835 results match your criteria Pharmaceuticals [Journal]


Late Neurological Consequences of Zika Virus Infection: Risk Factors and Pharmaceutical Approaches.

Pharmaceuticals (Basel) 2019 Apr 17;12(2). Epub 2019 Apr 17.

School of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro 21944-590, Brazil.

Zika virus (ZIKV) infection was historically considered a disease with mild symptoms and no major consequences to human health. However, several long-term, late onset, and chronic neurological complications, both in congenitally-exposed babies and in adult patients, have been reported after ZIKV infection, especially after the 2015 epidemics in the American continent. The development or severity of these conditions cannot be fully predicted, but it is possible that genetic, epigenetic, and environmental factors may contribute to determine ZIKV infection outcomes. Read More

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http://dx.doi.org/10.3390/ph12020060DOI Listing

Insights into the Molecular Mechanisms of Eg5 Inhibition by (+)-Morelloflavone.

Pharmaceuticals (Basel) 2019 Apr 16;12(2). Epub 2019 Apr 16.

Department of Environmental Studies, Graduate School of Fisheries and Environmental Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.

(+)-Morelloflavone (MF) is an antitumor biflavonoid that is found in the species. Recently, we reported MF as a novel inhibitor of ATPase and microtubules-gliding activities of the kinesin spindle protein (Eg5) in vitro. Herein, we provide dynamical insights into the inhibitory mechanisms of MF against Eg5, which involves binding of the inhibitor to the loop5/α2/α3 allosteric pocket. Read More

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https://www.mdpi.com/1424-8247/12/2/58
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http://dx.doi.org/10.3390/ph12020058DOI Listing
April 2019
2 Reads

The Importance of Iron Status for Young Children in Low- and Middle-Income Countries: A Narrative Review.

Pharmaceuticals (Basel) 2019 Apr 16;12(2). Epub 2019 Apr 16.

Laboratory of Human Nutrition, Institute of Food Nutrition and Health, Department of Health Sciences and Technology, ETH Zürich, CH-8092 Zürich, Switzerland.

Early childhood is characterised by high physiological iron demand to support processes including blood volume expansion, brain development and tissue growth. Iron is also required for other essential functions including the generation of effective immune responses. Adequate iron status is therefore a prerequisite for optimal child development, yet nutritional iron deficiency and inflammation-related iron restriction are widespread amongst young children in low- and middle-income countries (LMICs), meaning iron demands are frequently not met. Read More

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https://www.mdpi.com/1424-8247/12/2/59
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http://dx.doi.org/10.3390/ph12020059DOI Listing
April 2019
1 Read

Protective Effect of Cashew Gum (Anacardium occidentale L.) on 5-Fluorouracil-Induced Intestinal Mucositis.

Pharmaceuticals (Basel) 2019 Apr 3;12(2). Epub 2019 Apr 3.

Department of Morphology, Faculty of Medicine, Federal University of Ceará, s/n Delmiro de Farias Street, Porangabuçu Campus, 60416-030 Fortaleza, Brazil.

Intestinal mucositis is a common complication associated with 5-fluorouracil (5-FU), a chemotherapeutic agent used for cancer treatment. Cashew gum (CG) has been reported as a potent anti-inflammatory agent. In the present study, we aimed to evaluate the effect of CG extracted from the exudate of L. Read More

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http://dx.doi.org/10.3390/ph12020051DOI Listing

CDK11 Loss Induces Cell Cycle Dysfunction and Death of BRAF and NRAS Melanoma Cells.

Pharmaceuticals (Basel) 2019 Apr 2;12(2). Epub 2019 Apr 2.

Masonic Cancer Center, University of Minnesota, Minneapolis, MN 55455, USA.

Cyclin dependent kinase 11 (CDK11) is a protein kinase that regulates RNA transcription, pre-mRNA splicing, mitosis, and cell death. Targeting of CDK11 expression levels is effective in the experimental treatment of breast and other cancers, but these data are lacking in melanoma. To understand CDK11 function in melanoma, we evaluated protein and RNA levels of CDK11, Cyclin L1 and Cyclin L2 in benign melanocytes and BRAF- as well as NRAS-mutant melanoma cell lines. Read More

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http://dx.doi.org/10.3390/ph12020050DOI Listing

3-Vinylazetidin-2-Ones: Synthesis, Antiproliferative and Tubulin Destabilizing Activity in MCF-7 and MDA-MB-231 Breast Cancer Cells.

Pharmaceuticals (Basel) 2019 Apr 11;12(2). Epub 2019 Apr 11.

School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, 2 DO2R590 Dublin, Ireland.

Microtubule-targeted drugs are essential chemotherapeutic agents for various types of cancer. A series of 3-vinyl-β-lactams (2-azetidinones) were designed, synthesized and evaluated as potential tubulin polymerization inhibitors, and for their antiproliferative effects in breast cancer cells. These compounds showed potent activity in MCF-7 breast cancer cells with an IC value of 8 nM for compound 4-[3-Hydroxy-4-methoxyphenyl]-1-(3,4,5-trimethoxyphenyl)-3-vinylazetidin-2-one) which was comparable to the activity of Combretastatin A-4. Read More

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http://dx.doi.org/10.3390/ph12020056DOI Listing

Strategies for the Development of Glycomimetic Drug Candidates.

