Pharmacology, Toxicology and Environmental Health Commons^™

Protective Effect Of Deferiprone On 7-Ketocholesterol Formation In Hemin-Induced Ldl Oxidation, Usa Suwannasual, Thitima Pengsuparp, Rataya Luechapudiporn

The Thai Journal of Pharmaceutical Sciences

Hemin (iron (III)-protoporphyrin IX) is found that it is elevated in the plasma of thalassemic patients and is a possible cause of oxidative stress-promoting atherosclerosis. Deferiprone (L1), an iron chelator, can prevent free radical formation catalyze...

Development And Validation Of Rp-Hplc Method For Analysis And Stability Study Of 8-Carboxyphenyl-2'-Deoxyguanosine And 8-Bromo-2'-Deoxyguanosine, Kulwadee Sawatpaiboontawee, Panutsaya Sermthaveesub, Panuwat Sangsirimongkolying, Patratorn Kunakorntham, Sudarat Thongborriboon, Bodin Tuesuwan, Vorasit Vongsutilers

The Thai Journal of Pharmaceutical Sciences

Modifications on C8 position of purine base have been studied for their effects on B-DNA to Z-DNA conversion. The 8-bromo and 8-carboxyphenyl adduct are among the most potent Z-DNA facil tators and hence arc aimed to be utilized for Z-DNA based probe lor...

Isolation And Characterization Of Natural Alpha-Glucosidase Inhibitors From Antioxidant Rich Red Wine Grapes (Vitis Vinifera), Hoda Chaouki Kadouh

Wayne State University Dissertations

Background: Diabetes is currently a global public health problem affecting people at all ages. Dietary antioxidants have been associated with a reduced risk of type 2 diabetes. Grape pomace contains considerable amounts of polyphenols and it has been reported to exhibit an inhibitory activity against alpha- glucosidases. Alpha-glucosidases, in turn, play a major role in controlling starch digestion and therefore postprandial blood glucose, a target for diabetes management.

Objective: This study aims to investigate the anti-diabetes potential of a selection of six grape pomaces and prepare and purify active components in the active variety that specifically inhibit intestinal alpha-glucosidases. The …

Parent-Metabolite Pharmacokinetic Models For Tramadol – Tests Of Assumptions And Predictions, Sam Holford, Karel Allegaert, Brian J. Anderson, Butch Kukanich, Altamir B. Sousa, Amir Steinman, Bruno Pypendop, Reza Mehvar, Mario Giorgi, Nick Holford

Pharmacy Faculty Articles and Research

Allometric principles were used to discern cross-species differences in (±)-tramadol disposition and formation of its primary analgesic metabolite, (±)-O-desmethyl-tramadol (M1). Species differences in formation of M1 may help predict the analgesic effectiveness of tramadol. Tramadol was administered intravenously by a zero-order (constant infusion) process or rapid bolus dose and racemic concentrations of tramadol and M1 measured. Data were pooled to define differences between species (human, rat, cat, dog, goat, donkey and horse). A two-compartment linear disposition model with first-order elimination was used to describe tramadol and M1 disposition. Slow metabolizers were detected in 6% of the population and tramadol clearance …

Sensitization Of Human Cancer Cells To Gemcitabine By The Chk1 Inhibitor Mk-8776: Cell Cycle Perturbation And Impact Of Administration Schedule In Vitro And In Vivo, Ryan Montano, Ruth Thompson, Injae Chung, Huagang Hou, Nadeem Khan, Alan Eastman

Dartmouth Scholarship

Chk1 inhibitors have emerged as promising anticancer therapeutic agents particularly when combined with antimetabolites such as gemcitabine, cytarabine or hydroxyurea. Here, we address the importance of appropriate drug scheduling when gemcitabine is combined with the Chk1 inhibitor MK-8776, and the mechanisms involved in the schedule dependence.

Purifying The Human Rna-Lariat Debranching Enzyme, Ammar Saigal

Honors Program Theses and Research Projects

This project is my first official research endeavor and it involved becoming acquainted with a large variety of biochemistry and molecular biology techniques. The goal is to elucidate the structure of a protein common to most if not all cells of organisms within the Domain Eukarya, which is one of the three taxonomic domains into which all life is categorized. This is the domain most relevant to human beings as it includes plants, fungi, and animals (from a strictly biologically-taxonomic perspective, the species Homo sapiens to which you and I belong is considered belonging to the Kingdom Animalia [Animal]).

