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#28925130   2017/09/19 To Up

[Anti-inflammatory active fraction screening and mechanism of unripe Forsythiae Fructus based on ¹H-NMR metabolomics].

To screen the anti-inflammatory active fraction of unripe Forsythiae Fructus, and elucidate the action mechanism, water decoction, ethyl acetate portion, n-butanol portion and residue water extracts of unripe Forsythiae Fructus were administered into rats for continuously 15 days. The acute lung injury inflammatory model was established to observe the section structure of lung tissues. Levels of IL-6, TNF-α, IL-1β and IL-10 in bronchoalveolar lavage fluid were determined by ELISA kits, and changes in endogenous metabolites in serum were analyzed based on 1H-NMR metabolomics. The results showed that ethyl acetate portion of unripe Forsythiae Fructus had a better anti-inflammatory activity against acute lung injury, and could suppress the release of inflammatory factors of IL-6, TNF-α, IL-1β, significantly reduce contents of creatine, β-OH-butyrate, succinate, lysine, valine, isoleucine and glutamine, and elevate the content of GPC in serum. Ethyl acetate portion was proved to be the main fraction of anti-inflammatory activity from the perspective of endogenous metabolites in serum, and played an anti-inflammatory role by regulating creatine metabolism, choline metabolism, branched-chain amino acid metabolism and TCA cycles. This study could lay a foundation for studying pharmacodynamic material basis of unripe Forsythiae Fructus.

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Human PAI-1 (N-terminal A removed without changing Human, Allograft Inflamma Human Gro g Macrophage In Rat Tail Type I Collagen Bovine Type I Collagen ba Human Macrophage Inflamma Mouse Macrophage Inflamma Mouse Macrophage Inflamma Mouse Macrophage Inflamma Mouse Macrophage Inflamma Human Macrophage Inflamma

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#28901512   2017/09/13 To Up

Gambogic acid suppresses inflammation in rheumatoid arthritis rats via PI3K/Akt/mTOR signaling pathway.

Gamboge is the dried resin secreted by the Garcinia maingayi gambogic tree and is a substance that may be used to treat a variety of diseases, exhibits anti‑tumor and detoxification effects and prevents bleeding. The primary active constituent is gambogic acid. The present study aimed to investigate the anti‑inflammatory effects of gambogic acid in rheumatoid arthritis (RA) rats and to elucidate the mechanisms by which these effects occur. The swelling degree, the clinical arthritic scoring and pain threshold measurements were used to evaluate the effects of gambogic acid on RA. ELISA kits and western blot analysis were used to investigate inflammatory processes and the expression of RA‑associated proteins, respectively. The present results demonstrated that gambogic acid significantly inhibited the degree of right foot swelling, increased pain thresholds and reduced clinical arthritic scores of RA rats. Treatment with gambogic acid suppressed the activities of interleukin (IL)‑1β and IL‑6, promoted the protein expression of phosphorylated (p)‑Akt serine/threonine kinase (Akt), p‑mammalian target protein of rapamycin (mTOR) and inhibited hypoxia‑inducible factor‑1α and vascular endothelial growth factor expression in RA rats. The results of the present study therefore suggest that the anti‑inflammatory effects of gambogic acid in RA rats occur via regulation of the phosphoinositide 3‑kinase/Akt/mTOR signaling pathway.

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p53 Signaling Phospho-Spe AKT PKB Signaling Phospho GPCR Signaling to MAPK ER IGF-1R Signaling Phospho- mTOR Signalign Phospho-Sp TGF-Beta Signaling Phosph AMPK Signaling Phospho-Sp T-Cell Receptor Signaling Hh Signaling Pathway Anta PathwayReady™ PI3 K Akt BGT-226 Mechanisms: PI3K AP-1 Reporter – HEK293

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#28919672   2017/09/18 To Up

Preparation and evaluation of Salmonella Enteritidis antigen conjugated with nanogold for screening of poultry flocks.

The present work aimed to develop lateral flow immunochromatographic strip (ICS) test for detection of Salmonella Enteritidis (SE) specific antibodies in chicken sera.

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Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en Rabbit Anti-Salmonella en

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#28915240   2017/09/15 To Up

Improved reliability of serological tools for the diagnosis of West Nile fever in horses within Europe.