Authors:
Rachel Hevey

Pharmaceuticals (Basel) 2019 Apr 11;12(2). Epub 2019 Apr 11.

Molecular Pharmacy, Dept. Pharmaceutical Sciences, University of Basel, Klingelbergstr. 50, 4056 Basel, Switzerland.

Carbohydrates are a structurally-diverse group of natural products which play an important role in numerous biological processes, including immune regulation, infection, and cancer metastasis. Many diseases have been correlated with changes in the composition of cell-surface glycans, highlighting their potential as a therapeutic target. Unfortunately, native carbohydrates suffer from inherently weak binding affinities and poor pharmacokinetic properties. Read More

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http://dx.doi.org/10.3390/ph12020055DOI Listing

TRP Channels and Migraine: Recent Developments and New Therapeutic Opportunities.

Pharmaceuticals (Basel) 2019 Apr 9;12(2). Epub 2019 Apr 9.

School of Behavioral and Brain Sciences, Center for Advanced Pain Studies, The University of Texas at Dallas, Richardson, TX 75080, USA.

Migraine is the second-most disabling disease worldwide, and the second most common neurological disorder. Attacks can last many hours or days, and consist of multiple symptoms including headache, nausea, vomiting, hypersensitivity to stimuli such as light and sound, and in some cases, an aura is present. Mechanisms contributing to migraine are still poorly understood. Read More

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https://www.mdpi.com/1424-8247/12/2/54
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http://dx.doi.org/10.3390/ph12020054DOI Listing
April 2019
2 Reads

Evaluation of the Larvicidal Potential of the Essential Oil (Blanco) Benth in the Control of .

Pharmaceuticals (Basel) 2019 Apr 8;12(2). Epub 2019 Apr 8.

Laboratory of Pharmacognosy and Phytochemistry, Federal University of Amapa, Highway Jucelino Kubistichek, Km 02, 68.902-280 Macapa, Brazil; (L.B.B.).

The objective of this work was to collect information on the chemical constituents that demonstrate the larvicidal activity against , as well as the antioxidant, microbiological, and cytotoxicity potential of the essential oil of leaves. The chemical characterization was performed by gas chromatography coupled to mass spectrometer (GC-MS). The larvicidal activity was performed according to the protocol of the World Health Organization. Read More

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http://dx.doi.org/10.3390/ph12020053DOI Listing

2018 FDA Tides Harvest.

Pharmaceuticals (Basel) 2019 Apr 5;12(2). Epub 2019 Apr 5.

KRISP, School of Laboratory of Medicine and Medical Science, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa.

In 2018, the United States Food and Drug Administration (FDA) approved a total of 59 new drugs, three of them (5%) are TIDES (or also, -tides), two oligonucleotides and one peptide. Herein, the three TIDES approved are analyzed in terms of medical target, mode of action, chemical structure, and economics. Read More

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http://dx.doi.org/10.3390/ph12020052DOI Listing

Chemical Profile and Biological Activities of Essential Oil from L. Cultivated in Brazil.

Pharmaceuticals (Basel) 2019 Apr 1;12(2). Epub 2019 Apr 1.

Department of Pathology, Biological and Health Sciences Center, Federal University of Maranhão, São Luís 65085-580, MA, Brazil.

Essential oil from the leaves of L. (Compositae) cultivated in Brazil was investigated for its chemical composition and biological activities including antibacterial, antifungal, and anthelmintic. The constituents of essential oils isolated by hydro-distillation were examined by GC-MS and a total of 18 components were identified. Read More

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http://dx.doi.org/10.3390/ph12020049DOI Listing

Role of TRPV1 and TRPA1 Ion Channels in Inflammatory Bowel Diseases: Potential Therapeutic Targets?

Pharmaceuticals (Basel) 2019 Mar 30;12(2). Epub 2019 Mar 30.

Department of Pharmacology and Pharmacotherapy, Medical School and Molecular Pharmacology Research Group, Szentágothai Research Centre, University of Pécs, H-7624 Pécs, Hungary.

Inflammatory bowel diseases (IBD) have long been recognized to be accompanied by pain resulting in high morbidity. Transient receptor potential vanilloid 1 (TRPV1) and ankyrin 1 (TRPA1) ion channels located predominantly on the capsaicin-sensitive sensory neurons play a complex role in hyperalgesia and neurogenic inflammation. This review provides an overview of their expression and role in intestinal inflammation, in particular colitis, that appears to be virtually inconsistent based on the thorough investigations of the last twenty years. Read More

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http://dx.doi.org/10.3390/ph12020048DOI Listing
March 2019
1 Read

Chain-Branched Polyhydroxylated Octahydro--Indoles as Potential Leads against Lysosomal Storage Diseases.

Pharmaceuticals (Basel) 2019 Mar 29;12(2). Epub 2019 Mar 29.

Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.

Here, the synthesis and glycosidase inhibition properties of the two first known 3-ethyloctahydro-1-indole-4,5,6-triols are reported. This study shows the transformation of d-glucose into polyhydroxylated 1-(2-nitrocyclohexane) acetaldehydes, followed by a protocol involving the formation of the azacyclopentane ring. Results of inhibitory potency assays and docking calculations show that at least one of them could be a lead for optimization in the search for compounds that behave like folding chaperones in lysosomal storage diseases. Read More

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http://dx.doi.org/10.3390/ph12020047DOI Listing
March 2019
1 Read

The Effects of Hydration Parameters and Co-Surfactants on Methylene Blue-Loaded Niosomes Prepared by the Thin Film Hydration Method.

