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https://www.readbyqxmd.com/read/29144442/propagation-of-fibrillar-structural-forms-in-proteins-stopped-by-naturally-occurring-short-polypeptide-chain-fragments
#1
Irena Roterman, Mateusz Banach, Leszek Konieczny
Amyloids characterized by unbounded growth of fibrillar structures cause many pathological processes. Such unbounded propagation is due to the presence of a propagating hydrophobicity field around the fibril's main axis, preventing its closure (unlike in globular proteins). Interestingly, similar fragments, commonly referred to as solenoids, are present in many naturally occurring proteins, where their propagation is arrested by suitably located "stopper" fragments. In this work, we analyze the distribution of hydrophobicity in solenoids and in their corresponding "stoppers" from the point of view of the fuzzy oil drop model (called FOD in this paper)...
November 16, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29120370/amorphous-solid-dispersion-of-epigallocatechin-gallate-for-enhanced-physical-stability-and-controlled-release
#2
Yizheng Cao, Jing Teng, Jon Selbo
Epigallocatechin gallate (EGCG) has been recognized as the most prominent green tea extract due to its healthy influences. The high instability and low bioavailability, however, strongly limit its utilization in food and drug industries. This work, for the first time, develops amorphous solid dispersion of EGCG to enhance its bioavailability and physical stability. Four commonly used polymeric excipients are found to be compatible with EGCG in water-dioxane mixtures via a stepwise mixing method aided by vigorous mechanical interference...
November 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29099084/essential-oils-and-antifungal-activity
#3
REVIEW
Filomena Nazzaro, Florinda Fratianni, Raffaele Coppola, Vincenzo De Feo
Since ancient times, folk medicine and agro-food science have benefitted from the use of plant derivatives, such as essential oils, to combat different diseases, as well as to preserve food. In Nature, essential oils play a fundamental role in protecting the plant from biotic and abiotic attacks to which it may be subjected. Many researchers have analyzed in detail the modes of action of essential oils and most of their components. The purpose of this brief review is to describe the properties of essential oils, principally as antifungal agents, and their role in blocking cell communication mechanisms, fungal biofilm formation, and mycotoxin production...
November 2, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29104261/neurochemical-changes-and-c-fos-mapping-in-the-brain-after-carisbamate-treatment-of-rats-subjected-to-lithium-pilocarpine-induced-status-epilepticus
#4
José Eduardo Marques-Carneiro, Astrid Nehlig, Jean-Christophe Cassel, Eduardo Ferreira Castro-Neto, Julia Julie Litzahn, Anne Pereira de Vasconcelos, Maria da Graça Naffah-Mazacoratti, Maria José da Silva Fernandes
The administration of lithium-pilocarpine (LiPilo) in adult rats is a validated model reproducing the main clinical and neuropathological features of temporal lobe epilepsy (TLE). Previous studies have shown that carisbamate (CRS) has the property of modifying epileptogenesis in this model. When treated with CRS, about 50% of rats undergoing LiPilo status epilepticus (SE) develop non-convulsive seizures (NCS) instead of convulsive ones (commonly observed in TLE). The goal of this work was to determine some of the early changes that occur after CRS administration, as they could be involved in the insult- and epileptogenesis-modifying effects of CRS...
November 1, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29088082/acorenone-b-ache-and-bche-inhibitor-as-a-major-compound-of-the-essential-oil-distilled-from-the-ecuadorian-species-niphogeton-dissecta-benth-j-f-macbr
#5
James Calva, Nicole Bec, Gianluca Gilardoni, Christian Larroque, Luis Cartuche, Carlo Bicchi, José Vinicio Montesinos
This study investigated the chemical composition, physical proprieties, biological activity, and enantiomeric analysis of the essential oil from the aerial parts of Niphogeton dissecta (culantrillo del cerro) from Ecuador, obtained by steam distillation. The qualitative and quantitative analysis of the essential oil was realized by gas chromatographic and spectroscopic techniques (GC-MS and GC-FID). Acorenone B was identified by GC-MS and NMR experiments. The enantiomeric distribution of some constituents has been assessed by enantio-GC through the use of a chiral cyclodextrin-based capillary column...
