews, allows us to perceive a process of environmentalization on the contemporary Brazilian Catholicism. This process seems to …

Go to article

Repurposing Potential Of Posaconazole And Grazoprevir As Inhibitors Of Sars-Cov-2 Helicase, Syed Hani Abidi, Nahlah Makki Almansour, Daulet Amerzhanov, Khaled S. Allemailem, Wardah Rafaqat, Mahmoud A A. Ibrahim, Philip La Fleur, Martin Lukac, Syed Ali May 2021

Repurposing Potential Of Posaconazole And Grazoprevir As Inhibitors Of Sars-Cov-2 Helicase, Syed Hani Abidi, Nahlah Makki Almansour, Daulet Amerzhanov, Khaled S. Allemailem, Wardah Rafaqat, Mahmoud A A. Ibrahim, Philip La Fleur, Martin Lukac, Syed Ali

Department of Biological & Biomedical Sciences

As the Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) pandemic engulfs millions worldwide, the quest for vaccines or drugs against the virus continues. The helicase protein of SARS-CoV-2 represents an attractive target for drug discovery since inhibition of helicase activity can suppress viral replication. Using in silico approaches, we have identified drugs that interact with SARS-CoV-2 helicase based on the presence of amino acid arrangements matching binding sites of drugs in previously annotated protein structures. The drugs exhibiting an RMSD of ≤ 3.0 Å were further analyzed using molecular docking, molecular dynamics (MD) simulation, and post-MD analyses. Using these approaches, we …

Go to article

Development Of Long-Acting Antiviral Drug Nanoformulations, Denise Cobb May 2021

Development Of Long-Acting Antiviral Drug Nanoformulations, Denise Cobb

Theses & Dissertations

Antiretroviral therapy (ART) has improved the quality and duration of life for people living with human immunodeficiency virus (HIV) infection. However, opportunities to improve its profile abound. ART is limited by putative viral reservoir penetrance, emergence of viral mutations, inherent toxicities, and regimen non-adherence. These highlight the need improved drug delivery schemes. Previously, our lab has demonstrated that targeting mononuclear phagocytes for antiretroviral drug delivery extends drug half-life and improves penetrance into viral reservoirs, addressing these limitations of ART. Herein, we developed synthetic and biologic antiretroviral (ARV) drug nanocarriers improve the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of ARVs through …

Go to article

Stress, Alcohol Use, And Punitive Parenting During The Covid-19 Pandemic, Jennifer Price Wolf, Bridget Freisthler, Caileigh Chadwick May 2021

Stress, Alcohol Use, And Punitive Parenting During The Covid-19 Pandemic, Jennifer Price Wolf, Bridget Freisthler, Caileigh Chadwick

Faculty Research, Scholarly, and Creative Activity

Background
Emerging research suggests that parents are experiencing heightened stress during the COVID-19 pandemic. Parental stress is a risk factor for harsh or punitive parenting, and this association may be exacerbated by the use of alcohol.
Objective
We examine whether parental stress is associated with use of punitive parenting, as well as whether this association is modified by drinking pattern.
Participants & setting
We used advertisements and word-of-mouth to recruit 342 parents living in Central Ohio during the initial stay-at-home order for COVID-19.
Methods
We used geographic ecological momentary assessment (gEMA) to measure parental stress and punitive parenting during three …

Go to article

Glycosylation Of Immune Receptors In Cancer, Ruoxuan Sun, Alyssa Min Jung Kim, Seung-Oe Lim May 2021

Glycosylation Of Immune Receptors In Cancer, Ruoxuan Sun, Alyssa Min Jung Kim, Seung-Oe Lim

Purdue University Libraries Open Access Publishing Fund

Evading host immune surveillance is one of the hallmarks of cancer. Immune checkpoint therapy, which aims to eliminate cancer progression by reprogramming the antitumor immune response, currently occupies a solid position in the rapidly expanding arsenal of cancer therapy. As most immune checkpoints are membrane glycoproteins, mounting attention is drawn to asking how protein glycosylation affects immune function. The answers to this fundamental question will stimulate the rational development of future cancer diagnostics and therapeutic strategies.

Go to article

Pathogenesis Of Dry Eye In Graft Versus Host Disease (Gvhd): Role Of Ocular Mucins And Conjunctival Fibrosis, Kiumars Shamloo May 2021

Pathogenesis Of Dry Eye In Graft Versus Host Disease (Gvhd): Role Of Ocular Mucins And Conjunctival Fibrosis, Kiumars Shamloo

Pharmaceutical Sciences (PhD) Dissertations

Allogenic hematopoietic stem cell transplantation is a procedure that offers a possible cure for hematologic cancers and other hematologic disorders. Unfortunately, despite the increasing survival rate of patients, the quality of their life is adversely affected by the allogeneic bone marrow transplantation’s major side effect i.e Graft vs. Host Disease (GVHD). GVHD is a complex, multi-organ disease resulting from an immunological attack by donor engrafted immune cells to host organs, including the eye surface. Mostly based on the time of disease onset after transplantation, GVHD is divided into the acute and chronic phase. The eyes may be involved in both …

Go to article

First Prev Next Last