Pharmaceuticals (Basel) 2019 Mar 29;12(2). Epub 2019 Mar 29.

University of Sunderland, School of Pharmacy and Pharmaceutical Sciences, Sunderland SR1 3SD, UK.

This work aimed to investigate and optimise the effects of co-surfactants, hydration volume, and time on the entrapment of methylene blue (MB) within niosomes and the vesicle sizes of MB-loaded niosomes upon different storage temperatures. Niosomes were prepared by the thin film hydration method followed by gel permeation chromatography to obtain purified niosome suspensions. The probe sonication method was used to reduce the niosome vesicle size and distribution. Read More

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http://dx.doi.org/10.3390/ph12020046DOI Listing

APELA Expression in Glioma, and Its Association with Patient Survival and Tumor Grade.

Pharmaceuticals (Basel) 2019 Mar 26;12(1). Epub 2019 Mar 26.

Department of Pathology and the Center for Cancer Research, University of Tennessee Health Science Center, Memphis, TN 38163, USA.

Glioblastoma (GBM) is the most common and deadliest primary adult brain tumor. Invasion, resistance to therapy, and tumor recurrence in GBM can be attributed in part to brain tumor-initiating cells (BTICs). BTICs isolated from various patient-derived xenografts showed high expression of the poorly characterized Apelin early ligand A (APELA) gene. Read More

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http://dx.doi.org/10.3390/ph12010045DOI Listing
March 2019
2 Reads

Raman Microspectroscopy as a Tool to Elucidate the Efficacy of Topical Formulations Containing Curcumin.

Pharmaceuticals (Basel) 2019 Mar 23;12(1). Epub 2019 Mar 23.

São Carlos Institute of Physics, University of São Paulo, Trabalhador Sao-carlense Av., 400, São Carlos, SP 13566-590, Brazil.

The success of the onychomycosis treatment is directly associated with factors such as the choice of the medication, the administration route, and the pharmaceutical formulation. Photodynamic therapy (PDT) is an emerging and promising technique indicated for onychomycosis treatment. For this application, the main challenge is the efficient delivery of the photosensitizer (PS). Read More

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https://www.mdpi.com/1424-8247/12/1/44
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http://dx.doi.org/10.3390/ph12010044DOI Listing
March 2019
2 Reads

Microencapsulation of -Specific Bacteriophage Felix O1 Using Spray-Drying in a pH-Responsive Formulation and Direct Compression Tableting of Powders into a Solid Oral Dosage Form.

Pharmaceuticals (Basel) 2019 Mar 22;12(1). Epub 2019 Mar 22.

Department of Chemical Engineering, Loughborough University, Loughborough LE11 3TU, UK.

The treatment of enteric bacterial infections using oral bacteriophage therapy can be challenging since the harsh acidic stomach environment renders phages inactive during transit through the gastrointestinal tract. Solid oral dosage forms allowing site-specific gastrointestinal delivery of high doses of phages, e.g. Read More

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http://dx.doi.org/10.3390/ph12010043DOI Listing
March 2019
1 Read

Localization of Tc-GRP Analogs in GRPR-Expressing Tumors: Effects of Peptide Length and Neprilysin Inhibition on Biological Responses.

Pharmaceuticals (Basel) 2019 Mar 20;12(1). Epub 2019 Mar 20.

Molecular Radiopharmacy, INRASTES, NCSR "Demokritos", 15310 Athens, Greece.

The overexpression of gastrin-releasing peptide receptors (GRPRs) in frequently occurring human tumors has provided the opportunity to use bombesin (BBN) analogs as radionuclide carriers to cancer sites for diagnostic and therapeutic purposes. We have been alternatively exploring human GRP motifs of higher GRPR selectivity compared to frog BBN sequences aiming to improve pharmacokinetic profiles. In the present study, we compared two differently truncated human endogenous GRP motifs: GRP(14⁻27) and GRP(18⁻27). Read More

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http://dx.doi.org/10.3390/ph12010042DOI Listing

BACE-1 and γ-Secretase as Therapeutic Targets for Alzheimer's Disease.

Pharmaceuticals (Basel) 2019 Mar 19;12(1). Epub 2019 Mar 19.

Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.

Alzheimer's disease (AD) is a growing global health concern with a massive impact on affected individuals and society. Despite the considerable advances achieved in the understanding of AD pathogenesis, researchers have not been successful in fully identifying the mechanisms involved in disease progression. The amyloid hypothesis, currently the prevalent theory for AD, defends the deposition of β-amyloid protein (Aβ) aggregates as the trigger of a series of events leading to neuronal dysfunction and dementia. Read More

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http://dx.doi.org/10.3390/ph12010041DOI Listing
March 2019
1 Read

Physical Stability and Viscoelastic Properties of Co-Amorphous Ezetimibe/Simvastatin System.

Pharmaceuticals (Basel) 2019 Mar 19;12(1). Epub 2019 Mar 19.

Institute of Physics, University of Silesia, SMCEBI, 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland.

