Pharmacology Commons^™

How To Deal With Frenemy Nrf2: Targeting Nrf2 For Chemoprevention And Cancer Therapy, Ya-Chu Tang, Yung-Jen Chuang, Hsin-Huei Chang, Shin-Hun Juang, Gow-Chin Yen, Jang-Yang Chang, Ching-Chuan Kuo

Journal of Food and Drug Analysis

Induction of antioxidant proteins and phase 2 detoxifying enzymes that neutralize reactive electrophiles are important mechanisms for protection against carcinogenesis. Normal cells provide multifaceted pathways to tightly control NF-E2- related factor 2 (NRF2)-mediated gene expression in response to an assault by a range of endogenous and exogenous oncogenic molecules. Transient activation of NRF2 by its activators is able to induce ARE-mediated cytoprotective proteins which are essential for protection against various toxic and oxidative damages, and NRF2 activators thereby have efficacy in cancer chemoprevention. Because NRF2 has a cytoprotective function, it can protect normal cells from carcinogens like an angel, but …

Effects Of Green Tea–Derived Natural Products On Resistance Exercise Training In Sarcopenia: A Retrospective Narrative Mini-Review, Hung-Wen Liu, Sue-Joan Chang

Journal of Food and Drug Analysis

Skeletal muscle function deficits result in metabolic disease development and physical dysfunction in older adults. Sarcopenia is characterized by a decrease in muscle mass and strength with advancing age, and it increases the risks of mobility impairments, disease development, and mortality. Lifestyle interventions involving a combination of diet and exercise to prevent and attenuate sarcopenia warrant substantial research attention. Resistance exercise training under supervision is a safe and the most effective approach to reducing age-related muscle loss and improving multiple aspects of overall health in the older population. The beneficial effects of resistance exercise training on skeletal muscle mass may …

Development Of Telodendrimer Nanocarriers For Daptomycin Delivery, Hao Yue

Theses - ALL

The immune system plays a crucial role in fighting pathogens, but infections can occur if the immune system is unable to overcome them, leading to severe damage and death. Antibiotics and drug delivery techniques have helped save countless lives and improve the quality of life for patients. Daptomycin (Dap) is a powerful antibiotic used to treat gram-positive bacterial infections. However, its hydrophobic nature limits its effectiveness, and it requires the presence of calcium ions (Ca2+) for activation. In this study, a series of telodendrimer (TD) nanoparticle delivery systems were synthesized to improve daptomycin delivery. The TD nanoparticle systems showed effective …

Development Of Telodendrimer Nanocarriers For Daptomycin Delivery, Hao Yue

Theses - ALL

The immune system plays a crucial role in fighting pathogens, but infections can occur if the immune system is unable to overcome them, leading to severe damage and death. Antibiotics and drug delivery techniques have helped save countless lives and improve the quality of life for patients. Daptomycin (Dap) is a powerful antibiotic used to treat gram-positive bacterial infections. However, its hydrophobic nature limits its effectiveness, and it requires the presence of calcium ions (Ca2+) for activation. In this study, a series of telodendrimer (TD) nanoparticle delivery systems were synthesized to improve daptomycin delivery. The TD nanoparticle systems showed effective …

Pharmacological And Pharmacokinetic Studies Of A KCa2.2 Positive Allosteric Modulator, Mohammad Asikur Rahman

Pharmaceutical Sciences (PhD) Dissertations

Small-conductance Ca²⁺-activated potassium channels (K_Ca2.x) family is widely expressed in neurons, the heart, and endothelial cells. K_Ca2.x channels are named small conductance Ca²⁺-activated potassium channels due to their comparatively low single-channel conductance and are activated solely by rises in intracellular Ca²⁺. The family has three subtypes: K_Ca2.1, K_Ca2.2, and K_Ca2.3, encoded by KCNN1, KCNN2, and KCNN3 genes, respectively. K_Ca2.x channels regulate neuronal excitability and responsiveness to synaptic input patterns. Small-conductance Ca²⁺-activated potassium channels subtype 2 (K_Ca2.2, …

Altering United States Drug Policy And Shifting The Focus Of Drug Use From Conviction Toward Drug Addiction Treatment, Natalie Marra

Honors Projects

While these substances were not always controlled by law, drug use has been as issue throughout time going back thousands of years and continues to be a concern in the twenty-first century. Possession, distribution, and manufacturing of controlled substances outside of what is considered legal can lead to fines and or jail time and can also increases the severity of other crimes committed either due to or under the influence of drugs. As of Saturday June 10th, 2023, 44.5% of Federal inmates are incarcerated for drug offenses, including possession, distribution, and manufacturing1. Drug offenses make up the largest percentage of …

