Pharmacology, Toxicology and Environmental Health Commons^™

Role Of Hyperglycemia And Aldosterone On Renal Ace2 And Albuminuria In Db/Db Mice, Harshita Chodavarapu

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Diabetic nephropathy (DN) is one of the microvascular complications of type II diabetes and a leading cause for the development of end stage renal disease. Renin angiotensin system (RAS) plays a pivotal role in the development and progression of diabetic nephropathy. Hyperglycemia activates RAS and increases tissue and circulating levels of angiotensin II (Ang II) and aldosterone. A new component of RAS, angiotensin converting enzyme 2 (ACE2), has been shown to be renoprotective in early stages of diabetes. The aim of this study is to test the hypothesis that strict glycemic control using rosiglitazone or treatment with mineralocorticoid receptor (MR) …

Analysis Of Archived Dried Blood Spots By Mass Spectrometry For Vitamin D And Real-Time Pcr For Its Enzymes And Receptor, Amod N. Joshi

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Vitamin D is an essential micronutrient required for maintenance of the skeletal system and its deficiency leads to diminished availability of calcium for maintaining bone mineralization. Vitamin D deficiency (VDD) during pregnancy and/or in early infancy can lead to rickets and a fragile bone state resulting in fractures with minimal forces. Such multiple unexplained fractures (MUF) present in infants at less than 6 months of age are often misdiagnosed as cases of child abuse. Therefore, it is important to evaluate the status of vitamin D in early infancy. The analysis of dried blood spots (DBS) provides a unique screening method …

Response Of Neuroinflammatory And Neurodegenerative Markers Following Sub-Lethal Sarin Exposure And Subsequent Treatment Via An In-Vivo Caspase Inhibitor, Douglas F. Chmura

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Organophosphorus nerve agents are amongst the most deadly chemical compounds ever synthesized. Sarin is an organophosphate (OP) ester that irreversibly forms a phosphoester bond at the active site of acetylcholinesterase and thereby induces a rapid and lethal cholinergic crisis. It remains an active threat to vulnerable civilian populations due to its ease of synthesis and known use by rogue nations and terrorist groups. Death is the most extreme consequence of sarin toxicity. Current treatments fail to provide protection against progressive cognitive impairments years after mild exposure. Q-VD-OPh is an in-vivo caspase inhibitor with potent anti-apoptotic and anti-inflammatory properties. In this …

Synthesis, Characterization And Manipulation Of Creighton Silver Nanoparticles For Future Cytotoxicity Studies, Sesha Lakshmi Paluri

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Nowadays, 24% of the nanomaterial-based consumer products contain silver nanoparticles (AgNPs) and exploit the well-known antimicrobial properties of silver. Although AgNPs have a wide range of biomedical research and industrial applications, very little is known about their toxicity. The main goal of this study is to synthesize, characterize and manipulate Creighton colloidal AgNPs for future cytotoxicity studies. These "naked" AgNPs were free from chemically aggressive capping/stabilizing agents, reaction byproducts or organic solvents. To achieve this goal, colloidal AgNPs were successfully: a) synthesized in large volumes (5L) using a slightly modified Creighton method by the reduction of silver nitrate with sodium …

Low Dose Nerve Agent Sarin Causes Dilated Cardiomyopathy And Autonomic Imbalance In Mice, Swapnil Vijay Shewale

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Sarin, a lethal chemical nerve agent, may be a causative factor in multifactorial syndrome implicated in the Gulf War and Tokyo terrorist attacks. While high dose results in seizure and death, low dose exposure may lead to autonomic imbalance and chronic cardiac pathologies. In the present study, echocardiography and electrocardiography were used to examine the late onset effects of a low dose sarin on cardiac structure and function in mice. Stress responsiveness of the hypothalamic pituitary adrenal (HPA) axis was also tested. Findings demonstrate changes consistent with a dilated cardiomyopathy, including left ventricular dilatation, reduced contractility, and altered electrophysiological and …

Synthesis, Biochemical And Molecular Modelling Studies Of Antiproliferative Azetidinones Causing Microtubule Disruption And Mitotic Catastrophe, Niamh O'Boyle, Miriam Carr, Lisa M. Greene, Niall O. Keely, Andrew Js Knox, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan

