Pharmacology Commons^™

Analysis And Identification Of Phenolic Compounds With Antiproliferative Activity From Chinese Olive (Canarium Album L.) Fruit Extract By Hplc-Dad-Spe-Tt-Nmr, Yu-Te Yeh, Chien-Kuang Chen, Yi-Chun Liao, Shoei-Sheng Lee, Shu-Chen Hsieh

Journal of Food and Drug Analysis

Chinese olives (Canarium album L.) are rich in phenolic compounds, exhibiting a broad spectrum of potential clinical applications. This study is the first report on the isolation and elucidation of bioactive compounds with high antiproliferative activity from the ethyl acetate fraction of a Chinese olive fruit methanolic extract (CO-EtOAc). We used the WST-1 assay to determine which subfractions of CO-EtOAc had significant antiproliferative activity using the murine colon cancer cell line CT26. Subsequently, the functional compounds were characterized by the hyphenated technique and high-performance liquid chromatography-diode array detector-solid phase extraction-transfer tube-nuclear magnetic resonance (HPLC-DAD-SPE-TT-NMR). Thirteen phenolic constituents were identified …

Glycine-Rich Peptides From Fermented Chenopodium Formosanum Sprout As An Antioxidant To Modulate The Oxidative Stress, Chen-Che Hsieh, Shu-Han Yu, Hsing-Chun Kuo, Darin Khumsupan, Hsiao-Chu Huang, Yu-Wei Liou, Chen-Yu Kao, Szu-Chuan Shen, Kuan-Chen Cheng

Journal of Food and Drug Analysis

Rhizopus oligosporus was utilized in the solid-state fermentation of Chenopodium formosanum sprouts (FCS) in a bioreactor. Subsequently, the antioxidant activity of food proteins derived from FCS was investigated. Results showed that glycine-rich peptide (GGGGGKP, G-rich peptide), identified from the < 2 kDa FCS proteins, had antioxidant values. According to SwissADME, AllerTOP, ToxinPred, and BIOPEP-UWM analyses, G-rich peptide was identified as safe, non-toxic, and non-allergenic. Afterward, the peptide was examined using in silico and in vitro studies to evaluate its potential alleviating oxidative stress caused by particulate matter. This study proposed plausible mechanisms that involve the binding of G-rich peptide which inhibited phosphorylation of the v-rel avian reticuloendotheliosis viral oncogene homolog A (RELA) subunit on NF-κB pathway. The inhibition then resulted in down regulation of NF-κB transcription and genetic expression of inflammatory …

Investigation Of Microwave Extraction Of Red Cabbage And Its Neurotherapeutic Potential, Halil Koyu, Serdar Demir, Mehmet Zeki Haznedaroglu

Journal of Food and Drug Analysis

In the pursuit of bioactive compounds with health benefits from food and medicinal plants, optimization of process to reduce solvent, raw material, energy and time consumption has been a valuable research objective. Sustainable management and efficient use of natural resources are of critical importance for sustainability goals. In this manner, microwave extraction of red cabbage which has been a mass cultivated plant for food purposes, was optimized for maximizing acetylcholinesterase, butyrylcholinesterase, tyrosinase inhibitory activity and bioactive content. Quantitative analysis of total phenol, flavonoid and anthocyanin content were performed using spectrophotometry and UPLC-DAD-ESI-MS/MS. Optimum conditions were determined as 600 W, 100% …

Abundance Of Prevotella Copri In Gut Microbiota Is Inversely Related To A Healthy Diet In Patients With Type 2 Diabetes, Chih-Yiu Tsai, Po-Yu Liu, Meng-Chuan Huang, Chiao-I Chang, Hsin-Yun Chen, Yu-Hsien Chou, Chi-Neu Tsai, Chia-Hung Lin

