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https://www.readbyqxmd.com/read/29793153/effects-of-mg-2-on-recovery-of-nmda-receptors-from-inhibition-by-memantine-and-ketamine-reveal-properties-of-a-second-site
#1
Nathan G Glasgow, Madeleine R Wilcox, Jon W Johnson
Memantine and ketamine are NMDA receptor (NMDAR) open channel blockers that are thought to act via similar mechanisms at NMDARs, but exhibit divergent clinical effects. Both drugs act by entering open NMDARs and binding at a site deep within the ion channel (the deep site) at which the endogenous NMDAR channel blocker Mg2+ also binds. Under physiological conditions, Mg2+ increases the IC50 s of memantine and ketamine through competition for binding at the deep site. Memantine also can inhibit NMDARs after associating with a second site accessible in the absence of agonist, a process termed second site inhibition (SSI) that is not observed with ketamine...
May 12, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29792945/cross-linking-by-epichlorohydrin-and-diepoxybutane-correlates-with-cytotoxicity-and-leads-to-apoptosis-in-human-leukemia-hl-60-cells
#2
Phuong M Le, Vanesa L Silvestri, Samuel C Redstone, Jordanne B Dunn, Julie T Millard
The bifunctional alkylating agents epichlorohydrin (ECH) and diepoxybutane (DEB) have been linked to increased cancer risks in industrial workers. These compounds react with DNA and proteins, leading to genotoxic effects. We used the comet assay to monitor formation of cross-links in HL-60 cells treated with ECH, DEB, and the structurally related anti-cancer drug mechlorethamine (HN2). We report a time- and dose-dependent cytotoxicity that correlated with cross-linking activity, following the order HN2 > DEB > ECH...
May 21, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29792920/inner-ear-drug-delivery-recent-advances-challenges-and-perspective
#3
Jinsong Hao, S Kevin Li
Effective and safe treatment of auditory and vestibular diseases has become increasingly dependent on inner ear drug delivery systems. This review highlights recent advances in inner ear drug delivery research and technologies. The focus is on strategies to overcome delivery barriers and to improve drug residence and targeting, with special attention to in vivo animal and human studies. The research in gene and stem cell delivery to the inner ear is briefly reviewed. Newly developed research tools to address experimental challenges and safety issues are discussed...
May 21, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29792857/tgf-%C3%AE-plays-a-vital-role-in-triple-negative-breast-cancer-tnbc-drug-resistance-through-regulating-stemness-emt-and-apoptosis
#4
Xiaodan Xu, Lu Zhang, Xiaogang He, Ping Zhang, Caihong Sun, Xiaojun Xu, Yaojuan Lu, Feifei Li
Triple negative breast cancer (TNBC) is the most malignant subtype of breast cancer in which the cell surface lacks usual targets for drug to exhibit its effects. Epirubicin (Epi) is widely used for TNBC, but a substantial number of patients develop Epi resistance that is usually associated with poor prognosis. Transforming growth factor (TGF-β) is a multifunctional cytokine. In recent study, it appears that TGF-β influences the cancer stem cell population, thus, the drug resistance of cancer may also be affected...
May 21, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29792851/collagen-induced-arthritis-in-dark-agouti-rats-as-a-model-for-study-of-immunological-sexual-dimorphisms-in-the-human-disease
#5
Mirjana Dimitrijević, Nevena Arsenović-Ranin, Biljana Bufan, Mirjana Nacka-Aleksić, Mirjana Lazarević Macanović, Petar Milovanović, Marija Đurić, Jelena Sopta, Gordana Leposavić
Collagen-induced arthritis (CIA) is a frequently used animal model of rheumatoid arthritis, human autoimmune disease that exhibits clear sex bias in incidence and clinical course. Female Dark Agouti rats immunized for CIA showed also greater incidence and higher arthritic score than their male counterparts. The study investigated sex differences in mechanisms controlling the primary immune responses in draining lymph nodes (dLNs), as a factor contributing to this dimorphism. The higher frequencies of CD4 + CD25 + Foxp3- cells, presumably activated effector T (Teff) cells, and IL-17+, IFN-γ + and IL-17 + IFN-γ + T cells were found in female comapared with male rat dLNs...
