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Tao Chen et al.
SpringerPlus, 4, 652-652 (2015-11-07)
Hetrombopag as the derivative of ethylidene hydrazine carboxamide was recently developed into a novel patented non-peptide thrombopoietin mimetic and thrombopoietin receptor agonist to treat idiopathic thrombocytopenic purpura. To study the pharmacokinetics of hetrombopag, a highly sensitive, rapid and reliable liquid
Yoshiyuki Morishima et al.
American journal of clinical pathology, 143(2), 241-247 (2015-01-18)
Edoxaban, an oral direct factor Xa inhibitor, does not require routine monitoring. However, assessment of the anticoagulant effects may be required in certain situations. We investigated the effects of edoxaban on prothrombin time (PT), activated partial thromboplastin time (aPTT), and
Marcus Klein et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(2), 273-283 (2014-12-07)
Inflammatory processes are associated with compromised metabolism and elimination of drugs in the liver, largely mediated by proinflammatory cytokines, such as interleukin-6. The Hepa-RG cell line is an established surrogate for primary human hepatocytes (PHH) in drug metabolism and toxicity
Hai-Qing Song et al.
Acta biomaterialia, 12, 156-165 (2014-12-03)
Owing to their unique properties such as low cytotoxicity and excellent biocompatibility, poly(aspartic acid) (PAsp) and polysaccharides are good candidates for the development of new biomaterials. In order to construct better gene delivery systems by combining polysaccharides with PAsp, in
Nishad Jayasundara et al.
Toxicological sciences : an official journal of the Society of Toxicology, 143(2), 469-481 (2014-11-22)
Polycyclic aromatic hydrocarbons (PAHs) induce developmental defects including cardiac deformities in fish. The aryl hydrocarbon receptor (AHR) mediates the toxicity of some PAHs. Exposure to a simple PAH mixture during embryo development consisting of an AHR agonist (benzo(a)pyrene-BaP) with fluoranthene
Xia Han et al.
Biomolecules & therapeutics, 23(4), 357-366 (2015-07-15)
Isorhamnetin (3-methylquercetin) is a flavonoid derived from the fruits of certain medicinal plants. This study investigated the photoprotective properties of isorhamnetin against cell damage and apoptosis resulting from excessive ultraviolet (UV) B exposure in human HaCaT keratinocytes. Isorhamnetin eliminated UVB-induced
Hong-Fang Jiang et al.
Oncology letters, 8(3), 1139-1142 (2014-08-15)
Daphnoretin is an active constituent of
Remigiusz Żurawiński et al.
Organic & biomolecular chemistry, 13(25), 7000-7012 (2015-06-02)
The synthesis of two cross-conjugated prostaglandin analogues of known neurotrophic activity and their new hydroxy derivatives was accomplished starting from the diastereoisomeric (+)-camphor protected 3-[(dimethoxyphosphoryl)methyl]-4,5-dihydroxycyclopent-2-enones. The cytotoxicity of these compounds was determined against HeLa, K562, HL-60 human cancer cell lines
Pablo J Giraudi et al.
Experimental and molecular pathology, 98(1), 85-92 (2014-12-24)
Non-alcoholic fatty liver disease is characterized by an initial accumulation of triglycerides that can progress to non-alcoholic steatohepatitis, which can ultimately evolve to cirrhosis and hepatocellular carcinoma. Hepatic stellate cells play a key role in liver fibrogenesis by an increased
Jun-Hui Choi et al.
Journal of bioscience and bioengineering, 120(2), 181-186 (2015-03-18)
Dendropanax morbifera H. Lev. is well known in Korean traditional medicine for improvement of blood circulation. In this study, rutin, a bioflavonoid having anti-thrombotic and anticoagulant activities was isolated from a traditional medicinal plant, D. morbifera H. Lev. The chemical
Peng Luo et al.
Molecular medicine reports, 12(1), 1163-1168 (2015-03-18)
Congestive heart failure (CHF) remains the single most prevalent cause of mortality and morbidity; therefore, the identification of novel biomarkers is required for the diagnosis of CHF. The aim of the present study was to examine whether microRNA (miR)-423-5p is
Tengyuan Liu et al.
Journal of neuroinflammation, 11, 107-107 (2014-06-15)
Neuroinflammation mediated by activation of microglia and interruption of the blood-brain barrier (BBB) is an important factor that contributes to neuron death and infarct area diffusion in ischemia reperfusion injury. Finding novel molecules to regulate neuroinflammation is of significant clinical
Alban Bujard et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 77, 273-278 (2015-06-30)
The Parallel Artificial Membrane Permeability Assay (PAMPA) is a well-known high throughput screening (HTS) technique for predicting in vivo passive absorption. In this technique, two compartments are separated by an artificial membrane that mimics passive permeability through biological membranes such
Archana Shenoy et al.
The EMBO journal, 34(9), 1180-1194 (2015-02-27)
The molecular basis of astrocyte differentiation and maturation is poorly understood. As microRNAs have important roles in cell fate transitions, we set out to study their function during the glial progenitor cell (GPC) to astrocyte transition. Inducible deletion of all
Lillian Seu et al.
AIDS research and therapy, 11, 27-27 (2014-09-03)
The level (or frequency) of circulating monocyte subpopulations such as classical (CD14(hi)CD16(-)) and non-classical (CD14(dim)CD16(+)) monocytes varies during the course of HIV disease progression and antiretroviral therapy (ART). We hypothesized that such variation and/or differences in the degree to which
Jochen J Frietsch et al.
Oncotarget, 5(14), 5257-5271 (2014-06-11)
Chronic myeloid leukemia (CML) is characterized by a genomic translocation generating a permanently active BCR-ABL oncogene with a complex pattern of atypically tyrosine-phosphorylated proteins that drive the malignant phenotype of CML. Recently, the LIM and SH3 domain protein 1 (LASP1)
Son T Nguyen et al.