Journal of Food and Drug Analysis

While the gut microbiota is known to be influenced by habitual food intake, this relationship is seldom explored in type 2 diabetes patients. This study aims to investigate the relationship between dietary patterns and gut microbial species abundance in 113 type 2 diabetes patients (mean age, 58 years; body mass index, 29.1; glycohemoglobin [HbA1c], 8.1%). We analyzed the gut microbiota using 16S amplicon sequencing, and all patients were catogorized into either the Bacteroides enterotype (57.5%, n = 65) or the Prevotella enterotype (42.5%, n = 48) using the partitioning around medoids clustering algorithm, based on the most representative genera. Patients …

Therapeutic Effects Of Orally Administration Of Viable And Inactivated Probiotic Strains Against Murine Urinary Tract Infection, Vo Thi Hong Van, Zhen-Shu Liu, Yueh Jen Hsieh, Wei-Chen Shiu, Bo-Yuan Chen, Yu-We Ku, Po-Wen Chen

Journal of Food and Drug Analysis

Urinary tract infections (UTIs) are highly prevalent bacterial infections that pose significant health risks. Specific probiotic strains have been recommended for UTI control and management of antibiotic resistance. Otherwise, paraprobiotics, defined as inactivated probiotic cells, offer potential advantages by minimizing risks associated with live microorganisms. However, the effectiveness of heat-killed probiotic strains against UTIs remains uncertain. Additionally, lactoferrin (LF), an iron-binding glycoprotein, exhibits immunomodulatory, antimicrobial, and anti-inflammatory properties. Recently, we had developed recombinant LF-expression probiotics, which can display considerate antibacterial activities against select food-borne pathogens in vitro. Thus, the present study aimed to evaluate the antibacterial activities of heat-killed natural …

Recent Advances In Combined Avant-Garde Technologies (Thermal-Thermal, Non-Thermal-Non-Thermal, And Thermal-Non-Thermal Matrix) To Extract Polyphenols From Agro Byproducts, Isaac Duah Boateng

Journal of Food and Drug Analysis

Because food byproducts (waste) are rich in phytoconstituents, valorizing them is crucial for global food security. However, conventional extraction (CE), including decoction, maceration, Soxhlet, etc., for agro byproducts’ polyphenol extraction are time-consuming and rely significantly on vast volumes of potentially aggressive solvents. Hence, Avant-garde extraction technologies, including non-thermal (high hydrostatic pressure (HHPE), pulsed-electric field (PEF), high voltage electrical discharges (HVED), etc.) and thermal extraction (supercritical fluid (SCF), subcritical water extraction (SWE), microwave-assisted extraction (MAE), etc.), as well as their thermal combinations (SCF-PLE, SCCO2-SWE, SCCO2-MAE, etc.), non-thermal combinations (HHPE+UAE, PEF+UAE, HVED+UAE, etc.) and combined thermal-non-thermal (MAE-UAE, etc.) are increasingly replacing CE. …

Delta-9-Tetrahydrocannabinol And Cannabidiol Effect On Dopamine Transporter Expression And Function, Delia M. Guzman

Student Theses

Drug addiction is a major endemic crisis in the United States with a higher prevalence than any other country. Marijuana and hallucinogens make up a great percentage of the drugs of abuse in Americans ranging from 15 to 64 years old. Marijuana contains over 500 active compounds that contribute to its effects, the major components being delta-9-tetrahydrocannabinol (Δ-9-THC) and cannabidiol (CBD). Understanding the pharmacological mechanism as well as the effects that they elicit through the dopaminergic reward system is a key factor in being able to understand why addiction is so prevalent in our society. This research was aimed to …

Kinome Profiling Identifies Mark3 And Stk10 As Potential Therapeutic Targets In Uveal Melanoma, Usman Baqai, Alison M. Kurimchak, Isabella Trachtenberg, Timothy J. Purwin, Jelan I. Haj, Anna Han, Kristine Luo, Nikole Fandino Pachon, Angela Jeon, Vivian Chua, Michael A. Davies, J Silvio Gutkind, Jeffrey L. Benovic, James S. Duncan, Andrew E. Aplin

