Search results for "Phenanthridines"
showing 10 items of 11 documents
1-ethyl-3-(6-methylphenanthridine-8-il) urea modulates TLR3/9 activation and induces selective pro-inflammatory cytokine expression in vitro.
2017
We have previously demonstrated the nucleic acid binding capacity of phenanthridine derivatives (PHTs). Because nucleic acids are potent inducers of innate immune response through Toll-like receptors (TLRs), and because PTHs bear a structural resemblance to commonly used synthetic ligands for TLR7/8, we hypothesized that PHTs could modulate/activate immune response. We found that compound M199 induces secretion of IL-6, IL-8 and TNFα in human PBMCs and inhibits TLR3/9 activation in different cellular systems (PBMCs, HEK293 and THP-1 cell lines).
In vitro antifungal properties of mouthrinses containing antimicrobial agents
1997
The purpose of this study was to investigate the in vitro antifungal properties of seven commercial mouthrinses containing antimicrobial agents. These included cetylpyridinium chloride (CPC), chlorhexidine digluconate (CHX), hexetidine (HEX), sanguinarine (SNG), and triclosan (TRN). The minimum fungicidal concentration (MFC) against six species of yeasts was determined by a broth macrodilution method. The kill-time of mouthrinses at half the concentration of the commercial formulations was also determined. MFCs were achieved with each mouthrinse, except the SNG-containing mouthrinse, against all the organisms being tested. However, the CPC-containing mouthrinse appeared more active than the…
Superoxide Flux in Endothelial Cells via the Chloride Channel-3 Mediates Intracellular Signaling
2007
Reactive oxygen species (ROS) have been implicated in both cell signaling and pathology. A major source of ROS in endothelial cells is NADPH oxidase, which generates superoxide (O2.−) on the extracellular side of the plasma membrane but can result in intracellular signaling. To study possible transmembrane flux of O2.−, pulmonary microvascular endothelial cells were preloaded with the O2.−-sensitive fluorophore hydroethidine (HE). Application of an extracellular bolus of O2.−resulted in rapid and concentration-dependent transient HE oxidation that was followed by a progressive and nonreversible increase in nuclear HE fluorescence. These fluorescence changes were inhibited by superoxide dism…
Multiple signal transduction pathways regulate clusterin (gp 80) gene expression in MDCK cells
1996
ABSTRACT Clusterin (gp 80, apolipoprotein J, TRPM-2) is a widely expressed multifunctional glycoprotein. Its demonstrated and proposed functions include the transport of lipids and membrane fragments, the inhibition of the cytolytic action of the terminal complement complex and the modulation of cell—cell interactions. The expression of the gene is enhanced during tissue injury and remodelling and by hormone-withdrawal-induced apoptosis of prostate and mammary cells. We show here that, in the kidney-derived epithelial cell line MDCK, clusterin mRNA is repressed by glucocorticoids and by progesterone. Treatment with epidermal growth factor also represses clusterin gene expression in MDCK cel…
Inhibitors acting on nucleic acid synthesis in an oncogenic RNA virus.
1971
IN infection with an oncogenic RNA virus, synthesis of viral RNA seems to be catalysed by an RNA dependent DNA polymerase in the host cell1–4. Several specific inhibitors of viral DNA polymerases have been found5–7 and Spiegelman8 has shown that the activity of viral enzymes depends strongly on the chemical composition of the template. We report here first a new highly specific poison of the Rauscher murine leukaemia virus (RMLV) DNA polymerases; second, several inactivators of the RNA and DNA template involved in the RMLV enzyme systems; and third, the action of actinomycin D on viral DNA polymerases and on host DNA/RNA polymerase. The results are discussed with respect to the influence of…
In vitro activities of antimicrobial agents against Candida species
1999
Objective. Antimicrobial mouthrinses may represent a valid alternative to topical antifungal agents. However, the action of antimicrobials could be affected by the different ingredients incorporated into mouthrinse products. The purpose of the present study was to investigate the in vitro antifungal and fungicidal activities of antimicrobials alone. Study Design. A broth macrodilution method was used to determine the minimum inhibitory concentration of 4 antimicrobial agents against Candida species. Minimum fungicidal concentration was also determined. Results. All antimicrobials showed antifungal activity against all tested organisms, but cetylpyridinium chloride received significantly low…
Interactions between the yeast mitochondrial and nuclear genomes: isogenic suppressive and hypersuppressive petites differ in their resistance to the…
1990
In a previous paper we have shown that the alkaloid lycorine inhibits growth of rho+, mit- and rho-, strains of Saccharomyces cerevisiae, whereas strains devoid of mitochondrial DNA (rho degrees) are resistant to more than 200 micrograms/ml of the alkaloid. In this report we show that hypersuppressive petites are almost as resistant as rho degrees mutants, whereas isogenic rho- petites, which have retained longer segments of the genome, are sensitive to the drug.
General approach for the analysis of various alkaloid classes using capillary electrophoresis and capillary electrophoresis-mass spectrometry
1997
Abstract The analysis of various alkaloid classes employing capillary electrophoresis (CE) and on-line combined CE-mass spectrometry (CE-MS) is described. A CE method is presented for the analysis of alkaloids without derivatisation or purification. The separation of four different groups of alkaloids consisting of monoterpenoid indole alkaloids, protoberberines/benzophenanthridines, β-carboline alkaloids, and isoquinolines from poppy by free zone capillary electrophoresis has been obtained using a 1:1 mixture of 100 mmol 1 −1 ammonium acetate (pH 3.1) and acetonitrile. The influence of alkaloid structure on the electrophoretic mobility is discussed. The CE-MS reconstructed total ion curren…
Additive effects of cherlerythrine chloride combination with erlotinib in human non-small cell lung cancer cells
2017
Several studies implicate that lung cancer progression is governed by the interaction between epidermal growth factor receptor (EGFR) signaling and protein kinase C (PKC) pathways. Combined the targeting of EGFR and PKC may have an additive or synergistic effects in lung cancer treatment. The aim of this study is to explore the potential utility by inhibiting these two pathways with the combination of erlotinib and chelerythrine chloride in non-small cell lung cancer (NSCLC) cell lines. The erlotinib-less sensitive cell lines SK-MES-1 and A549 were treated with erlotinib or chelerythrine by themselves or in combination with each other. The cell viability, clonogenic survival, cell migration…
Pyrrolo[1,2-f]phenanthridines and related non-rigid analogues as antiviral agents.
2002
Abstract The pyrrolo[1,2- f ]phenanthridines 8 – 22 and the corresponding non-rigid analogues 23 – 41 were synthesised and their ability to inhibit the replication of HIV-1 was tested. Only the polycyclic derivatives 10 , 11 , and 13 showed a weak anti -HIV activity, whereas several pyrrolo-phenanthridines ( 8 , 10 , 16 – 18 ) were found to stimulate the multiplication of MT-4 cells at low concentrations. Derivative 10 demonstrated to possess the unique property of stimulating the multiplication of lymphocytes joined to HIV inhibition.