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Pharmacological inertness

Ye Ji Kim, Sun Min Kim, Chunghyeon Yu, Youngmin You, Eun Jin Cho, Jung Woon Yang, Sung Wng Kim
Halogenated organic compounds (HOCs) are important man-made chemicals widely used in chemical industry, biology and pharmacology; however, the persistence and inertness of organic halides cause human health problems and considerable environmental pollution. Thus, the elimination of halogen atoms from organic halides has been considered a central task in synthetic chemistry. In dehalogenation reactions, the inorganic bases remove halogen atoms, forming leaving groups and carbanions. Though the stable formation of free carbanion is the most decisive factor in determining the pathway and efficiency of reactions, the importance of carbanion stability in dehalogenation has long been overlooked...
January 9, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
Manouchehr Teymouri, Nastaran Barati, Matteo Pirro, Amirhosein Sahebkar
Dimethoxycurcumin (DiMC) is a synthetic analogue of curcumin with superior inter-related pro-oxidant and anti-cancer activity, and metabolic stability. Numerous studies have shown that DiMC reserves the biologically beneficial features, including anti-inflammatory, anti-carcinogenic and cytoprotective properties, almost to the same extent as curcumin exhibits. DiMC lacks the phenolic-OH groups as opposed to curcumin, dimethoxycurcumin, and bis-demethoxycurcumin that all vary in the number of methoxy groups per molecule, and has drawn the attentions of researchers who attempted to discover the structure-activity relationship (SAR) of curcumin...
December 20, 2016: Journal of Cellular Physiology
Alejandro Ansón-Casaos, Laura Grasa, Desirée Pereboom, José Emilio Mesonero, Alvaro Casanova, María Divina Murillo, María Teresa Martínez
Single-walled carbon nanotubes (SWCNTs) are thoroughly purified and dispersed in an aqueous solution of high molecular weight poly-L-lysine (pLlys). Human intestinal epithelial Caco-2/TC7 cells are incubated with the SWCNT dispersions in pLlys, and their effects on cell viability are studied by image flow cytometry. No significant changes are observed in the cell culture wells up to pLlys concentrations of 10 μg ml(-1). However, high mortality is detected at pLlys concentrations of 100 μg ml(-1). The presence of oxygen-free SWCNTs does not modify the effects of pLlys on cell cultures at any of the tested concentrations (≤1 μg ml(-1))...
December 2016: IET Nanobiotechnology
Himanshu Sharma, Bharti Sharma
Background-The Placebo is defined as an inert substance with a potent therapeutic effect. Its effect is attributed to its psychological and neurobiological effect. Its use in Psychiatric drug practice in drug trials and clinical practice is common, especially in India .Currently there is a debate whether to use it or not as there are ethical, moral and legal issues. Also, its mechanism of action is not known. Discussion-The Indian Psychiatry scenario is muddled in relation to use of placebo in Randomized Controlled Trials or Psychiatric clinical practice...
August 10, 2016: Central Nervous System Agents in Medicinal Chemistry
Simone Prömel, Franziska Fiedler, Claudia Binder, Jana Winkler, Torsten Schöneberg, Doreen Thor
G-protein signalling is an evolutionary conserved concept highlighting its fundamental impact on developmental and functional processes. Studies on the effects of G protein signals on tissues as well as an entire organism are often conducted in Caenorhabditis elegans. To understand and control dynamics and kinetics of the processes involved, pharmacological modulation of specific G protein pathways would be advantageous, but is difficult due to a lack in accessibility and regulation. To provide this option, we designed G protein-coupled receptor-based designer receptors (DREADDs) for C...
2016: Scientific Reports
Evan Wicker, Patrick A Forcelli
Temporal lobe epilepsy is the most common form of medically-intractable epilepsy. While seizures in TLE originate in structures such as hippocampus, amygdala, and temporal cortex, they propagate through a crucial relay: the midline/intralaminar thalamus. Prior studies have shown that pharmacological inhibition of midline thalamus attenuates limbic seizures. Here, we examined a recently developed technology, Designer Receptors Exclusively Activated by Designer Drugs (DREADDs), as a means of chemogenetic silencing to attenuate limbic seizures...
September 2016: Experimental Neurology
Mingzhi Su, Huayue Li, Haibo Wang, Eun La Kim, Hyung Sik Kim, Eun-Hee Kim, Jaewon Lee, Jee H Jung
Two new cystine knot peptides, asteropsins F (ASPF) and G (ASPG), were isolated from the marine sponge Asteropus sp. ASPF and ASPG are composed of 33 and 32 amino acids, respectively, and contain six cysteines which are involved in three disulfide bonds. They shared the characteristic features of the asteropsin family, such as, N-terminal pyroglutamate modification, incorporation of cis prolines, and the unique anionic profile, which distinguish them from other knottin families. Tertiary structures of the peptides were determined by high resolution NMR...
