Chemicals and Drugs Commons^™

A Single Center Observational Study On Emergency Department Clinician Non-Adherence To Clinical Practice Guidelines For Treatment Of Uncomplicated Urinary Tract Infections, Catherine Zatorski, Mark Zocchi, Sara Cosgrove, Cynthia Rand, Gillian Brooks, Larissa May

Emergency Medicine Faculty Publications

Background

The Emergency Department (ED) is a frequent site of antibiotic use; poor adherence with evidence-based guidelines and broad-spectrum antibiotic overuse is common. Our objective was to determine rates and predictors of inappropriate antimicrobial use in patients with uncomplicated urinary tract infections (UTI) compared to the 2010 International Clinical Practice Guidelines (ICPG).

Methods

A single center, prospective, observational study of patients with uncomplicated UTI presenting to an urban ED between September 2012 and February 2014 that examined ED physician adherence to ICPG when treating uncomplicated UTIs. Clinician-directed antibiotic treatment was compared to the ICPG using a standardized case definition for …

Circulating Fibroblast Growth Factor-2, Hiv-Tat, And Vascular Endothelial Cell Growth Factor-A In Hiv-Infected Children With Renal Disease Activate Rho-A And Src In Cultured Renal Endothelial Cells., Jharna R Das, J Silvio Gutkind, Patricio E. Ray

Pediatrics Faculty Publications

Renal endothelial cells (REc) are the first target of HIV-1 in the kidney. The integrity of REc is maintained at least partially by heparin binding growth factors that bind to heparan sulfate proteoglycans located on their cell surface. However, previous studies showed that the accumulation of two heparin-binding growth factors, Vascular Endothelial Cell Growth Factor-A (VEGF-A) and Fibroblast Growth Factor-2 (FGF-2), in combination with the viral protein Tat, can precipitate the progression of HIV-renal diseases. Nonetheless, very little is known about how these factors affect the behavior of REc in HIV+ children. We carried out this study to determine how …

Microvascular Endothelial Cells-Derived Microvesicles Imply In Ischemic Stroke By Modulating Astrocyte And Blood Brain Barrier Function And Cerebral Blood Flow, Qunwen Pan, Caixia He, Hua Liu, Xiaorong Liao, Bingyan Dai, Yanfang Chen, Yi Yang, Bin Zhao, Ji C. Bihl, Xiaotang Ma

Pharmacology and Toxicology Faculty Publications

Background

Endothelial cell (EC) released microvesicles (EMVs) can affect various target cells by transferring carried genetic information. Astrocytes are the main components of the blood brain barrier (BBB) structure in the brain and participate in regulating BBB integrity and blood flow. The interactions between ECs and astrocytes are essential for BBB integrity in homeostasis and pathological conditions. Here, we studied the effects of human brain microvascular ECs released EMVs on astrocyte functions. Additionally, we investigated the effects of EMVs treated astrocytes on regulating BBB function and cerebral ischemic damage.

Results

EMVs prepared from ECs cultured in normal condition (n-EMVs) or …

Comparison Of Drug Delivery With Autoinjector Versus Manual Prefilled Syringe And Between Three Different Autoinjector Devices Administered In Pig Thigh, Robert Hill, John Wilmot, Beth Belluscio, Kevin Cleary, David Lindisch, Robin Tucker, Emmanuel Wilson, Rajesh Shukla

Radiology Faculty Publications

Parenteral routes of drug administration are often selected to optimize actual dose of drug delivered, assure high bioavailability, bypass first-pass metabolism or harsh gastrointestinal environments, as well as maximize the speed of onset. Intramuscular (IM) delivery can be preferred to intravenous delivery when initiating intravenous access is difficult or impossible. Drugs can be injected intramuscularly using a syringe or an automated delivery device (autoinjector). Investigation into the IM delivery dynamics of these methods may guide further improvements in the performance of injection technologies. Two porcine model studies were conducted to compare differences in dispersion of injectate volume for different methods …

Investigation Of Tattoo Pigments By Raman Spectroscopy, Betsy Jean Yakes, Tara Jade Michael, Marianita Perez-Gonzalez, Bhakti Petigara Harp

United States Food and Drug Administration: Publications

As a result of the increase in the practice of tattooing, the US Food and Drug Administration has identified a need for improved analytical methods to detect the pigments and potential impurities in the inks. Raman spectroscopy allows for nondestructive identification of compounds and is commonly used in art, archaeology, and forensics; however, the technique has only limitedly been applied to the identification of tattoo pigments. In this study, approximately 30 inorganic, organometallic, and organic pigmentswere evaluated with Raman spectroscopy by using 532, 633, and 780-nmlasers. Individual optimization of the instrumental parameters was performed for each pigment in order to …

