Pharmacology Commons^™

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 …

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 …

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, …

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 …

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 …

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 …

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 …

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 …

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.

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 …

Opioid And Naloxone Training In A Rural School District, Allyson C. Waldron

UNLV Theses, Dissertations, Professional Papers, and Capstones

The opioid epidemic is a national health emergency in the United States, with over 128 people dying each day due to an opioid overdose. It is estimated that 4.3 million people over the age of 12 use opioids without a medical need, and 1.3 million youth ages 12-17 use opioids inappropriately. Drug overdose deaths have become the leading cause of accidental death in the United States, prompting the U.S. Surgeon General and the World Health Organization to advise that more Americans have access to naloxone and understand how to use this life-saving drug correctly. Naloxone is an opioid antagonist, used …

Evaluation Of Α-Pyrrolidindovalerophenone (Α-Pvp) And Its Isomers In Male And Female Sprague-Dawley Rats Trained To Discriminate Mdpv, Kaley Cargile

Masters Theses

Recreational use of synthetic cathinones, 3,4-methylenedioxypyrovalerone (MDPV) and α‐pyrrolidinovalerophenone (α‐PVP), has become increasingly popular, thus prompting characterization of their behavioral and neurochemical effects. MDPV has been studied for several years now, though there is still much unknown about α‐PVP, and its isomers. The primary objective of this study was to characterize the discriminative effects of α‐PVP and its isomers in comparison to MDPV. Male and female Sprague-Dawley rats were trained to discriminate 0.5mg/kg MDPV from saline injections under a fixed ratio 20 (FR 20) schedule of food reinforcement. Substitution tests were conducted with MDPV (0.05-0.5mg/kg), α‐PVP (0.05-0.5mg/kg), (S)-α‐PVP (0.05-1mg/kg) and …

Importance Of Understanding Genetic Predisposition, Andrew Carter

Thinking Matters Symposium

Hypersensitivity reactions can be sudden and are often fatal. Many of these reactions occur as a result of allergies to prescribed medication. Adverse drug reactions or (ADR’s) were show in a recent study to affect over 6% of hospitalized patients and resulted in over 100,000 deaths a year in the US alone. This poster will review the importance of understanding genetic predisposition, through articles about possible genetic causes of allergies to penicillin and other beta-lactams. Changes in a specific HLA gene located on chromosome 6 showed a correlation to penicillin reactions in over 600,000 participants. Another study found a conclusive …

Oxidative Potential And Composition Of Fine Particulate Matter At Two Locations In Mississippi, Victoria Claire Stevens

Honors Theses

Air pollution exposure has negative health effects on individuals across the globe. Negative impacts on human health have been documented in studies following both short-term and long-term exposure to air pollution, and these adverse effects have been seen even at the lowest levels of exposure. Fine particulate matter (PM_2.5) has specifically been linked to these negative health effects. These effects come from many sources, but one large contribution to the negative health effects comes from oxidative stress. In this study, samples were collected from Hernando, MS and Gulfport, MS in September 2013 and November 2013. Black carbon (BC) …

Galectin-3 Mediated Inflammatory Response Contributes To Neurological Recovery By Qishenyiqi In Subacute Stroke Model, Yule Wang, Shuang He, Xinyan Liu, Zhixiong Li, Lin Zhu, Guangxu Xiao, Xiaoli Du, Hongxia Du, Wen Zhang, Yiqian Zhang, John Orgah, Benjamin Feng, Boli Zhang, Yan Zhu

Peer Reviewed Articles

Effective therapies for stroke are still limited due to its complex pathological manifestations. QiShenYiQi (QSYQ), a component-based Chinese medicine capable of reducing organ injury caused by ischemia/reperfusion, may offer an alternative option for stroke treatment and post-stroke recovery. Recently, we reported a beneficial effect of QSYQ for acute stroke via modulation of the neuroinflammatory response. However, if QSYQ plays a role in subacute stroke remains unknown. The pharmacological action of QSYQ was investigated in experimental stroke rats which underwent 90 min ischemia and 8 days reperfusion in this study. Neurological and locomotive deficits, cerebral infarction, brain edema, and BBB integrity …

Bibliometric Analysis Of Pakistan Journal Of Pharmaceutical Sciences From 2005 To 2020, Waseem Hassan

Library Philosophy and Practice (e-journal)

Background:

The major aim of this study is to evaluate the research productivity of Pakistan Journal of Pharmaceutical Sciences (PJPS) from 2005 to 2020. For the purpose, bibliometric analysis was performed.

Methodology:

From March to April 2021, the data was retrieved from Scopus, one of the largest databases in the world. journal. Later it was analyzed by MS Excel. Based on the Scopus database, this is the 1^st bibliometric report about PJPS.