July 1, 2016: Bioorganic & Medicinal Chemistry
Wenpeng Zhang, Yanyan Li, Peng Zou, Man Wu, Zhenqing Zhang, Tao Zhang
Accumulating evidence from the last decade has shown that many pharmaceutical excipients are not pharmacologically inert but instead have effects on metabolic enzymes and/or drug transporters. Hence, the absorption, distribution, metabolism, and elimination (ADME) of active pharmaceutical ingredients (APIs) may be altered due to the modulation of their metabolism and transport by excipients. The impact of excipients is a potential concern for Biopharmaceutics Classification System (BCS)-based biowaivers, particularly as the BCS-based biowaivers have been extended to class 3 drugs in certain dosage forms...
July 2016: AAPS Journal
Michelle Rengarajan, Arnold Hayer, Julie A Theriot
Vascular endothelial cells act as gatekeepers that protect underlying tissue from blood-borne toxins and pathogens. Nevertheless, endothelial cells are able to internalize large fibrin clots and apoptotic debris from the bloodstream, although the precise mechanism of such phagocytosis-like uptake is unknown. We show that cultured primary human endothelial cells (HUVEC) internalize both pathogenic and non-pathogenic Listeria bacteria comparably, in a phagocytosis-like process. In contrast with previously studied host cell types, including intestinal epithelial cells and hepatocytes, we find that endothelial internalization of Listeria is independent of all known pathogenic bacterial surface proteins...
May 2016: PLoS Pathogens
M Müller, S Kamping, J Benrath, H Skowronek, J Schmitz, R Klinger, H Flor
BACKGROUND: Placebo analgesia refers to the reduction in pain due to the administration of an inert treatment. It is induced by expectations of pain relief which are enhanced by learning mechanisms. In healthy humans, prior positive experiences enhance the placebo response. However, the effects of patients' prior experiences with treatment on placebo responses have not yet been examined. This study investigated how verbal information, learning and treatment history influence the magnitude of placebo analgesia in chronic pain...
October 2016: European Journal of Pain: EJP
Simone Göschl, Hristo P Varbanov, Sarah Theiner, Michael A Jakupec, Markus Galanski, Bernhard K Keppler
The current study aims to elucidate the possible reasons for the significantly different pharmacological behavior of platinum(IV) complexes with cisplatin-, carboplatin- or nedaplatin-like cores and how this difference can be related to their main physicochemical properties. Chlorido-containing complexes are reduced fast (within hours) by ascorbate and are able to unwind plasmid DNA in the presence of ascorbate, while their tri- and tetracarboxylato analogs are generally inert under the same conditions. Comparison of the lipophilicity, cellular accumulation and cytotoxicity of the investigated platinum compounds revealed the necessity to define new structure-property/activity relationships (SPRs and SARs)...
July 2016: Journal of Inorganic Biochemistry
Christoph Heier, Ulrike Taschler, Maja Radulovic, Philip Aschauer, Thomas O Eichmann, Susanne Grond, Heimo Wolinski, Monika Oberer, Rudolf Zechner, Sepp D Kohlwein, Robert Zimmermann
Fatty acid ethyl esters (FAEEs) are non-oxidative metabolites of ethanol that accumulate in human tissues upon ethanol intake. Although FAEEs are considered as toxic metabolites causing cellular dysfunction and tissue damage, the enzymology of FAEE metabolism remains poorly understood. In this study, we used a biochemical screen in Saccharomyces cerevisiae to identify and characterize putative hydrolases involved in FAEE catabolism. We found that Yju3p, the functional orthologue of mammalian monoacylglycerol lipase (MGL), contributes >90% of cellular FAEE hydrolase activity, and its loss leads to the accumulation of FAEE...
May 27, 2016: Journal of Biological Chemistry
Manuel Aureliano, C André Ohlin, Michele O Vieira, M Paula M Marques, William H Casey, Luís A E Batista de Carvalho
The decaniobate ion, (Nb10 = [Nb10O28](6-)) being isoelectronic and isostructural with the decavanadate ion (V10 = [V10O28](6-)), but chemically and electrochemically more inert, has been useful in advancing the understanding of V10 toxicology and pharmacological activities. In the present study, the solution chemistry of Nb10 and V10 between pH 4 and 12 is studied by Raman spectroscopy. The Raman spectra of V10 show that this vanadate species dominates up to pH 6.45 whereas it remains detectable until pH 8...