Articles

The structure-activity relationships of antiproliferative β-lactams, focusing on modifications at the 4-position of the β-lactam ring, is described. Synthesis of this series of compounds was achieved utilizing the Staudinger and Reformatsky reactions. The antiproliferative activity was assessed in MCF-7 cells, where the 4-(4-ethoxy)phenyl substituted compound 26 displayed the most potent activity with an IC₅₀ value of 0.22 μM. The mechanism of action was demonstrated to be by inhibition of tubulin. Cell exposure to combretastatin A-4 and 26 led to arrest of MCF-7 cells in the G2/M phase of the cell cycle and induction of apoptosis. Additionally, mitotic catastrophe for …

Lead Identification Of Β-Lactam And Related Imine Inhibitors Of The Molecular Caperone Heat Shock Protein 90, Niamh O'Boyle, Andrew Js Knox, Trevor P. Price, D. Clive Williams, Daniela M. Zisterer, David G. Lloyd, Mary J. Meegan

Articles

Heat shock protein 90 is an emerging target for oncology therapeutics. Inhibitors of this molecular chaperone, which is responsible for the maintenance of a number of oncogenic proteins, have shown promise in clinical trials and represent a new and exciting area in the treatment of cancer. Heat shock protein 90 inhibitors have huge structural diversity, and here we present the identification of inhibitors based on β-lactam and imine templates. β-Lactam 5 and imines 12 and 18 exhibit binding to heat shock protein 90-α with IC₅₀ values of 5.6 μM, 14.5 μM and 22.1 μM respectively. The binding affinity displayed …

Effects Of Marmin Isolated From Aegle Marmelos Correa On L-Histidine Decarboxylase Enzyme In Rbl-2h3 Cells, Agung Endro Nugroho, Novrizal Abdi, Sugeng Riyanto, Kazutaka Maeyama, Zullies Ikawati

The Thai Journal of Pharmaceutical Sciences

Marmin or (7-(6’,7’-dihydroxygeranyl-oxy) coumarin is a compound isolated from Aegle marmelos Correa, in the study, we investigated the effects of marmin on the L-histidine decarboxylase (HDC), a rate-limiting histamine synthesizing enzyme, in rat ma...

Rapid Titrimetric And Spectrophotometric Assay Of Tramadol In Bulk Drug And In Formulation Using N-Bromosuccinimide And Methyl Orange As Reagents, K. B. Vinay, H. D., N. Rajendraprasad, M. S. Raghu, P. J. Ramesh, M. X. Cijo, K. Basavaiah

The Thai Journal of Pharmaceutical Sciences

Tramadol is a centrally acting analgesic used for prevention and treatment of moderate to severe pain. Two simple, rapid and sensitive methods by titrimetric and spectrophotometric techniques are described for the determination of tramadol hydrochloride ...

Allylmercaptocaptopril Attenuates Sodium Selenite Induced Experimental Cataractogenesis: An In Vitro And In Vivo Study, K. S. Lakshmi, Shrinivas Sharma

The Thai Journal of Pharmaceutical Sciences

The present study sought to assess the efficacy of the allylmercaptocaptopril เท preventing seleniteinduced cataractogenesis in an experimental setting. The first, in vitro phase of the study was performed on lenses from Wistar rats incubated for 24 ...

Influence Of Surfactants On Crystal Form Of Mefenamic Acid, Kaival P., Kulkarni P.K., Mudit Dixit, Ashwini G. Kni

The Thai Journal of Pharmaceutical Sciences

Mefenamic acid is an anti inflammatory and poorly water-soluble drug. Since the drug powder can stick to any type of surface, and is not easy to handle in granulation and tabletting process, it is more desirable to recrystallize the mefenamic acid in suc...

