305,139 results match your criteria Compound Presentations


β-Elemene Inhibits Human Sperm Function by Affecting Sperm Vitality and Intracellular Calcium.

Cell Physiol Biochem 2018 Dec 6;51(5):2019-2029. Epub 2018 Dec 6.

State Key Laboratory of Biocontrol and Guangdong Provincial Key Laboratory of Plant Resources, School of Life Sciences, Sun Yat-Sen University, Guangzhou,

Background/aims: β-Elemene is a bioactive sesquiterpene compound that exhibits a potent anti-tumor effect and is used in various clinical applications. However, little is known about its effect on the male reproductive system. The objective of this study was to investigate the in vitro actions of β-elemene on human sperm function and elucidate the underlying mechanism. Read More

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December 2018
3 Reads

Neuroprotective effects of a novel carnosine-hydrazide derivative on hippocampal CA1 damage after transient cerebral ischemia.

Eur J Med Chem 2018 Nov 28;163:207-214. Epub 2018 Nov 28.

Department of Neurosurgery, Kurume University, School of Medicine, Fukuoka, Japan. Electronic address:

Ischemia-reperfusion injuries produce reactive oxygen species that promote the peroxide lipid oxidation process resulting in the production of an endogenic lipid peroxide, 4-hydroxy-trans-2-nonenal (4-HNE), a highly cytotoxic aldehyde that induces cell death. We synthesized a novel 4-HNE scavenger - a carnosine-hydrazide derivative, l-carnosine hydrazide (CNN) - and examined its neuroprotective effect in a model of transient ischemia. PC-12 cells were pre-incubated with various doses (0-50 mmol/L) of CNN for 30 min, followed by incubation with 4-HNE (250 μM). Read More

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November 2018
1 Read

A multifunctional compound ebselen reverses memory impairment, apoptosis and oxidative stress in a mouse model of sporadic Alzheimer's disease.

J Psychiatr Res 2018 Nov 27;109:107-117. Epub 2018 Nov 27.

Laboratório de Síntese, Reatividade e Avaliação Farmacológica e Toxicológica de Organocalcogênios, Departamento de Bioquímica e Biologia Molecular, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria, CEP 97105-900, Santa Maria, Rio Grande do Sul, Brazil. Electronic address:

Alzheimer 's disease (AD) is characterized by progressive cognitive decline including memory impairment, cortical dysfunction, and neuropsychiatric disturbances. The drug discovery to treat AD consists to develop compounds able to act in multiple molecular targets involved in the pathogenesis of the disease and the repositioning of old drugs for new application. This way, the intracerebroventricular (icv) injection of streptozotocin (STZ) has been used as a metabolic model of sporadic AD. Read More

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November 2018

Engineering of pectin-dopamine nano-conjugates for carrying ruthenium complex: A potential tool for biomedical applications.

J Inorg Biochem 2018 Nov 28;191:135-142. Epub 2018 Nov 28.

Institute of Environmental Toxicology and Environmental Ecology, Yancheng Teachers University, Yancheng City, Jiangsu Province 224007, People's Republic of China. Electronic address:

In this work, we designed polysaccharide-metal complex of dopamine-modified pectin linking ruthenium compound, which exhibited a certain inhibition specificity to human renal cell adenocarcinoma cell line 786-O. The chemical structure and physical properties of the polysaccharide-metal complex were well characterized by multiple analysis methods. The multi-spectral results revealed that pectin-dopamine have been successfully coordinated by ruthenium complex to form nano-conjugates, which self-assembled into relatively regular nanospheres of approximately 200 nm. Read More

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November 2018
4 Reads

Protective effect of forsythoside B against lipopolysaccharide-induced acute lung injury by attenuating the TLR4/NF-κB pathway.

Int Immunopharmacol 2018 Dec 3;66:336-346. Epub 2018 Dec 3.

Key Laboratory of Prevention and Management of Chronic Kidney Disease of Zhanjiang City, Affiliated Hospital of Guangdong Medical University, Zhanjiang, Guangdong, 524001, China. Electronic address:

Acute lung injury (ALI), which is mainly triggered by infection, pneumonia, vasculitis, and sepsis, has no specific and effective therapy except for primary supportive treatment or bedside care. Excessive inflammation caused by innate immune cells is the major characteristic of ALI. Forsythoside B, a phenylethanoside compound, possesses good antioxidant and anti-bacterial properties in vivo and in vitro. Read More

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December 2018
2 Reads
2.472 Impact Factor

A paper sizing agent based on leather collagen hydrolysates modified by glycol diglycidyl ether and its compound performance.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

College of Arts and Sciences, Shaanxi University of Science & Technology, Xi'an, 710021, China.