October 31, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29064422/systemic-interleukin-4-administration-after-spinal-cord-injury-modulates-inflammation-and-promotes-neuroprotection
#6
Rui Lima, Susana Monteiro, José P Lopes, Pedro Barradas, Natália L Vasconcelos, Eduardo D Gomes, Rita C Assunção-Silva, Fábio G Teixeira, Mónica Morais, Nuno Sousa, António J Salgado, Nuno A Silva
Traumatic spinal cord injury (SCI) causes dramatic disability and dysfunction in the motor, sensory and autonomic systems. The severe inflammatory reaction that occurs after SCI is strongly associated with further tissue damage. As such, immunomodulatory strategies have been developed, aimed at reducing inflammation, but also at shaping the immune response in order to protect, repair and promote regeneration of spared neural tissue. One of those promising strategies is the intraspinal administration of the cytokine interleukin-4 (IL-4) that was shown to promote a phenotype on specific immune cells associated with neuroprotection and repair...
October 24, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29053577/electrographic-changes-accompanying-recurrent-seizures-under-ketogenic-diet-treatment
#7
Chiara Lucchi, Maddalena Marchiò, Elisa Caramaschi, Carmela Giordano, Rocco Giordano, Azzurra Guerra, Giuseppe Biagini
The ketogenic diet (KD) is increasingly used to treat epilepsy refractory to antiepileptic drugs and other neurological disorders. In animal models, the KD was found to increase the threshold to seizures induced by different convulsive stimulations. However, in models in which suprathreshold stimuli were used, a paradoxical seizure worsening was consistently observed in KD-fed animals. To better define this phenomenon, we characterized the electrographic response to seizures induced in mice which were treated with the KD, and then corneally stimulated at 6-Hz in four different sessions...
October 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29035298/molecular-docking-and-3d-pharmacophore-modeling-to-study-the-interactions-of-chalcone-derivatives-with-estrogen-receptor-alpha
#8
Muchtaridi Muchtaridi, Hasna Nur Syahidah, Anas Subarnas, Muhammad Yusuf, Sharon D Bryant, Thierry Langer
Tamoxifen is the most frequently used anti-estrogen adjuvant treatment for estrogen receptor-positive breast cancer. However, it is associated with an increased risk of several serious side-effects, such as uterine cancer, stroke, and pulmonary embolism. The 2',4'-dihydroxy-6-methoxy-3,5-dimethylchalcone (ChalcEA) from plant leaves of Eugenia aquea, has been found to inhibit the proliferation of MCF-7 human breast cancer cells in a dose-dependent manner, with an IC50 of 74.5 μg/mL (250 μM). The aim of this work was to study the molecular interactions of new ChalcEA derivatives formed with the Estrogen Receptor α (ERα) using computer aided drug design approaches...
October 16, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29023372/parp-inhibition-by-flavonoids-induced-selective-cell-killing-to-brca2-deficient-cells
#9
Cathy Su, Alexis H Haskins, Chisato Omata, Yasushi Aizawa, Takamitsu A Kato
High consumption of dietary flavonoids might contribute to a reduction of cancer risks. Quercetin and its glycosides have PARP inhibitory effects and can induce selective cytotoxicity in BRCA2-deficient cells by synthetic lethality. We hypothesized that common flavonoids in diet naringenin, hesperetin and their glycosides have a similar structure to quercetin, which might have comparable PARP inhibitory effects, and can induce selective cytotoxicity in BRCA2-deficient cells. We utilized Chinese hamster V79 wild type, V-C8 BRCA2-deficient and its gene-complemented cells...
October 12, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28991183/orexin-receptor-multimerization-versus-functional-interactions-neuropharmacological-implications-for-opioid-and-cannabinoid-signalling-and-pharmacogenetics
#10
Miles D Thompson, Takeshi Sakurai, Innocenzo Rainero, Mary C Maj, Jyrki P Kukkonen
Orexins/hypocretins are neuropeptides formed by proteolytic cleavage of a precursor peptide, which are produced by neurons found in the lateral hypothalamus. The G protein-coupled receptors (GPCRs) for these ligands, the OX₁ and OX₂ orexin receptors, are more widely expressed throughout the central nervous system. The orexin/hypocretin system has been implicated in many pathways, and its dysregulation is under investigation in a number of diseases. Disorders in which orexinergic mechanisms are being investigated include narcolepsy, idiopathic sleep disorders, cluster headache and migraine...
October 8, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28974047/heparin-mimetics-their-therapeutic-potential
#11
REVIEW
Shifaza Mohamed, Deirdre R Coombe
Heparin mimetics are synthetic and semi-synthetic compounds that are highly sulfated, structurally distinct analogues of glycosaminoglycans. These mimetics are often rationally designed to increase potency and binding selectivity towards specific proteins involved in disease manifestations. Some of the major therapeutic arenas towards which heparin mimetics are targeted include: coagulation and thrombosis, cancers, and inflammatory diseases. Although Fondaparinux, a rationally designed heparin mimetic, is now approved for prophylaxis and treatment of venous thromboembolism, the search for novel anticoagulant heparin mimetics with increased affinity and fewer side effects remains a subject of research...