Department of Pharmacology, Physiology, and Cancer Biology Faculty Papers

Most uveal melanoma cases harbor activating mutations in either GNAQ or GNA11. Despite activation of the mitogen-activated protein kinase (MAPK) signaling pathway downstream of Gαq/11, there are no effective targeted kinase therapies for metastatic uveal melanoma. The human genome encodes numerous understudied kinases, also called the "dark kinome". Identifying additional kinases regulated by Gαq/11 may uncover novel therapeutic targets for uveal melanoma. In this study, we treated GNAQ-mutant uveal melanoma cell lines with a Gαq/11 inhibitor, YM-254890, and conducted a kinase signaling proteomic screen using multiplexed-kinase inhibitors followed by mass spectrometry. We observed downregulated expression and/or activity of 22 kinases. …

Cognitive Task Analysis Of Clinicians’ Drug–Drug Interaction Management During Patient Care And Implications For Alert Design, Alissa L. Russ-Jara, Nervana Elkhadragy, Karen J. Arthur, Julie B. Dilulio, Laura G. Militello, Amanda P. Ifeachor, Peter A. Glassman, Alan J. Zillich, Michael Weiner

Purdue University Libraries Open Access Publishing Fund

Background Drug–drug interactions (DDIs) are common and can result in patient harm. Electronic health records warn clinicians about DDIs via alerts, but the clinical decision support they provide is inadequate. Little is known about clinicians’ real-world DDI decision-making process to inform more effective alerts.

Objective Apply cognitive task analysis techniques to determine informational cues used by clinicians to manage DDIs and identify opportunities to improve alerts.

Design Clinicians submitted incident forms involving DDIs, which were eligible for inclusion if there was potential for serious patient harm. For selected incidents, we met with the clinician for a 60 min interview. Each …

Chemical Composition, Mineral Profile, Anti-Bacterial, And Wound Healing Properties Of Snail Slime Of Helix Aspersa Müller, Marouane Aouji, Amine Rkhaila, Bouchra Bouhaddioui, Malak Zirari, Hala Harifi, Youness Taboz, Lalla Aicha Lrhorfi, Rachid Bengueddour

BioMedicine

Mucus is a substance made by snails that serves a variety of purposes and is increasingly employed in the medical and cosmetic industries. It includes bioactive compounds with a range of biological characteristics that could be useful in the treatment of particular issues. This study assessed the wound-healing efficiency, antibacterial activity, chemical and mineral composition of Helix aspersa Müller slime. Inductively Coupled Argon Plasma Atomic Emission Spectrometry (ICP-OES) was used for mineral analysis, while Gas chromatography coupled to mass spectrometry (GC-MS) analysis was used for chemical characterization. The findings showed that the H. aspersa Müller slime had inhibitory activity on …

Elucidation Of Molecular Mechanisms Underlying Novel Multi-Targeted Therapy Strategies For, Qianqian Hu

USF Tampa Graduate Theses and Dissertations

EML4-ALK fusion non-small cell lung cancer (NSCLC) represents a distinct subset of lung cancers that possesses unique molecular and clinical features, paving the way for targeted therapeutic interventions. Despite the promise of ALK-directed therapies, challenges such as metastasis at the time of diagnosis and treatment resistance persist, necessitating deeper research into the underlying mechanisms and potential solutions. In the context of these challenges, our study embarked on two specific objectives. The first goal, elucidated in Chapter 2, revolved around brain metastasis, an event critically facilitated by cell migration. Here, we assessed the anti-migratory activities of several clinical ALK inhibitors in …

Enteroendocrine Cell Regulation Of The Gut-Brain Axis, Joshua Barton, Annie Londregan, Tyler Alexander, Ariana Entezari, Manuel Covarrubias, Scott Waldman

