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

08:54 EST 20th January 2019 | BioPortfolio

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Showing "Cyclo 10mg 200mg" PubMed Articles 1–25 of 86

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...

Significantly improved production of Welan gum by Sphingomonas sp. WG through a novel QS-interfering dipeptide cyclo(L-Pro-L-Phe).

A variety of physiological functions such as exopolysaccharide synthesis, antibiotic production, and primary metabolism are tightly controlled by quorum sensing in microorganisms. In this study, a marine-derived bacterium Sphingomonas sp. WG was found to possess a cyclo(L-Pro-L-Phe)-mediated quorum sensing mechanism. The cyclo(L-Pro-L-Phe) produced by Sphingomonas sp. WG functions as a signalling molecule in this quorum sensing system. It is the first attempt to characterize cyclic dipeptides as quorum sens...


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...

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...

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.

Cyclo(His-Pro) inhibits NLRP3 inflammasome cascade in ALS microglial cells.

Neuroinflammation, i.e. self-propelling progressive cycle of microglial activation and neuron damage, as well as improper protein folding, are recognized as major culprits of neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALS). Mutations in several proteins have been linked to ALS pathogenesis, including the G93A mutation in the superoxide dismutase 1 (SOD1) enzyme. SOD1(G93A) mutant is prone to aggregate thus inducing both oxidative stress and neuroinflammation. In this study we used hS...

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...

Control of protein adsorption to cyclo olefin polymer by the Hofmeister effect.

Cyclo olefin polymer (COP) is an attractive plastic because it has low protein adsorption despite its hydrophobic chemical structure. Here, the adsorption of model proteins to the COP was evaluated in comparison with a representative plastic, polystyrene (PSt), using reflectometry interference spectroscopy (RIfS) technology. The effects of different salts on adsorption were then examined. The adsorption of bovine serum albumin onto COP increased in the presence of kosmotropic salts, whereas adsorption of Ig...

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...

Macrofilaricidal efficacy of single and repeated oral and subcutaneous doses of flubendazole in Litomosoides sigmodontis infected jirds.

Flubendazole (FBZ) is highly efficacious against filarial nematodes after parenteral administration and presents a promising macrofilaricidal drug candidate for the elimination of onchocerciasis and other filariae. In the present study the efficacy of a newly developed bioavailable amorphous solid dispersion (ASD) oral formulation of FBZ was investigated in the Litomosoides sigmodontis jird model. FBZ was administered to chronically infected, microfilariae-positive jirds by single (40mg/kg), repeated (2, 6 ...

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...

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...

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.

Paraburkholderia phosphatilytica sp. nov., a phosphate-solubilizing bacterium isolated from forest soil.

A novel Gram-stain-negative, aerobic, non-spore-forming, non-motile and rod-shaped bacterial strain, 7QSK02, was isolated from forest soil of Dinghushan Biosphere Reserve, Guangdong Province, China. It grew at 12-37 °C, at pH 4.0-7.5 and in the presence of 0-1.0 % (w/v) NaCl on R2A agar medium, with optimum growth at 28 °C, pH 5.5 and 0 % NaCl. Strain 7QSK02 was closely related to members of the genus Paraburkholderia: P. acidipaludis NBRC 101816 (98.1 % 16S rRNA gene sequence similarity), P. ...

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.

Short-course, oral flubendazole does not mediate significant efficacy against Onchocerca adult male worms or Brugia microfilariae in murine infection models.

The Onchocerca ochengi adult implant and Brugia malayi microfilariemic Severe-Combined Immunodeficient (SCID) mouse models are validated screens to measure macrofilaricidal and microfilaricidal activities of candidate onchocerciasis drugs. The purpose of this study was to assess whether 5 daily sub-cutaneous (s.c.) injections of standard flubendazole (FBZ) suspension (10mg/kg), a single s.c. injection (10mg/kg) or 5 daily repeated oral doses of FBZ amorphous solid dispersion (ASD) formulation (0.2, 1.5 or 1...

Silencing the ACAT1 Gene in Human SH-SY5Y Neuroblastoma Cells Inhibits the Expression of Cyclo-Oxygenase 2 (COX2) and Reduces β-Amyloid-Induced Toxicity Due to Activation of Protein Kinase C (PKC) and ERK.

BACKGROUND Acyl-coenzymeA: cholesterol acyltransferase (ACAT) 1, a key enzyme converting excess free cholesterol to cholesterol esters, has been demonstrated to be associated with the pathogenesis of Alzheimer disease (AD). However, the mechanism underlying the protective role of ACAT1 blockage in AD progression remains elusive. MATERIAL AND METHODS Human neuroblastoma SH-SY5Y cells were treated for 24 h with increasing concentrations of aggregated Aβ₂₅₋₃₅ (5, 15, 25, and 45 μmol) with or withou...

Highly Diastereo- and Enantioselective Synthesis of Cyclo-heptabindoles via Chiral Phosphoric Acid-Catalyzed (4+3)-Cycloaddition.

A highly enantio- and diastereoselective formal (4+3)- cycloaddition of 1,3-diene-1-carbamates with 3-indolylmethanols using a chiral phosphoric acid catalyst is reported. The approach described herein provides efficient access to 6-amino-tetrahydrocyclohepta[b]indoles in good yields with excellent levels of enantioselectivity (>98:2 dr and up to 98% ee) and mostly complete diastereoselectivity. Mild reaction conditions, easy scale-up, and versatile derivatization highlight the practicality of this methodol...

Bioanalytical method development and its application to pharmacokinetics studies on Simvastatin in the presence of Piperine and two of its synthetic derivatives.

Piperine has been widely used as a bioenhancer. Simvastatin belongs to a group of medicines known as statins. It acts by inhibiting HMG CoA reductase and acts primarily as a hypolipidemic agent. In this study some derivatives of Piperine were synthesized. They were studied for their bioenhencing effect [10mg/kg] and this effect was compared with that of Piperine. The pharmacokinectic profile of Simvastatin alone and in combination with Piperine and Piperine derivatives were investigated by validated HPLC me...


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