Repeated Asenapine Treatment Produces A Sensitization Effect In Two Preclinical Tests Of Antipsychotic Activity, Rongyin Qin, Yingzhu Chen, Ming Li

Department of Psychology: Faculty Publications

Among several commonly used atypical antipsychotic drugs, olanzapine and risperidone cause a sensitization effect in the conditioned avoidance response (CAR) and phencyclidine (PCP)- induced hyperlocomotion paradigms – two well established animal tests of antipsychotic drugs, whereas clozapine causes a tolerance effect. Asenapine is a novel antipsychotic drug recently approved for the treatment of schizophrenia and manic disorders. It shares several receptor binding sites and behavioral features with other atypical antipsychotic drugs. However, it is not clear what type of repeated effect (sensitization or tolerance) asenapine would induce, and whether such an effect is transferrable to other atypicals. In this study, …

Comparison Of Theophylline And 8-Cyclopentyltheophylline On The Heart Rates Of Neonatal Rats, Stephanie Arnold

Undergraduate Honors Theses

Neonatal apnea is a serious condition that affects the health of infants, especially those born prematurely. To stimulate breathing, methylxanthine drugs, such as theophylline and caffeine, are administered to reverse this condition in humans and avoid the use of breathing-assistance equipment. These drugs cause stimulation of the central nervous system and the heart, however, both detrimental side effects in preterm infants. Antagonism of adenosine receptors is the proposed mechanism of methylxanthine action. Synthetic chemists have produced xanthine analogs with increased affinity for adenosine receptors that could lead to respiratory stimulation while reducing cardiostimulant effects. For this study, theophylline and 8-cyclopentyltheophylline …

Investigating Apoptosis Pathway In Chronic Lymphocytic Leukemia: Stromal Influence And Therapeutic Activation, Viralkumar M. Patel

Dissertations and Theses (Open Access)

Chronic lymphocytic leukemia (CLL) is a B-cell malignancy. High levels of Bcl-2 and IAP family proteins are responsible for apoptotic-resistance and accumulation of mature CLL lymphocytes in bone-marrow, lymph nodes and peripheral blood. Besides pro-survival proteins, supporting stromal cells as well as soluble factors in the microenvironment of bone-marrow and lymph nodes provide survival advantage to CLL leukemic cells.

Though the stromal – leukemia cell interactions has been studied extensively, in-depth-knowledge on the regulation of apoptotic pathway proteins in the context of microenvironment is still limited. To address this, the first part of our study focused on comprehensive analysis of …

Importance Of Clinical Toxicology Teaching And Its Impact In Improving, Nadeem Ullah Khan, Jabeen Fayyaz, Uzma R. Khan, Asher Feroze

Department of Emergency Medicine

Objective: To assess the impact of a one-day clinical toxicology workshop in improving knowledge.
Methods: A one-day clinical toxicology workshop was conducted as a pre-conference workshop of the Annual Emergency Medicine Conference at the Aga Khan University Hospital, Karachi, in April 2012. The course was composed of poisoning-related common clinical scenarios. The pre-test and post-test understanding was used to assess the impact of the course in improving knowledge. The participants also evaluated the workshop as a whole thorough written evaluation forms. SPSS 19 was ued for statistical analysis of the data.
Result: There were 22 participants in the course. The …

High Dose, Variable Length, N-Acetylcysteine (Hinac) Therapy For Late-Presenting Acetaminophen Poisoning, Jessica K. Eygnor Do, Suprina Dorai Md, Philip W. Moore Do, J Ward Donovan Md, Keith K. Burkhart Md

Department of Emergency Medicine

No abstract provided.

Planarians Require An Intact Brain To Behaviorally React To Cocaine, But Not To React To Nicotine, Oné R. Pagán, Sean Deats, Debra Baker, Erica Montgomery, Galia Wilk, Matthew Tenaglia, Joshua Semon

Biology Faculty Publications

Planarians possess a rudimentary brain with many features in common with vertebrate brains. They also display a remarkable capacity for tissue regeneration including the complete regeneration of the nervous system. Using the induction of planarian seizure-like movements (pSLMs) as a behavioral endpoint, we demonstrate that an intact nervous system is necessary for this organism to react to cocaine exposure, but not necessary to react to nicotine administration. Decapitated planarians (Girardia tigrina) display pSLMs indistinguishable from intact worms when exposed to nicotine, but cocaine-induced pSLMs are reduced by about 95% upon decapitation. Decapitated worms recover their normal sensitivity to cocaine within …

Physiologically-Based Pharmacokinetic Modeling For Predicting Caffeine/Theophylline-Ciprofloxacin Interactions, David M. Ng, Ali Navid

