Pharmacology, Toxicology and Environmental Health Commons^™

Discovery Of Piperlongumine Derivatives As Anti-Leukemic And Anti-Prostate Cancer Agents, Yi Liao

Wayne State University Dissertations

Piperlongumine (PL) is an electrophilic anti-cancer natural product. Through non-covalent or covalent interactions with cellular targets, PL inactivates multiple oncogenic pathways and suppresses key components of cellular anti-oxidant/anti-electrophile defense systems. These actions result in pleiotropic anticancer effects and are expected to be effective to heterogeneous acute myeloid leukemia (AML) and prostate cancer (PCa). We applied two approaches to enhance the anticancer potency of PL: 1) To design PL-histone deacetylase inhibitor hybrid drugs (PL-HDACis; e.g., 1-58), and 2) To dimerize PL pharmacophore to generate a dimeric PL (DiPL) warhead that is suitable for further conjugation (e.g., 5-17). Both 1-58 and 5-17 …

Sensitivity Of Quagga Mussels (Dreissena Rostriformis Bugensis) To Cyanobacteria At Multiple Life History Stages, Anna Boegehold

Wayne State University Dissertations

Quagga mussels (Dreissena rostriformis bugensis) originate from brackish waters of the Ponto-Caspian area and are nuisance invasive species in North American and European freshwaters. Their invasion has caused major economic and ecological damages in the Laurentian Great Lakes. Through selective filter feeding, quagga mussels have promoted the growth of cyanobacteria. Harmful cyanobacteria blooms have the potential to produce toxins, which can be toxic to humans and wildlife. Although quagga mussels can increase the prevalence of cyanobacteria blooms, it is unknown how they are physiologically affected by cyanobacteria and understanding these dynamics can be useful in the management of this invasive …

Exosomes Released From Multiple Myeloma Cells Influence The Angiogenic Function Of Endothelial Cells By Regulating Microrna-29b, Qinmao Ye

Browse all Theses and Dissertations

Multiple myeloma is a hematological malignancy characterized by clonal proliferation of plasma cells generally caused by chromosomal abnormalities. It occurs in the bone marrow, which is the microenvironment of multiple myeloma. Exosomes (EXs) are 30-100 nm membrane-derived micro-vesicles containing various of bioactive molecules, such as microRNAs, to mediate the cell-cell interaction. Numerous studies reported that exosomes play a significant role in tumor microenvironment. Angiogenesis has the important implication in tumor exacerbation to supply nutrients to promote the progression of cancer cells through endothelial cells (ECs). Some studies demonstrated that microRNA-29b (miR-29b) can suppress tumor development and inhibit angiogenesis. Therefore, in …

Regulation Of Microvesicle Particle Release In Keratinocytes, Azeezat Afolake Awoyemi

Browse all Theses and Dissertations

Microvesicle particles (MVPs) are produced from cellular membranes and are thought to mediate cell-cell communication, including in response to stressors such as UVB radiation and thermal burn injury. Previous studies have shown that stress-induced MVP release requires the platelet-activating factor (PAF) receptor in human keratinocytes and that pharmacological inhibition of acid sphingomyelinase (ASM) blocked this release. To validate a genetic role for ASM in MVP release, we used CRISPR-Cas9 gene silencing in human keratinocytes and primary fibroblasts derived from ASM-knockout mice. Though MVP release was partially blocked in ASM-deficient mouse fibroblasts, the inability to fully knockdown ASM in HaCaT cells …

Individual Understanding Of The Risks Associated With Polypharmacy, Michelle Patricia Mchenry

Walden Dissertations and Doctoral Studies

With many individuals experiencing multimorbidity, individuals are being prescribed more medications. Although there are benefits to taking medications to manage symptoms and treat disease processes, there are also risks to taking multiple medications. The purpose of this phenomenological study was to explore participants' understanding of the risks associated with practicing polypharmacy. Game theory, credibility theory, and belief bias were the conceptual frameworks used to explain how individuals experienced their care and being prescribed 5 or more medications. Eight participants residing in subsidized housing in a small Midwest city, who were taking 5 or more medications volunteered to take part in …

An Optimized Solid-Phase Reduction And Capture Strategy For The Study Of Reversibly-Oxidized Cysteines And Its Application To Metal Toxicity, John Andrew Hitron

Theses and Dissertations--Toxicology and Cancer Biology

The reversible oxidation of cysteine by reactive oxygen species (ROS) is both a mechanism for cellular protein signaling as well as a cause of cellular injury and death through the generation of oxidative stress. The study of cysteine oxidation is complicated by the methodology currently available to isolate and enrich oxidized-cysteine containing proteins. We sought to simplify this process by reducing the time needed to process samples and reducing sample loss and contamination risk.