Results:

From 2005 to 2020, PJPS published 3301 articles. The per year publication and citation details are provided. In all publications (n=3301), 8066 authors, 6018 institutes or …

Paeoniflorin And Hydroxysafflor Yellow A In Xuebijing Injection Attenuate Sepsis-Induced Cardiac Dysfunction And Inhibit Proinflammatory Cytokine Production, Xin-Tong Wang, Zhen Peng, Ying-Ying An, Ting Shang, Guangxu Xiao, Shuang He, Xi Chen, Hang Zhang, Tao Wang, Jun-Hua Zhang, Xiumei Gao, Yan Zhu, Benjamin Feng

Peer Reviewed Articles

Sepsis-induced myocardial dysfunction is a major contributor to the poor outcomes of septic shock. As an add-on with conventional sepsis management for over 15 years, the effect of Xuebijing injection (XBJ) on the sepsis-induced myocardial dysfunction was not well understood. The material basis of Xuebijing injection (XBJ) in managing infections and infection-related complications remains to be defined. A murine cecal ligation and puncture (CLP) model and cardiomyocytes in vitro culture were adopted to study the influence of XBJ on infection-induced cardiac dysfunction. XBJ significantly improved the survival of septic-mice and rescued cardiac dysfunction in vivo. RNA-seq revealed XBJ attenuated …

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 …

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. …

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 …

Suitability Of Sugar Alcohols As Antidiabetic Supplements: A Review, Nontokozo Z. Msomi, Ochuko L. Erukainure, Md. Shahidul Islam

Journal of Food and Drug Analysis

The major goals in the management of diabetes are to maintain normal control of glucose metabolism and glycemia. Dietary modification is one of the most recommended treatment modalities for diabetic patients. The use of foods sweetened with sugar alcohols (also known as polyols) such as xylitol, sorbitol, mannitol, maltitol, lactitol, isomalt and erythritol, has brought an escalating interest. Since some sugar alcohols do not raise plasma glucose, as they are partially digested and metabolised. Diet composition and adequacy may be altered by replacing carbohydrates with sugar alcohols. It has been established that these polyols are appropriate sugar substitutes for a …

Mapping Km Methods And Tools Across The Pharmaceutical Product Lifecycle, Martin Lipa, Paige Kane

Level 3

Knowledge management is positioned as an enabler of ICH Q10, and the visibility and availability of product and process knowledge across the entire pharmaceutical product lifecycle is vital to the sustained success of an organization and to the effectiveness of an organization’s pharmaceutical quality system as defined by ICH Q10. This paper illustrates where knowledge management has a role to play within each product lifecycle phase. This paper goes on to further define phase-appropriate KM methods and tools to help address these needs and create end-to-end product and process knowledge visibility and availability.

Protecting Intestinal Microenvironment Alleviates Acute Graft-Versus-Host Disease, Zhengcan Zhou, Ting Shang, Xiurong Li, Hongyan Zhu, Yu-Bo Qi, Xin Zhao, Xi Chen, Zhe-Xin Shi, Guixiang Pan, Yue-Fei Wang, Guanwei Fan, Xiumei Gao, Yan Zhu, Benjamin Feng

Peer Reviewed Articles

Acute gut graft-versus-host disease (aGVHD) is a leading threat to the survival of allogeneic hematopoietic stem cell transplantation (allo-HSCT) recipients. Abnormal gut microbiota is correlated with poor prognosis in allo-HSCT recipients. A disrupted intestinal microenvironment exacerbates dysbiosis in GVHD patients. We hypothesized that maintaining the integrity of the intestinal barrier may protect gut microbiota and attenuate aGVHD. This hypothesis was tested in a murine aGVHD model and an in vitro intestinal epithelial culture. Millipore cytokine array was utilized to determine the expression of proinflammatory cytokines in the serum. The 16S rRNA sequencing was used to determine the abundance and diversity …

Inhibition Of Biofilm Formation By The Synergistic Action Of Egcg-S And Antibiotics, Shrameeta Shinde, Lee Lee, Tinchun Chu

Department of Biology Faculty Scholarship and Creative Works

Biofilm, a stress-induced physiological state, is an established means of antimicrobial tolerance. A perpetual increase in multidrug resistant (MDR) infections associated with high mortality and morbidity have been observed in healthcare settings. Multiple studies have indicated that the use of natural products can prevent bacterial growth. Recent studies in the field have identified that epigallocatechin gallate (EGCG), a green tea polyphenol, could disrupt bacterial biofilms. A modified lipid-soluble EGCG, epigallocatechin-3-gallate-stearate (EGCG-S), has enhanced the beneficial properties of green tea. This study focuses on utilizing EGCG-S as a novel synergistic agent with antibiotics to prevent or control biofilm. Different formulations of …

Synthesis Of New Anilinoquinazoline Derivatives As Potential Anticancer Agents: Antiproliferative Activity, Molecular Docking And Molecular Dynamics Studies, Muhammad Kumayl Abdul Wahab

Student Works (2020-2029)

Current reversible epidermal growth factor (EGFR) tyrosine kinase inhibitors of the non-small cell lung cancer (NSCLC) have been resisted by T790M mutation, while irreversible inhibitors introduced to overcome the mutation have faced resistance from C797S mutation. In the effort to discover potential reversible EGFR inhibitors, two series of anilinoquinazoline derivatives were synthesized and characterized, studied for their in vitro antiproliferative activity against NSCLC cell lines, namely A549, H1650 and H1975, and studied for the plausible binding mode in epidermal growth factor receptor kinases with different mutations through molecular docking. In the first series, the anilinoquinazoline scaffold was derivatized through the …