Department of Pharmacology, Physiology, and Cancer Biology Faculty Papers

Enteroendocrine cells (EECs) are an essential interface between the gut and brain that communicate signals about nutrients, pain, and even information from our microbiome. EECs are hormone-producing cells expressed throughout the gastrointestinal epithelium and have been leveraged by pharmaceuticals like semaglutide (Ozempic, Wegovy), terzepatide (Mounjaro), and retatrutide (Phase 2) for diabetes and weight control, and linaclotide (Linzess) to treat irritable bowel syndrome (IBS) and visceral pain. This review focuses on role of intestinal EECs to communicate signals from the gut lumen to the brain. Canonically, EECs communicate information about the intestinal environment through a variety of hormones, dividing EECs into …

Assessing The Potentiation Of The (Alpha4)3(Beta2)2 Nicotinic Acetylcholine Receptor By Analogs Of The Allosteric Agonist Cmpi, Josue Gaona, Marcos Bermudez, Wilder Felix, Amaya Rolling, Ganesh Thakur, Ayman K. Hamouda

School of Medicine Student Publications and Presentations

The (α4)3(β2)2 nicotinic acetylcholine receptor (nAChR) is the major heteromeric nAChR isoform expressed in the cortex and is believed to play a role in memory, cognition, and neuronal survival during aging. As such, selective potentiators of the (α4)3(β2)2 nAChR have potential therapeutic benefits in conditions associated with decline in the output of nAChR in the brain. In previous work, we have studied the pharmacology of the allosteric agonist CMPI (3-(2-chlorophenyl)-5-(5-methyl-1-(piperidin-4-yl)- 1H-pyrazol-4-yl) isoxazole) at the (α4)3(β2)2 nAChR and identified its binding site at the α4:α4 subunit extracellular interface. As part of our ongoing efforts to define structural features that confer CMPI …

Synthetic Contraceptive Hormones Occlude The Ability Of Nicotine To Reduce Ethanol Consumption In Ovary-Intact Female Rats, Erin E. Maher, Ashley M. White, Ashley Craig, Shailesh N. Khatri, Percell T. Kendrick Jr., Mary E. Matocha, Emma O. Bondy, Nikhil Pallem, Grace W. Breakfield, Madison Botkins, Olivia Sweatt, William C. Griffin, Brent A. Kaplan, Jessica Jane Weafer, Joshua S. Beckmann, Cassandra D. Gipson

Markey Cancer Center Faculty Publications

Rates of tobacco and alcohol use in women are rising, and women are more vulnerable than men to escalating tobacco and alcohol use. Many women use hormonal birth control, with the oral contraceptive pill being the most prevalent. Oral contraceptives contain both a progestin (synthetic progesterone) and a synthetic estrogen (ethinyl estradiol; EE) and are contraindicated for women over 35 years who smoke. Despite this, no studies have examined how synthetic contraceptive hormones impact this pattern of polysubstance use in females. To address this critical gap in the field, we treated ovary-intact female rats with either sesame oil (vehicle), the …

Antidiabetic Potential Of Vitex Mombassae Fruits Extract In Streptozotocin-Nicotinamide Induced Diabetic Wistar Rat Model, Mussa B. Mbegeze, Joan J.E. Munissi, Flora Stephano, Ramadhani S.O. Nondo, Stephen S. Nyandoro

Tanzania Journal of Science

Besides changes in life styles and improper dietary patterns, the rapidly increasing burden of diabetes mellitus type 2 is correlated with antidiabetic agents currently in clinical use, which are costly, less effective, and present undesirable side effects. Natural products from plants are promising alternative sources for developing more effective and cost friendly antidiabetic agents. This study therefore investigated the antidiabetic potential of Vitex mombassae fruits extract (VMFE) in streptozotocin-nicotinamide induced diabetic Wistar rat model. Oral acute toxicity test was conducted in male Wistar rat using up and down method by following OECD Guideline 423 (2002). No clinical signs of toxicity …

Anticancer Potential Of The Leaf Extracts From The Selected Croton Species, Peter V. Fayyu, Joan J.E. Munissi, Stephen S. Nyandoro, Flora Stephano