We accomplished this by eliminating precipitation steps needed for the protocol by (a) introducing an in-solution NEM-quenching step prior to reduction and (b) replacing soluble dithiothreitol …

Protein Participants Of Cytosolic Internalization Of The Ouabain-Bound Na⁺/K⁺Atpase Receptor In Human B-3 Lens Epithelial Cells, Joshua Lysle Stricker

Browse all Theses and Dissertations

The primary function of Na⁺/K⁺ATPase (NKA) discovered by Jens Christian Skou in 1958, through electrogenic exchange of 3 Na⁺ for 2 K⁺ ions (Robert L Post, 1958), is the homeostatic preservation of their electrochemical gradient across the plasma membrane (PM) of almost all species and their derived cell lines. Cardiotonic steroids (CTS), such as cardenolides or bufadienolides, are well established inhibitors of NKA. Fox glove plant extracts containing CTS, including digitalis, were first described by William Withering (1744-91) for their positive inotropic effect in heart failure patients. Later research identified the mechanism of their action through direct inhibition of NKA …

Exposure To Polybrominated Diphenyl Ethers (Pbdes) In American And Canadian Workers: Biomonitoring Data From Two National Surveys, Sabrina Gravel, Jérôme Lavoué, France Labrèche

Études primaires

Polybrominated diphenyl ethers (PBDEs) are flame retardants commonly found in many household and industrial products. They can be detected in the serum of the general population, and in even higher concentrations in workers of certain industries, due to an additional occupational exposure. The purpose of this analysis is to determine background exposure levels of PBDEs in the general working population, using national surveys where working status was self-reported. Participants aged 20–65 were selected from the 2003–2004 U.S. National Health and Nutrition Examination Survey (n = 1141) and the 2007–2009 Canadian Health Measures Survey (n = 1337). Only four congeners were …

The Forensic Characterization Of Bacterial And Fungal Organisms In Traditional Chinese Medicine, Julia Grzymkowski, Christopher J. Ehrhardt, Justin L. Poklis, Michelle R. Peace

Undergraduate Research Posters

There has been an increase in use of Traditional Chinese Medicine (TCM) in the United States because they are less expensive and believed to be more effective with less adverse effects in comparison to traditional pharmaceutics. Therefore, sales have increased in the US, despite articles and case studies demonstrating the dangers, such as injury and death, related to TCM, stemming from improper labelling, toxic contaminants, and, in some cases, the presence of pathogenic bacteria. The aim of this study was to perform a survival experiment to demonstrate the importance of proper herbal brewing technique and to conduct a molecular and …

Design, Synthesis And Biological Evaluation Of Inhibitors Against Both Human And Mouse Microsomal Prostaglandin E2 Synthase-1 Enzymes, Kai Ding

Theses and Dissertations--Chemistry

As the principal pro-inflammatory prostanoid, prostaglandin E₂ (PGE₂) serves as mediator of pain and fever in inflammatory reactions. The biosynthesis of PGE₂ starts from arachidonic acid (AA). Cyclooxygenase (COX)-1 and/or COX-2 converts AA to prostaglandin H₂ (PGH₂), and PGE₂ synthases transform PGH₂ to PGE₂. Current mainstream approach for treating inflammation-related symptoms remains the application of traditional non-steroidal anti-inflammatory drugs (tNSAIDs) and selective COX-2 inhibitors (coxibs). As both categories shut down the biosynthesis of all downstream prostanoids, their application renders several deleterious effects including gastrointestinalulceration and cardiovascular risk. Microsomal prostaglandin …

Study Of The Mechanism Of Action For Ru(Ii) Polypyridyl Complexes As Potential Anticancer Agents, Yang Sun

Theses and Dissertations--Chemistry

Application of chemotherapeutic agents in current cancer treatment has been limited by adverse effects as poor selectivity results in systemic toxicity; most chemotherapy approaches also experience inherited or acquired drug resistance which lead to reduced treatment outcome. Research efforts have focused on the discovery of novel chemotherapies that overcome the limitations mentioned above. Ru(II) polypyridyl complexes with anti-cancer properties have been extensively studied as traditional cytotoxic agents and photodynamic therapy agents due to their photophysical and photochemical characteristics.