STAR Program Research Presentations

Dynamics of interactions between the drugs caffeine, theophylline, and ciprofloxacin are predicted using physiologically-based pharmacokinetic (PBPK) modeling. Pharmacokinetic means the model determines where the drugs are distributed in the body over time. Physiologically-based means the anatomy and physiology of the human body are reflected in the structure and functioning of the model. Multiple drugs can interact to increase or decrease their beneficial and/or undesired effects. This is important because some common substances, such as caffeine in coffee, soft drinks, and energy drinks, are actually drugs that affect the body. Ciprofloxacin is an inhibitor of caffeine and theophylline metabolism; such inhibition …

Selected Neuropharmacology Of Resurgence, Adam D. Pyszczynski

All Graduate Theses and Dissertations, Spring 1920 to Summer 2023

The reemergence of problem behavior (i.e., relapse) is a key concern in most behavioral interventions. Resurgence refers to the reappearance of a previously rewarded behavior when reward for an alternative behavior is also discontinued. It is especially relevant to the reappearance of problem behavior because many behavioral interventions discontinue reward for aberrant behavior while simultaneously rewarding an appropriate response.

Understanding the underlying neuropharmacology of behavioral phenomena such as resurgence is important because it helps elucidate the neural processes at the root of such behavior, and also has implications for pharmacotherapies. Existing information about the neuropharmacology of resurgence is scarce, but …

Design, Synthesis And Development Of Transporter Targeting Agents For Image-Guided Therapy And Drug Delivery, Ning Tsao

Dissertations and Theses (Open Access)

The purpose of this study was to design, synthesize and develop novel transporter targeting agents for image-guided therapy and drug delivery. Two novel agents, N4-guanine (N4amG) and glycopeptide (GP) were synthesized for tumor cell proliferation assessment and cancer theranostic platform, respectively. N4amG and GP were synthesized and radiolabeled with ^99mTc and ⁶⁸Ga. The chemical and radiochemical purities as well as radiochemical stabilities of radiolabeled N4amG and GP were tested. In vitro stability assessment showed both ^99mTc-N4amG and ^99mTc-GP were stable up to 6 hours, whereas ⁶⁸Ga-GP was stable up to 2 hours. Cell culture studies …

Liposomal Fasudil, A Rho-Kinase Inhibitor, For Prolonged Pulmonary Preferential Vasodilation In Pulmonary Arterial Hypertension, Vivek Gupta, Nilesh Gupta, Imam H. Shaik, Reza Mehvar, Ivan F. Mcmurty, Masahiko Osa, Eva Nozik-Grayck, Fakhrul Ahsan

Pharmacy Faculty Articles and Research

Current pharmacological interventions for pulmonary arterial hypertension (PAH) require continuous infusions, multiple inhalations, or oral administration of drugs that act on various pathways involved in the pathogenesis of PAH. However, invasive methods of administration, short duration of action, and lack of pulmonary selectivity result in noncompliance and poor patient outcomes. In this study, we tested the hypothesis that encapsulation of an investigational anti-PAH molecule fasudil (HA-1077), a Rho-kinase inhibitor, into liposomal vesicles results in prolonged vasodilation in distal pulmonary arterioles. Liposomes were prepared by hydration and extrusion method and fasudil was loaded by ammonium sulfate-induced transmembrane electrochemical gradient. Liposomes were …

The Effects Of Selected Drugs On The Memory Recall Of Sleep Deprived Mice, Jenn Pauldurai

Capstone Research Projects

Humans often make use of the neurotransmission altering effects of drugs such as caffeine, ephedrine, and ethanol. These drugs induce changes in memory and learning ability, specifically when used for sleep deprivation. English white mice (Mus musculus) have been shown to exhibit similar cognitive changes when administered drugs while sleep deprived. A sample of 20 mice was divided into three experimental groups (each group receiving a different drug) and one control group. Maze-testing demonstrated that mice performance decreased with sleep deprivation (Treatment-1) but all groups returned to baseline performance when injected (IP) with selected drugs (Treatment-2), regardless of …

Modulation Of Synaptic Transmission By Adenosine In Layer 2/3 Of The Rat Visual Cortex In Vitro, Nicholas M. Bannon

Master's Theses

No abstract provided.