The purpose of this paper is to examine the physical stability as well as viscoelastic properties of the binary amorphous ezetimibe⁻simvastatin system. According to our knowledge, this is the first time that such an amorphous composition is prepared and investigated. The tendency toward re-crystallization of the amorphous ezetimibe⁻simvastatin system, at both standard storage and elevated temperature conditions, have been studied by means of X-ray diffraction (XRD). Read More

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http://dx.doi.org/10.3390/ph12010040DOI Listing

Development of a Microwave-assisted Chemoselective Synthesis of Oxime-linked Sugar Linkers and Trivalent Glycoclusters.

Pharmaceuticals (Basel) 2019 Mar 14;12(1). Epub 2019 Mar 14.

Department of Chemistry, California State University, Sacramento, 6000 J Street, Sacramento, CA 95819-6057, USA.

A rapid, high-yielding microwave-mediated synthetic procedure was developed and optimized using a model system of monovalent sugar linkers, with the ultimate goal of using this method for the synthesis of multivalent glycoclusters. The reaction occurs between the aldehyde/ketone on the sugars and an aminooxy moiety on the linker/trivalent core molecules used in this study, yielding acid-stable oxime linkages in the products and was carried out using equimolar quantities of reactants under mild aqueous conditions. Because the reaction is chemoselective, sugars can be incorporated without the use of protecting groups and the reactions can be completed in as little as 30 min in the microwave. Read More

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http://dx.doi.org/10.3390/ph12010039DOI Listing

Potential of the Other Genetic Information Coded by the Viral RNA Genomes as Antiviral Target.

Pharmaceuticals (Basel) 2019 Mar 13;12(1). Epub 2019 Mar 13.

Instituto de Parasitología y Biomedicina López-Neyra, (IPBLN-CSIC); Av. del Conocimiento 17, PTS Granada, Armilla, 18016 Granada, Spain.

In addition to the protein coding information, viral RNA genomes code functional information in structurally conserved units termed functional RNA domains. These RNA domains play essential roles in the viral cycle (e.g. Read More

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https://www.mdpi.com/1424-8247/12/1/38
Publisher Site
http://dx.doi.org/10.3390/ph12010038DOI Listing
March 2019
4 Reads

Baricitinib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Janus Kinases.

Pharmaceuticals (Basel) 2019 Mar 12;12(1). Epub 2019 Mar 12.

Formerly head of the Department of Organic Chemistry (FS), University of Mons-UMONS, 7000 Mons, Belgium.

In 2018, Baricitinib was approved by the Food and Drig Administration (FDA) for the treatment of rheumatoid arthritis. Baricitinib exerts its action by targeting Janus kinases (JAK). In this study, we describe the necessary steps for preparing the drug using two alternative routes. Read More

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https://www.mdpi.com/1424-8247/12/1/37
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http://dx.doi.org/10.3390/ph12010037DOI Listing
March 2019
8 Reads

In Silico Study to Identify New Antituberculosis Molecules from Natural Sources by Hierarchical Virtual Screening and Molecular Dynamics Simulations.

Pharmaceuticals (Basel) 2019 Mar 12;12(1). Epub 2019 Mar 12.

Graduate Program in Biotechnology, State University of Feira de Santana, 44036-900 Feira de Santana, BA, Brazil.

Tuberculosis (TB) is an infection caused by , responsible for 1.5 million documented deaths in 2016. The increase in reported cases of resistance to the main drugs show the need for the development of new and efficient drugs for better TB control. Read More

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http://dx.doi.org/10.3390/ph12010036DOI Listing
March 2019
1 Read

Phages for Phage Therapy: Isolation, Characterization, and Host Range Breadth.

Authors:
Paul Hyman

Pharmaceuticals (Basel) 2019 Mar 11;12(1). Epub 2019 Mar 11.

Department of Biology/Toxicology, Ashland University, 401 College Ave., Ashland, OH 44805, USA.

For a bacteriophage to be useful for phage therapy it must be both isolated from the environment and shown to have certain characteristics beyond just killing strains of the target bacterial pathogen. These include desirable characteristics such as a relatively broad host range and a lack of other characteristics such as carrying toxin genes and the ability to form a lysogen. While phages are commonly isolated first and subsequently characterized, it is possible to alter isolation procedures to bias the isolation toward phages with desirable characteristics. Read More

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http://dx.doi.org/10.3390/ph12010035DOI Listing
March 2019
1 Read

Chemical Characterization, Antioxidant, Cytotoxic and Microbiological Activities of the Essential Oil of Leaf of (Hemsl) A. Gray (Asteraceae).

Pharmaceuticals (Basel) 2019 Mar 4;12(1). Epub 2019 Mar 4.

Laboratory of Pharmacognosy and Phytochemistry-Federal University of Amapá-Highway Jucelino Kubistichek, Km-02. Macapá, 68.902-280 Amapá, Brazil.

The present study aimed to evaluate the chemical composition, antioxidant potential, and the cytotoxic and antimicrobial activity of the essential oil of the plant species (Hemsl) A. Gray. The essential oil obtained was used to identify the chemical compounds present through the techniques of GC-MS and NMR. Read More

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http://dx.doi.org/10.3390/ph12010034DOI Listing

Characterisation of an Isogenic Model of Cisplatin Resistance in Oesophageal Adenocarcinoma Cells.

Pharmaceuticals (Basel) 2019 Feb 20;12(1). Epub 2019 Feb 20.

Department of Surgery, Trinity Translational Medicine Institute, St. James's Hospital, Trinity College Dublin, Dublin 8, Ireland.

