Pharmacology Commons^™

Mitigation Of Nicotine Reward And Withdrawal By The N-Acyl Amino Acids: N-Oleoyl Glycine And N-Oleoyl Alanine, Kimberly Karin

Theses and Dissertations

A growing body of research is exploring the efficacy of N-acyl amino acids (N-oleoyl glycine; OlGly and N-oleoyl alanine; OlAla) in rodent models of drug reward and dependence. In particular, OlGly attenuated the reinforcing effects of nicotine in the mouse nicotine-induced conditioned place preference (CPP) paradigm and reduced somatic and affective signs of mecamylamine-precipitated withdrawal in nicotine-dependent mice. Based on the addition of a methyl group on the head group, OlAla was proposed to have increased metabolic stability compared to OlGly. While OlAla has been assessed in assays of reward and withdrawal of opioids, cocaine, and …

Characterizing The Effects Of Antiandrogens And Senolytics To Enhance The Therapeutic Response To Castration-Resistant Prostate Cancer, Justin M. Silverman

Theses and Dissertations

Prostate cancer is the most frequently diagnosed cancer in males and the second most common cause of cancer deaths. Androgen deprivation therapy, whether through surgical or chemical castration, is the mainstay for treatment of advanced prostate cancer; however, despite an initial response, most patients eventually develop a progressive PSA rise, and castration- sensitive prostate cancer gives rise to castration-resistant prostate cancer. The standard of care therapy includes the antiandrogens such as enzalutamide and abiraterone acetate as well as the microtubule poison, docetaxel, and various immunotherapies; however, while prostate cancer research is progressing, there continues to be a compelling need for …

Development Of A Chemical Biology Approach To Uncover The Influence Of Sequence Variations On Ces1 Activity In Live Cells, Samuel James Knebel

Masters Theses

Drug metabolism is the biochemical process of modifying drugs to detoxify and remove them through enzymatic transformations. These biotransformation’s occur primarily in the liver and are critical to understanding how pharmaceutical compounds are chemically altered inside the human body. Human carboxylesterases (CESs) catalyze the hydrolysis of esters, amides, thioesters, and carbamates. CES-mediated hydrolysis plays an important role in the metabolism of many drugs including the first FDA approved antiviral treatment for COVID-19, remdesivir (Veklury), the seizure control medication rufinamide (Banzel), and the flu antiviral drug oseltamivir (Tamiflu). CES activity is known to be influenced by a variety of factors including …

Effect Of Spinach Enriched With Zinc And Ω-3/Vitamin E Treatment Against Fluoride-Induced Nephrotoxicity And Bone Calcification Disturbance In Rats, Anfal Djouadi, Samir Derouiche

The Thai Journal of Pharmaceutical Sciences

Objective: The goal of this study was to evaluate the alone or associated spinach, zinc, and ω-3/Vitamin E capacity to improve the renal function and bone calcification altered by fluoride in Wistar rats. Methods: In this study, 36 female Wistar albino rats were used; divided into six groups (n = 6); all groups except the control rats received orally 400 ppm of fluoride as sodium fluoride (NaF) in drinking water during 70 days and then four groups treated in the past 15 days by: Spinach powder, zinc, ω-3/Vitamin E, and spinach+ zinc + ω-3/Vitamin E. Some biochemical and histological markers …

The Efficacy Of Vitamin B6 And Alpha-Lipoic Acid In Preventing Levetiracetam Depressant-Like Behavior In Mice, Azadeh Mesripour, Nasime S. Musavie

The Thai Journal of Pharmaceutical Sciences

Background: Some antiepileptic drugs for instance levetiracetam cause depression in patients. Vitamin B6 is a cofactor involved in the neurotransmitter synthesis. α-Lipoic acid (ALA) is a mitochondrial cofactor that can prevent neuronal damage. The aim of this study was to evaluate the effectiveness of B6 and ALA for preventing levetiracetam depression in mice. Methods: Male NMRI mice (weighing 25 ± 3 g) were used. Levetiracetam (20 mg/kg), and pretreatments with ALA (20, 40 mg/kg), Vitamin B6 (100 mg/kg), or imipramine (10 mg/kg) as the control positive were all administered intraperitonealy for 14 consecutive days. The locomotor test and forced swimming …