Self-Administered Intranasal Etripamil Using A Symptom-Prompted, Repeat-Dose Regimen For Atrioventricular-Nodal-Dependent Supraventricular Tachycardia (Rapid): A Multicentre, Randomised Trial, Bruce S Stambler, A John Camm, Marco Alings, Paul Dorian, Hein Heidbuchel, Jaco Houtgraaf, Peter R. Kowey, Jose L Merino, Blandine Mondésert, Jonathan P Piccini, Sean D Pokorney, Philip T Sager, Atul Verma, J Marcus Wharton, David B Bharucha, Francis Plat, Silvia Shardonofsky, Michael Chen, James E Ip

Department of Medicine Faculty Papers

BACKGROUND: Etripamil is a fast-acting, intranasally administered calcium-channel blocker in development for on-demand therapy outside a health-care setting for paroxysmal supraventricular tachycardia. We aimed to evaluate the efficacy and safety of etripamil 70 mg nasal spray using a symptom-prompted, repeat-dose regimen for acute conversion of atrioventricular-nodal-dependent paroxysmal supraventricular tachycardia to sinus rhythm within 30 min.

METHODS: RAPID was a multicentre, randomised, placebo-controlled, event-driven trial, conducted at 160 sites in North America and Europe as part 2 of the NODE-301 study. Eligible patients were aged at least 18 years and had a history of paroxysmal supraventricular tachycardia with sustained, symptomatic episodes …

Investigation Of Antidiabetic Activities Of Cu(Ii) Complex Of Anacardium Occidentale Leaves Crude Extract, Mary Adelaide Oladipo, Folasade Omobolanle Ajao, Adewusi John Adepoju, Kayode Taiwo Ishola, Deborah Omowumi Afolabi

Tanzania Journal of Science

Many synthetic chemical drugs have been widely used for the treatment of diabetes. However, many of these drugs are not locally available, are less effective, and are unaffordable for many diabetic patients in developing and underdeveloped countries. Therefore, in order to search for a locally available, effective, and cost-effective antidiabetic agent, this study synthesized the Cu(II) complex of crude leaf extract of Anacardium occidentale and investigated its antidiabetic activity in alloxan induced albino rats. The leaf crude extract and its metal complex were characterized using atomic absorption spectroscopy (AAS) and infrared (IR) spectroscopy. Experimental diabetic animals were induced by a …

Ameliorative Effects Of Vitamins C And E On Haematotoxicity And Spleen Histopathology Induced By Dichlorvos Insecticide In Female Wistar Rats, Halima Mfaume, Harishchandra Pratap, Claudius Luziga, Felister Urasa

Tanzania Journal of Science

This research aimed to assess the toxicological effects of dichlorvos insecticide (2,2-dichlorovinyl dimethyl phosphate or DDVP) on haematological indices of female Wistar rats and to investigate the antioxidant properties of vitamins C and E in ameliorating haematotoxicity. The rats were divided into 6 groups; control-water, control-oil, dichlorvos group, dichlorvos + vitamin C group, dichlorvos + vitamin E group and dichlorvos + vitamin C + E group. Dichlorvos and vitamins were orally administered to rats with an interval of half an hour between treatments. The control-oil group was given 2 ml corn oil and the control-water group was given water adlib. …

Using Lanthanide Ions As Magnetic And Sensing Probes For The Detection Of Tetracycline From Complex Samples, Yan-Cen Zhan, Chin-Poa Chiu, Yu-Chie Chen

Journal of Food and Drug Analysis

Tetracycline (TC) is a broad-spectrum antibiotic and has been added to animal feeds to grow livestock under healthy conditions, making it important to have effective methods for rapidly detecting TC in complex samples. In this study, a novel method that uses lanthanide ions (i.e. Eu³⁺ and Gd³⁺) as magnetic and sensing probes for the detection of TC from aqueous samples is explored. When dissolving Gd³⁺ in tris(hydroxymethyl)aminomethane (Tris) buffer at pH 9, magnetic Gd³⁺-Tris conjugates can be readily generated. The magnetic Gd³⁺-Tris conjugates possess trapping capacity toward TC from sample solutions via …

Urolithin A Exhibits A Neuroprotective Effect Against Alzheimer’S Disease By Inhibiting Dyrk1a Activity, Huang-Ju Tu, Chih-Jou Su, Chao-Shiang Peng, Tony Eight Lin, Wei-Chun Huang Fu, Kai-Cheng Hsu, Tsong-Long Hwang, Shiow-Lin Pan