Cisplatin (cis-diamminedichloroplatinum) is widely used for the treatment of solid malignancies; however, the development of chemoresistance hinders the success of this chemotherapeutic in the clinic. This study provides novel insights into the molecular and phenotypic changes in an isogenic oesophageal adenocarcinoma (OAC) model of acquired cisplatin resistance. Key differences that could be targeted to overcome cisplatin resistance are highlighted. Read More

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http://dx.doi.org/10.3390/ph12010033DOI Listing
February 2019
4 Reads

Development and Characterization of Chitosan Microparticles-in-Films for Buccal Delivery of Bioactive Peptides.

Pharmaceuticals (Basel) 2019 Feb 20;12(1). Epub 2019 Feb 20.

Escola Superior de Biotecnologia, Centro de Biotecnologia e Química Fina, Rua Arquiteto Lobão Vital, 172, 4200-374 Porto, Portugal.

Nowadays, bioactive peptides are used for therapeutic applications and the selection of a carrier to deliver them is very important to increase the efficiency, absorption, release, bioavailability and consumer acceptance. The aim of this study was to develop and characterize chitosan-based films loaded with chitosan microparticles containing a bioactive peptide (sequence: KGYGGVSLPEW) with antihypertensive properties. Films were prepared by the solvent casting method, while the microparticles were prepared by ionic gelation. Read More

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http://dx.doi.org/10.3390/ph12010032DOI Listing
February 2019

Conformation and Cross-Protection in Group B Streptococcus Serotype III and Serotype 14: A Molecular Modeling Study.

Pharmaceuticals (Basel) 2019 Feb 13;12(1). Epub 2019 Feb 13.

Department of Chemistry, University of Cape Town, Cape Town 7701, South Africa.

Although the branched capsular polysaccharides of serotype III (GBSIII PS) and serotype 14 (Pn14 PS) differ only in the addition of a terminal sialic acid on the GBSIII PS side chains, these very similar polysaccharides are immunogenically distinct. Our simulations of GBSIII PS, Pn14 PS and the unbranched backbone polysaccharide provide a conformational rationale for the different antigenic epitopes identified for these PS. We find that side chains stabilize the proximal β dGlc(1→6) β dGlcNAc backbone linkage, restricting rotation and creating a well-defined conformational epitope at the branch point. Read More

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http://dx.doi.org/10.3390/ph12010028DOI Listing
February 2019
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2-Nitroimidazole-Furanoside Derivatives for Hypoxia Imaging-Investigation of Nucleoside Transporter Interaction, F-Labeling and Preclinical PET Imaging.

Pharmaceuticals (Basel) 2019 Feb 15;12(1). Epub 2019 Feb 15.

Werner Siemens Imaging Center, Department of Preclinical Imaging and Radiopharmacy, Eberhard Karls University of Tübingen, Röntgenweg 13, 72076 Tübingen, Germany.

The benefits of PET imaging of tumor hypoxia in patient management has been demonstrated in many examples and with various tracers over the last years. Although, the optimal hypoxia imaging agent has yet to be found, 2-nitroimidazole (azomycin) sugar derivatives-mimicking nucleosides-have proven their potential with [F]FAZA ([F]fluoro-azomycin--arabinoside) as a prominent representative in clinical use. Still, for all of these tracers, cellular uptake by passive diffusion is postulated with the disadvantage of slow kinetics and low tumor-to-background ratios. Read More

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http://dx.doi.org/10.3390/ph12010031DOI Listing
February 2019

Iron in Lung Pathology.

Pharmaceuticals (Basel) 2019 Feb 15;12(1). Epub 2019 Feb 15.

Department of Medicine, David Geffen School of Medicine at the University of California, Los Angeles, CA 90095, USA.

The lung presents a unique challenge for iron homeostasis. The entire airway is in direct contact with the environment and its iron particulate matter and iron-utilizing microbes. However, the homeostatic and adaptive mechanisms of pulmonary iron regulation are poorly understood. Read More

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http://dx.doi.org/10.3390/ph12010030DOI Listing
February 2019
1 Read

Inflammation and Depression: A Nervous Plea for Psychiatry to Not Become Immune to Interpretation.

Pharmaceuticals (Basel) 2019 Feb 14;12(1). Epub 2019 Feb 14.

Aquitaine Institute for Integrative and Cognitive Neuroscience (INCIA) UMR CNRS 5287, University of Bordeaux, 146 rue Léo Saignat, 33076 Bordeaux, France.

The possibility that inflammation plays a causal role in major depression is an important claim in the emerging field of immunopsychiatry and has generated hope for new treatments. The aims of the present review are first to provide some historical background and to consider the evidence in favor of the claim that inflammation is causally involved in major depression. The second part discusses some of the possibilities allowed for by the use of broad 'umbrella' concepts, such as inflammation and stress, in terms of proposing new working hypotheses and potential mechanisms. Read More

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http://dx.doi.org/10.3390/ph12010029DOI Listing
February 2019

Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson's Disease.

Pharmaceuticals (Basel) 2019 Feb 5;12(1). Epub 2019 Feb 5.

Department of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Rua Cesario Mota Junior 61, Sao Paulo 01221-020, Brazil.