West Nile Fever is a zoonotic disease caused by a mosquito-borne flavivirus, WNV. By its clinical sensitivity to the disease, the horse is a useful sentinel of infection. Because of the virus' low-level, short-term viraemia in horses, the primary tools used to diagnose WNV are serological tests. Inter-laboratory proficiency tests (ILPTs) were held in 2010 and 2013 to evaluate WNV serological diagnostic tools suited for the European network of National Reference Laboratories (NRLs) for equine diseases. These ILPTs were designed to evaluate the laboratories' and methods' performances in detecting WNV infection in horses through serology. The detection of WNV immunoglobulin G (IgG) antibodies by ELISA is widely used in Europe, with 17 NRLs in 2010 and 20 NRLs in 2013 using IgG WNV assays. Thanks to the development of new commercial IgM capture kits, WNV IgM capture ELISAs were rapidly implemented in NRLs between 2010 (4 NRLs) and 2013 (13 NRLs). The use of kits allowed the quick standardisation of WNV IgG and IgM detection assays in NRLs with more than 95% (20/21) and 100% (13/13) of satisfactory results respectively in 2013. Conversely, virus neutralisation tests (VNTs) were implemented in 33% (7/21) of NRLs in 2013 and their low sensitivity was evidenced in 29% (2/7) of NRLs during this ILPT. A comparison of serological diagnostic methods highlighted the higher sensitivity of IgG ELISAs compared to WNV VNTs. They also revealed that the low specificity of IgG ELISA kits meant that it could detect animals infected with other flaviviruses. In contrast VNT and IgM ELISA assays were highly specific and did not detect antibodies against related flaviviruses. These results argue in favour of the need for and development of new, specific serological diagnostic assays that could be easily transferred to partner laboratories.

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West Nile virus Real Time West Nile virus Real Time West Nile virus Real Time West Nile Virus Envelope West Nile Virus (Pre-M), West Nile Virus Pre M rec West Nile Virus E Prot. R Nile Red *UltraPure Grade Nile Blue A *Fluorescence Q Fever (phases 1 2) IgG Q Fever (phases 1 2) IgM Nile Red, A lipophilic dy

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#28922541   2017/09/18 To Up

Effects of collagen peptides intake on skin ageing and platelet release in chronologically aged mice revealed by cytokine array analysis.

Action mechanisms underlying various biological activities of collagen peptides (CPs) remained to be elucidated. Cytokines may play an important role in mediating these health benefits of CPs. This study aimed to systemically examine the cytokines in skin and blood regulated by CPs intake. Thirteen-month-old female Kunming mice were administered with CPs for 2 months (0 or 400 mg/kg bodyweight/day). The cytokines in skin and plasma were analysed using a 53-cytokine array and corresponding ELISA kits. In skin, CPs intake significantly down-regulated placenta growth factor (PIGF-2), insulin-like growth factor (IGF)-binding protein (IGFBP) -2 and IGFBP-3, and up-regulated platelet factor 4 (PF4), serpin E1 and transforming growth factor (TGF)-β1 . CPs treatment also increased the type I collagen mRNA and protein levels and improved the aged skin collagen fibres. In plasma, nine cytokines were significantly down-regulated by CPs intake compared to the model group: fibroblast growth factor (FGF)-2, heparin-binding (HB) epidermal growth factor (EGF)-like growth factor (HB-EGF), hepatocyte growth factor (HGF), platelet-derived growth factor (PDGF)-AB/BB, vascular endothelial growth factor (VEGF), chemokine (C-X-C motif) ligand 1 (KC), matrix metalloproteinase (MMP)-9, interleukin (IL)-1α and IL-10; 2 cytokines were significantly up-regulated, including TGF-β1 and serpin F1. Furthermore, CPs intake significantly decreased the level of platelet release indicators in the plasma and washed platelets, including PF4, granule membrane protein (GMP)-140, β-thromboglobulin and serotonin. These results provide a mechanism underlying anti-skin ageing by CPs intake and highlight potential application of CPs as a healthcare supplement to combat cancer and cardiovascular disease by inhibiting platelet release.

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Skin cancer test tissue a Cytokine antibody array i Mouse Cytokine Array G200 Mouse Cytokine Array G200 Mouse Cytokine Array G100 Non-Human Primate Cytoki Non-Human Primate Cytoki Human Cytokine Array Q700 Non-Human Primate Cytoki Mouse Cytokine Array G100 Mouse Cytokine Array Q6 Mouse Cytokine Array Q6

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#28662964   2017/06/30 To Up

Synthesis and biological activity of cyclolinopeptide A analogues modified with γ(4)-bis(homo-phenylalanine).