October 2, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28953234/procedures-for-the-gmp-compliant-production-and-quality-control-of-18-f-psma-1007-a-next-generation-radiofluorinated-tracer-for-the-detection-of-prostate-cancer
#12
Jens Cardinale, René Martin, Yvonne Remde, Martin Schäfer, Antje Hienzsch, Sandra Hübner, Anna-Maria Zerges, Heike Marx, Ronny Hesse, Klaus Weber, Rene Smits, Alexander Hoepping, Marco Müller, Oliver C Neels, Klaus Kopka
Radiolabeled tracers targeting the prostate-specific membrane antigen (PSMA) have become important radiopharmaceuticals for the PET-imaging of prostate cancer. In this connection, we recently developed the fluorine-18-labelled PSMA-ligand [(18)F]PSMA-1007 as the next generation radiofluorinated Glu-ureido PSMA inhibitor after [(18)F]DCFPyL and [(18)F]DCFBC. Since radiosynthesis so far has been suffering from rather poor yields, novel procedures for the automated radiosyntheses of [(18)F]PSMA-1007 have been developed...
September 27, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29036881/comparison-of-in-vitro-assays-in-selecting-radiotracers-for-in-vivo-p-glycoprotein-pet-imaging
#13
Renske M Raaphorst, Heli Savolainen, Mariangela Cantore, Evita van de Steeg, Aren van Waarde, Nicola A Colabufo, Philip H Elsinga, Adriaan A Lammertsma, Albert D Windhorst, Gert Luurtsema
Positron emission tomography (PET) imaging of P-glycoprotein (P-gp) in the blood-brain barrier can be important in neurological diseases where P-gp is affected, such as Alzheimer´s disease. Radiotracers used in the imaging studies are present at very small, nanomolar, concentration, whereas in vitro assays where these tracers are characterized, are usually performed at micromolar concentration, causing often discrepant in vivo and in vitro data. We had in vivo rodent PET data of [(11)C]verapamil, (R)-N-[(18)F]fluoroethylverapamil, (R)-O-[(18)F]fluoroethyl-norverapamil, [(18)F]MC225 and [(18)F]MC224 and we included also two new molecules [(18)F]MC198 and [(18)F]KE64 in this study...
September 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28902172/behavioral-and-neurochemical-consequences-of-pentylenetetrazol-induced-kindling-in-young-and-middle-aged-rats
#14
Alexandre Ademar Hoeller, Cristiane Ribeiro de Carvalho, Pedro Leite Costa Franco, Douglas Affonso Formolo, Alexandre Kracker Imthon, Henrique Rodighero Dos Santos, Ingrid Eidt, Gabriel Roman Souza, Leandra Celso Constantino, Camila Leite Ferreira, Rui Daniel Prediger, Rodrigo Bainy Leal, Roger Walz
(1) Objectives: Epilepsy disorder is likely to increase with aging, leading to an increased incidence of comorbidities and mortality. In spite of that, there is a lack of information regarding this issue and little knowledge of cognitive and emotional responses in aging subjects following epileptogenesis. We investigated whether and how aging distress epilepsy-related behavioral and biochemical outcomes are associated with cognition and emotion. (2) Methods: Young and middle-aged Wistar rats (3 or 12 months old) were treated with pentylenetetrazol (PTZ, 35 mg/kg) and injected on alternated days for 20 (young rats) and 32 days (middle-aged rats)...
September 13, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28872590/synthesis-of-nitric-oxide-donors-derived-from-piloty-s-acid-and-study-of-their-effects-on-dopamine-secretion-from-pc12-cells
#15
Daniele Sanna, Gaia Rocchitta, Maria Serra, Marcello Abbondio, Pier Andrea Serra, Rossana Migheli, Lidia De Luca, Eugenio Garribba, Andrea Porcheddu
This study investigated the mechanisms and kinetics of nitric oxide (NO) generation by derivatives of Piloty's acid (NO-donors) under physiological conditions. In order to qualitatively and quantitatively measure NO release, electron paramagnetic resonance (EPR) was carried out with NO spin trapping. In addition, voltammetric techniques, including cyclic voltammetry and constant potential amperometry, were used to confirm NO release from Piloty's acid and its derivatives. The resulting data showed that Piloty's acid derivatives are able to release NO under physiological conditions...