Bacterial Endotoxin Detection In Hyaluronic Acid-Based Medical Devices, Larissa F. Baeva, Srilekha Sarkar Das, Victoria M. Hitchins

United States Food and Drug Administration: Publications

A simple and rapid method has been developed for testing bacterial endotoxin in hyaluronic acid (HA)-based medical devices. High-molecular-weight HA (HMW HA) in solution or HA-based medical devices was digested by the enzyme hyaluronidase to reduce solution viscosity by truncating the long chains of HA and to test for bacterial endotoxin. The bacterial endotoxin level was detected and measured by kinetic chromogenic Limulus Amebocyte Lysate (LAL) assay. The method was applied to two different ophthalmic viscosurgical devices (OVDs) and one dermal filler, and may easily be adapted to use with up to 3% HA solutions and other HA-based medical devices.

Privacy And Accountability In Black-Box Medicine, Roger Allan Ford, W. Nicholson Price Ii

Law Faculty Scholarship

Black-box medicine—the use of big data and sophisticated machine learning techniques for health-care applications—could be the future of personalized medicine. Black-box medicine promises to make it easier to diagnose rare diseases and conditions, identify the most promising treatments, and allocate scarce resources among different patients. But to succeed, it must overcome two separate, but related, problems: patient privacy and algorithmic accountability. Privacy is a problem because researchers need access to huge amounts of patient health information to generate useful medical predictions. And accountability is a problem because black-box algorithms must be verified by outsiders to ensure they are accurate and …

Endothelial Progenitor Cells And Neural Progenitor Cells Synergistically Protect Cerebral Endothelial Cells From Hypoxia/Reoxygenation-Induced Injury Via Activating The Pi3k/Akt Pathway, Jinju Wang, Yusen Chen, Yi Yang, Xiang Xiao, Shuzhen Chen, Cheng Zhang, Bradley S. Jacobs, Bin Zhao, Ji C. Bihl, Yanfang Chen

Pharmacology and Toxicology Faculty Publications

Background

Protection of cerebral endothelial cells (ECs) from hypoxia/reoxygenation (H/R)-induced injury is an important strategy for treating ischemic stroke. In this study, we investigated whether co-culture with endothelial progenitor cells (EPCs) and neural progenitor cells (NPCs) synergistically protects cerebral ECs against H/R injury and the underlying mechanism.

Results

EPCs and NPCs were respectively generated from inducible pluripotent stem cells. Human brain ECs were used to produce an in vitro H/R-injury model. Data showed: 1) Co-culture with EPCs and NPCs synergistically inhibited H/R-induced reactive oxygen species (ROS) over-production, apoptosis, and improved the angiogenic and barrier functions (tube formation and permeability) in …

Analyses Of Endothelial Cells And Endothelial Progenitor Cells Released Microvesicles By Using Microbead And Q-Dot Based Nanoparticle Tracking Analysis, Jinju Wang, Yun Zhong, Xiaotang Ma, Xiang Xiao, Chuanfang Cheng, Yusen Chen, Ifeanyi Iwuchukwu, Kenneth J. Gaines, Bin Zhao, Shiming Liu, Jeffrey B. Travers, Ji C. Bihl, Yanfang Chen

Pharmacology and Toxicology Faculty Publications

Accurate analysis of specific microvesicles (MVs) from biofluids is critical and challenging. Here we described novel methods to purify and detect MVs shed from endothelial cells (ECs) and endothelial progenitor cells (EPCs) by combining microbeads with fluorescence quantum dots (Q-dots) coupled nanoparticle tracking analysis (NTA). In the in vitroscreening systems, we demonstrated that 1) anti-CD105 (EC marker) and anti-CD34 (EPC marker) conjugated-microbeads had the highest sensitivity and specificity for isolating respective MVs, which were confirmed with negative controls, CD41 and CD235a; 2) anti-CD144 (EC marker) and anti-KDR (EPC marker) conjugated-Q-dots exhibited the best sensitivity and specificity for their respective …

Ascorbic Acid For The Treatment Of Rasburicase Induced Methemoglobinemia In The Setting Of Acute Renal Failure, David J. Reeves, Lindsay Saum, Ruemu Birhiray

Scholarship and Professional Work – COPHS

Purpose A case of apparent rasburicase-induced methemoglobinemia and acute kidney injury treated with i.v. ascorbic acid because of suspected glucose-6-phosphate dehydrogenase (G6PD) deficiency is reported.

