Search results for "Inhibitory effect"
showing 10 items of 36 documents
Dependence of hepatic gluconeogenesis on PO2: inhibitory effects of halothane
1987
The dependence of gluconeogenesis and O2 uptake on PO2 in isolated rat hepatocytes is presented. Maintenance of steady-state PO2 was achieved with an oxystat system (Biochem. J. 236: 765–769, 1986). O2 uptake showed a half-maximal (K0.5) value of 0.5 Torr PO2, whereas the glucose synthesis rate was half-maximal at 1.2 Torr PO2. Halothane at concentrations greater than 1 mM exerted a parallel inhibition of O2 uptake and glucose synthesis at all PO2 levels studied. In contrast, at halothane concentrations less than 1 mM, inhibition of glucose synthesis occurred only at less than 20 Torr PO2. At these low concentrations, halothane was without significant effects on cellular O2 uptake. In isol…
Auranofin and related heterometallic gold(I)-thiolates as potent inhibitors of methicillin-resistant Staphylococcus aureus bacterial strains.
2014
A series of new heterometallic gold(I) thiolates containing ferrocenyl-phoshines were synthesized. Their antimicrobial properties were studied and compared to that of FDA-approved drug, auranofin (Ridaura), prescribed for the treatment of rheumatoid arthritis. MIC in the order of one digit micromolar were found for most of the compounds against Gram-positive bacteria Staphylococcus aureus and CA MRSA strains US300 and US400. Remarkably, auranofin inhibited S. aureus, US300 and US400 in the order of 150-300 nM. This is the first time that the potent inhibitory effect of auranofin on MRSA strains has been described. The effects of a selected heterometallic compound and auranofin were also stu…
Soldier formation regulated by a primer pheromone from the soldier frontal gland in a higher termite, Nasutitermes lujae
1984
In the nasute higher termite Nasutitermes lujae , the differentiation of new soldiers is suppressed or delayed by the soldiers themselves. Experimental data strongly suggest that this inhibitory effect results from the action of a primer pheromone secreted by the frontal gland of soldiers. The pheromone must be contacted directly. Thus, the frontal gland of termite soldiers assumes a new role in addition to alarm and defense, although this extension cannot be generalized to all termite species. The soldier inhibitory pheromone is evidently only one of multiple factors contributing soldier regulation in termite societies.
Synthesis and biological properties of the seven alanine-modified analogues of the marine cyclopeptide hymenamide C
2002
The synthesis and biological activity of the marine cyclopeptide hymenamide C(1), showing an inhibitory effect on human neutrophil elastase degranulation release, were recently described. Based on this result, it was decided to undertake a systematic structure-activity relationship study of this cyclopeptide, based on the Ala-scan technique, in order to obtain useful information for the rational design of additional analogues. The synthesis and characterization of the seven Ala modified analogues are reported and their biological and pharmacological properties are described.
Red blood cell sodium and potassium after hydrochlorothiazide.
1981
In six of seven healthy males 6 days of hydrochlorothiazide (HCT), 50 mg twice daily, without potassium supplements resulted in a rise in red blood cell (RBC) sodium concentration. Serum potassium concentration fell in all subjects. Four days after discontinuing HCT, intracellular sodium and extracellular potassium concentrations had normalized. Throughout the evaluation period the course of mean relative intracellular sodium was almost a mirror image of mean relative extracellular potassium. Thus, either the decline of serum potassium or of HCT (because of its inhibitory effect on Na-K-ATPase activity) might have diminished Na-K-ATPase–dependent active RBC sodium efflux with a resultant ri…
Drimane Sesquiterpenoids from Marasmius sp. Inhibiting the Conidial Germination of Plant-Pathogenic Fungi
2012
From the basidiomycete Marasmius sp., strain IBWF 96046, three new sesquiterpenoids based on the drimane skeleton were isolated and named marasmene B and marasmals B and C. In this study, their isolation, structure elucidation, and biological evaluation are described. The compounds have a pronounced inhibitory effect on the conidial germination of several plant-pathogenic fungi.
Phenological model performance to warmer conditions: application to Pinot noir in Burgundy.
2014
<p style="text-align: justify;"><strong>Aim</strong>: The current work aims to assess the performance of two phenological models - a linear model (<em>Grapevine Flowering</em> <em>Véraison</em> model, <em>GFV</em>) and a curvilinear model (<em>Wang and</em> <em>Engel</em> model, <em>WE</em>) - to warmer temperature conditions for the grapevine variety Pinot noir in Burgundy.</p><p style="text-align: justify;"><strong>Methods and results</strong>: Simulations using historical data from the 1973-2005 period were similar between models and consistent with observations. To mimic pot…
The inhibitory effect of long-term associative representation on working memory
2020
Studies on how long-term memory affects working memory (WM) have found that long-term memory can enhance WM processing. However, these studies only use item memory as the representation of long-term memory. In addition to item memory, associative memory is also an essential part of long-term memory. The associative memory and item memory involve different cognitive mechanisms and brain areas. The purpose of the present study was to investigate how associative memory affects WM processing. Before the WM task, participants were asked to store 16 pairs of dissimilar pictures into long-term memory. The participants would obtain the associative memory of these pairs of pictures in the long-term …
Demonstration of a correlation between young leaves, apex and young bunches specific to a young grapevine cutting in the first period of its developm…
2001
<p style="text-align: justify;">The development of hardwood cutting of grapevine comprise 4 succesive phases. Phase I: first period of shoot extension. Phase II: characterized by a slow growth due to a very low activity of the terminal bud. Phase III: reactivation of the growth consecutive to a resumption of the apical activity. Phase IV: when the growth becomes maximal.</p><p style="text-align: justify;">The objective of this work has been to identify the cause of the slowdown of the activity of apical bud during the phase II.</p><p style="text-align: justify;">In a first experiment, we have compared the effects of three modes of defoliation applied from the b…
Design, synthesis, biological evaluation and molecular modelling of substituted pyrrolo[2,1-a]isoquinolinone derivatives: discovery of potent inhibit…
2021
We report here the design, synthesis and biological evaluation of a new series of substituted pyrrolo[2,1-a]isoquinolin-3-one derivatives, some of which have strong inhibitory activity against both AChE and BChE enzymes. The design of these new inhibitors was carried out taking rivastigmine as the starting structure. Thus, on the basis of an exhausting molecular modeling study using combined techniques (docking, dynamic molecular simulations and QTAIM calculations), we obtained new ligands possessing stronger inhibitory effects than rivastigmine, the reference compound. QTAIM analysis gave us detailed information about the molecular interactions stabilizing the different ligand–enzyme compl…