Cyclolinopeptide A (CLA), an immunosuppressive nonapeptide derived from linen seeds, was modified with S or R-γ(4)-bis(homo-phenylalanine) in positions 3 or 4, or both 3 and 4. These modifications changed the flexibility of new analogues and distribution of intramolecular hydrogen bonds. Analogues 11 c(Pro(1)-Pro(2)-Phe(3)-S-γ(4)-hhPhe(4)-Leu(5)-Ile(6)-Ile(7)-Leu(8)-Val(9)), 13 c(Pro(1)-Pro(2)-S-γ(4)-hhPhe(3)-R-γ(4)-hhPhe(4)-Leu(5)-Ile(6)-Ile(7)-Leu(8)-Val(9)) and 15 c(Pro(1)-Pro(2)-R-γ(4)-hhPhe(3)-Phe(4)-Leu(5)-Ile(6)-Ile(7)-Leu(8)-Val(9)) existed as a mixture of stable cis/trans isomers of Pro-Pro peptide bond. The comparison of the relative spatial orientations in crystal state of the two carbonyl groups, neighboring γ-amino acids, revealed conformational similarities to α-peptides. The addition of two -CH2- groups in γ-amino acids led to a more rigid conformation, although a more flexible one was expected. A significant difference in the relative orientation of the carbonyl groups was found for cyclic γ-peptides with a dominance of an antiparallel arrangement. As carbonyl groups may be engaged in the interactions with plausible receptors through hydrogen bonds, a similar biological activity of the modified peptides was expected. Our biological studies showed that certain cyclic, but not the corresponding linear peptides, lowered the viability of peripheral blood mononuclear cells (PBMC) at 100μg/mL concentration. The proliferation of PBMC induced by phytohemagglutinin A (PHA) was strongly inhibited by cyclic peptides only, in a dose-dependant manner. On the other hand, lipopolysaccharide (LPS)-induced tumor necrosis factor alpha (TNF-α) production in whole blood cell cultures was inhibited by both linear and cyclic peptides. Peptide 15 c(Pro(1)-Pro(2)-R-γ(4)-hhPhe(3)-Phe(4)-Leu(5)-Ile(6)-Ile(7)-Leu(8)-Val(9)) blocked the expression of caspase-3, inhibited the expression of caspases-8 and -9 in 24h culture of Jurkat cells, and caused DNA fragmentation in these cells, as an indicator of apoptosis. Thus, we revealed a new mechanism of immunosuppressive action of a nonapeptide.

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#28756668   2017/07/31 To Up

Synthesis of 2-Aryl-5-alkyl-fulleropyrrolidines: Metal-Free-Mediated Reaction of [60]Fullerene with Aromatic Aldehydes and Inactive Primary Amines.

The metal-free-mediated thermal reaction of [60]fullerene with aromatic aldehydes and inactive primary amines bearing electron-donating groups at the α-position afforded a series of 2-aryl-5-alkyl-fulleropyrrolidines, including the scarce 2-aryl-5-benzyl-fulleropyrrolidines as a mixture of cis and trans isomers. With rare exceptions, the mixture of cis and trans isomers could be easily isolated by column chromatography, with a preference of cis isomers as major products. A plausible mechanism for the formation of fulleropyrrolidines is also proposed.

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Single Peptoid Ligand Syn Peptoid Library Synthesis Primary antibody STAT1 a Primary antibody DR3 Ant Primary antibody DR3 Ant Primary antibody DR4 Ant Primary antibody DR5 Ant Rat Inactive rhomboid pro 4 Methylumbelliferyl sulf 5 (2 Aminoethylamino) 1 n Pyrene 8 hydroxy 1,4,6 tr NBD aminohexanoic acid N

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#28267339   2017/03/07 To Up

Structural Elucidation of cis/trans Dicaffeoylquinic Acid Photoisomerization Using Ion Mobility Spectrometry-Mass Spectrometry.

Due to the recently uncovered health benefits and anti-HIV activities of dicaffeoylquinic acids (diCQAs), understanding their structures and functions is of great interest for drug discovery efforts. DiCQAs are analytically challenging to identify and quantify since they commonly exist as a diverse mixture of positional and geometric (cis/trans) isomers. In this work, we utilized ion mobility spectrometry coupled with mass spectrometry to separate the various isomers before and after UV irradiation. The experimental collision cross sections were then compared with theoretical structures to differentiate and identify the diCQA isomers. Our analyses found that naturally the diCQAs existed predominantly as trans/trans isomers, but after 3 h of UV irradiation, cis/cis, cis/trans, trans/cis, and trans/trans isomers were all present in the mixture. This is the first report of successful differentiation of cis/trans diCQA isomers individually, which shows the great promise of IMS coupled with theoretical calculations for determining the structure and activity relationships of different isomers in drug discovery studies.