Barriers And Facilitators Of Wound Care Services Provided By Community Pharmacists In Selangor, Malaysia: An Exploratory Qualitative Study, Hamidi Drahman, Mohd Shahezwan Abd Wahab, Mohd Faiz Mustaffa, Azyyati Mohd Suhaimi

The Thai Journal of Pharmaceutical Sciences

Introduction: Community pharmacists (CPs) are often the first point of contact for patients to obtain health-related advice, including on wound management. Wound care services have been proposed as a community pharmacy practice area to be promoted in Malaysia. Objectives: This study aims to explore the types of wound care services provided by Malaysian CPs, and the factors associated with its provision. Methods: This study utilized the qualitative method to collect in-depth information about the barriers and facilitators associated with the provision of wound care services among a sample of CPs. Interview transcripts were analyzed using thematic content analysis. Results: Twenty-three …

Docking, Synthesis Of Some Novel Flavonoid Analogues, And Their Biological Evaluation, Ishwar Bhat K, Afiya Abdul Aziz, Abhishek Kumar, Vijaya Bhaskar K, Vijay Kumar M

The Thai Journal of Pharmaceutical Sciences

Cancer remains a major class of morbidity and mortality despite basic and clinical research and trials of promising new therapies. In the current era, many drugs are marketed with flavonoid nucleus. Based on this information, this study aims to synthesize and screen flavones for their anticancer activity. Docking studies for cytotoxic activity of flavonoid derivatives targeting tankyrase enzyme were performed. A new series of flavonoid derivatives were prepared from chalcones. Chalcones were prepared between substituted benzaldehyde and 2-hydroxy acetophenone in the presence of potassium hydroxide as catalyst. The flavone derivatives were characterized based on IR, 1H NMR, and Mass spectral …

Application Of Concept Mapping In Telepharmacy Model Development For Prescription Filling At Primary Care Clusters, Nusaraporn Kessomboon, Siwapond Prasertsuk, Jirachaya Suttima, Nur-Ainee Korsem

The Thai Journal of Pharmaceutical Sciences

Background: Although the Pharmacy Council of Thailand has announced a standard telepharmacy service procedure, there may be some details or limitations that are specific to the primary care cluster (PCC) in the real situation. Objective: This research aimed to create a telepharmacy service model for the PCC using concept mapping techniques. Methodology: Group discussions were held, each participant will submit their opinions and graded of importance and possibilities of each opinion. After that, the data obtained were statistically analyzed to create a concept mapping. Results: From the group discussion, (n = 10) can be concluded that the optimum telepharmacy services …

Characterization Of Quality Attribute And Specification For Standardization Of Acemannan Extracted From Aloe Vera For Tissue Regeneration, Siriwan Seeleamngam, Polkit Sangvanich, Pasutha Thunyakitpisal, Vorasit Vongsutilers

The Thai Journal of Pharmaceutical Sciences

Acemannan extracted from Aloe vera was well characterized as an acetylated mannose polysaccharide which have promising clinical profile for tissue regeneration. Quality aspect of acemannan is required to develop the herbal extract for practical industrial application and reliable therapeutic use. The research aim is to investigate the qualify attributes of acemannan that have impact on its safety and efficacy. Quality of three production batches of acemannan were evaluated based on ICH quality guidelines and pharmacopeial standard. The quality aspect of acemannan were determined by analytical technique including FT-IR, SEC-HPLC, RP-HPLC, GC, and loss on drying to ensure its identify and …

Hepatotoxic Effect Of Cadmium And Available Therapeutic Options, Tomilola Olaolu, Favour Jibulu, Rotimi Damilare

The Thai Journal of Pharmaceutical Sciences

Hepatoxicity, also known as toxic hepatitis, is a condition, in which the liver becomes inflamed due to exposure to such substances as chemicals, medications, herbal products, or excessive alcohol consumption. Cadmium is a major environmental pollutant from agricultural and industrial sources and has been reported to induce hepatotoxicity. Cadmium can also be found in phosphate fertilizers, detergents, and refined petroleum products as an impurity and used industrially in the production of polyvinyl chloride product stabilizers and the fabrication of nickel-cadmium batteries. Cadmium can be absorbed into the human body through the gastrointestinal tract, respiratory, and dermal routes. Cadmium-induced hepatic damage …