May 21, 2018: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/29792594/an-nmdar-positive-and-negative-allosteric-modulator-series-share-a-binding-site-and-are-interconverted-by-methyl-groups
#6
Riley Perszyk, Brooke M Katzman, Hirofumi Kusumoto, Steven A Kell, Matthew P Epplin, Yesim A Tahirovic, Rhonda L Moore, David Menaldino, Pieter Burger, Dennis C Liotta, Stephen F Traynelis
N-methyl-d-aspartate receptors (NMDARs) are an important receptor in the brain and have been implicated in multiple neurological disorders. Many non-selective NMDAR-targeting drugs are poorly tolerated, leading to efforts to target NMDAR subtypes to improve the therapeutic index. We describe here a series of negative allosteric NMDAR modulators with submaximal inhibition at saturating concentrations. Modest changes to the chemical structure interconvert negative and positive modulation. All modulators share the ability to enhance agonist potency and are use-dependent, requiring the binding of both agonists before modulators act with high potency...
May 24, 2018: ELife
https://www.readbyqxmd.com/read/29792471/sex-differences-in-the-anorexigenic-effects-of-dexfenfluramine-and-amphetamine-in-baboons
#7
Richard W Foltin, Suzette M Evans
The anorexigenic effects of intramuscular d-amphetamine HCl (0.06-0.50 mg/kg) and dexfenfluramine HCl (0.25-2.0 mg/kg) were determined in experimentally naïve baboons. A group of 8 adult male baboons was tested prior to a group of 7 adult female baboons. A 120-min session occurred at 9:00 a.m. during which baboons could respond for food pellets. Drug was given 30 min prior to the 9:00 a.m. morning session. Beginning at 11:00 a.m., baboons had a 6-hr multiple-meal session during which they could have up to 4 food pellet meals...
May 24, 2018: Experimental and Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29792435/measuring-drug-induced-changes-in-metabolite-populations-of-live-bacteria-real-time-analysis-by-raman-spectroscopy
#8
Paul R Carey, Grant R Whitmer, Michael J Yoon, Michael N Lombardo, Marianne Pusztai-Carey, Hossein Heidari-Torkabadi, Tao Che
Raman difference spectroscopy is shown to provide a wealth of molecular detail on changes within bacterial cells caused by infusion of antibiotics or hydrogen peroxide. E. coli strains paired with chloramphenicol, DHFR propargyl-based inhibitors, meropenem, or hydrogen peroxide provide details of the depletion of protein and nucleic acid populations in real time. Additionally, other reproducible Raman features appear and are attributed to changes in cell metabolite populations. An initial candidate for one of the metabolites involves population increases of citrate, an intermediate within the TCA cycle...
May 24, 2018: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/29792199/nanoparticle-delivery-of-grape-seed-derived-proanthocyanidins-to-airway-epithelial-cells-dampens-oxidative-stress-and-inflammation
#9
S Castellani, A Trapani, A Spagnoletta, L di Toma, T Magrone, S Di Gioia, D Mandracchia, G Trapani, E Jirillo, M Conese
BACKGROUND: Chronic respiratory diseases, whose one of the hallmarks is oxidative stress, are still incurable and need novel therapeutic tools and pharmaceutical agents. The phenolic compounds contained in grape are endowed with well-recognized anti-oxidant, anti-inflammatory, anti-cancer, and anti-aging activities. Considering that natural anti-oxidants, such as proanthocyanidins, have poor water solubility and oral bioavailability, we have developed a drug delivery system based on solid lipid nanoparticles (SLN), apt to encapsulate grape seed extract (GSE), containing proanthocyanidins...
May 23, 2018: Journal of Translational Medicine
https://www.readbyqxmd.com/read/29792136/zinc-dependent-histone-deacetylase-inhibitors-in-cancer-therapeutics-recent-update
#10
Panagiotis I Georgianos, Maria Divani, Theodoros Eleftheriadis, Peter R Mertens, Vassilios Liakopoulos
BACKGROUND: Despite optimal management of diabetic kidney disease (DKD) with intensive glycemic control and administration of agents blocking the renin-angiotensin-aldosterone-system, the residual risk for nephropathy progression to end-stage-renal-disease (ESRD) remains high. Sodium-glucose co-transporter type 2 (SGLT-2)-inhibitors represent a newly-introduced anti-diabetic drug class with pleiotropic actions extending above their glucose-lowering efficacy. Herein, we provide an overview of preclinical and clinical-trial evidence supporting a protective effect of SGLT-2 inhibitors on DKD...