Bioorganic & medicinal chemistry, 23(9), 2024-2034 (2015-03-31)
Recently we described a novel pyranopyridine inhibitor (MBX2319) of RND-type efflux pumps of the Enterobacteriaceae. MBX2319 (3,3-dimethyl-5-cyano-8-morpholino-6-(phenethylthio)-3,4-dihydro-1H-pyrano[3,4-c]pyridine) is structurally distinct from other known Gram-negative efflux pump inhibitors (EPIs), such as 1-(1-naphthylmethyl)-piperazine (NMP), phenylalanylarginine-β-naphthylamide (PAβN), D13-9001, and the pyridopyrimidine derivatives. Here
Samina Akhter et al.
BioMed research international, 2015, 356729-356729 (2015-07-30)
This research investigated the protective role of Leea macrophylla extract on CCl4-induced acute liver injury in rats. Different fractions of Leea macrophylla (Roxb.) crude extract were subjected to analysis for antioxidative effects. Rats were randomly divided into four groups as
Jing Wang et al.
Acta pharmacologica Sinica, 36(7), 821-830 (2015-05-26)
NLRP3 inflammasome plays an important role in renal injury and may be a therapeutic target in the treatment of patients with progressive chronic kidney disease. In this study we investigated whether angiotensin II (Ang II)-induced NLRP3 inflammasome activation was linked
Marie Tremblay-Franco et al.
PloS one, 10(10), e0141698-e0141698 (2015-10-31)
Along with the well-established effects on fertility and fecundity, perinatal exposure to endocrine disrupting chemicals, and notably to xeno-estrogens, is strongly suspected of modulating general metabolism. The metabolism of a perinatally exposed individual may be durably altered leading to a
Aneta Novotna et al.
PloS one, 9(7), e101832-e101832 (2014-07-08)
Azole antifungal ketoconazole (KET) was demonstrated to activate aryl hydrocarbon receptor (AhR). Since clinically used KET is a racemic mixture of two cis-enantiomers (2R,4S)-(+)-KET and (2S,4R)-(-)-KET, we examined the effects of KET enantiomers on AhR signaling pathway. (+)-KET dose-dependently activated
Emmanuelle Havis et al.
Development (Cambridge, England), 141(19), 3683-3696 (2014-09-25)
The molecular signals driving tendon development are not fully identified. We have undertaken a transcriptome analysis of mouse limb tendon cells that were isolated at different stages of development based on scleraxis (Scx) expression. Microarray comparisons allowed us to establish
Kui Y Yang et al.
Progress in neuro-psychopharmacology & biological psychiatry, 57, 100-109 (2014-12-03)
In our current study, we investigated the role of spinal glutamate recycling in the development of orofacial inflammatory pain. DL-threo-β-benzyloxyaspartate (TBOA) or methionine sulfoximine (MSO) was administered intracisternally to block spinal glutamate transporter and glutamine synthetase activity in astroglia. Intracisternal
Safflower yellow inhibits angiotensin II-induced adventitial fibroblast proliferation and migration.
Yueqiang Liu et al.
Journal of pharmacological sciences, 126(2), 107-114 (2014-09-19)
Safflower yellow (SY) has been widely used in Chinese medicine for the treatment of ischemic cardiocerebrovascular disease. Recent studies have indicated that SY has a reverse effect on vascular remodeling (VR). However, its detailed mechanisms require further study to provide
Xiaoshuang Zhou et al.
Molecular medicine reports, 12(2), 2643-2649 (2015-05-06)
The metabolic products of intracellular mevalonate (MVA) are important for the growth of eukaryotic cells. These products include cholesterol and several non-sterol isoprenoids. It has been reported that 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors ameliorate glomerular injury in several experimental models
Alexander Portillo et al.
Biochimica et biophysica acta, 1854(3), 218-228 (2014-12-30)
Assembly of amyloid proteins into aggregates requires the ordering of the monomers in oligomers and especially in such highly organized structures as fibrils. This ordering is accompanied by structural transitions leading to the formation of ordered β-structural motifs in proteins
Shirong Zhang et al.
Oncotarget, 6(8), 5832-5845 (2015-02-26)
Afatinib is a second-generation of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor and has shown a significant clinical benefit in non-small cell lung cancer (NSCLC) patients with EGFR-activating mutations. However, the potential therapeutic effects of afatinib combining with other
Stefan Wagner et al.
Bioorganic & medicinal chemistry, 23(12), 2839-2847 (2015-04-25)
Phosphopeptide mimetics containing the 4-phosphonocarbonyl phenylalanine (pcF) as a photo-active phosphotyrosine isoster are developed as potent, light-switchable inhibitors of the protein tyrosine phosphatase PTP1B. The photo-active inhibitors 6-10 are derived from phosphopeptide substrates and are prepared from the suitably protected
Gabriele Greve et al.
Journal of cancer research and clinical oncology, 141(12), 2171-2180 (2015-05-27)
The retinoic acid signaling pathway, crucial for differentiation, is silenced by epigenetic mechanisms in many cancers. Epigenetically active, chromatin-modifying agents offer a novel treatment approach, by reactivating aberrantly silenced genes in tumor cells and by sensitizing them to subsequent treatments.
Seyedeh Mahdieh Hashemi et al.
Bioorganic & medicinal chemistry, 23(7), 1481-1491 (2015-03-06)
In order to find new azole antifungals, we have recently designed a series of triazole alcohols in which one of the 1,2,4-triazol-1-yl group in fluconazole structure has been replaced with 4-amino-5-aryl-3-mercapto-1,2,4-triazole motif. In this paper, we focused on the structural
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