April 25, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
James C Barrese, Juan Aceros, John P Donoghue
OBJECTIVE: Signal attenuation is a major problem facing intracortical sensors for chronic neuroprosthetic applications. Many studies suggest that failure is due to gliosis around the electrode tips, however, mechanical and material causes of failure are often overlooked. The purpose of this study was to investigate the factors contributing to progressive signal decline by using scanning electron microscopy (SEM) to visualize structural changes in chronically implanted arrays and histology to examine the tissue response at corresponding implant sites...
April 2016: Journal of Neural Engineering
Ida Ritacco, Gloria Mazzone, Nino Russo, Emilia Sicilia
Platinum(IV) complexes are an important class of compounds that can act as prodrugs, and due to their inertness, if correctly designed, they could have low toxicity outside the cancer cell and improve the pharmacological properties of the platinum(II) anticancer agents that are currently used in the clinic. Because of the efforts that are concentrated on the use of axial ligands able to control the reduction potentials, lipophilicity, charge, selectivity, targeting, and cell uptake of the Pt(IV) complexes, we considered to be of interest to probe the inertness of such complexes that is assumed to be a fulfilled prerequisite...
February 15, 2016: Inorganic Chemistry
Iñigo Valiente-Alandi, Allison E Schafer, Burns C Blaxall
The extracellular matrix (ECM) is a complex and dynamic scaffold that maintains tissue structure and dynamics. However, the view of the ECM as an inert architectural support has been increasingly challenged. The ECM is a vibrant meshwork, a crucial organizer of cellular microenvironments. It plays a direct role in cellular interactions regulating cell growth, survival, spreading, proliferation, differentiation and migration through the intricate relationship among cellular and acellular tissue components. This complex interrelationship preserves cardiac function during homeostasis; however it is also responsible for pathologic remodeling following myocardial injury...
February 2016: Journal of Molecular and Cellular Cardiology
Florian Chouchou, Jean-Marc Chauny, Pierre Rainville, Gilles J Lavigne
The placebo effect is a neurobiological and psychophysiological process known to influence perceived pain relief. Optimization of placebo analgesia may contribute to the clinical efficacy and effectiveness of medication for acute and chronic pain management. We know that the placebo effect operates through two main mechanisms, expectations and learning, which is also influenced by sleep. Moreover, a recent study suggested that rapid eye movement (REM) sleep is associated with modulation of expectation-mediated placebo analgesia...
2015: PloS One
Miriam S Teixeira, Cuneyt M Alper, Brian S Martin, Narmin Helal, Brendan M Cullen Doyle, William J Doyle
OBJECTIVE: Determine if the middle ear (ME) trans-mucosal nitrous oxide (N2O) gas exchange rate can be pharmacologically modulated by the nasal application of a vasoconstrictor. METHODS: In a randomized, double-blind, crossover study, 20 adults received a nasal spray challenge containing either oxymetazoline or saline (placebo). At each session, subjects were fitted with a non-rebreathing mask and breathed room air for 20 minutes, 50% N2O:50% O2 for 20 minutes, and 100% O2 for 10 minutes...
May 2016: Annals of Otology, Rhinology, and Laryngology
Catherine M Cowan, Shmma Quraishe, Sarah Hands, Megan Sealey, Sumeet Mahajan, Douglas W Allan, Amritpal Mudher
Aggregation of highly phosphorylated tau is a hallmark of Alzheimer's disease and other tauopathies. Nevertheless, animal models demonstrate that tau-mediated dysfunction/toxicity may not require large tau aggregates but instead may be caused by soluble hyper-phosphorylated tau or by small tau oligomers. Challenging this widely held view, we use multiple techniques to show that insoluble tau oligomers form in conditions where tau-mediated dysfunction is rescued in vivo. This shows that tau oligomers are not necessarily always toxic...
November 26, 2015: Scientific Reports
Chetan Yewale, Sushilkumar Patil, Atul Kolate, Girish Kore, Ambikanandan Misra
Transport of a drug across the biological membrane of the gastrointestinal tract has turned out to be a critical barrier against the success of any oral drug delivery technology. The unique advantages of the oral route, along with need for an oral substitute of invasive parenteral formulations and the reduction of intersubject variability in plasma profiles, has been an incentive for the use of excipients with absorption-enhancing properties to boost the bioavailability of poorly absorbed drugs. The development of such excipients is not a simple task, so understanding enhancement mechanisms in relation to physiology can facilitate the identification of structure-function relationships as well as the development of newer agents for customary applications...
2015: Critical Reviews in Therapeutic Drug Carrier Systems
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