May 23, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29792023/fern-9-11-ene-2%C3%AE-3%C3%AE-diol-action-on-insulin-secretion-in-hyperglycemic-conditions
#11
Allisson Jhonatan Gomes Castro, Luisa Helena Cazarolli, Gabrielle Da Luz, Delsi Altenhofen, Hemily Batista Da Silva, Francieli Kanumfre Carvalho, Moacir Geraldo Pizzolatti, Fátima Rmb Silva
The objective of this study was to investigate the effect and the mechanism of action of fernenediol as insulin secretagogue. Wistar rats were treated with 0.1; 1 and 10 mg/kg fernenediol and then induced hyperglycemia by oral glucose. The glycaemia, insulin, LDH, calcium and hepatic glycogen were analyzed. Considering the intestine and pancreas as targets for the triterpene action, the duodenum was used to verify the influence of fernenediol on intestinal glycosidases. Additionally, pancreatic islets were used for studies of 14 C-deoxyglucose uptake and influx of 45 Ca2+ in hyperglycemic medium with/without fernenediol in the presence/absence of an inhibitor/activator of KATP channels, glibenclamide, diazoxide, nifedipine, calcium chelator (BAPTA- AM) and H-89 and ST the inhibitors of the PKA and PKC enzymes...
May 24, 2018: Biochemistry
https://www.readbyqxmd.com/read/29791931/effectiveness-of-a-crocus-sativus-extract-on-burn-wounds-in-rats
#12
Esmat Alemzadeh, Ahmad Oryan
Crocus sativus is a spice with various pharmacological properties. Crocin, picrocrocin, and safranal are the main compositions of saffron that have recently been considered in the therapy of many diseases. High-performance liquid chromatography analysis revealed presence of these compounds in our saffron extract. This study was carried out to evaluate the effect of saffron on burn wound healing at an in vivo model. Saffron was topically applied on burn wounds in rats; the percentage of wound closure, wound contraction, and the levels of main cytokines and growth factors were measured...
May 23, 2018: Planta Medica
https://www.readbyqxmd.com/read/29791894/highly-tumorigenic-diffuse-large-b-cell-lymphoma-cells-are-produced-by-coculture-with-stromal-cells
#13
Zhiguang Lin, Bobin Chen, Ting Wu, Xiaoping Xu
BACKGROUND/AIMS: Diffuse large B cell lymphoma (DLBCL) is heterogeneous. We aimed to explore how tumor microenvironment promotes lymphoma cell aggressiveness and heterogeneity. METHODS: We created a coculture system using human DLBCL cells and mouse bone marrow stromal cells. Proliferative capacity, drug resistance, clonogenicity, and tumorigenicity were compared in lymphoma cells from the coculture system and lymphoma cells cultured alone. Expression of Notch signaling associated genes was evaluated using real-time reverse transcriptase PCR and Western blot...
May 23, 2018: Acta Haematologica
https://www.readbyqxmd.com/read/29791803/bacteria-activated-janus-particles-driven-by-chemotaxis
#14
Zihan Huang, Pengyu Chen, Guo-Long Zhu, Ye Yang, Ziyang Xu, Li-Tang Yan
In the development of biocompatible nano/micro-motors for drug and cargo delivery, motile bacteria represent an excellent energy source for biomedical applications. Despite intense research of the fabrication of bacteria-based motors, how to effectively utilize the instinctive responses of bacteria to environmental stimuli in the fabrication process, particularly, chemotaxis, remains an urgent and critical issue. Here, by developing a molecular-dynamics model of bacterial chemotaxis, we present an investigation of the transport of a bacteria-activated Janus particle driven by chemotaxis...
May 23, 2018: ACS Nano
https://www.readbyqxmd.com/read/29791260/assessment-of-the-power-required-for-optimal-use-of-current-inhalation-devices
#15
Gerhard Pohlmann, Jens M Hohlfeld, Peter Haidl, Jelena Pankalla, Rolf Michael Cloes
BACKGROUND: Inhalation of medications is the cornerstone in the treatment of patients with lung diseases. A variety of inhalation devices exists and each device has specific requirements to achieve optimum inhalation of the drug. The goal of this study was to establish a clear overview on performance requirements of standard inhalation devices that should be met by the patient's breathing power and to develop a new method to measure the individual performance data. MATERIALS AND METHODS: An optimum and still acceptable required breathing power (P in watts) was calculated for each device with the aid of individual device flow rates (determined by a literature search) and the flow resistances (by measuring the pressure drop over the different inhalation devices)...