Summary A 46-year-old African-American man with a recent diagnosis of multiple myeloma and renal insufficiency was admitted to the hospital with a cough, hemoptysis, and fatigue. His medical history included hypertrophic cardiomyopathy, ventricular tachycardia, attention deficit/hyperactivity disorder, and pleural effusion. No treatments for multiple myeloma were started before hospital admission. Levofloxacin 750 mg orally daily for possible pneumonia, lenalidomide 10 mg orally daily, and dexamethasone 20 mg orally weekly were administered. Plasmapheresis was also initiated. …

Endocidal Regulation Of Secondary Metabolites In The Producing Organisms, Shiyou Li, Ping Wang, Wei Yuan, Zushang Su, Steven H. Bullard

Faculty Publications

Secondary metabolites are defined as organic compounds that are not directly involved in the normal growth, development, and reproduction of an organism. They are widely believed to be responsible for interactions between the producing organism and its environment, with the producer avoiding their toxicities. In our experiments, however, none of the randomly selected 44 species representing different groups of plants and insects can avoid autotoxicity by its endogenous metabolites once made available. We coined the term endocides (endogenous biocides) to describe such metabolites that can poison or inhibit the parent via induced biosynthesis or external applications. Dosage-dependent endocides can selectively …

Effect Of The Il-1 Receptor Antagonist Kineret® On Disease Phenotype In Mdx Mice., Margaret E. Benny Klimek, Arpana Sali, Sree Rayavarapu, Jack Van Der Meulen, Kanneboyina Nagaraju

Genomics and Precision Medicine Faculty Publications

Duchenne muscular dystrophy (DMD) is an X-linked muscle disease caused by mutations in the dystrophin gene. The pathology of DMD manifests in patients with progressive muscle weakness, loss of ambulation and ultimately death. One of the characteristics of DMD is muscle inflammation, and dystrophin-deficient skeletal muscles produce higher levels of the pro-inflammatory cytokine interleukin 1β (IL-1β) in response to toll like receptor (TLR) stimulation compared to controls; therefore, blocking the IL-1β pathway could improve the disease phenotype in mdx mice, a mouse model of DMD. Kineret® or IL-1Ra is a recombinant IL-1 receptor antagonist approved by the FDA for treating …

Biosimilars: Potential Implications For Clinicians, Misty G. Eleryan, Sophia Akhiyat, Monica Rengifo-Pardo, Alison Ehrlich

Dermatology Faculty Publications

With the expiration of patent protection for several biologics looming, the production of highly similar therapeutic agents has begun to emerge on the pharmaceutical market. These alternative drugs are referred to as biosimilars. Many anticipate that the introduction of these agents will result in a reduction in health care costs, which may create a more affordable biopharmaceutical market and also improve patient access. In contrast to generics, which are exact copies of their original products, biosimilars are not identical to their reference products. Due to concern about the safety and efficacy of biosimilars, separate regulatory approval pathways have been developed …

Micrornas Are Involved In The Development Of Morphine-Induced Analgesic Tolerance And Regulate Functionally Relevant Changes In Serpini1., Jenica D. Tapocik, Kristin Ceniccola, Cheryl L. Mayo, Melanie L. Schwandt, Matthew Solomon, Bi-Dar Wang, Truong V. Luu, Jacqueline Olender, Thomas Harrigan, Thomas M. Maynard, Greg I. Elmer, Norman H. Lee

Pharmacology and Physiology Faculty Publications

Long-term opioid treatment results in reduced therapeutic efficacy and in turn leads to an increase in the dose required to produce equivalent pain relief and alleviate break-through or insurmountable pain. Altered gene expression is a likely means for inducing long-term neuroadaptations responsible for tolerance. Studies conducted by our laboratory (Tapocik et al., 2009) revealed a network of gene expression changes occurring in canonical pathways involved in neuroplasticity, and uncovered miRNA processing as a potential mechanism. In particular, the mRNA coding the protein responsible for processing miRNAs, Dicer1, was positively correlated with the development of analgesic tolerance. The …

Can A Metallated Cyclen Species Be Used To Prepare New Odorants?, Jalynn Taylor-Farmer

UROP Posters

Scientists in the fragrance industry are constantly searching for new odors to create as well as new, more efficient processes to create them. Scientists mainly look for new ways to synthesize fragrances that will reduce the impact on the environment, produce them at lower costs, produce higher yields, and sometimes to produce a more potent odor [4]. In this research, we investigated the use of metallic macrocycles and/or metal-dioxygen chemistry to prepare new fragrances.