Hptlc-Densitometric Method Development And Validation For Simultaneous Determination Of Lamivudine, Nevirapine And Zidovudine In Fixed Dose Combinations, Gebremedhin Solomon, Ariaya Hymete, Abdel-Maaboud I. Mohamed, Adnan A. Bekhit

The Thai Journal of Pharmaceutical Sciences

In this study an HPTLC-densitometric method was developed for the simultaneous determination of lamivudine, nevirapine and zidovudine in pharmaceutical dosage forms which are used widely as first line HIV/AIDS treatment. Chromatographic separation of the...

Ion-Pair Titrimetric Assays Of Quetiapine Fumarate In Pharmaceuticals Using Sodium Tetraphenylboron And Sodium Lauryl Sulphate, N. Rajendraprasad, K. Basavaiah, Kanakapura B. Vinay

The Thai Journal of Pharmaceutical Sciences

Two simple, rapid, precise and accurate titrim etric methods employing sodium tetraphenylboron (STPB) and sodium lauryl sulphate (SLS) as titrants are described for the quantitative determination of quetiapine fumarate (QTF) in bulk drug and tablets. The...

Simultaneous Determination Of Ampicillin Sodium And Sulbactam Sodium In Binary Mixtures And Commercial Dosage Forms Using Chemometrics - Assisted Spectrophotometric Techniques, Zelalem M, Abdel-Maaboud I., Adnan A. Bekhit, Ariaya Hymete

The Thai Journal of Pharmaceutical Sciences

The binary mixture of ampicillin sodium and sulbactam sodium is officially analyzed by HPLC but can not be simultaneously determined by the normal spectrophotometric techniques since their absorption spectra have a strong degree of overlapping. The curre...

Minocycline And Magnesium In Combination Attenuates Oxidative Stress And Decreases Ischemic Neuronal Damage In Vivo, Pallab Bhattacharya, Anand Kr., Sudip Paul

The Thai Journal of Pharmaceutical Sciences

A neuroprotective strategy through a combination therapy is always being superior to any other singular therapeutic interventions, as these acts through a multifaceted approach within the brain during focal cerebral ischemia. Therefore, the development o...

Use Of Bromate - Bromide Mixture As A Reagent For The Determination Of Dothiepin Hydrochloride In Pharmaceuticals, Sameer A.M. Abdulrahman, Kanakapura Basavaiah

The Thai Journal of Pharmaceutical Sciences

The present study describes one titrimetric and two spectrophotometric methods for the determination of dothiepin hydrochloride (DOTH) in bulk drug and in tablets. The methods employed bromate-bromide mixture in acid medium as an oxidimetric as well as b...

Synthesis And Cytotoxicity Study Of Magnetoliposomes Loaded Doxorubicin, Surachai Ngamratanapaiboon, Issara Sramala, Wichet Leelamanit

The Thai Journal of Pharmaceutical Sciences

The limitation of clinical use of doxorubicin is its side effects especially a cumulative dose-dependent cardiotoxicity. To overcome this, doxorubicin can be targeted to accumulate on the site of action and limit dispersion in healthy tissue. Magnetic li...

Antioxidant Properties Of Squeezed Mangosteen Juice, Monrudee Sukma, Tanasait Ngawhirunpat, Praneet Opanasopit, Pongpun Siripong

The Thai Journal of Pharmaceutical Sciences

The aim of this study was to investigate antioxidant effects of squeezed mangosteen (Garcinia mangostana) juice as preferable diet for human consumption. Mangosteen juice was prepared from the aril part. Antioxidant properties were evaluated by total ant...

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The Thai Journal of Pharmaceutical Sciences

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Identification Of Activities Involved In Cag/Ctg Repeat Instability, Nelson Lap Shun Chan

University of Kentucky Doctoral Dissertations

CAG/CTG repeat instability is associated with at least 14 neurological disorders, including Huntington’s disease and Myotonic dystrophy type 1. In vitro and in vivo studies have showed that CAG/CTG repeats form a stable hairpin that is believed to be the intermediate for repeat expansion and contraction.

Addition of extra DNA is essential for repeat expansion, so DNA synthesis is one of the keys for repeat expansion. In vivo studies reveal that 3’ CTG slippage with subsequent hairpin formation (henceforth called the 3’ CTG slippage hairpin) occurs during DNA synthesis. It is proposed that hairpin tolerance machinery is activated because prolonged …