Parkinson's disease (PD) is a neurodegenerative disease characterized by the loss of dopaminergic neurons in the , leading to alteration of the integrity of dopaminergic transporters (DATs). In recent years, some radiopharmaceuticals have been used in the clinic to evaluate the integrity of DATs. These include tropane derivatives such as radiolabeled β-CIT and FP-CIT with iodine-123 (I), and TRODAT-1 with metastable technetium-99 (Tc). Read More

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http://dx.doi.org/10.3390/ph12010025DOI Listing
February 2019
1 Read

Neurodegeneration with Brain Iron Accumulation Disorders: Valuable Models Aimed at Understanding the Pathogenesis of Iron Deposition.

Pharmaceuticals (Basel) 2019 Feb 9;12(1). Epub 2019 Feb 9.

Fondazione IRCCS Istituto Neurologico Carlo Besta, 20126 Milano, Italy.

Neurodegeneration with brain iron accumulation (NBIA) is a set of neurodegenerative disorders, which includes very rare monogenetic diseases. They are heterogeneous in regard to the onset and the clinical symptoms, while the have in common a specific brain iron deposition in the region of the basal ganglia that can be visualized by radiological and histopathological examinations. Nowadays, 15 genes have been identified as causative for NBIA, of which only two code for iron-proteins, while all the other causative genes codify for proteins not involved in iron management. Read More

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http://dx.doi.org/10.3390/ph12010027DOI Listing
February 2019

Curcumin and (-)- Epigallocatechin-3-Gallate Protect Murine MIN6 Pancreatic Beta-Cells Against Iron Toxicity and Erastin-Induced Ferroptosis.

Pharmaceuticals (Basel) 2019 Feb 6;12(1). Epub 2019 Feb 6.

Department of Nutritional Sciences, School of Life Course Sciences, King's College London. Franklin-Wilkins-Building, 150 Stamford Street, London, SE1 9NH, UK.

Ferroptosis is a form of programmed cell death that is characterized by lipid peroxidation and is inducible by iron and the accumulation of reactive oxygen species (ROS). It is triggered by erastin but inhibited by antioxidants such as -tocopherol, -carotene, polyphenols, and iron chelators such as deferoxamine (DFO), nitrilotriacetic acid (NTA), and ethylenediaminetetraacetic acid (EDTA). This study investigated the protective effects of two polyphenols, curcumin and (-)- epigallocatechin-3-gallate (EGCG), against iron loading and erastin-mediated ferroptosis in MIN6 cells. Read More

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http://dx.doi.org/10.3390/ph12010026DOI Listing
February 2019
6 Reads

Camphor, Applied Epidermally to the Back, Causes Snout- and Chest-Grooming in Rats: A Response Mediated by Cutaneous TRP Channels.

Pharmaceuticals (Basel) 2019 Feb 2;12(1). Epub 2019 Feb 2.

Graduate Program in Neuroscience and Cognition, Federal University of ABC, São Bernardo do Campo 09606-070, SP, Brazil.

Thermoregulatory grooming, a behavioral defense against heat, is known to be driven by skin-temperature signals. Because at least some thermal cutaneous signals that drive heat defenses are likely to be generated by transient receptor potential (TRP) channels, we hypothesized that warmth-sensitive TRPs drive thermoregulatory grooming. Adult male Wistar rats were used. Read More

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http://dx.doi.org/10.3390/ph12010024DOI Listing
February 2019
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Modulators of Transient Receptor Potential (TRP) Channels as Therapeutic Options in Lung Disease.

Pharmaceuticals (Basel) 2019 Feb 1;12(1). Epub 2019 Feb 1.

Walther-Straub-Institute of Pharmacology and Toxicology, Member of the German Center for Lung Research(DZL), LMU Munich, Nussbaumstr. 26, D-80336 Munich, Germany.

The lungs are essential for gas exchange and serve as the gateways of our body to the external environment. They are easily accessible for drugs from both sides, the airways and the vasculature. Recent literature provides evidence for a role of Transient Receptor Potential (TRP) channels as chemosensors and essential members of signal transduction cascades in stress-induced cellular responses. Read More

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http://dx.doi.org/10.3390/ph12010023DOI Listing
February 2019
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Correction: Mateusz, S., et al. Iron Supplementation in Suckling Piglets: An Ostensibly Easy Therapy of Neonatal Iron Deficiency Anemia. Pharmaceuticals 2018, 11, 128.

Pharmaceuticals (Basel) 2019 Jan 29;12(1). Epub 2019 Jan 29.

Department of Molecular Biology, Institute of Genetics and Animal Breeding, Polish Academy of Sciences, Jastrzębiec, 05-552 Magdalenka, Poland.

The authors wish to make the following corrections to this paper [¹]: the term "liposomal" should be replaced with the term "sucrosomial" in the following places [... Read More

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http://dx.doi.org/10.3390/ph12010022DOI Listing
January 2019
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On the Absolute Stereochemistry of Tolterodine: A Circular Dichroism Study.

Pharmaceuticals (Basel) 2019 Jan 26;12(1). Epub 2019 Jan 26.

Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via Moruzzi 13, 56124 Pisa, Italy.

Tolterodine () is a potent muscarinic receptor antagonist used in the treatment of overactive urinary bladder (OAB) syndrome. Tolterodine is chiral and it was patented, and is currently marketed, as the l-tartrate salt of the ()-enantiomer. However, the existing literature does not offer an ultimate proof of a stereoselective mode of action of . Read More

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http://dx.doi.org/10.3390/ph12010021DOI Listing
January 2019
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Identification of Potential Inhibitors from Pyriproxyfen with Insecticidal Activity by Virtual Screening.