Cyclen (1,4,7,10-tetraazacyclododecane) has significant uses in many pharmaceutical and medicinal research developments such as advances in targeted cancer and Alzheimer’s agents. Macrocyclic amines like cyclen are …

Uvb Generates Microvesicle Particles Via Platelet-Activating Factor-Receptor Signaling: A Novel Pathway By Which A Skin-Specific Stimulus Exerts Systemic Effects, Jeffrey B. Travers, Christine M. Rapp, Katherine E. Fahy, Christina E. Borchers, Richard Simman, Langni Liu, Yanfang Chen, Ji C. Bihl

Pharmacology and Toxicology Faculty Publications

Though Ultraviolet B radiation (290-320 nm; UVB) exerts profound systemic effects, it is absorbed only in the epidermis. One important question in photobiology is how UVB signals are emanated from the epidermis. Microvesicle particles (MVP) are small (200-1000nm diameter) membrane-bound vesicles released by numerous cell types and can be found in the circulation. MVP can contain both nuclear and cytoplasmic components and are thought to provide a mechanism by which cells transmit signals systemically. Though various stressors have been demonstrated to generate MVP, the ability of UVB to exert this effect has not been demonstrated. Previous studies from ours and …

The Novel Methods For Analysis Of Exosomes Released From Endothelial Cells And Endothelial Progenitor Cells, Jinju Wang, Runmin Guo, Yi Yang, Bradley S. Jacobs, Suhong Chen, Ifeanyi Iwuchukwu, Kenneth J. Gaines, Yanfang Chen, Richard Simman, Guiyuan Lv, Keng Wu, Ji C. Bihl

Pharmacology and Toxicology Faculty Publications

Exosomes (EXs) are cell-derived vesicles that mediate cell-cell communication and could serve as biomarkers. Here we described novel methods for purification and phenotyping of EXs released from endothelial cells (ECs) and endothelial progenitor cells (EPCs) by combining microbeads and fluorescence quantum dots (Q-dots®) techniques. EXs from the culture medium of ECs and EPCs were isolated and detected with cell-specific antibody conjugated microbeads and second antibody conjugated Q-dots by using nanoparticle tracking analysis (NTA) system. The sensitivities of the cell origin markers for ECs (CD105, CD144) and EPCs (CD34, KDR) were evaluated. The sensitivity and specificity were determined by using positive …

Development Of A Chemical Genetic Screen To Determine Synergistic Compounds With Laromustine In Treating Glioblastoma Multiforme Cultured Cells, Ryan Weeks

Honors Theses

Laromustine is a chemotherapeutic sulfonylhydrazine prodrug used in clinical trials to treat acute myeloid leukemia (AML) and glioblastoma multiforme (GBM). While treatment of AML with laromustine has more demonstrative clinical success, there are enough promising data against GBM to pursue additional pre-clinical and clinical experiments. To determine the synergistic effects caused by treating cultured GBM cells with laromustine and a library of FDA-approved compounds, a chemical genetic screen was developed. To optimize the screen, optimal cultured GBM cell seed density, growth period and maximum well capacity were determined. The treatment period for a lethal dose of laromustine in cultured GBM …

The Influence Of Safety, Efficacy, And Medical Condition Severity On Natural V. Synthetic Drug Preference, Brian P. Meier, Courtney M. Lappas

Psychology Faculty Publications

Research indicates that there is a preference for natural v. synthetic products, but the influence of this preference on drug choice in the medical domain is largely unknown. We present 5 studies in which participants were asked to consider a hypothetical situation in which they had a medical issue requiring pharmacological therapy. Participants ( N = 1223) were asked to select a natural, plant-derived, or synthetic drug. In studies 1a and 1b, approximately 79% of participants selected the natural v. synthetic drug, even though the safety and efficacy of the drugs were identical. Furthermore, participants rated the natural drug as …

Is The High Frequency Of Postoperative Atrial Fibrillation After Cardiac And Lung Surgeries Related To Hypomagnesemia And Releases Of Ceramides And Platelet-Activating Factor?, Burton M. Altura, Nilank C. Shah, Gatha J. Shah, Aimin Zhang, Wenyan Li, Bella T. Altura

Touro College of Osteopathic Medicine (Middletown) Publications and Research

The authors discuss the possible role of hypomagnesemia, ceramides and platelet-activating factor in the incidence of postoperative atrial fibrillation after cardiac and lung surgeries.

