Search results for " inhibition"
showing 10 items of 435 documents
Influence of Galvanic Microcells on Growth of Pathogenic Bacteria and Candida Yeast
2017
The aim of the study was to evaluate the influence of electrodes on growth of pathogenic bacteria and Candida albicans yeast. In the study, following references bacteria strains were used: Staphylococcus aureus ATTC 6538; Enterococcus faecalis ATTC 29212 (V); Enterococcus hirae ATTC 105441 (VI) and yeast strain Candida albicans ATTC 10231 (C40). Microelectrodes were prepared by ALCOR Center. Estimation of the biocidal effect of electrodes was carried out by medium poisoning method. The assessment of adhesion to the surface was performed by a modified Hawser’s method. Presence of adhesion was assessed by SEM analysis. The highest inhibition zones were obtained for Staphylococcus aureus ATTC …
Natural products as inhibitors of recombinant cathepsin L of Leishmania mexicana.
2015
Cysteine proteinases (cathepsins) from Leishmania spp. are promising molecular targets against leishmaniasis. Leishmania mexicana cathepsin L is essential in the parasite life cycle and a pivotal in virulence factor in mammals. Natural products that have been shown to display antileishmanial activity were screened as part of our ongoing efforts to design inhibitors against the L. mexicana cathepsin L-like rCPB2.8. Among them, agathisflavone (1), tetrahydrorobustaflavone (2), 3-oxo-urs-12-en-28-oic acid (3), and quercetin (4) showed significant inhibitory activity on rCPB2.8 with IC50 values ranging from 0.43 to 18.03 µM. The mechanisms of inhibition for compounds 1–3, which showed Ki values…
Synthesis and activity of phosphinic tripeptide inhibitors of cathepsin C
2004
Phosphinic tripeptide analogues Gly-Xaaψ[P(O)(OH)CH2]-Gly have been developed as inhibitors of cathepsin C (DPP I), a lysosomal, papain-like cysteine protease. The target compounds were synthesised by addition of methyl acrylate to the appropriate phosphinic acids followed by the N-terminus elongation using mixed anhydride procedure. The latter step has been demonstrated to be a suitable method for N-terminal extension of the phosphinic pseudopeptide analogues without requirement of hydroxyphosphinyl protection. The title compounds appeared to be moderate inhibitors of the cathepsin C. However, although designed as transition state analogues, they surprisingly exhibited noncompetitive mode …
Sphingomyelin inhibition of Ciona intestinalis (Tunicata) cytotoxic hemocytes assayed against sheep erythrocytes
1995
Hemocytes from the ascidian, Ciona intestinalis, are capable of lysing erythrocytes in vitro following cell membrane contact. With the aim of examining the mechanism of cytotoxicity, we performed inhibition experiments with lipid components of erythrocyte membranes. Cholesterol is not an inhibitor, whereas, among the phospholipids tested, (sphingomyelin, phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine) sphingomyelin inhibits the hemolytic activity of hemocytes. However, thin layer chromatography showed that sphingomyelinase activity was not contained in the chloroform-methanol extracts from hemocyte debris. The inhibition capacity of the components ceramide and phosphorylc…
Antitumor effects of curcumin and structurally β-diketone modified analogs on multidrug resistant cancer cells
2007
Abstract Using concepts of bioisostery a series of curcumin analogs were synthesized: the diketonic system of the compound was elaborated into enaminones, oximes, and the isoxazole heterocycle. The cell growth inhibitory and apoptosis inducing effects of the new analogs were evaluated by in vitro assays in the hepatocellular carcinoma HA22T/VGH cells, as well as in the MCF-7 breast cancer cell line and in its multidrug resistant (MDR) variant MCF-7R. Increased antitumor activity on all cell lines was found with the isoxazole analog and especially with the benzyl oxime derivative; in the HA22T/VGH cell model, the latter compound inhibited constitutive NF-κB activation.
Growth control in mammalian cells by cell-cell contacts.
1990
Growth of normal diploid mammalian cells in vitro is strongly regulated by the actual cell density. Cell-cell contacts via specific plasma membrane glycoproteins whose glycan moieties interact with specific receptors has been found to be a main growth regulatory principle. Malignant growth is suggested to result from impaired function of these receptors.
Cooling of the cerebellar interpositus nucleus abolishes somatosensory cortical learning-related activity in eyeblink conditioned rabbits.
2005
Nictitating membrane movement and multiple-unit activity in the somatosensory cortex were recorded from rabbits during paired (N = 6) and unpaired (N = 5) presentations of a tone conditioned stimulus (CS) and an airpuff unconditioned stimulus (US). A behavioural conditioned response (CR) to the CS and an accompanying neural response in the somatosensory cortex developed only in the paired group. Inactivation of the cerebellar interpositus nucleus abolished both the acquired CR and the accompanying neural response. However, the CS facilitated both behavioural and neural responses to the US during the inactivation. Thus, the absence of the CR could not be accounted for by the general inabilit…
Influenza A virus infection inhibits the efficient recruitment of Th2 cells into the airways and the development of airway eosinophilia.
2003
Abstract Most infections with respiratory viruses induce Th1 responses characterized by the generation of Th1 and CD8+ T cells secreting IFN-γ, which in turn have been shown to inhibit the development of Th2 cells. Therefore, it could be expected that respiratory viral infections mediate protection against asthma. However, the opposite seems to be true, because viral infections are often associated with the exacerbation of asthma. For this reason, we investigated what effect an influenza A (flu) virus infection has on the development of asthma. We found that flu infection 1, 3, 6, or 9 wk before allergen airway challenge resulted in a strong suppression of allergen-induced airway eosinophil…
Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet.
2009
In this study the development of a procedure based on capillary electrophoresis after enzymatic reaction at capillary inlet methodology for the screening and in vitro evaluation of the biological activity of acetylcholinesterase (AChE) inhibitors is presented. The progress of the enzymatic reaction of the hydrolysis of acetylthiocholine at pH 8 in the presence of AChE and the inhibitor studied is determined by measuring at 230 nm the peak area of the reaction product thiocholine (TCh). In the method employed the capillary was first filled with 30 mM borate-phosphate buffer (pH 8.0) and subsequently, plugs of: (i) water, (ii) AChE solution, (iii) substrate solution with or without inhibitor,…
Antihypertensive effect of a bovine lactoferrin pepsin hydrolysate: Identification of novel active peptides
2012
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