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PubMed Journals Articles About "Cyclo 10mg 200mg" RSS

13:30 EST 14th November 2018 | BioPortfolio

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Showing "Cyclo 10mg 200mg" PubMed Articles 1–25 of 94

To Be or Not to Be Protonated: Cyclo-N¯ in Crystal and Solvent.

Pentazole (HN5) and its anion (cyclo-N5-) have been elusive for nearly a century due to the unstable N5 ring. Recently, Zhang et al. reported the first synthesis and characterization of the pentazolate anion cyclo-N5- in (N5)6(H3O)3(NH4)4Cl salt at ambient conditions (Science, 2017, 355, 374). However, if the cyclo-N5- in (N5)6(H3O)3(NH4)4Cl salt is protonated or not has been debated (Science, 2018, 359, eaao3672; Science, 2018, 359, aas8953). Herein, we employed ab initio molecular dynamics (AIMD) simulati...


Stable and Persistent Acyclic Diaminocarbenes with Cycloalkyl Substituents and Their Transformation to β-Lactams by Uncatalysed Carbonylation with CO.

Four new acyclic diaminocarbenes (ADACs), viz. [(cyclo-CnH2n - 1)2N]2C (n = 5 - 7) and iPr2N-C-N(cyclo-C6H11)2, were synthesised by reacting the corresponding formamidinium hexafluorophosphates with NaN(SiMe3)2. Their nucleophilicities and electrophilicities were respectively judged from the 1JCH values determined for the N2CH unit of the corresponding formamidinium cations and from the 77Se NMR chemical shifts of the selenourea derivatives obtained from the reaction of elemental selenium with the correspon...

Enhancement of self-aggregation properties of linear elastin-derived short peptides by simple cyclization: strong self-aggregation properties of cycloFPGVG, consisting only of natural amino acids.

Elastin-like peptides (ELP) consist of distinctive repetitive sequences, such as (VPGVG), exhibit temperature-dependent reversible self-assembly (coacervation), and have been considered to be useful for the development of thermo-responsive materials. Further fundamental studies evaluating coacervative properties of novel nonlinear ELPs could present design concepts for new thermo-responsive materials. In this study, we prepared novel ELPs, cyclic (FPGVG) (cyclo[FPGVG], n = 1-5), and analyzed its self-assemb...


Ultrasound Cyclo-Plasty in Patients with Glaucoma: 1-Year Results from a Multicentre Prospective Study.

The aim of this study was to evaluate the safety and efficacy of ultrasound cyclo-plasty (UCP) for reducing intraocular pressure (IOP) in patients with glaucoma.

Identification of an early stage biofilm inhibitor from Veillonella tobetsuensis.

Oral biofilm, the cause of dental caries and periodontal diseases, consists of multiple bacterial species. Streptococcus spp. and Veillonella spp. have been reported as to be initial and early colonizers of oral biofilms. Our previous studies showed that Veillonella tobetsuensis may play an important role on the development of S. gordonii biofilms without coaggregation involving extracellular biomolecules. In this study, the effect of a cyclic dipeptide autoinducer from culture supernatants from V. tobetsue...

Syntheses, Crystal Structures and Properties of a series of 3D Metal-Inorganic Frameworks containing Pentazolate Anion.

Pentazolate anion (cyclo-N₅¯), and/or N₃¯, NO₃¯ were used as the ligands to obtain a series of nitrogen-rich energetic 3D MOFs [Cu(N₅)(N₃)]n, [Ag(N₅)]n, [Ba(N₅)(NO₃)(H₂O)₃]n, and [NaBa₃(N₅)₆(NO₃)(H₂O)₃]n by self-assembly. These frameworks were characterized by single-crystal X-ray diffraction, SEM, IR and Raman spectroscopy, elemental analysis, and thermal analysis. All the frameworks exhibited regular supramolecular structures and excellent stability at room temperature w...

Coupling of Guanine with cyclo-l-Trp-l-Trp Mediated by a Cytochrome P450 Homologue from Streptomyces purpureus.