Postprandial Paraoxonase 1 Activity Following Consumption Of Recommended Amounts Of Mixed Meals In Healthy Males, Noriko Kameyama, Chizuko Maruyama, Kazuhiko Kotani, Russell Caccavello, Alejandro Gugliucci, Sadako Matsui, Taro Maruyama

Faculty Publications & Research of the TUC College of Osteopathic Medicine

Aim: Postprandial lipid level increases induce oxidative stress, which is involved in atherogenesis. The antioxidant properties of paraoxonase 1 (PON1) have attracted attention. However, changes in postprandial PON1 levels differ across prior studies, and changes in PON1 lactonase activity, potentially relevant to PON1 physiology, after the consumption of ordinary meals are unknown. Herein we evaluated postprandial serum lipid levels and PON1 changes following mixed-meal consumption of the amounts recommended for ordinary meals.
Methods: Nine healthy male volunteers consumed three different meals in a randomized cross-over design. The test meals were as follows: S, white rice; SMF, S with …

Medical Marijuana And Pain Management: The Physician’S Catch 22, James M. Mckivigan

College of Health & Human Services (TUN) Publications and Research

In this paper, concerns connected to the usage of marijuana in treating patients are extensively analyzed. It is revealed that physicians have been in conflict with the federal government as to whether to use cannabis for medical purposes or if they should consider prescribing other drugs. A large percentage of physicians admit that marijuana could be an effective drug in treating patients, especially those with acute pain, nausea, AIDS, muscle spasms, and cancer, among other ailments. However, patients and physicians are scared of the strict laws that criminalize the use of marijuana for medical and recreational purposes. Physicians are also …

Pharmacokinetics And Distribution In Interstitial And Pulmonary Epithelial Lining Fluid Of Danofloxacin In Ruminant And Preruminant Calves, D. A. Mzyk, R. E. Baynes, K. M. Messenger, M. Martinez, G. W. Smith

United States Food and Drug Administration: Publications

The objective of this study was to compare active drug concentrations in the plasma vs. different effector compartments including interstitial fluid (ISF) and pulmonary epithelial lining fluid (PELF) of healthy preruminating (3-week-old) and ruminating (6-month-old) calves. Eight calves in each age group were given a single subcutaneous (s.c.) dose (8 mg/kg) of danofloxacin. Plasma, ISF, and bronchoalveolar lavage (BAL) fluid were collected over 96 h and analyzed by high-pressure liquid chromatography. PELF concentrations were calculated by a urea dilution assay of the BAL fluids. Plasma protein binding was measured using a microcentrifugation system. For most preruminant and ruminant calves, the …

Regulation Of Chronic And Acute Inflammatory Disease By Microrna And Microbiota, Pegah Mehrpouya-Bahrami

Theses and Dissertations

Inflammation is implicated in cancer development, degenerative diseases, allergies as well as artherosecelorsis. Dysregulated immune responses lead to chronic inflammation and tissue damage. Finding the ways to terminate inflammatory responses when no longer needed, demands further investigation. Herein, we investigated the modulation of acute and chronic inflammatory disease models by inducing antiinflammatory state. Acute inflammatory model was induced with SEB, an enterotoxin produced by a ubiquitous Gram-positive coccus, Staphylococcus aureus (S. aureus), which exerts profound toxic effects on the immune system, which leads to the cytokine storm and adverse immune response. SEB is the main cause of nosocomial infections, acute …

Differences In Resting-State Functional Connectivity Of Chronic Migraine, With And Without Medication Overuse Headache, And The Effectiveness Of Sphenopalatine Ganglion Block As A Treatment For Repairing Dysfunctional Connectivity., Kaitlin Krebs

Theses and Dissertations

Chronic Migraine (CM) is a debilitating neurological condition that occurs when the migraine frequency progresses to a chronic state of more than 15 headache days per month. The overuse of analgesic medication (MOH) is one of the most prominent risk factor of this chronification and little is known about why it is a cause. The repetitive inhibition of the Sphenopalatine Ganglion is one promising treatment that is used to treat chronic migraine. The purpose of this study is to determine if a specific pattern of disruption is present for chronic migraine, both with and without medication overuse headache, and if …

Morphogenic Effects Of Dopamine In Cultured Rat Hippocampal Astrocytes, Ashley L. Galloway