September 5, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28820457/role-of-cyp2c9-cyp2c19-and-ephx-polymorphism-in-the-pharmacokinetic-of-phenytoin-a-study-on-uruguayan-caucasian-subjects
#16
Natalia Guevara, Cecilia Maldonado, Manuel Uría, Raquel González, Manuel Ibarra, Silvana Alvariza, Antonella Carozzi, Carlos Azambuja, Pietro Fagiolino, Marta Vázquez
Phenytoin (PHT) oxidative route leads to its main metabolite p-hydroxyphenytoin (p-HPPH), by means of CYP2C9 and CYP2C19. Formation of p-HPPH proceeds via a reactive arene-oxide intermediate. This intermediate can also be converted into PHT dihydrodiol by microsomal epoxide hydrolase (EPHX). The three enzymes are polymorphically expressed and the genetic variants are responsible for changes in the enzyme activity. In order to evaluate the effect that these polymorphisms have on PHT metabolism, PHT and p-HPPH plasma concentrations were measured and the genotype for the three enzymes was assessed in 50 Uruguayan epileptic patients...
August 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28809784/folate-receptor-positive-gynecological-cancer-cells-in-vitro-and-in-vivo-characterization
#17
Klaudia Siwowska, Raffaella M Schmid, Susan Cohrs, Roger Schibli, Cristina Müller
The folate receptor (FR) is expressed in a variety of gynecological cancer types. It has been widely used for tumor targeting with folic acid conjugates of diagnostic and therapeutic probes. The cervical KB tumor cells have evolved as the standard model for preclinical investigations of folate-based (radio) conjugates. In this study, a panel of FR-expressing human cancer cell lines-including cervical (HeLa, KB, KB-V1), ovarian (IGROV-1, SKOV-3, SKOV-3.ip), choriocarcinoma (JAR, BeWo) and endometrial (EFE-184) tumor cells-was investigated in vitro and for their ability to grow as xenografts in mice...
August 15, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28792472/glycosaminoglycan-interactions-with-chemokines-add-complexity-to-a-complex-system
#18
REVIEW
Amanda E I Proudfoot, Zoë Johnson, Pauline Bonvin, Tracy M Handel
Chemokines have two types of interactions that function cooperatively to control cell migration. Chemokine receptors on migrating cells integrate signals initiated upon chemokine binding to promote cell movement. Interactions with glycosaminoglycans (GAGs) localize chemokines on and near cell surfaces and the extracellular matrix to provide direction to the cell movement. The matrix of interacting chemokine-receptor partners has been known for some time, precise signaling and trafficking properties of many chemokine-receptor pairs have been characterized, and recent structural information has revealed atomic level detail on chemokine-receptor recognition and activation...
August 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28792452/complexes-of-oligoribonucleotides-with-d-mannitol-inhibit-hemagglutinin-glycan-interaction-and-suppress-influenza-a-virus-h1n1-a-fm-1-47-infectivity-in-vitro
#19
Nataliia Melnichuk, Larisa Semernikova, Zenoviy Tkachuk
The influenza virus hemagglutinin (HA) mediates both receptor (glycan) binding and membrane fusion for cell entry and has been the basis for subtyping influenza viruses. The oligoribonucleotides-d-mannitol (ORNs-d-M) complexes possess an anti-influenza activity in vitro and in vivo. In the present studies, we have found that ORNs-d-M interferes with hemagglutinin (HA)-glycan interaction and suppress viral infection in host cells. HA-glycan interactions were evaluated to indirectly quantify the amount of influenza virus titer by an agglutination assay...
August 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28763030/the-binding-effect-of-proteins-on-medications-and-its-impact-on-electrochemical-sensing-antipsychotic-clozapine-as-a-case-study
#20
George E Banis, Thomas Winkler, Patricia Barton, Sheryl E Chocron, Eunkyoung Kim, Deanna L Kelly, Gregory F Payne, Hadar Ben-Yoav, Reza Ghodssi
Clozapine (CLZ), a dibenzodiazepine, is demonstrated as the optimal antipsychotic for patients suffering from treatment-resistant schizophrenia. Like many other drugs, understanding the concentration of CLZ in a patient's blood is critical for managing the patients' symptoms, side effects, and overall treatment efficacy. To that end, various electrochemical techniques have been adapted due to their capabilities in concentration-dependent sensing. An open question associated with electrochemical CLZ monitoring is whether drug-protein complexes (i...
August 1, 2017: Pharmaceuticals
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