Most research has focused on the design of Ru(II) polypyridyl complexes that have affinities to nucleic acids as inspired by the classic …

Validated Thin-Layer Chromatography-Densitometric Method For Simultaneous Determination Of Piperine And Plumbagin In “Benjakul” Thai Polyherbal Formulation And Its Antioxidant Activities, Savita Chewchinda, Pattamapan Lomarat, Pongtip Sithisarn

The Thai Journal of Pharmaceutical Sciences

The purpose of this study was to evaluate antioxidant activity and quantitative analysis of piperine and plumbagin content in “Benjukul (BEN)” Thai polyherbal formulation by TLC densitometric method. BEN was recognized in the list of herbal medicinal...

Antihypercholesterol Activity Of Costus Speciosus Water Extract, Hari Susanti, Subagus Wahyuono, Ratna Asmah Susidarti, Ika Puspita Sari

The Thai Journal of Pharmaceutical Sciences

Hypercholesterol is one of cause of cardiovascular disease. Costus speciosus is known empirically as an antihypercholesterol remedy. The study was conducted to determine the effect of water extract of Costus speciosus (CS) on cholesterol blood serum leve.

Characterization Of Lactic Acid Producing Bacillus Coagulans Strains With Their Antibacterial Activity And L-Lactic Acid Production, Vasana Tolieng

The Thai Journal of Pharmaceutical Sciences

Objectives: Screening of antibacterial activity, identification, and L-lactic acid production of spore forming Bacillus isolates. Materials and methods: Fourteen Bacillus isolates were characterized based on their phenotypic characteristics and 16SrRNA .

Cost-Effectiveness Analysis Of Aripiprazole Compared With Risperidone In Treatment Of Acute Schizophrenia Patients In Thailand, Wiwat Thavornwattanayong

The Thai Journal of Pharmaceutical Sciences

OBJECTIVES: Schizophrenia is the third leading cause of loss of life years in Thailand. Currently, aripiprazole is the latest drug for the treatment of acute schizophrenia in Thailand but its cost-effectiveness has not been studied. The purpose of this s.

A Novel Assay For Evaluation Of The Total Antioxidant Capacity (Tac) Using A Nontoxic Probe, Sirirat Panich

The Thai Journal of Pharmaceutical Sciences

A novel and simple method for measuring total antioxidant capacity (TAC) was established. Herein, the new assay is based on generating the deep blue Imipramine (IMI) free radical by oxidising IMI with ammonium tetra vanadate (NH4VO3) in acid medium. Once.

In Silico Evaluation Of Molecular Interactions Between Known ?-Glucosidase Inhibitors And Homologous ?-Glucosidase Enzymes From Saccharomyces Cerevisiae, Rattus Norvegicus, And Ganc-Human, Teni Ernawati

The Thai Journal of Pharmaceutical Sciences

The aim of this study was to observe molecular interactions between alpha glucosidase inhibitor waith alpha glucosidase enzyme derived from Saccharomyces cereviseae, Rattus norvegicus and GANC-human. Therefore, they were used against four of the well-kno.

Intended High-Performance Liquid Chromatography Procedure For The Quantification Of Norfloxacin And Its Potential Impurities In Active Pharmaceutical Ingredient And Tablet Dosage Forms, Bikshal Babu Kasimala, Venkateswara Rao Anna, Useni Reddy Mallu, L. Maheshwara Reddy

The Thai Journal of Pharmaceutical Sciences

Norfloxacin [NFXC] is an active pharmaceutical ingredient belongs to 4-quinolone antibacterial agent used for the prophylaxis of gram +ve and gram-ve bacterial infections. A reliable stability-indicating RP-HPLC method was developed for the separation an.

Development And Validation Of Novel Stability-Indicating High-Performance Liquid Chromatography Method For The Determination Of Miglitol In Pharmaceuticals, Kanakapura Basavaiah, Nagaraju Rajendraprasad

The Thai Journal of Pharmaceutical Sciences

A reversed phase high performance liquid chromatographic (RP-HPLC) method for the determination of miglitol (MGL) in pharmaceuticals is presented. The assay was performed on a Phenomenex Luna C18 (150 × 4.6 mm; 5µm particle size) column using phosphate...

Quantitative Structure–Activity Relationship Modeling Of S-Triazines And 2-Arylpyrimidines As Selective Pde4b Inhibitors, Anand Gaurav, Gabriel Akyirem Akowuah, Choo Shiuan Por

The Thai Journal of Pharmaceutical Sciences

A QSAR analysis was conducted on a series of 2-arylpyrimidine and s-triazine derivatives as selective PDE4B inhibitors. Primary objective of the study is to develop predictive QSAR models for s-triazines and 2-arylpyrimidines as selective PDE4B and to id.

Ethical Cases On Pharmacy Profession Practice In Thailand During A.D. 1995 To 2015, Wanna Sriviriyanupap, Usawadee Sutapuk

The Thai Journal of Pharmaceutical Sciences

Background: Code of ethics for the pharmacy profession was established to enforce all pharmacists to abide by a rule for a good pharmacy professional practice. Objective: to study the ethical problems, related to the pharmacy profession practice, and to .