In this research, collagen hydrolysates with different average molecular weights (Mn¯) from leather collagen were chosen as raw materials. Five environmental-friendly sizing agents (SA) were prepared by cross-linking collagen hydrolysates with glycol diglycidyl ether (GDE) and further grafting them with butyl acrylate (BA) and styrene (St). Then the compound sizing agents (SGDESA-x, x = 1, 2, 3 and 4) were obtained by simple physical mixing of GDESA and starch. Read More

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December 2018
2 Reads

Design, synthesis and anti-tumor evaluation of novel steroidal glycoconjugate with furoxan derivatives.

Steroids 2018 Dec 3. Epub 2018 Dec 3.

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China. Electronic address:

In this study, eighteen novel steroidal-furoxan derivatives with 3-glycosyl or 3-methoxy moiety (12a-c, 13a-c, 17a-c, 26a-c, 27a-c and 28a-c) were synthesized and their anti-proliferative activity was evaluated against eight drug-sensitive and three drug-resistant cancer cell lines HeLa, A2780, LNCaP, PC-3, MDA-MB-231, MCF-7, SW480, A549, MCF-7/ADR, A2780/CDDP and A2780/T. Most of them displayed significant anti-cancer potency in vitro with IC values at the nanomole level. Among them, 3-methoxy steroidal-furoxan hybrids expressed much better activity than that of 3-glycosyl substitute ones, while estrane and 5α-H-androstane scaffold were slightly more favorable to the improvement of anti-proliferative activity. Read More

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December 2018
3 Reads

CNB-001, a pleiotropic drug is efficacious in embolized agyrencephalic New Zealand white rabbits and ischemic gyrencephalic cynomolgus monkeys.

Exp Neurol 2018 Dec 3. Epub 2018 Dec 3.

Cellular Neurobiology Laboratories, The Salk Institute, La Jolla, CA, USA.

Ischemic stroke is an acute neurodegenerative disease that is extremely devastating to patients, their families and society. Stroke is inadequately treated even with endovascular procedures and reperfusion therapy. Using an extensive translational screening process, we have developed a pleiotropic cytoprotective agent with the potential to positively impact a large population of brain ischemia patients and revolutionize the process used for the development of new drugs to treat complex brain disorders. Read More

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December 2018
2 Reads

Comparison of efficacy of SHENQI compound and rosiglitazone in the treatment of diabetic vasculopathy analyzing multi-factor mediated disease-causing modules.

PLoS One 2018 6;13(12):e0207683. Epub 2018 Dec 6.

Teaching Hospital, School of Clinical Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China.

Atherosclerosis-predominant vasculopathy is a common complication of diabetes with high morbidity and high mortality, which is ruining the patient's daily life. As is known to all, traditional Chinese medicine (TCM) SHENQI compound and western medicine rosiglitazone play an important role in the treatment of diabetes. In particular, SHENQI compound has a significant inhibitory effect on vascular lesions. Read More

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December 2018

Loss of ARHGEF1 causes a human primary antibody deficiency.

J Clin Invest 2018 Dec 6. Epub 2018 Dec 6.

ARHGEF1 is a RhoA-specific guanine nucleotide exchange factor expressed in hematopoietic cells. We used whole-exome sequencing to identify compound heterozygous mutations in ARHGEF1, resulting in the loss of ARHGEF1 protein expression in two primary-antibody-deficient siblings presenting with recurrent severe respiratory tract infections and bronchiectasis. Both ARHGEF1-deficient patients showed an abnormal B cell immunophenotype, with a deficiency in marginal-zone and memory B cells and an increased frequency of transitional B cells. Read More

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December 2018

Kinetically selective and potent inhibitors of HDAC8.

Biol Chem 2018 Dec 1. Epub 2018 Dec 1.

Department of Chemical Engineering and Biotechnology, University of Applied Sciences Darmstadt, 64295 Darmstadt, Germany.

HDAC8 is an established and validated target for T-cell lymphoma and childhood neuroblastoma. The active site binding pocket of HDAC8 is highly conserved among all zinccontaining representatives of the histone deacetylase family. This explains that most HDACs are unselectively recognized by similar inhibitors featuring a zinc binding group (ZBG), a hydrophobic linker and a head group. Read More

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December 2018

Selectivity map for molecular beam epitaxy of advanced III-V quantum nanowire networks.

Nano Lett 2018 Dec 6. Epub 2018 Dec 6.

Selective area growth is a promising technique to enable fabrication of scalable III-V nanowire networks required to test proposals for Majorana-based quantum computing devices. However, the contours of the growth parameter window resulting in selective growth remain undefined. Herein, we present a set of experimental techniques which unambiguously establish the parameter space window resulting in selective III-V nanowire networks growth by molecular beam epitaxy. Read More

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December 2018

Interplay of Cysteine Exposure and Global Protein Dynamics in Small-molecule Recognition by a Regulator of G-protein Signaling Protein.

Proteins 2018 Dec 6. Epub 2018 Dec 6.