Journal of Food and Drug Analysis

Alzheimer’s disease (AD) is a devastating neurodegenerative disease with more than 50 million people suffer from it. Unfortunately, none of the currently available drugs is able to improve cognitive impairment in AD patients. Urolithin A (UA) is a metabolite obtained from ellagic acid and ellagitannin through the intestinal flora, and it has antioxidant and anti-inflammatory properties. Previous reports found that UA had neuroprotective effects in an AD animal model, but the detailed mechanism still needs to be elucidated. In this study, we performed kinase-profiling to show that dual-specific tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is the main target of UA. Studies …

Chemometrics-Assisted Spectroscopic Methods For Rapid Analysis Of Combined Anti-Malarial Tablets, Panawan Pruksapha, Putthiporn Khongkaew, Chaweewan Suwanvecho, Nantana Nuchtavorn, Chutima Phechkrajang, Leena Suntornsuk

Journal of Food and Drug Analysis

Combination of piperaquine (PQ) (320 mg) and dihydroartemisinin (DHA) (40 mg) is an anti-malarial formulation, which is recommended by World Health Organization (WHO). Simultaneous analysis of PQ and DHA can be problematic due to the lack of chromophores or fluorophores in DHA molecule. Whereas PQ possesses strong UV absorption and it presents in 8 times of DHA contents in the formulation. In this study, two spectroscopic methods, Fourier transform infrared (FTIR) and Raman spectroscopy, were developed for the determination of both drugs in combined tablets. The FTIR and Raman spectra were recorded in the attenuate total reflectance (ATR) and scattering …

Three-Dimensional Strategies In The Quantitative Resolution Of Kinetic Uv Absorbance Measurements For Monitoring The Oxidation Of Quercetin By Oxidant Agents And Analyzing Dietary Supplement Product, Erdal Di̇nç, Asiye Üçer, Nazangül Ünal

Journal of Food and Drug Analysis

Three-dimensional strategies involving the application of parallel factor analysis (PARAFAC) to the kinetic UV absorbance measurements were elaborated to monitor the oxidation of quercetin with oxidant agents (K₂Cr₂O₇ and KIO₃) and to quantify analyte in a dietary supplement product. Loadings (spectral, kinetic and concentration profiles) were obtained by the PARAFAC deconvolution. Spectral identification, kinetics and quantification of the relevant analyte in the presence of interferent(s) were performed. The elaborated chemometric strategies were carefully validated to demonstrate the capability of the method. Assay results of the PARAFAC strategies were statistically compared to that of …

Resveratrol Stimulates Star Expression And Progesterone Production By Gper-Mediated Downregulation Of Snail Expression In Human Granulosa Cells, Tinglin Song, Jiaye Chen, Sizhu Yang, Boqun Liu, Lingling Zhang, Qian Zhang, Jung-Chien Cheng, Lanlan Fang

Journal of Food and Drug Analysis

Steroidogenic acute regulatory protein (StAR) plays a critical role in the regulation of progesterone (P4) production. Resveratrol (RSV), a natural polyphenol, has beneficial effects on reproductive function. However, its effects on StAR expression and P4 production in human granulosa cells remain undetermined. In this study, we showed the treatment of RSV upregulated StAR expression in human granulosa cells. G protein-coupled estrogen receptor (GPER) and ERK1/2 signaling were involved in RSV-stimulated StAR expression and P4 production. In addition, the expression of a transcriptional repressor, Snail, was downregulated by RSV, which contributed to the RSV-induced induction of StAR expression and P4 production.

Selective Detection Of Tricyclazole By Optical Technique Using Thiomalic Acid–Modified Au And Ag Nanoparticle Mixtures, Yu-Shu Pan, Tsunghsueh Wu, Cho-Chun Hu, Tai-Chia Chiu, Chen-Hao Yeh, Yang-Wei Lin

Journal of Food and Drug Analysis

This study proposes the use of thiomalic acid–modified Au and Ag nanoparticle mixtures (TMA-Au/AgNP mixes) for the selective detection of tricyclazole. Upon the addition of tricyclazole, the color of TMA-Au/AgNP mixes solution changes from orange-red to lavender (red-shift). According to the density-functional theory calculations, tricyclazole-induced aggregation of TMA-Au/AgNP mixes through electron donor–acceptor interactions was proved. The sensitivity and selectivity of the proposed method are affected by the amount of TMA, volume ratio of TMA-AuNPs to TMA-AgNPs, pH value, and buffer concentration. The ratio of absorbance (A₆₅₄/A₅₂₀) of TMA-Au/AgNP mixes solution is proportional to the concentration of …