Overcoming Tumor Drug Resistance By Activating Amp-Activated Protein Kinase And Destabilizing Oncoproteins, Min Shen

Wayne State University Dissertations

Although considerable progress has been achieved in the field of cancer therapeutics, primary or acquired drug resistance remains a fundamental cause of therapeutic failure in cancer therapy. Among different mechanisms characterized that are responsible for tumor drug resistance, there is increasing evidence suggesting that dysregulation of gene expression, especially oncogene or tumor suppressor gene expression, at either gene transcription or protein synthesis level, can contribute to the drug-resistant phenotype. AMP-activated protein kinase (AMPK) is a well-known major cellular energy sensor, which negatively regulates metabolic pathways such as protein synthesis, fatty acid oxidation and glucose consumption. Activation of AMPK may suppress …

Psychologists And Medications In The Era Of Interprofessional Care: Collaboration Is Less Problematic And Costly Than Prescribing, William N. Robiner, Tim R. Tumlin, Tanya Tompkins

Faculty Publications

Increasing emphasis on interprofessionalism and teamwork in healthcare renders psychologists’ collaborations critical and invites reexamination of psychologists’ roles related to medications. The Collaboration Level outlined by the APA’s Ad Hoc Task Force is more achievable and in synch with health reform than prescription privileges (RxP). RxP remains controversial due to training and safety concerns, lacking support from health professionals, psychologists, and consumers. Differences in educational preparation of psychologists relative to prescribing professionals are discussed. Enactment of only three of 170 RxP initiatives reveals RxP to be a costly, ineffectual agenda. Alternatives (e.g., integrated care, collaboration, telehealth) increase access without risks …

Androgen Receptor-Target Genes In African American Prostate Cancer Disparities, Bi-Dar Wang, Qi Yang, Kristin Ceniccola, Fernando Bianco, Ramez Andrawis, Thomas W. Jarrett, Harold A. Frazier, Steven R. Patierno, Norman H. Lee

Pharmacology and Physiology Faculty Publications

The incidence and mortality rates of prostate cancer (PCa) are higher in African American (AA) compared to Caucasian American (CA) men. To elucidate the molecular mechanisms underlying PCa disparities, we employed an integrative approach combining gene expression profiling and pathway and promoter analyses to investigate differential transcriptomes and deregulated signaling pathways in AA versus CA cancers. A comparison of AA and CA PCa specimens identified 1,188 differentially expressed genes. Interestingly, these transcriptional differences were overrepresented in signaling pathways that converged on the androgen receptor (AR), suggesting that the AR may be a unifying oncogenic theme in AA PCa. Gene promoter …

The Analgesic And Anticonvulsant Effects Of Piperine In Mice, I A. Bukhari, M S. Alhumayyd, A L. Mahesar, A H. Gilani

Department of Biological & Biomedical Sciences

Piperine, is the major active principal of black pepper. In traditional medicine, black pepper has been used as an analgesic, anti-inflammatory agent and in the treatment of epilepsy. This study was conducted to evaluate the in vivo analgesic and anticonvulsant effects of piperine in mice. The analgesic and anticonvulsant effects of piperine were studied in mice using acetic acid-induced writhing, tail flick assay, pentylenetetrazole (PTZ)- and picrotoxin (PIC)-induced seizures models. The intraperitoneal (i.p.) administration of piperine (30, 50 and 70 mg/kg) significantly inhibited (P<0.01) the acetic acid-induced writhing in mice, similar to the effect of indomethacin (20 mg/kg i.p.). In the tail flick assay, piperine (30 and 50 mg/kg, i.p.) and morphine (5 mg/kg, i.p.) caused a significant increase (P<0.01) in the reaction time of mice. Pre-treatment of animals with naloxone (5 mg/kg i.p.), reversed the analgesic effects of both piperine and morphine in the tail flick assay. Piperine (30, 50 and 70 mg/kg, i.p.) and standard drugs, valproic acid (200 mg/kg, i.p.), carbamazepine (30 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.) significantly (P<0.01) delayed the onset of PTZ-and PIC-induced seizures in mice. These findings indicate that piperine exhibits analgesic and anticonvulsant effects possibly mediated via opioid and GABA-ergic pathways respectively. Moreover, piperine being the main constituent of black pepper, may be contributing factor in the medicinal uses of black pepper in pain and epilepsy

The Effects Of Acute Nicotine Administration On Memory Formation And Neural Activity In The Hippocampus, Perirhinal Cortex, And Medial Septum: Implications For Neurodegenerative Disorders, Matthew Wishnoff

Behavioral Neuroscience Honors Papers

Within the general public, nicotine is commonly thought of as a harmful molecule due to its role in tobacco addiction. However, nicotinic stimulation of the cholinergic system has also been shown to enhance cognitive functioning. This enhancement is thought to be caused by an increase in the release of the neurotransmitter, acetylcholine (ACh), which is responsible for mediating a variety of cognitive processes, such as REM sleep and memory formation. Recent research by Melichercik and colleagues shows that systemic nicotine administration enhances memory acquisition for both object location and object recognition memory in rats, as assessed by a modified version …

Statistical Optimization Of Mesalamine Pulsatile Release Ph Dependent Coated Pellets For Possible Ileo-Cecal Targeting, Hemant H. Gangurde, Mayur A., S. Tamizharasi, T. Sivakumar

The Thai Journal of Pharmaceutical Sciences

No abstract provided.