A cyclo-l-Trp-l-Trp tailoring P450 with novel function from Streptomyces purpureus was identified by heterologous expression in S. coelicolor and in vitro assays the recombinant protein. Structural elucidation revealed that this enzyme catalyzes the transfer of a guanine moiety to the indole ring of the cyclodipeptide via a C-N bond. Adduct products of CDP and guanine are unprecedented in nature, and CDP modification by coupling with guanine has not been reported prior to this study.

Roasted barley extract (mugi-cha) containing cyclo (D-Phe-L-Pro) prevents lowering of cutaneous blood flow and skin temperature under air-conditioning - A randomized, double-blind, placebo-controlled, crossover study.

Roasted barley extract (RBE), also known as mugi-cha, is a well-known healthy non-caffeinated beverage and its health functionality has been widely reported. Our previous clinical study showed that RBE affects cutaneous blood flow and skin temperature after cold water immersion, and that cyclo (D-Phe-L-Pro) is responsible for its effect. In this study, we investigated whether cyclo (D-Phe-L-Pro)-containing RBE prevents the decrease in cutaneous blood flow and skin temperature in an excessively air-condition...

Rutin, a quercetin glycoside, alleviates acute endotoxemic kidney injury in C57BL/6 mice via suppression of inflammation and up-regulation of antioxidants and SIRT1.

Acute kidney injury (AKI) is a common complication following severe sepsis, its incidence is increasing, and it is associated with a high rate of morbidity and mortality. Rutin is a glycoside of the bioflavonoid quercetin with various protective effects due to its antioxidant and anti-inflammatory potential. In this research, we tried to assess the protective effect of rutin administration in a model of AKI in C57BL/6 mice. For induction of AKI, lipopolysaccharide (LPS) was injected once (10mg/kg, i.p.) and...

Fusarihexins A and B: Novel Cyclic Hexadepsipeptides from the Mangrove Endophytic Fungus Fusarium sp. R5 with Antifungal Activities.

Two novel cyclic hexadepsipeptides, fusarihexin A (1: ) and fusarihexin B (2: ), and two known compounds, cyclo-(L-Leu-L-Leu-D-Leu-L-Leu-L-Val) (3: ) and cyclo-(L-Leu-L-Leu-D-Leu-L-Leu-L-Ile) (4: ), were isolated from the marine mangrove endophytic fungus sp. R5. Their chemical structures were elucidated on the basis of spectroscopic data and Marfey's analysis. In an bioassay, fusarihexin A (1: ) remarkably inhibited three plant pathogenic fungi: (Penz.) Sacc., which causes anthracnose in many fruits and...

High-temperature stable and sterilizable waveguide Bragg grating in planar cyclo-olefin copolymer.

In this Letter, we demonstrate a high-temperature stable polymer planar waveguide Bragg grating based on cyclo-olefin copolymers. The high glass transition temperature of the polymer material amounting to 178°C, in conjunction with a high-temperature stable UV-curable adhesive used to connect the polymer sensor to a standard single-mode fiber, enables temperature readings of up to 160°C while exhibiting a temperature sensitivity of -7.3  pm/°C. The reflected power of the Bragg wavelength remains cons...

Identification and quantification of ethylene oxide in sterilized medical devices using multiple headspace GC/MS measurement.

This manuscript, based on the ISO 10993-7 approach, describes a multiple HS-GC measurement of residual EO present in sterilized plastic samples. The quantification of EO is done, according to the ISO standard, by addition of EO amounts extracted for each repeated extraction. During the method development, the specificity of the detection of EO regarding acetaldehyde (structural isomer of EO) which may be formed from EO has been ensured and different tests were performed to check a possible influence of the ...

Bidirectional Regulation of COX-2 Expression Between Cancer Cells and Macrophages.

Our aim was to investigate the crosstalk between tumor and immune cells (M2 macrophages) and its effects on cyclo-oxygenase-2 (COX2) regulation in canine mammary tumors (CMT).