Department of Chemical Engineering, University of New Hampshire, Durham, NH.

Regulator of G protein signaling (RGS) proteins play a pivotal role in regulation of G protein-coupled receptor (GPCR) signaling and are therefore becoming an increasingly important therapeutic target. Recently discovered thiadiazolidinone (TDZD) compounds that target cysteine residues have shown different levels of specificities and potencies for the RGS4 protein, thereby suggesting intrinsic differences in dynamics of this protein upon binding of these compounds. In this work, we investigated using atomistic molecular dynamics (MD) simulations the effect of binding of several small-molecule inhibitors on perturbations and dynamical motions in RGS4. Read More

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December 2018

Detection and prioritization of developmentally neurotoxic and/or neurotoxic compounds using zebrafish.

Toxicol Sci 2018 Dec 5. Epub 2018 Dec 5.

BIOBIDE, Donostia - San Sebastián, Gipuzkoa, Spain.

The standard methods for toxicity testing using rodent models cannot keep pace with the increasing number of chemicals in our environment due to time and resource limitations. Hence, there is an unmet need for fast, sensitive and cost-effective alternate models to reliably predict toxicity. As part of Tox21 Phase III's effort, a 90-compound library was created and made available to researchers to screen for neurotoxicants using novel technology and models. Read More

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December 2018

Enantioselective synthesis and absolute configuration determination of hydroxywilfordic acid in sesquiterpene pyridine alkaloids.

Org Biomol Chem 2018 Dec 6. Epub 2018 Dec 6.

College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 21936, Republic of Korea.

An enantioselective synthetic route to hydroxywilfordic acid, a key subunit of sesquiterpene pyridine alkaloids such as wilfortrine, was developed. Asymmetric cyanation using Jacobsen's (R,R)-amino-thiourea and hydrolysis were performed to afford chiral α-hydroxy-α-methyl acid as the (S)-isomer. Naturally derived hydroxywilfordate prepared by methanolysis of wilfortrine was found to be the (R)-isomer upon comparison with the synthetic compound. Read More

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December 2018

Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.

J Med Chem 2018 Dec 6. Epub 2018 Dec 6.

Antifibrinolytic drugs provide important pharmacological interventions to reduce morbidity and mortality from excessive bleeding during surgery and after trauma. Current drugs used for inhibiting the dissolution of fibrin, the main structural component of blood clots, are associated with adverse events due to lack of potency, high doses and non-selective inhibition mechanisms. These deficiencies warrant the development of a new generation highly potent and selective fibrinolysis inhibitors. Read More

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December 2018
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Melanogenesis-Inhibitory and Cytotoxic Activities of Triterpene Glycoside Constituents from the Bark of Albizia procera.

J Nat Prod 2018 Dec 6. Epub 2018 Dec 6.

Department of Natural Medicine Chemistry, School of Traditional Chinese Pharmacy , China Pharmaceutical University , 24 Tongjiaxiang , Nanjing 210009 , People's Republic of China.

Five oleanane-type triterpene glycosides including three new ones, proceraosides E-G (1-3), were isolated from a MeOH-soluble extract of Albizia procera bark. The structures of 1-3 were determined by use of NMR spectra, HRESIMS, and chemical methods. Compounds 1-5 exhibited inhibitory activities against the proliferation of the A549, SKBR3, AZ521, and HL60 human cancer cell lines (IC 0. Read More

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December 2018
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Synthesis of novel derivatives of 7,8-dihydro-6H-imidazo[2,1-b][1,3]benzothiazol-5-one and their virus-inhibiting activity against influenza A virus.

Arch Pharm (Weinheim) 2018 Dec 6. Epub 2018 Dec 6.

Fluoro and Agrochemicals Division (Organic Chemistry Division-II), CSIR - Indian Institute of Chemical Technology, Hyderabad, India.

Influenza remains a highly pathogenic and hardly controlled human infection. The ability of selecting drug-resistant variants necessitates the search and development of novel anti-influenza drugs. Herein, we describe the synthesis and evaluation of a series of novel 2-substituted 7,8-dihydro-6H-imidazo[2,1-b][1,3]benzothiazol-5-ones 3a-k for their virus-inhibiting activity against influenza A virus. Read More

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December 2018
1 Read

Deciphering crystal packing effects in the spin crossover of six [Fe(2-pic)]Cl solvatomorphs.

Dalton Trans 2018 Dec 6. Epub 2018 Dec 6.

Institut für Physik, Universität zu Lübeck, Ratzeburger Allee 160, D-23562 Lübeck, Germany.