Pharmaceuticals (Basel) 2019 Jan 25;12(1). Epub 2019 Jan 25.

Postgraduate Program in Biotechnology and Biodiversity-Network BIONORTE, Federal University of Amapá, Macapá, Amapá 68903-419, Brazil.

is the main vector of dengue fever transmission, yellow fever, Zika, and chikungunya in tropical and subtropical regions and it is considered to cause health risks to millions of people in the world. In this study, we search to obtain new molecules with insecticidal potential against via virtual screening. Pyriproxyfen was chosen as a template compound to search molecules in the database Zinc_Natural_Stock (ZNSt) with structural similarity using ROCS (rapid overlay of chemical structures) and EON (electrostatic similarity) software, and in the final search, the top 100 were selected. Read More

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http://dx.doi.org/10.3390/ph12010020DOI Listing
January 2019
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TRPV1 Inhibits the Ventilatory Response to Hypoxia in Adult Rats, but Not the CO₂-Drive to Breathe.

Pharmaceuticals (Basel) 2019 Jan 24;12(1). Epub 2019 Jan 24.

Department of Animal Morphology and Physiology, Faculty of Agricultural and Veterinarian Sciences, UNESP at Jaboticabal, Rod. Prof. Paulo Donato Castellane s/n, Jaboticabal SP 14870-000, Brazil.

Receptors of the transient receptor potential (TRP) channels superfamily are expressed in many tissues and have different physiological functions. However, there are few studies investigating the role of these channels in cardiorespiratory control in mammals. We assessed the role of central and peripheral TRPV1 receptors in the cardiorespiratory responses to hypoxia (10% O₂) and hypercapnia (7% CO₂) by measuring pulmonary ventilation ( V ˙ E ), heart rate (HR), mean arterial pressure (MAP) and body temperature (Tb) of male Wistar rats before and after intraperitoneal (AMG9810 [2. Read More

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http://dx.doi.org/10.3390/ph12010019DOI Listing
January 2019
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[Lu]Lu-PSMA-617 Salivary Gland Uptake Characterized by Quantitative Autoradiography.

Pharmaceuticals (Basel) 2019 Jan 24;12(1). Epub 2019 Jan 24.

Department of Nuclear Medicine, University Medical Center Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, Germany.

Irradiation of salivary glands remains the main dose-limiting side effect of therapeutic PSMA-inhibitors, especially when using alpha emitters. Thus, further advances in radiopharmaceutical design and therapy strategies are needed to reduce salivary gland uptake, thereby allowing the administration of higher doses and potentially resulting in improved response rates and better tumor control. As the uptake mechanism remains unknown, this work investigates the salivary gland uptake of [Lu]Lu-PSMA-617 by autoradiography studies on pig salivary gland tissue and on PSMA-overexpressing LNCaP cell membrane pellets. Read More

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http://dx.doi.org/10.3390/ph12010018DOI Listing
January 2019
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L-Ferritin: One Gene, Five Diseases; from Hereditary Hyperferritinemia to Hypoferritinemia-Report of New Cases.

Pharmaceuticals (Basel) 2019 Jan 23;12(1). Epub 2019 Jan 23.

BloodGenetics SL, Esplugues de Llobregat, 08950 Barcelona, Spain.

Ferritin is a multimeric protein composed of light (L-ferritin) and heavy (H-ferritin) subunits that binds and stores iron inside the cell. A variety of mutations have been reported in the L-ferritin subunit gene ( gene) that cause the following five diseases: (1) hereditary hyperferritinemia with cataract syndrome (HHCS), (2) neuroferritinopathy, a subtype of neurodegeneration with brain iron accumulation (NBIA), (3) benign hyperferritinemia, (4) L-ferritin deficiency with autosomal dominant inheritance, and (5) L-ferritin deficiency with autosomal recessive inheritance. Defects in the gene lead to abnormally high levels of serum ferritin (hyperferritinemia) in HHCS and benign hyperferritinemia, while low levels (hypoferritinemia) are present in neuroferritinopathy and in autosomal dominant and recessive L-ferritin deficiency. Read More

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http://www.mdpi.com/1424-8247/12/1/17
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http://dx.doi.org/10.3390/ph12010017DOI Listing
January 2019
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Can the Efficacy of [F]FDG-PET/CT in Clinical Oncology Be Enhanced by Screening Biomolecular Profiles?

Pharmaceuticals (Basel) 2019 Jan 23;12(1). Epub 2019 Jan 23.

Trinity Translational Medicine Institute, Department of Surgery, Trinity College Dublin, D08W9RT Dublin, Ireland.

Positron Emission Tomography (PET) is a functional imaging modality widely used in clinical oncology. Over the years the sensitivity and specificity of PET has improved with the advent of specific radiotracers, increased technical accuracy of PET scanners and incremental experience of Radiologists. However, significant limitations exist-most notably false positives and false negatives. Read More

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http://dx.doi.org/10.3390/ph12010016DOI Listing
January 2019
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Micellisation Mechanism and Behaviour of Soluplus®⁻Furosemide Micelles: Preformulation Studies of an Oral Nanocarrier-Based System.