Synthesis, biophysical and functional studies of two BP100 analogues modified by a hydrophobic chain and a cyclic peptide.

Antimicrobial peptides (AMPs) work as a primary defense against pathogenic microorganisms. BP100, (KKLFKKILKYL-NH), a rationally designed short, highly cationic AMP, acts against many bacteria, displaying low toxicity to eukaryotic cells. Previously we found that its mechanism of action depends on membrane surface charge and on peptide-to-lipid ratio. Here we present the synthesis of two BP100 analogs: BP100‑alanyl‑hexadecyl‑1‑amine (BP100-Ala-NH-CH) and cyclo(1‑4)‑d‑Cys, Ile, Leu, Cys-BP100 (...

Quorum quelling efficacy of marine cyclic dipeptide -cyclo(L-leucyl-L-prolyl) against the uropathogen Serratia marcescens.

In the current study, the anti-QS efficacy of cyclic dipeptide -cyclo(L-leucyl-L-prolyl) (CLP) of marine origin was explored against S. marcescens. Minimal -inhibitory (MIC) and -bactericidal concentrations (MBC) of CLP against both reference and a clinical isolate of S. marcescens was identified to be 200 and 400 μg/mL, respectively. CLP proficiently inhibited the QS controlled prodigiosin production in S. marcescens, which affirm its anti-QS efficacy towards S. marcescens. At sub-MICs (100 μg/mL), C...

Arg/Trp-Rich Cyclic α/β-Antimicrobial Peptides: The Roles of H-bonding and Hydrophobic/Hydrophilic Solvent Accessible Surface Areas upon the Activity and Membrane Selectivity.

The bacterial selectivity of an amphiphilic library of small Arg/Trp-rich cyclic α/β-tetra-, α/β-penta-, and α/β-hexapeptides, which contained asymmetric backbone configurations and differed in hydrophobicity and content of alternating D,L-amino acids, was investigated against Bacillus subtilis and Escherichia coli. The structural analyses showed that the peptides tend to form assemblies of different shapes. All-L-peptides, especially the most hydrophobic pentamers, were stronger anti-B. subtilis. Wit...

A sustained virological response after eight weeks of treatment with sofosbuvir, ledipasvir and ribavirin in a decompensated cirrhotic patient with hepatitis C virus genotype 1b.

A 68-year-old Japanese man with decompensated cirrhosis due to hepatitis C virus (HCV) genotype 1b infection was treated with sofosbuvir (SOF; 400mg/day), ledipasvir (LDV; 90mg/day), and ribavirin (RBV; 400mg/day). Before treatment, his Child-Pugh and Model for End-Stage Liver Disease (MELD) scores were 10 (class C) and 13 points, respectively. Although RBV was initially administered at two-thirds the normal dose due to anemia, his hemoglobin level gradually declined, and was reduced to 200mg daily on day 1...

Quantitative analysis of the cyclic peptide GG-8-6 in rat plasma using LC-MS/MS and its application to a pharmacokinetic study.

Hepatocellular carcinoma (HCC) is the second leading cause of cancer-related death worldwide. The discovery of new anticancer compounds is of great significance. GG-8-6, cyclo-(Val-Leu-Pro-Ile-Leu-Leu-Leu-Val-Leu), a new synthetic cyclic peptide, might be a potential candidate for developing new anti-HCC drugs. GG-8-6 shares no structural homology to current anti-HCC drugs. Therefore, it was necessary to develop a quantitative method for the determination of GG-8-6 in vivo. Herein, a simple, specific and se...

Evaluation of neuroprotective effects of Wedelolactone and Gallic acid on aluminium-induced neurodegeneration: Relevance to sporadic Amyotrophic lateral sclerosis.

Al exposure causes an alteration in the several ions in the body and causes toxicity. Such as apoptosis, oxidative stress, disruption in neuronal transport, mitochondrial damage, excitotoxicity, generation of inflammatory mediators, and microglial activation. These multiple mechanisms lead to the several neurodegenerative diseases, including sporadic amyotrophic lateral sclerosis (sALS). The study aims to unravel the mechanisms behind the neuroprotective effects of wedelolactone (WL) and gallic acid (GA) ag...