Development Of Amino Acid Salt-Based Curcumin@Lysine Acetate Co-Amorphous System Using Liquid-Assisted Grinding For Improved Solubility And Dissolution, Udaykumar Patil, Snehal Rawal, Jidnyasa Pantwalawalkar, Sopan Nangare, Dilip Dagade, Pravin Patil, Namdeo R. Jadhav

The Thai Journal of Pharmaceutical Sciences

Curcumin, multivalued phytoceutical, exhibits appreciable safety. However, its therapeutic utility is significantly compromised due to low aqueous solubility, and thus, poor absorption and low bioavailability become apparent. To surpass this limitation, the present work aims to develop amino acid salt-based curcumin@lysine acetate co-amorphous system for improved solubility and dissolution. Initially, screening of curcumin-amino acid mixtures was performed for saturation solubility assessment. Considering the outcome, lysine acetate was formulated to generate a co-amorphous mixture (COAM) by liquid-assisted grinding and evaluated for saturation solubility and different spectroscopical characterizations. Curcumin-lysine acetate COAM tablet formulation was developed by direct compression method and evaluated for …

Solubility Enhancement Of Diacerein By Spray Drying Technique, Formulation Development, And In Vivo Study, Devidas G. Bachhav, Somashekhar S. Khadabadi, Leena P. Deore, Vilas B. Ghavate

The Thai Journal of Pharmaceutical Sciences

Purpose: The aim of the present research was solubility and dissolution rate enhancement of diacerein by spray drying technique. Materials and Methods: Solid dispersions of diacerein with PEG-600, guar gum, poloxamer-188 and aerosil were prepared in different ratios using 32 factorial designs. FTIR, DSC, XRD and SEM were performed to study the interaction between drug and polymers and evaluated for in-vitro drug release study. Results and Discussion:In spray dried solid dispersion formulations there was decrease in crystallinity of diacerein, which leads to increase in dissolution of diacerein from solid dispersions. Diacerein 50 mg immediate release tablets formulated (using spray dried …

Determination Of Anti-Herpes Simplex Virus Type 1 Activity Of The Air Filter Coated With Silver Ions Using A Modified Method Of Iso 21702:2019, Mali Wirotesangthong, Ariya Khanboon, Kanyanat Piewpong

The Thai Journal of Pharmaceutical Sciences

Background: Since severe acute respiratory syndrome coronavirus 2 causing coronavirus disease 2019 pandemic has emerged, various air membrane filters with antimicrobial agents have been explored and investigated for inactivating virus particles. Objectives: The purpose of this study was to determine an antiviral activity of the air filter coated with silver ions using the method of ISO 21702:2019. Materials and Methods: Herpes simplex virus type 1 (HSV-1), KOS strain, an enveloped virus causing skin, mucous membrane, and respiratory tract infection (RTI) were tested with the non-porous surface coated with or without silver ions (control filter) for 0, 24 h at 25°C. …

Gut-Lung Axis Of The Microbiome Alterations After Ultrafine Particles And Ozone Inhalation, Md Habibul Hasan Mazumder

Graduate Theses, Dissertations, and Problem Reports (ETD)

Air pollution poses a significant threat to public health. It is a mixture of particulate matter, gaseous substances, and other secondary substances. Despite epidemiological research indicating the interactive effects of various components of air pollution, existing studies and regulatory limits often focus on single-exposure scenarios. The emerging understanding of the microbiome’s role in regulating immune response, metabolism, and pathophysiology of various diseases points towards interactions between environmental exposures and microbial dysbiosis. In this dissertation, mice were exposed to relevant deposited doses of carbon black (CB) and ozone (O3), and lung inflammation as well as the lung-gut axis of the microbiome …

Modulatory Effects Of Deacetylated Sialic Acids On Breast Cancer Resistance Protein-Mediated Multidrug Resistance And Receptor Tyrosine Kinase-Targeted Therapy, Isaac Tuffour

Electronic Theses and Dissertations

Multidrug resistance (MDR) remains a major challenge in cancer treatment, accounting for over 90% of chemotherapeutic failures. Cancers utilize sugar residues to engage in multidrug resistance. The underlying mechanism of action involving glycans, specifically the glycan sialic acid (Sia) and its various functional group alterations, has not been explored. ATP-binding cassette (ABC) transporter proteins, key proteins utilized by cancers to engage in MDR pathways, contain Sias in their extracellular domains. Modulating the expression of acetylated-Sias on Breast Cancer Resistance Protein (BCRP), a significant ABC transporter implicated in MDR, in lung and colon cancer cells directly impacted the ability of cancer …