Permaganometric Determination Of Sumatriptan Succinate In Pure Drug And Pharmaceutical Formulation, K.N. Prashanth, K. Basavaiah, M.S. Riaghu

The Thai Journal of Pharmaceutical Sciences

Based on the reduction of permanganate by sumatriptan succinate (STS) in acidic medium, two simple, sensitive and cost-effective methods were described for the determination of STS in bulk drug and in formulation. In titrimetry (method A), STS was oxidized by a known excess of potassium permanganate (KMnO₄) in H₂SO₄ medium followed by determination of unreacted permanganate by titration with ferrous ammonium sulphate. In spectrophotometry (method B), STS was treated with a measured excess of permanganate in acid medium and the unreacted oxidant was measured at 545 nm. The molar combining ratio in titrimetry and the optimum assay conditions were studied. …

Antibacterial Activitry Of Crude Extracts From Edible Mushrooms Pleurotus Citrinopileatus And Tricholoma Crassum Berk, Prontep Chomcheon, Bancha Kheawkum, Pornsinee Sriwiset, Suphak Dulsamphan, Chalernkieat Dulsamphan

The Thai Journal of Pharmaceutical Sciences

The purpose of this research was to study antibacterial activity of crude extracts derived from the culture broths of two edible mushrooms, Pleurotus citrinopileatus and Tricholoma crassum Berk, cultivated in submerged fermentation. Potato dextrose broth (PDB) and yeast extract sucrose broth (YES) were used as culture media. Each culture filtrate was extracted and evaporated to yield a crude extract. Antibacterial activities against Escherichia coli ATCC 25922 and Staphylococcus aureus ATCC 25923 were determined by paper disc diffusion assay. Crude extract (1 mg) of P. citrinopileatus culturing PDB showed the widest inhibition zones against E. coli ATCC 25922 (34.47 ± 0.50 …

In Vitro Stimulatory Effect Of Grandiflorenic Acid Isolated From Wedelia Trilobata (L.) Leaves On L929 Fibroblast Cells, Neelam Balekar, Titpawan Nakpheng, Teerapol Srichana

The Thai Journal of Pharmaceutical Sciences

Wedelia trilobata (L.) has been used in traditional medicine in the Caribbean and Central America for stubborn wounds, sores, swelling and arthritic painful joints. The aim of the study was to evaluate the activity of grandiflorenic acid obtained from le...

Evaluation Of The Wound Healing Potential Of Albizzia Lebbeck (L.) Bark, Neelam Balekar, Dinesh Kumar, Rajesh Kumar Upadhyay

The Thai Journal of Pharmaceutical Sciences

The present study was performed to substantiate the traditional claim of the wound healing activity of stem bark of Albizzia lebbeck Linn. in rats. The effects of aqueous and ethanolic extracts of stem bark of A. lebbeck (5% and 10% w/v topically and 250...

Development And Validation Of Hptlc Densitometric Method For Simultaneous Determination Of Antazoline Hydrochloride And Tetryzoline Hydrochloride In Eye Drop And Its Application As Stability Indicator, Anbessa Bekele Ariaya Hymete, Adnan A. Bekhit

The Thai Journal of Pharmaceutical Sciences

A sensitive, selective, precise, accurate and stability indicating high-performance thin layer chromatographic (HPTLC)-densitometric method for analysis of antazoline hydrochloride and tetryzoline hydrochloride was developed. The method employed HPTLC al...

Association Of Abcb1 Polymorphism With Lamotrigine-Resistant Epilepsy In Thais, Korakot Buathet, Yotin Chinvarun, Somchai Towanabut, Pornpimol Kijsanayotin

The Thai Journal of Pharmaceutical Sciences

Along with clinical and environmental factors, genetic variability in P-glycoprotein (P-gp) encoded by the ATP-binding cassette (ABC)B1 gene may influence inter-individual variability in antiepileptic drug response by limiting drug absorption and brain a...