In this work we investigate how the crystal packing affects the spin crossover (SCO) of [FeII(2-pic)3]Cl2. Four alcohol solvatomorphs of this compound have been reported to present a transition from a singlet low spin (LS, S = 0) to a quintet high spin (HS, S = 5) state at different temperatures, whereas two other solvatomorphs remain in the HS state along the entire range of temperatures explored. Given that all these solvatomorphs are isostructural, this behavior hints at crystal packing effects playing an important role in the spin transition. Read More

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December 2018

Synthesis of modified β-methoxyphenylalanines via diazonium chemistry and their incorporation in desoxycyclomarin analogues.

Org Biomol Chem 2018 Dec 6. Epub 2018 Dec 6.

Institute of Organic Chemistry, Saarland University, P.O. Box 151150, 66041 Saarbrücken, Germany.

The marine natural products cyclomarins have remarkable anti-mycobacterial and antiplasmodial activities. The heptapeptic structure of this compound class comprisis four highly interesting non-canonical amino acids, including a rather unusual syn β-methoxyphenylalanine. To get a deeper insight into the structure-activity realtionship of cyclomarines, a straightforward protocol for the stereoselective synthesis of this building block was developed, based on diazonium chemistry. Read More

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December 2018
1 Read

Variable sialic acid content in milk of Indian cattle and buffalo across different stages of lactation.

J Dairy Res 2018 Dec 6:1-4. Epub 2018 Dec 6.

ICAR- National Bureau of Animal Genetic Resources,Karnal 132 001, Haryana,India.

The aim of this Research Communication was to contribute to the knowledge of milk sialic acid concentration of bovines with specific focus on India. Sialic acids (SA) are important constituents of mammalian milks. Buffaloes are the main milk producing species in India, therefore, our research focused on both cow and buffalo. Read More

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December 2018

Evaluation of Cytotoxic Potentials of Some Isoindole-1,3-Dione Derivatives on HeLa, C6 and A549 Cancer Cell Lines.

Med Chem 2018 Dec 5. Epub 2018 Dec 5.

Department of Chemistry, Faculty of Sciences, Atatürk University, 25240 Erzurum. Turkey.

Background: Norcantharimides are known as norcantharidine derivatives and contain an isoindole skeleton structure. Isoindole derivatives have positively effect on inflammatory pathologies including cancers.

Objective: Considering this information, firstly, isoindole derivatives containing different functional groups 4-13 have been synthesized from 2-alkyl/aryl-3a,4,7,7a-tetrahydro-1H-isoindole-1,3(2H)-dione. Read More

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December 2018

Synthesis, Characterization, Antibacterial and Antioxidant Potency of N-Substituted-2-Sulfanylidene-1,3-Thiazolidin-4-one Derivatives and QSAR Study.

Med Chem 2018 Dec 5. Epub 2018 Dec 5.

Faculty of Agrobiotehnical Sciences Osijek, Josip Juraj Strossmayer University of Osijek, Osijek. Croatia.

Background: Rhodanine is known for its potential and important role in the medicinal chemistry since its derivatives exhibit a wide range of pharmacological activities such as antibacterial, antifungal, antidiabetic, antitubercular, anti-HIV, antiparasitic, antioxidant, anticancer, anti-proliferative and anthelmintic agents.

Objectives: Since N-substituted rhodanine synthons are rarely commercially available, it is desirable to develop a straight forward synthetic approach for the synthesis of these key building blocks. The objective was to synthesize a series of rhodanine derivatives and to investigate their antimicrobial and antioxidant activity. Read More

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December 2018
1 Read

Metyltetraprole, a novel putative complex III inhibitor, targets known QoI-resistant strains of Zymoseptoria tritici and Pyrenophora teres.

Pest Manag Sci 2018 Dec 5. Epub 2018 Dec 5.

Health & Crop Science Research Laboratory, Sumitomo Chemical Co., Ltd., Takatsukasa 4-chome Takarazuka, Hyogo, 665-8555, Japan.

Background: Metyltetraprole is a new fungicide with unique tetrazolinone-moiety and similar side chain to a known QoI, pyraclostrobin. In this study, we describe a unique bioactivity of metyltetraprole especially on QoI-resistant strains of Zymoseptoria tritici and Pyrenophora teres.

Results: Metyltetraprole exhibited potent antifungal activity against Ascomycetes; it was especially effective against Z. Read More

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December 2018
2 Reads

The antibiotic action of methylarsenite is an emergent property of microbial communities.

Mol Microbiol 2018 Nov 22. Epub 2018 Nov 22.

Department of Cellular Biology and Pharmacology, Herbert Wertheim College of Medicine, Florida International University, Miami, FL, 33199, USA.

Arsenic is the most ubiquitous environmental toxin. Here, we demonstrate that bacteria have evolved the ability to use arsenic to gain a competitive advantage over other bacteria at least twice. Microbes generate toxic methylarsenite (MAs(III)) by methylation of arsenite (As(III)) or reduction of methylarsenate (MAs(V)). Read More

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November 2018

Dermoscopic evaluation of melanocytic nevi changes after photoepilation techniques: a prospective study.