Development Of A Lateral Flow Immunoassays-Based Method For The Screening Of Ractopamine In Foods And Evaluation Of The Optimal Strategy In Combination Of Screening And Confirmatory Tests, Yuan-Chih Chen, Jen-Yi Hsu, Chien-Sheng Chen, Yi-Ting Chen, Pao-Chi Liao

Journal of Food and Drug Analysis

Ractopamine has been authorized as a feed additive and permitted in animal husbandry. With the establishment of the regulation to limit the concentration of ractopamine, a rapid screening method for ractopamine is urgently needed. Additionally, how to combine the screening and confirmatory tests of ractopamine is also critical to maximizing the efficiency of testing. Here, we developed a lateral flow immunoassays-based method for the screening of ractopamine in foods and proposed a cost-benefit analysis approach to optimize cost allocation between screening and confirmatory tests. After verifying the analytical and clinical performance of the screening method, a mathematical model was established …

Sleep-Promoting Activity Of Amylase-Treated Ashwagandha (Withania Somnifera L. Dunal) Root Extract Via Gaba Receptors, Chun Woong Park, Ki-Bae Hong, Hyung Joo Suh, Yejin Ahn

Journal of Food and Drug Analysis

Ashwagandha (Withania somnifera L. Dunal), an Indian medicinal plant that has been used for centuries to treat insomnia, exhibits a variety of biological activities, such as improving cognitive function, immunity and anxiety. In this study, the effect of enzyme-treated Ashwagandha root extract (EA) and on sleep was evaluated using rodent models. Starch contained in the Ashwagandha root extract was removed by amylase treatment to prepare EA. To evaluate the sleep-promoting activity of EA, a pentobarbital-induced sleep test and electroencephalogram analysis were performed. In addition, the sleep-promoting mechanism of EA was elucidated by analyzing the expression of sleep-related receptors. In …

The Inhibitory Effect Of Quercetin-3-Glucuronide On Pulmonary Injury In Vitro And In Vivo, Pei-Rong Yua, Jen-Ying Hsu, Chiao-Yun Tseng, Jing-Hsien Chen, Hui-Hsuan Lin

Journal of Food and Drug Analysis

Pulmonary injury is defined as a progressive inflammation. Extensive pro-inflammatory cytokines are secreted from alveolus, associated with the production of reactive oxygen species (ROS) and apoptosis. The model of endotoxin lipopolysaccharide (LPS)-stimulated lung cells has been applied to mimic the pulmonary injury. Some antioxidants and anti-inflammatory compounds can be used as chemopreventive agents of pulmonary injury. Quercetin-3-glucuronide (Q3G) has been showed to exert antioxidant, anti-inflammatory, anti-cancer, anti-aging and anti-hypertension effects. The aim of the study is to examine the inhibitory potential of Q3G on pulmonary injury and inflammation in vitro and in vivo. Firstly, human lung fibroblasts MRC-5 cells pre-treated …

Electrochemically Synthesized Green Fluorescent Carbon Dots For Quantitation Of Hypochlorite And Carbendazim, Kuan-Min Lo, Yu-Shen Lin, Je-Wen Liou, Tai-Chia Chiu, Cho-Chun Hu

Journal of Food and Drug Analysis

Green emission carbon dots (CDs) electrochemically prepared from 2,6-pyridinedicarboxylic acid and o-phenylenediamine were applied separately for the quantitation of hypochlorite and carbendazim. The characteristic and optical properties of the CDs were studied through fluorescence, UV–vis absorption, X-ray photoelectron spectroscopy, and transmission electron microscopy. The synthesized CDs were mainly 0.8–2.2 nm in size, with an average size of 1.5 nm. The CDs exhibited green luminescence centered at 520 nm when excited by 420 nm light. The green emission of the CDs is quenched after the addition of hypochlorite, mainly through the redox reaction between hypochlorite and hydroxyl groups on the CDs …

Preparation Procedures Of Food And Beverage Samples For Oxygen Bomb Calorimetry: A Scoping Review And Reporting Checklist, Zane Hopper, Ben Desbrow, Shelley Roberts, Chris Irwin

Journal of Food and Drug Analysis

Standardised bomb calorimetry methods are essential to accurately quantify the gross energy within food and beverages, yet no accepted protocols exist. The objective of this review was to synthesise literature on food and beverage sample preparation methods used for conducting bomb calorimetry. This synthesis enhances our understanding of the extent to which methodological variances may currently affect estimates of the caloric values of dietary items. Five electronic databases were searched for peer reviewed literature on food and beverage energy measurement via bomb calorimetry. Data were extracted on seven identified methodological themes, including: (1) initial homogenisation, (2) sample dehydration, (3) post-dehydration …