May 23, 2018: Journal of Aerosol Medicine and Pulmonary Drug Delivery
https://www.readbyqxmd.com/read/29791165/effect-of-polymer-chain-length-on-the-physical-stability-of-amorphous-drug-polymer-blends-at-ambient-pressure
#16
Justyna Pacułt, Marzena Rams-Baron, Beata Chrząszcz, Renata Jachowicz, Marian Paluch
Rational selection of polymers for amorphous drug stabilization is necessary for further successful development of solid dispersion technology. In this paper we investigated the effect of polymer chain length on the inhibition of amorphous drug recrystallization. To consider this problem we prepared a drug-polymer blends (in 10:1 drug to polymer ratio) containing bicalutamide (BIC) and polyvinylpyrrolidone (PVP) with different chain lengths K10, K30, K90. We applied broadband dielectric spectroscopy to compare the molecular dynamics of investigated samples and thoroughly recognize their crystallization tendencies from supercooled liquid state...
May 23, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29791068/cdpbc-a-software-application-for-estimation-of-concentration-dependent-plasma-binding-capacity-of-small-molecule
#17
Om Prakash, Upendra Nath Dwivedi
Drug-plasma binding (DPB) is an important aspect during pharmacokinetics (PK) studies. DPB of small molecule cannot be evaluated through computational means. Here we present CDPBC; a standalone application for evaluation of small molecule for its capacity (concentration dependent) of binding with plasma proteins. This application is freely available at URL (https://github.com/undwive di/CDPBC.git). The application is enriched with evaluation of five major proteins of plasma. Input for application is a docked complex against the suggested PDBs of plasma proteins...
May 23, 2018: Molecular Informatics
https://www.readbyqxmd.com/read/29790849/-n-methyl-d-aspartate-receptor-antibody-encephalitis-the-janus-faced-disorder
#18
Ildiko Sipos
The recognition of the antibody-mediated encephalitis as a separate entity among the immune disorders of the central nervous system was one of the greatest breakthroughs of the last two decades in neurology. Unlike viral or tumor-related encephalitis, the antibody-mediated form has a good response to immunotherapy, which gives a special clinical importance to the discovery. Anti-N-methyl-D-aspartate receptor (anti-NMDAR) encephalitis is one of the first fully characterized antibody-mediated encephalitises. This article attempts to summarize the clinical features of this complex neuropsychiatric disorder with the aim to help its early recognition and to report the clinical course and the outcome of our six seropositive anti-NMDAR cases...
March 2018: Neuropsychopharmacologia Hungarica
https://www.readbyqxmd.com/read/29790428/multi-ethnic-sult1a1-copy-number-profiling-with-multiplex-ligation-dependent-probe-amplification
#19
Raymon Vijzelaar, Mariana R Botton, Lisette Stolk, Suparna Martis, Robert J Desnick, Stuart A Scott
AIM: To develop a SULT1A1 multiplex ligation-dependent probe amplification assay and to investigate multi-ethnic copy number variant frequencies. METHODS: A novel multiplex ligation-dependent probe amplification assay was developed and tested on 472 African-American, Asian, Caucasian, Hispanic and Ashkenazi Jewish individuals. RESULTS: The frequencies of atypical total copy number (i.e., greater or less than two) were 38.7% for Hispanics, 38...
May 23, 2018: Pharmacogenomics
https://www.readbyqxmd.com/read/29790418/enhanced-brain-penetration-of-pretomanid-by-intranasal-administration-of-an-oil-in-water-nanoemulsion
#20
Adeola Shobo, Annapurna Pamreddy, Hendrik G Kruger, Maya M Makatini, Tricia Naicker, Thavendran Govender, Sooraj Baijnath
AIM: To enhance the drug delivery to the brain with an oil-in-water nanoemulsion of pretomanid via intranasal (IN) administration. MATERIALS & METHODS: The study involved 70 male Sprague-Dawley rats (160-180 g) that received either 20 mg/kg body weight (b.w.) a nanoemulsion or a 20 mg/kg b.w. of pretomanid in solution via the IN route. The drug was quantified by liquid chromatography-tandem mass spectrometry to investigate whole tissue-drug concentrations, and mass spectrometric imaging to visualize drug localization in the brain...
May 2018: Nanomedicine
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