J Eur Acad Dermatol Venereol 2018 Dec 6. Epub 2018 Dec 6.

Dermatology Clinic - Department of Medical Science and Public Health, University of Cagliari, Via Ospedale 54, 09124, Cagliari, Italy.

Background: The clinical and dermoscopic changes of melanocytic nevi under the effects of photo-epilation are poorly known.

Objective: Prospective study on clinical and dermatoscopic effects of photoepilation on melanocytic nevi.

Methods: Eighteen patients exposed to photo-epilation gave consent to a follow-up program from 2008 to 2017 at the Videodermatoscopic Office of the Dermatology Clinic of Cagliari (Italy), with clinical and dermoscopic assessment. Read More

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December 2018

A validated workflow for drug detection in oral fluid by non-targeted liquid chromatography-tandem mass spectrometry.

Anal Bioanal Chem 2018 Dec 6. Epub 2018 Dec 6.

Institute of Legal Medicine and Core Facility Metabolomics, Medical University of Innsbruck, Muellerstr. 44, 6020, Innsbruck, Austria.

Oral fluid is recognized as an important specimen for drug testing. Common applications are monitoring in substance abuse treatment programs, therapeutic drug monitoring, pain management, workplace drug testing, clinical toxicology, and driving under the influence of drugs (DRUID). In this study, we demonstrate that non-targeted LC-MS/MS with subsequent compound identification by tandem mass spectral library search is a valuable tool for comprehensive detection and confirmation of drugs in oral fluid samples. Read More

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December 2018

Computational Analyses Connect Small-Molecule Sensitivity to Cellular Features Using Large Panels of Cancer Cell Lines.

Methods Mol Biol 2019 ;1888:233-254

Chemical Biology and Therapeutics Science Program, Broad Institute of Harvard and MIT, Cambridge, MA, USA.

We recently pioneered several analyses of small-molecule sensitivity data collected from large-scale perturbation of hundreds of cancer cell lines with hundreds of small molecules, with cell viability measured as a readout of compound sensitivity. We performed these studies using cancer cell lines previously annotated with cellular, genomic, and basal gene-expression features. By combining small-molecule sensitivity data with these other datasets, we identified new candidate biomarkers of sensitivity, gained insights into small-molecule mechanisms of action, and proposed candidate hypotheses for cancer dependencies (including candidate combination therapies). Read More

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January 2019
1 Read

The Use of Large-Scale Chemically-Induced Transcriptome Data Acquired from LINCS to Study Small Molecules.

Methods Mol Biol 2019 ;1888:189-203

Department of Bioscience and Bioinformatics, Faculty of Computer Science and Systems Engineering, Kyushu Institute of Technology, Iizuka, Fukuoka, Japan.

Identification of the modes of action of bioactive compounds is an important issue in chemical systems biology. In this chapter we review a recently developed data-driven approach using large-scale chemically induced transcriptome data acquired from the Library of Integrated Network-based Cellular Signatures to elucidate the modes of action of bioactive compounds. First, we present a method for pathway enrichment analyses of regulated genes to reveal biological pathways activated by compounds. Read More

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January 2019

Exome Sequencing of Drug-Resistant Clones for Target Identification.

Methods Mol Biol 2019 ;1888:175-187

Department of Biochemistry, UT Southwestern Medical Center, Dallas, TX, USA.

Many small molecule compounds with anticancer activities are discovered through phenotype-based screens. However, discovering the targets of these small molecules has been challenging. The gold standard for target identification requires the discovery of mutations in the target protein that block the effects of small molecules in vitro as well as in vivo. Read More

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January 2019

Quantitative, Real-Time Measurements of Intracellular Target Engagement Using Energy Transfer.

Methods Mol Biol 2019 ;1888:45-71

Promega Corporation, Fitchburg, WI, USA.

Intracellular target affinity and residence time are fundamental aspects of pharmacological mechanism (Lu and Tonge, Curr Opin Chem Biol 14:467-474, 2010). Although various robust biochemical approaches exist to measure these binding characteristics, analysis of compound binding with isolated targets may not accurately reflect engagement in the milieu of living cells. To realize the influence of cellular context, methods are needed that are capable of quantifying affinity and residence time in the presence of the intracellular factors that may impact target engagement. Read More

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January 2019

Phenotypic Screening Using Mouse and Human Stem Cell-Based Models of Neuroinflammation and Gene Expression Analysis to Study Drug Responses.

Methods Mol Biol 2019 ;1888:21-43

Center for Regenerative Therapies Dresden (CRTD), Technische Universität Dresden, Dresden, Germany.