Thiotepa Based Intensified Reduced-Intensity Conditioning Adult Double-Unit Cord Blood Hematopoietic Stem Cell Transplantation Results in Decreased Relapse Rate and Improved Survival Compared to Transplantation Following Standard Reduced-Intensity Conditioning: a Retrospective Cohort Comparison.

The "Minnesota" reduced intensity conditioning (RIC) cord-blood transplantation (CBT) regimen (standard-RIC) of fludarabine (Flu, 200mg/m), cyclophosphamide (Cy, 50mg/kg), and 200cGy or 300cGy total body irradiation (TBI) is the most published RIC CBT regimen. Though well tolerated, high relapse rates remain a concern with this regimen. Intensification of conditioning may reduce relapse without increasing transplant related mortality (TRM). We performed a retrospective cohort comparison of outcomes in adult...

SUBSTITUTION THERAPY WITH AMPHETAMINE-ISOTHERAPIC ATTENUATES AMPHETAMINE TOXICOLOGICAL ASPECTS OF ADDICTION.

amphetamine (AMPH) is related to development of addiction, anxiety-like behaviors and impairments of memory after chronic use. In the current experiment, an ultra-high dilution (10mg/mL) of AMPH was used, consisting of the AMPH isotherapic (AMPH-ISO), which can be used as a replacement therapy to treat AMPH addiction.

Anti-proliferative potential of cyclotetrapeptides from Bacillus velezensis RA5401 and their molecular docking on G-Protein-Coupled Receptors.

Elucidation of bioactive chemical compounds from rhizobacteria is highly utilized in pharmaceuticals and naturopathy, due to their health benefits to human and plants. In current study, four cyclopeptides along with one phenyl amide were isolated from the ethyl acetate extract of Bacillus velezensis sp. RA5401. Their structures were determined and characterized as cycle (L-prolyl-L-leucyl) (1), cyclo (L-prolyl-l-valine) (2), cycle (L-phenylanalyl-L-propyl) (3), cyclo (D-pro-L-tyr-L-pro-L-tyr) (4) and N-(2-p...

Yamamoto Coupling for the Synthesis of Benzophenes and Acene-based Cyclooctatetraenes.

Two TIPS-ethynylated dibromoacenes were used in a shotgun Yamamoto-reaction with 1,2-dibromobenzene or 4,5 dibro¬mo-veratrol. Four soluble benzo¬nonaphenes/benzo¬undeca¬phenes were isolated in satisfactory yields. Examples of tetracene- and pentacene-fused tetrabenzo¬cyclo¬octatetraenes also isolated from this reaction are reported. All compounds were characterized by UV/Vis and fluorescence spectroscopy, cyclic voltammetry, X-ray crystallo¬graphy as well as DFT and NICS calculations.

Integrin αvβ3-associated DAAM1 is essential for collagen-induced invadopodia extension and cell haptotaxis in breast cancer cells.

The formin protein dishevelled-associated activator of morphogenesis 1 (DAAM1) polymerizes straight actin filaments and mediates migration of cancer cells. However, how DAAM1 governs cell haptotaxis in response to collagen remains unexplored in breast cancer cells. We hypothesized that DAAM1 mediates invadopodia extension and cell haptotaxis in response to type IV collagen in association with integrin receptors. Using Boyden chamber membranes coated with type IV collagen, we show here that type IV collagen ...

High residual platelet reactivity after switching from clopidogrel to low-dose prasugrel in Japanese patients with end-stage renal disease on hemodialysis.

High on-treatment platelet reactivity (HPR) under clopidogrel treatment is frequently observed in hemodialysis (HD) patients. In such patients, 10mg of prasugrel has reportedly inhibited platelet reactivity more adequately compared with 75mg of clopidogrel. However, the efficacy of 3.75mg prasugrel in Japanese HD patients is largely unknown.


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