Population Pharmacokinetics Analysis Of Vancomycin In Critically Ill Patients, Wanchai Treyaprasert

The Thai Journal of Pharmaceutical Sciences

Objectives: The aim of this study was to determine population pharmacokinetic parameters of vancomycin in adult critically ill patients and to investigate the covariates affecting population pharmacokinetic parameters. Methods: Plasma concentration data..

Effect Of Temperature And Time On Free Amino Acid Profile In Thai Chicken Bone Soup Stock Preparation, Nattida Chotechuang, Matichon Lokkhumlue, Pawinee Deetae

The Thai Journal of Pharmaceutical Sciences

Soup stock is the basic material for cooking various types of food, including Thai food. General practice to prepare Thai soup stock is to gentle boil chicken bone soup stock between 85-95°C for 1-3 hours to get good quality soup stock. Free amino aci..

Apigenin And Baicalin, Each Alone Or In Low Dose Combination, Attenuated Chloroquine Induced Male Infertility In Adult Rats, Amira Akilah, Mohamed Balaha, Mohamed-Nabeih Abd-El Rahman, Sabiha Hedya

The Thai Journal of Pharmaceutical Sciences

Male infertility is a worldwide health problem, which accounts for about 50% of all cases of infertility and considered as the commonest single defined cause of infertility. Recently, apigenin and baicalin exhibited a powerful antioxidant and antiapoptot.

The Protective Effect Of Lycopene-Rich Products On Skin Photodamage: A Systematic Review And Meta-Analysis Of Randomized Controlled Trials, Witoo Dilokthornsakul, Teerapon Dhippayom, Piyameth Dilokthornsakul

The Thai Journal of Pharmaceutical Sciences

Background: Ultraviolet (UV) radiation has known as a major cause of photodamage, photoaging and skin cancer as it involves in reactive oxygen species generation. Several natural antioxidants including lycopene has been suggested for photoprotection. How.

Suitability Of Alternative Atp Potency Assay For Lot Release Of Tokyo Bcg- 172-1 Vaccines In Thailand, Supaporn Phumiamorn

The Thai Journal of Pharmaceutical Sciences

The potency assay of the BCG vaccine is routinely performed by a conventional viable count on a solid medium. This assay method is not only time-consuming, but can give variable results because of the tendency to clump of mycobacterium. The intracellular.

A Simple High-Performance Liquid Chromatographic Method For Quantitative Analysis Of Brazilin In Caesalpinia Sappan L. Extracts, Sakan Warinhomhaun, Boonchoo Sritularak, Dusadee Charnvanich

The Thai Journal of Pharmaceutical Sciences

The specific aim of the study was to develop and validate a simple reversed-phase high-performance liquid chromatographic (HPLC) method for assay of brazilin in Caesalpinia sappan L. (sappanwood) extracts. Validation of the HPLC method was conducted unde.

Access To Medicines For Breast, Colorectal, And Lung Cancer In Thailand, Pornsroung Saerekul, Tharin Limsakun, Puree Anantachoti, Rungpetch Sakulbumrungsil

The Thai Journal of Pharmaceutical Sciences

Cancer drugs have become prohibitive, and consequently their accessibility has increasingly been of great concern in many countries. Particularly, the information about cancer drug access in Thailand has been sporadic. Therefore, the goal of the study wa.

Anti-Inflammatory Effect Of Centella Asiatica Extract On Prevented Aortic Intima-Media Thickening In Diabetic Rats, Amalia Anita Hawas, Dwi Aris Agung Nugrahaningsih, Eti Nurwening Sholikhah, Sadli Syarifuddin, Rahmi Ayu Wijayaningsih, Ngatidjan

The Thai Journal of Pharmaceutical Sciences

Objectives: To explore the effect of C. asiatica extract on intima-media thickness, eNOS expression, and macrophage M1/M2 ratio in diabetic rats aorta. Materials and Methods: Wistar rats consisted of normal group and diabetic group which divided into neg.

Effect Of Ipomoea Hederacea Jacq. Methanolic Extract On Blood Pressure And Relaxation Of Rat Thoracic Aorta: Evidence Indicated The Release Of No And H2s, Chaweewan Jansakul

The Thai Journal of Pharmaceutical Sciences

Seeds of Ipomoeahederacea Jacq. (IH) are used in traditional medicine to manage ailments pertaining to the vasculature, circulatory system and related disorders. However no study exists to validate their usage for said ailments. The present study was con.