Tanzania Journal of Science

The reported investigations were aimed at establishing anticancer potential of the leaf extracts from Croton dictyophlebodes (CDE), C. kilwae (CKE) and C. longipedicellatus ssp austrotanzanicus (CLE). In vitro cytotoxicity assays of the extracts were performed against human laryngeal cancer cell line (HEp-2) and human breast cancer cell line (MCF-7), while in vivo toxicological studies were done using Swiss albino mice (Mus musculus) following the Organization for Economic Cooperation and Development guideline number 423 of 2001. Results for in vitro assays revealed that CDE and CLE induced cytotoxicity to MCF-7 and HEp-2 cell lines at EC50 values of 86 and 63 …

Neuroendocrine Regulation Of Chemokine Receptor-Mediated Leukocyte Migration Via Heteromeric G Protein-Coupled Receptor Complexes, Garrett Enten

USF Tampa Graduate Theses and Dissertations

Neuroendocrine regulation of the innate immune system is a well-documentedphenomenon. The underlying mechanisms, however, are not well understood. Here we show that at least 20 members of the human chemokine receptor (CR) family heteromerize with one or more members of the α1-adrenergic receptor (AR) family and that all CRs, apart from CXCR1, heteromerize with arginine vasopressin receptor 1A (AVPR1A) in recombinant systems. These heteromeric complexes are detectable in human monocytes and the monocytic leukemia cell line THP-1. Though currently technical limitations prevent the direct visualization of endogenously expressed higher-order hetero-oligomeric receptor complexes, we provide evidence through functional analysis and proximity-based …

Ethnobotanical Survey On The Knowledge And Use Of Medicinal Plants For Malaria Management Among University Students, Felista W. Mwingira, Deokary J. Matiya, Neema G. Mogha

Tanzania Journal of Science

Malaria remains a public health problem in Tanzania, escalated by the emergence of both parasite and vector resistance. Plant-based traditional medicines have been widely utilized as alternatives to malaria management. However, proper documentation is minimal, especially among the younger generation. This study assessed the knowledge of medicinal plants for malaria management among 532 Dar es Salaam University College of Education students. Overall, twenty-four plant species, most belonging to the family Asteraceae, were identified with Azaradichta indica being the most dominant species. These results reveal a substantial knowledge of medicinal plants for malaria management among university students.

Piperine Encourages Apoptosis In Human Cervical Adenocarcinoma Cells Through Ros Generation, Dna Fragmentation, Caspase-3 Activation And Cell Cycle Arrest, Asif Jafri, Juhi Rais, Sudhir Kumar, Md Arshad

Research Symposium

Background: Cancer is one of the most common destructive diseases and the second leading cause of death in humans. Among cancer, cervical cancer is the second most common malignancy among women globally. Thus, there is a continuous need to search for chemotherapeutic chemicals or naturally occurring drugs to resolve this global health problem. Piperine (1-piperoylpeperdine) is present in the fruits of black pepper (Piper nigrum Linn.) and long pepper (Piper longum Linn.). It possesses several pharmacological properties and in the present study we have evaluated its anti-cancer potential on human cervical adenocarcinoma (HeLa) cells.

Methods: The anti-proliferative effect …

Adipocyte-Derived Pxr Signaling Is Dispensable For Diet-Induced Obesity And Metabolic Disorders In Mices, Fang Wang, Jinwei Liu, Rebecca Hernandez, Se-Hyung Park, Ying-Jing Lai, Shuxia Wang, Bruce Blumberg, Changcheng Zhou

UK CARES Faculty Publications

Pregnane X receptor (PXR) is a xenobiotic receptor that can be activated by numerous chemicals including endogenous hormones, dietary steroids, pharmaceutical agents, and environmental chemicals. PXR has been established to function as a xenobiotic sensor to coordinately regulate xenobiotic metabolism by regulating the expression of many enzymes and transporters required for xenobiotic metabolism. Recent studies have implicated a potentially important role for PXR in obesity and metabolic disease beyond xenobiotic metabolism, but how PXR action in different tissues or cell types contributes to obesity and metabolic disorders remains elusive. To investigate the role of adipocyte PXR in obesity, we generated …