Effects Of Combined Ethanol And Nicotine Administration On Delay Discounting In Male And Female Sprague-Dawley Rats, Rebecca Lillian Chalme

Graduate Theses, Dissertations, and Problem Reports (ETD)

Ethanol (EtOH) and nicotine (NIC) are among the most commonly used and co-used drugs in the world. Co-use occurs in people who use one or both drugs chronically, but also in people who only consume one or both drugs acutely, often in a “bingeing and chipping” pattern. Given that each drug on its own has previously been shown to affect impulsive choice in delay-discounting procedures, with some indication that drug effects could vary by sex, the purpose of the present experiments was to investigate effects of combined EtOH and NIC at a range of dose combinations on delay discounting in …

Vapourized Cannabis Extract Administration Impairs Memory And Alters Neural Activity In Laboratory Rats, Megan Chladny

Theses and Dissertations (Comprehensive)

Although people have smoked cannabis for millennia, administration of cannabis by heating the dried plant material or distilled extracts to a temperature just below the combustion point (i.e., vapourization or "vaping") has rapidly increased over the past few years (Javadi-Payder, Cole, and Taffe, 2018; Manwell, Charchoglyan, Brewer, Matthews, Heipel, and Mallet, 2014). Conversely, most of the cannabinoid research using rodent models has used parenteral routes of administration to examine the effects of purified cannabis extracts such as ∆⁹-tetrahydrocannabinol (THC), making it difficult to directly compare laboratory research to human drug use. Building on previous studies showing that THC …

Nanofabrication For Precision Vaccinology, Karen Zagorski

Theses & Dissertations

Vaccines are among the most effective and safe therapeutics known to mankind. Historically the approach to the creation of new vaccines has been dominated by empirical research, trial, and error. This thesis focuses on the more modern, rational approaches to vaccinology based on the current understanding of the inner workings of the immune system. We used nanotechnology for the generation of novel immunogens, addressed several challenges, and characterized the immune responses.

The preparation, characterization, and troubleshooting of several vaccines against dimeric amyloid beta are covered in chapters 4-6. Despite being ultimately unsuccessful, this part provided a deeper understanding of the …

A Case Of Transverse Myelitis Secondary To Covid-19 Infection, Rahul Borra, Neal T. Patel, Raheel Shaikh, Mayur S. Parmar, Sujatha Borra

HPD Articles

Infection with COVID-19 (SARS-CoV-2) is associated with a variety of generalized and specific symptoms, including neurological complications of both the peripheral and central nervous systems. In this case report, we present the case of a previously healthy 55-year-old woman who was diagnosed with transverse myelitis following a previous infection with COVID-19. MRI showed progressive demyelination of the cervical and thoracic spinal cord, and cerebrospinal fluid (CSF) showed increased levels of protein and red blood cells and no markers of infection, including negative polymerase chain reaction (PCR) for COVID-19 antibodies. The patient was treated with a course of methylprednisolone, multiple treatments …

Investigation Of Human N-Acetyltransferases (Nat1 And Nat2) Genetic Polymorphisms In Susceptibility To Aromatic Amine And Alkylaniline Genotoxicity., Mariam Habil

Electronic Theses and Dissertations

Arylamine N-acetyltransferases, NAT1 and NAT2, catalyze the detoxification and/or activation of carcinogens. Single nucleotide polymorphisms or SNPs result in different human NAT1 and NAT2 genotypes. We hypothesize that different NATs alleles will impact levels of N-acetylation, HPRT mutations, DNA damage and oxidative stress induced by carcinogens. NER-deficient Chinese hamster ovary (CHO) cells transfected with human CYP1A2 and NAT1*4, NAT1*14B, NAT2*4, NAT2*5B or NAT2*7B have been used to investigate N-acetylation of benzidine, β-naphthylamine (BNA), and 4, 4’-methylene bis (2-chloroaniline) (MOCA) as aromatic amines and 3,4-dimethylaniline (3,4-DMA) as one of alkylanilines and their associated toxicity. Our …