High-throughput phenotypic screening enables the identification of new therapeutic targets even when the molecular mechanism underlying the disease is unknown. In the case of neurodegenerative disease, there is a dire need to identify new targets that can ameliorate, halt, or reverse degeneration. Stem cell-based disease models are particularly powerful tools for phenotypic screening because they use the same cell type affected in patients. Read More

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January 2019

Schisandrin B Improves the Renal Function of IgA Nephropathy Rats Through Inhibition of the NF-κB Signalling Pathway.

Inflammation 2018 Dec 5. Epub 2018 Dec 5.

Department of Nephrology, Affiliated Hospital of Southwest Medical University, No. 25, Tai Ping Street, Jiangyang District, 646000, Luzhou, China.

Schisandrin B (SchB) is an active compound extracted from the Chinese herb Schisandra chinensis and shows excellent anti-inflammatory activity. This study was performed to examine the effects of SchB in a rat model of IgA nephropathy (IgAN). IgAN was established in Sprague-Dawley rats by immunization with lipopolysaccharide (LPS), bovine serum albumin, and carbon tetrachloride. Read More

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December 2018

Effect of transcutaneous vagus nerve stimulation on muscle activity in the gastrointestinal tract (transVaGa): a prospective clinical trial.

Int J Colorectal Dis 2018 Dec 5. Epub 2018 Dec 5.

Department of Surgery, University Hospital of Bonn, Bonn, Germany.

Purpose: Postoperative ileus (POI) is a common complication after abdominal surgery. Invasive stimulation of the cervical vagus nerve is known to reduce inflammatory response and ameliorated POI after surgery in a mouse model. However, the transcutaneous vagus nerve stimulation (tVNS) is a possible non-invasive approach. Read More

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December 2018
1 Read

A thiopyran derivative with low murine toxicity with therapeutic potential on lung cancer acting through a NF-κB mediated apoptosis-to-pyroptosis switch.

Apoptosis 2018 Dec 5. Epub 2018 Dec 5.

Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, 325035, Zhejiang, China.

Pyroptosis is a novel manner of cell death that can be mediated by chemotherapy drugs. The awareness of pyroptosis is significantly increasing in the fields of anti-tumor research and chemotherapy drugs. Invoking the occurrence of pyroptosis is an attractive prospect for the treatment of lung cancer. Read More

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December 2018
6 Reads
3.685 Impact Factor

Sodium dichloroisocyanurate delays ripening and senescence of banana fruit during storage.

Chem Cent J 2018 Dec 5;12(1):131. Epub 2018 Dec 5.

Key Laboratory of Plant Resources Conservation and Sustainable Utilization, Guangdong Provincial Key Laboratory of Applied Botany, South China Botanical Garden, Chinese Academy of Sciences, Guangzhou, 510650, People's Republic of China.

Banana as a typical climacteric fruit soften rapidly, resulting in a very short shelf life after harvest. Sodium dichloroisocyanurate (NaDCC) is reported to be an effectively antibacterial compound. Here, we investigated the effects of NaDCC on ripening and senescence of harvested banana fruit at physiological and molecular levels. Read More

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December 2018

Centiloid scaling for quantification of brain amyloid with [F]flutemetamol using multiple processing methods.

EJNMMI Res 2018 Dec 5;8(1):107. Epub 2018 Dec 5.

Imaging Technology Group, GE Healthcare, The Grove Centre, White Lion Road, Amersham, Buckinghamshire, UK.

Introduction: A standardised method for quantifying β-amyloid PET tracers would allow comparison across different tracers and different sites. The development of the Centiloid scale has aimed to achieve this, applying a common scale to better aid the diagnosis and prognosis of Alzheimer's disease (AD) and to monitor anti-amyloid therapeutic interventions. Here, we apply the Centiloid method to [F]flutemetamol and [C]PiB (PiB, Pittsburgh compound B) PET images and derive the scaling factor to express their binding in Centiloids. Read More

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December 2018

Perfluorinated compounds binding to estrogen receptor of different species: a molecular dynamic modeling.

J Mol Model 2018 Dec 5;25(1). Epub 2018 Dec 5.

School of Pharmacy, Lanzhou University, Lanzhou, 730000, China.

Perfluorinated compounds (PFCs) were widely utilized in commercial and industrial applications, which could interfere with the endocrine systems of experimental animals and humans by interacting with estrogen receptors (ERs). Considering the possible differential binding preferences and relative binding affinities of PFCs to ERs of humans and other species, a cross-species comparison is necessary to effectively assess the health risk of PFCs to humans. In the present work, the species-specific binding characterizations between two PFCs, including perfluorooctane sulfonate (PFOS) and PFOS(4m, 5m), and the different ERαs from Rattus norvegicus, rainbow trout, and humans were explored based on a molecular dynamic modeling. Read More

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December 2018

Inhibition by general anesthetic propofol of compound action potentials in the frog sciatic nerve and its chemical structure.

Naunyn Schmiedebergs Arch Pharmacol 2018 Dec 5. Epub 2018 Dec 5.

