Search results for " inhibition"

ChemInform Abstract: Exploring the Anticancer Potential of Pyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-one Derivatives: The Effect on Apoptosis Induction…

2013

Abstract In order to investigate their anticancer potential, four new pyrazolo[1,2-a]benzo[1,2,3,4]tetrazinone derivatives, designed through the chemometric protocol VLAK, and three of the most active compounds of the previous series have been evaluated on some cellular events including proliferation, apoptosis induction, and cell cycle. The NCI one dose (10 μM) screening revealed that the 8,9-di-methyl derivative showed activity against Leukemia (CCRF-CEM) and Colon cancer cell line (COLO 205), reaching 81% and 45% of growth inhibition (GI), respectively. Replacement of the two methyl groups with two chlorine atoms maintained the activity toward Leukemia cell (CCRF-CEM, GI 77%) and selecti…

Antimicrobial efficacy of the supernatant of <i>Streptococcus dentisani</i> against microorganisms implicated in root canal infections

2019

The present study aimed to test the antimicrobial activity of Streptococcus dentisani (S. dentisani) supernatant against a collection of microorganisms implicated in dental root infections, and to analyze morphological changes induced in a selection of the tested microorganisms. A total of 22 microbial species were selected, and their growth was monitored by spectrophotometry in the presence and absence of the supernatant of S. dentisani at different assay concentrations (0.2×, 1×, 2×). The generation time and maximum growth rates were evaluated under every tested condition. Scanning electron microscope (SEM) images were obtained to assess the effect on the cell surface following incubation…

Antibacterial activity of different root canal sealers against Enterococcus faecalis

2017

Background The aim of the present study was to compare in vitro the antimicrobial activity of different root canal sealers against Enterococcus faecalis, prior and subsequent to setting. Material and methods Agar diffusion test (ADT) was used for evaluating the antibacterial activity of non-set sealer while the direct contact test (DCT) was used for after setting. Results ADT: Except for TotalFill BC Sealer all the others sealers tested showed antibacterial activity. BioRoot™RCS, MTA Fillapex and Sealapex Root Canal Sealer showed the lowest antibacterial activity, a significant increase in antibacterial effect for both Pulp Canal Sealer™ and AH plus sealers were found. Significantly higher …

Prepulse Inhibition and Vulnerability to Cocaine Addiction

2021

Cellul�re Immunreaktionen gegen�ber homologen leberspezifischen Antigenen (HLP) bei chronischen Leberentz�ndungen

1974

Es wird eine Zweiphasentechnik des Leukocyten-Migrations-Inhibitionstestes beschrieben und zum Nachweis einer cellularen Immunreaktion gegenuber Leberantigenen bei chronisch-entzundlichen Lebererkrankungen eingesetzt. Mit dieser Technik wurde bei 85% der Patienten mit hypergammaglobulinamischer Verlaufsform einer chronisch-aktiven Hepatitis und 42% der Patienten mit aktiv fortschreitenden kryptogenen Lebercirrhosen eine Migrationshemmung nachgewiesen. Lebergesunde Kontrollen zeigten keine, Patienten mit dem Zustand nach Hepatitis und chronisch-persistierender Hepatitis selten eine Leukocytenmigrationsinhibition gegenuber leberspezifischen Antigenen. 17% der Patienten mit chronisch-aktiver H…

Cortical Hypoactivity or Reduced Efficiency of Cortical Inhibition in Migraine?

2007

How To Design Selective Ligands for Highly Conserved Binding Sites: A Case Study Using N-Myristoyltransferases as a Model System

2019

A model system of two related enzymes with conserved binding sites, namely N-myristoyltransferase from two different organisms, was studied to decipher the driving forces that lead to selective inhibition in such cases. Using a combination of computational and experimental tools, two different selectivity-determining features were identified. For some ligands, a change in side-chain flexibility appears to be responsible for selective inhibition. Remarkably, this was observed for residues orienting their side chains away from the ligands. For other ligands, selectivity is caused by interfering with a water molecule that binds more strongly to the off-target than to the target. On the basis o…

Photo-inhibition of Ab fibrillation mediated by a newly designed fluorinated oxadiazole

2015

Uncontrolled aggregation of amyloid beta peptide (A?) is the main cause of Alzheimer's Disease. Therapeutic approaches of intervention in amyloid diseases include the use of small molecules able to stabilize the soluble A? conformation, or to redirect the amyloidogenic pathway towards non-toxic and non-fibrillar states. Fluorometric measurements revealed that the 3-(4'-trifluoromethylphenyl)-5-(4'-methoxyphenyl)-1,2,4-oxadiazole, when irradiated, is able to interact with monomeric A? peptide readdressing the aggregation pathway toward the formation of amorphous aggregates as evidenced by means of CD, AFM, and SAXS measurements. We hypothesize that this compound, under radiation, forms a rea…

Isolation, identification and toxicological characterization of TSS 1, a new mycotoxin of the rosenane class.

1990

11-β-hydroxy-7-deoxy-rosenonolactone (TSS1), a product of the pathogenic fungusTrichothecium roseum (Moniliaceae) was isolated from culture medium extracts and completely described in its structure by spectroscopical methods.TSS 1 was classified as a representative of the lactone series of the rosenane class and as a structural isomer to Rosenololactone (1) and Rosololactone (2, 3).TSS1 showed toxic effects in the growth inhibition test toE coli (EC 50: lOμg/mL) andB subtil is (EC 50: 17μg/mL), inhibited fermentation of yeast (EC 50: 2.8μg/mL) and suppressed motility ofAnemia satina larvae (EC 50: 45/μg/mL).Rosenonolactone, the best known representative of that mycotoxin class, showed only …

Isolation, structural and toxicological characterization of three new mycotoxins produced by the fungusAureobasidium pullulans.

1993

3 substances, B1, B2, and E1 were isolated from culture medium extracts ofAureobasidium pullulans by reversed phase liquid chromatography and subsequent liquid chromatographic purification steps on silica gel.The 3 compounds inhibited the metabolism ofSaccharomyces cerevisiae and showed toxic effects in the growth inhibition test toEscherichia coli andBacillus subtilis.Elementary analysis and mass spectroscopical methods revealed sum formulas of C23H22O6, C22H20O6 and C24H28O3 for B1 B2, and E1 and molecular weights of 394, 380, and 364, respectively. Mass spectroscopical, UV-, IR-,(13)C-NMR, and(1)H-NMR-spectroscopical investigations revealed polycyclic, non-aromatic compounds containing s…