Theses and Dissertations

Dopamine is critical for processing of reward and addictive behaviors brought about by drugs of abuse. Scientific investigation of drugs of abuse and their effects on CNS function has traditionally been directed at understanding the role of neurons. However, astrocytes, which constitute approximately half of all human brain cells, play a dynamic role in many essential nervous system functions, including neurotransmission, ion homeostasis, and immune defense. Dopamine effects on astrocytes have been historically understudied, yet research indicates that astrocytes express dopamine receptors and are sensitive to dopaminergic activity. Importantly, astrocytes, comprise a morphologically heterogeneous population of cells, and a distinction …

The Role Of Epidermal Stem/Progenitor-Like Cells In Hpv-Mediated Pre-Neoplastic Transformation, Yvon L. Woappi

Theses and Dissertations

The role of epidermal basal stem cells in dysplasia is a matter of great interest in the human papillomavirus (HPV)-driven cancers. To assess the relationship between “stemness” and HPV-mediated transformation, we made use of 3-D suspension culture and fluorescence activated cell sorting (FACS) to purify stem/progenitor-like cells from primary normal human keratinocyte (NHKc) cultures. We found that NHKc cells derived from multicellular keratinocyte spheroids were enriched for a basal subpopulation of epidermal stem-like cells, that could be maintained for prolonged time in culture and used to conduct transfection experiments with full-length HPV16 DNA. Thus, by using these stem cell enrichment …

Deciphering The Interacting Regions And Functions Of The Rad51d-Nono Protein Complex During Dna Damage Response, Latarsha Porcher

Theses and Dissertations

Genomic instability is one of the major components represented in the “Hallmarks of Cancer.” DNA interstrand crosslinks and double-stranded breaks are two of the most severe causes of genomic instability. Homologous recombination (HR) plays a major role in resolving both types of DNA lesions, requiring a homologous template and the RAD51 paralog complex of proteins. One member of this complex is the RAD51D ovarian cancer susceptibility gene product. To better elucidate RAD51D modifications and functions, several protein interaction screens were performed, and one of the novel proteins identified was NONO (a.k.a. p54nrb). Decreased expression of either RAD51D or NONO conferred …

Multiple Sirna Delivery Against Cell Cycle And Anti-Apoptosis Proteins Using Lipid-Substituted Polyethylenimine In Triplenegative Breast Cancer And Non-Malignant Cells, Manoj B. Parmar, Bárbara E. Arteaga Ballesteros, Timothy Fu, Remant Bahadur Kc, Hamidreza Montazeri Aliabadi, Judith C. Hugh, Raimar Löbenberg, Hasan Uludag

Pharmacy Faculty Articles and Research

Conventional breast cancer therapies have significant limitations that warrant a search for alternative therapies. Short-interfering RNA (siRNA), delivered by polymeric biomaterials and capable of silencing specific genes critical for growth of cancer cells, holds great promise as an effective and more specific therapy. Here, we employed amphiphilic polymers and silenced the expression of two cell cycle proteins, TTK and CDC20, and the anti-apoptosis protein survivin to determine the efficacy of polymer-mediated siRNA treatment in breast cancer cells as well as side effects in non-malignant cells in vitro. We first identified effective siRNA carriers by screening a library of lipid-substituted polyethylenimines …

Anticancer, Biophysical And Computational Investigations Of Half-Sandwich Ruthenium(Ii) Thiosemicarbazone Complexes: The Effect Of Arene Versus Thiacrown Face-Cap, Floyd A. Beckford, Alyssa Stott, P. Canisius Mbarushimana, Marc-Andre Leblanc, Kinsey Hall, Samantha Smith, Jimmie L. Bullock, Dennis J. Houghton, Alvin A. Holder, Nikolay Gerasimchuk, Antonio Gonzalez-Sarrías

Chemistry & Biochemistry Faculty Publications

A series of half-sandwich ruthenium complexes, two containing an arene face-cap and the other a thiacrown ether face-cap were synthesized to investigate the necessity of the arene for anticancer activity in this class of compounds. The complexes are formulated as [(h⁶-p-cymene)Ru(dmabTSC)Cl]PF₆, [(h⁶-benzene)Ru(dmabTSC)Cl]PF₆ (arene complexes), and [([9]aneS₃(dmabTSC)Cl]PF₆ (dmabTSC = dimethylaminobenzaldehye thiosemicarbazone). It was observed that none of the complexes showed good anticancer activity in vitro against HCT-116 and Caco-2 (colon adenocarcinoma) cells. All three complexes can bind strongly to calf-thymus DNA with binding constants on the order of 10 …