Department of Physiology, Saga Medical School, 5-1-1 Nabeshima, Saga, 849-8501, Japan.

Although the intravenous general anesthetic propofol (2,6-diisopropylphenol) has an ability to inhibit nerve conduction, this has not been fully examined. Various agents inhibit compound action potentials (CAPs) in a manner dependent on their chemical structures. To determine propofol's chemical structure that is important in nerve conduction inhibition, we examined the effects of propofol and its related compounds on fast-conducting CAPs recorded from the frog sciatic nerve by using the air-gap method. Read More

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December 2018

Special features of monolayer characteristics of N-alkanoyl substituted threonine amphiphiles.

Phys Chem Chem Phys 2018 Dec 6. Epub 2018 Dec 6.

Max Planck Institute of Colloids and Interfaces, D-14424 Potsdam/Golm, Germany.

The monolayers of N-alkanoyl substituted threonine amphiphiles, similar to those of other N-alkanoyl-substituted amino acid amphiphiles, point to substantial differences in the main characteristics compared to usual amphiphilic monolayers. π-A measurements of the enantiomeric and racemic forms of N-alkanoyl-substituted threonine monolayers with C16 and C18 chain lengths reveal that, independent of the alkyl chain length, all compression curves are located above the corresponding decompression curves. A theoretical model developed for the kinetics of two-dimensional condensation of Langmuir monolayers can describe this behavior concluding the attachment of monomers to large aggregates. Read More

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December 2018
1 Read

Fungal metabolite (+)-terrein suppresses IL-6/sIL-6R-induced CSF1 secretion by inhibiting JAK1 phosphorylation in human gingival fibroblasts.

Heliyon 2018 Nov 26;4(11):e00979. Epub 2018 Nov 26.

Department of Pathophysiology-Periodontal Science, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Okayama, 700-8525, Japan.

Control of bacterial infection-induced inflammatory responses is one of the effective therapeutic approaches of periodontal diseases. Natural products such as lipid mediators and metabolites from microorganisms have been used for decreasing inflammation. We previously reported that (+)-terrein inhibited activation of STAT3 and ERK1/2 in interleukin-6 (IL-6) signaling cascade, leading to prevent vascular endothelial growth factor (VEGF) secretion in human gingival fibroblasts (HGFs). Read More

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November 2018

CX-3543 Promotes Cell Apoptosis through Downregulation of CCAT1 in Colon Cancer Cells.

Biomed Res Int 2018 4;2018:9701957. Epub 2018 Nov 4.

Central Laboratory, Beijing Luhe Hospital, Capital Medical University, Beijing 101100, China.

Aim: Colon cancer-associated transcript-1 (CCAT1), located in the vicinity of transcription factor c-Myc, was first identified in colon cancer. A small-molecule compound CX3543 (Quarfloxin) selectively targeting Myc G-quadruplexes has entered phase II clinical trials for neuroendocrine carcinomas. The aim of the study was to explore the relationship between CX3543, CCAT1, and cell apoptosis in colon cancer cells. Read More

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November 2018

Risdiplam distributes and increases SMN protein in both the central nervous system and peripheral organs.

Pharmacol Res Perspect 2018 Dec 29;6(6):e00447. Epub 2018 Nov 29.

Roche Pharma Research and Early Development Roche Innovation Center Basel Switzerland.

Spinal muscular atrophy (SMA) is a rare, inherited neuromuscular disease caused by deletion and/or mutation of the Survival of Motor Neuron 1 ( gene. A second gene, , produces low levels of functional SMN protein that are insufficient to fully compensate for the lack of . Risdiplam (RG7916; RO7034067) is an orally administered, small-molecule pre-mRNA splicing modifier that distributes into the central nervous system (CNS) and peripheral tissues. Read More

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December 2018
1 Read

Synergistic interaction between the agonism of cebranopadol at nociceptin/orphanin FQ and classical opioid receptors in the rat spinal nerve ligation model.

Pharmacol Res Perspect 2018 Dec 28;6(6):e00444. Epub 2018 Nov 28.

Translational Science and Intelligence Grünenthal GmbH Aachen Germany.

Cebranopadol (trans-6'-fluoro-4',9'-dihydro--dimethyl-4-phenyl-spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-b]indol]-4-amine) is a novel analgesic nociceptin/orphanin FQ opioid peptide (NOP) and classical opioid receptor (MOP, DOP, and KOP) agonist with highly efficacious and potent activity in a broad range of rodent models of nociceptive, inflammatory, and neuropathic pain as well as limited opioid-type side effects such as respiratory depression. This study was designed to explore contribution and interaction of NOP and classical opioid receptor agonist components to cebranopadol analgesia in the rat spinal nerve ligation (SNL) model. Assessing antihypersensitive activity in SNL rats intraperitoneal (IP) administration of cebranopadol resulted in ED values of 3. Read More

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December 2018
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Second-generation pterocarpanquinones: synthesis and antileishmanial activity.