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trans-4-(Aminomethyl)cycl 3 Methylenecyclopropane t trans 2,3 Dimethylacrylic Mouse Anti-Non-Structural (+)-cis,trans-Abscisic Ac All trans Retinoic acid ( trans Aconitic acid CAS N (+)-cis,trans-Abscisic Ac BSB [(trans,trans) 1 Brom trans Indole 3 acrylic ac trans 3 (3 Pyridyl)acryli (cis trans)-2-(4-Benzofur

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#28445697   2017/04/26 To Up

Influence of Maturation on In Vivo Tissue to Plasma Partition Coefficients for Cis- and Trans-Permethrin.

Permethrin, the most widely used household insecticide in the United States, is marketed as a mixture of its cis (CIS) and trans (TRANS) isomers. The major objective of this investigation is to develop and utilize a reliable approach to determine in vivo partition coefficients (PCs) for CIS and TRANS in immature and adult Sprague-Dawley rats. Adult, postnatal day (PND) 21, and PND 15 rats were infused with environmentally relevant concentrations of CIS or TRANS via a subcutaneous osmotic pump for 48 or 72 h. The adult and PND 21 rats also received an oral loading dose. Systemic steady-state or equilibrium was attained in each age group within 72 h of the protocol. CIS and TRANS were both distributed to tissues according to their neutral lipid content, with adipose tissue exhibiting much higher tissue:plasma PCs than skeletal muscle, liver, or brain. Liver:plasma and brain:plasma PCs were consistently at or lower than unity. Tissue:plasma PCs were generally higher for CIS than for TRANS, although the isomers are of comparable lipophilicity. Significantly higher blood levels of CIS apparently saturate plasma binding, resulting in greater tissue deposition of the isomer. CIS and TRANS tissue:plasma PCs were found to be inversely related to the rats' age, although TRANS brain:plasma PCs were comparable in immature and mature animals. These data support the conclusion that age-dependent partitioning is an important determinant of the pharmacokinetics of permethrin. Such partitioning could influence the risk assessment of these insecticides in infants and children when incorporated into physiologically based pharmacokinetic models.

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BCMA (B cell maturation p BSB [(trans,trans) 1 Brom BCMA (B cell maturation p trans,trans 2,4 Hexadien ROS Brite™ 700 *Optimiz Directed In Vivo Angiogen Human PAI 1 Elastase Spec PARP in vivo Pharmacodyna Pyrene N Hexadecylsulfona Anti CML Monoclonal Antib Fluorescein di beta D gal MarkerGeneTM Fluorescent

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#28224762   2017/02/22 To Up

Stereoisomerization of Cyclic Silanols.

Stereoisomerization of readily available all-cis-1,3,5,7-tetrahydroxy-1,3,5,7-tetraisobutylcyclotetrasiloxane (1 a) was carried out under acidic conditions to afford cis-trans-cis (1 b), all-trans (1 c), and cis-cis-trans (1 d) isomers. The compounds in the reaction mixture could be easily separated into 1 a and a mixture of 1 b, 1 c, and 1 d by the treatment with chloroform. Compounds 1 b, 1 c, and 1 d were further separated and isolated, and each structure was identified. The experimental results indicated that the most plausible mechanism is a substitution reaction at the silicon center via a pentacoordinate intermediate without a cyclic siloxane bond cleavage reaction. The obtained isomer 1 a or 1 b further reacted with dichlorodiphenylsilane in the presence of triethylamine to give syn-type laddersiloxane (2 a) or anti-type laddersiloxane (2 b), respectively.

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Adenosine-3',5'-cyclic mo Adenosine 3',5' cyclic mo Adenosine 3' ,5' cyclic m Cyclic AMP Direct Chemilu Rabbit Anti-Cyclic AMP (c Ambroxol Cyclic Impurity- Ambroxol Cyclic Impurity AICAR 3’,5’-Cyclic Ph Adenosine-3’,5’-cycli Adenosine 2’,3’-Cycli Adenosine 2’,3’-Cycli 2 Aminophenylboronic acid