Pharmaceuticals (Basel) 2019 Jan 19;12(1). Epub 2019 Jan 19.

Department of Pharmacy, University of Oslo, 0316 Oslo, Norway.

In this study, self-assembling Soluplus® micelles were examined for inherent properties. Through calorimetric analysis, the critical micelle concentration (CMC) could be determined at 25 and 37 °C, and the influence of three media (Milli-Q water, phosphate-buffered saline (PBS) with a pH of 7.4 and 0. Read More

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http://dx.doi.org/10.3390/ph12010015DOI Listing
January 2019
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Structural and In Vitro Functional Comparability Analysis of Altebrel™, a Proposed Etanercept Biosimilar: Focus on Primary Sequence and Glycosylation.

Pharmaceuticals (Basel) 2019 Jan 17;12(1). Epub 2019 Jan 17.

Mass Spectrometric Proteomics, Institute of Clinical Chemistry and Laboratory Medicine, Campus Forschung, N27 Raum 00.008, Universitätsklinikum Hamburg-Eppendorf, Martinistr. 52, 20246 Hamburg, Germany.

The demand for reliable comparability studies of biosimilars grows with their increased market share. These studies focus on physicochemical, structural, functional and clinical properties to ensure that a biosimilar has no significant differences to the originator product and can be released into the market without extensive clinical trials. In the current study, Enbrel (etanercept, the originator) and Altebrel™ (the proposed biosimilar) underwent direct comparison. Read More

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http://dx.doi.org/10.3390/ph12010014DOI Listing
January 2019
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Cholecystokinin-2 Receptor Targeting with Novel C-terminally Stabilized HYNIC-Minigastrin Analogs Radiolabeled with Technetium-99m.

Pharmaceuticals (Basel) 2019 Jan 15;12(1). Epub 2019 Jan 15.

Department of Nuclear Medicine, Medical University of Innsbruck, Anichstrasse 35, A-6020 Innsbruck, Austria.

The high overexpression of cholecystokinin-2 receptors (CCK2R) in tumors, such as medullary thyroid carcinoma, allows for highly specific diagnostic and therapeutic targeting with radiolabeled peptide probes derived from natural ligands for the receptor. Based on the ideal imaging characteristics, high availability and low cost of technetium-99m (Tc)-labeled radiopharmaceuticals we have developed two hydrazinonicotinic acid (HYNIC) conjugated minigastrin analogs allowing labeling at high specific activity. The CCK2R targeting peptide conjugates show specific amino acid substitutions in the C-terminal receptor-specific sequence with the aim to increase stability and tumor targeting. Read More

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http://www.mdpi.com/1424-8247/12/1/13
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http://dx.doi.org/10.3390/ph12010013DOI Listing
January 2019
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Optimization of the Automated Synthesis of [11C]mHED-Administered and Apparent Molar Activities.

Pharmaceuticals (Basel) 2019 Jan 14;12(1). Epub 2019 Jan 14.

Division of Nuclear Medicine, Department of Biomedical Imaging and Image-guided Therapy, Medical University of Vienna, 1090Vienna, Austria.

The tracer -Hydroxyephedrine ([[11C]HED) is one of the most applied PET tracers for cardiac imaging, whose radiosynthesis was already reported in 1990. While not stated in the literature, separation difficulties and an adequate formulation of the product are well known challenges in its production. Furthermore, the precursor (metaraminol) is also a substrate for the norepinephrine transporter, and can therefore affect the image quality. Read More

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http://dx.doi.org/10.3390/ph12010012DOI Listing
January 2019
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The Therapeutic Potential of Naringenin: A Review of Clinical Trials.

Pharmaceuticals (Basel) 2019 Jan 10;12(1). Epub 2019 Jan 10.

Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol 61615585, Iran.

Naringenin is a flavonoid belonging to flavanones subclass. It is widely distributed in several fruits, bergamot, tomatoes and other fruits, being also found in its glycosides form (mainly naringin). Several biological activities have been ascribed to this phytochemical, among them antioxidant, antitumor, antiviral, antibacterial, anti-inflammatory, antiadipogenic and cardioprotective effects. Read More

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http://www.mdpi.com/1424-8247/12/1/11
Publisher Site
http://dx.doi.org/10.3390/ph12010011DOI Listing
January 2019
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Juvenile Arthritis Patients Suffering from Chronic Inflammation Have Increased Activity of Both IDO and GTP-CH1 Pathways But Decreased BH4 Efficacy: Implications for Well-Being, Including Fatigue, Cognitive Impairment, Anxiety, and Depression.

Pharmaceuticals (Basel) 2019 Jan 8;12(1). Epub 2019 Jan 8.

Division of Pharmacology, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, Faculty of Science, Universities 99, 3584 CG Utrecht, The Netherlands.

Juvenile idiopathic arthritis (JIA) represents joint inflammation with an unknown cause that starts before the age of 16, resulting in stiff and painful joints. In addition, JIA patients often report symptoms of sickness behavior. Recent animal studies suggest that proinflammatory cytokines produce sickness behavior by increasing the activity of indoleamine-2,3-dioxygenase (IDO) and guanosinetriphosphate⁻cyclohydrolase-1 (GTP⁻CH1). Read More

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http://dx.doi.org/10.3390/ph12010009DOI Listing
January 2019
3 Reads