J Venom Anim Toxins Incl Trop Dis 2018 29;24:35. Epub 2018 Nov 29.

1Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, FIOCUZ, Av. Brasil, 4365, Pavilhao Leonidas Deane, sala 405A, Manguinhos, Rio de Janeiro, RJ 21040-900 Brazil.

Background: Despite the development of new therapies for leishmaniasis, among the 200 countries or territories reporting to the WHO, 87 were identified as endemic for Tegumentary Leishmaniasis and 75 as endemic for Visceral Leishmaniasis. The identification of antileishmanial drug candidates is essential to fill the drug discovery pipeline for leishmaniasis. In the hit molecule LQB-118 selected, the first generation of pterocarpanquinones was effective and safe against experimental visceral and cutaneous leishmaniasis via oral delivery. Read More

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November 2018
3 Reads

Metabolic Pathway of Topramezone in Multiple-Resistant Waterhemp () Differs From Naturally Tolerant Maize.

Front Plant Sci 2018 21;9:1644. Epub 2018 Nov 21.

Department of Crop Sciences, University of Illinois at Urbana-Champaign, Urbana, IL, United States.

Waterhemp [ (Moq.) Sauer] is a problematic dicot weed in maize, soybean, and cotton production in the United States. Waterhemp has evolved resistance to several commercial herbicides that inhibit the 4-hydroxyphenylpyruvate-dioxygenase (HPPD) enzyme in sensitive dicots, and research to date has shown that HPPD-inhibitor resistance is conferred by rapid oxidative metabolism of the parent compound in resistant populations. Read More

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November 2018

Diagnosis, Clinical Trend, and Treatment of Diffuse Lamellar Keratitis after Femtosecond Laser-Assisted in situ Keratomileusis: A Case Report.

Case Rep Ophthalmol 2018 Sep-Dec;9(3):457-464. Epub 2018 Nov 14.

Balestrazzi Associated Ophthalmological Practice, Rome, Italy.

We report a severe case of diffuse lamellar keratitis (DLK) following femtosecond laser-assisted in situ keratomileusis (femto-LASIK). A 25-year-old man was submitted to 150 kHz iFS® IntraLase-assisted LASIK in both eyes for compound myopic astigmatism. The day after surgery, clinical examination showed a diffuse whitish granular cell reaction particularly in the right eye. Read More

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November 2018
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Biodegradability and biodegradation pathways of chlorinated cyclodiene insecticides by soil fungi.

Authors:
Ryota Kataoka

J Pestic Sci 2018 Nov;43(4):314-320

Department of Environmental Sciences, Faculty of Life and Environmental Sciences, University of Yamanashi, 4-4-37 Takeda, Kofu, Yamanashi, Japan.

An aerobic dieldrin-degrading fungus, strain DDF, and two aerobic endosulfan-degrading fungal strains, sp. strains W8 and Cm1-45, were isolated from soil contaminated with organochlorine pesticides. Strain DDF degraded more than 90% dieldrin during 10-days of incubation at 25°C and showed the production of a small amount of aldrin -diol. Read More

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November 2018

Structure-activity relationship of [1,5]azastibocines in cytotoxicity to vascular endothelial cells.

J Toxicol Sci 2018 ;43(12):735-740

Faculty of Pharmaceutical Sciences, Toho University.

It has been well established that organic-inorganic hybrid molecules can exhibit biological activities that are different from those of either their intramolecular metals in inorganic forms or their organic structures. We have previously reported that organoantimony compound Sb-phenyl-N-methyl-5,
6,7,12-tetrahydrodibenz[c,f][1,5]azastibocine (PMTAS) is nontoxic, but that the compound exhibits cytotoxicity in vascular endothelial cells when the antimony atom is replaced with a bismuth atom. In the present study, we investigated the cytotoxicity and intracellular accumulation of PMTAS and its analogs and found that the cytotoxicity of PMTAS analogs also decrease depending on the electron-withdrawing property of the substituent bound to the intramolecular antimony atom. Read More

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January 2018
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Q63, a novel DENV2 RdRp non-nucleoside inhibitor, inhibited DENV2 replication and infection.

J Pharmacol Sci 2018 Jun 25. Epub 2018 Jun 25.

State Key Laboratory of Organ Failure Research, Guangdong Provincial Key Laboratory of New Drug Screening, Guangzhou Key Laboratory of Drug Research for Emerging Virus Prevention and Treatment, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, PR China. Electronic address:

Dengue virus (DENV) annually infects 400 million people worldwide. Unfortunately, there is lack of widely protective vaccine or drugs against DENV. The viral RNA-dependent RNA polymerase (RdRp) of NS5 protein is highly conserved among different DENV subtypes, thus presenting itself as an attractive target for drug design. Read More

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