Investigation of the activity of new derivatives of 1,3-diazinone-4 and their acyclic precursors with respect to bacteria of the genus Proteus

The present paper provides a study of the activity of the new 1,3-diazinon-4 derivatives and their acyclic precursors under the laboratory cipher PYaTd1, PYaTs2, PYaTs3 and PYaTs4 against microorganisms of the genus Proteus, which is of high importance at the moment as the growing resistance of the Proteus to previously highly active antibiotics dictates the need to search for effective antimicrobial agents that meet modem safety requirement

Collision Dynamics and Solvation of Water Molecules in a Liquid Methanol Film

Environmental molecular beam experiments are used to examine water interactions with liquid methanol films at temperatures from 170 K to 190 K. We find that water molecules with 0.32 eV incident kinetic energy are efficiently trapped by the liquid methanol. The scattering process is characterized by an efficient loss of energy to surface modes with a minor component of the incident beam that is inelastically scattered. Thermal desorption of water molecules has a well characterized Arrhenius form with an activation energy of 0.47{\pm}0.11 eV and pre-exponential factor of 4.6 {\times} 10^(15{\pm}3) s^(-1). We also observe a temperature dependent incorporation of incident water into the methanol layer. The implication for fundamental studies and environmental applications is that even an alcohol as simple as methanol can exhibit complex and temperature dependent surfactant behavior.Comment: 8 pages, 5 figure

Characterization of the Endothelial Cell Cytoskeleton following HLA Class I Ligation

Vascular endothelial cells (ECs) are a target of antibody-mediated allograft rejection. In vitro, when the HLA class I molecules on the surface of ECs are ligated by anti-HLA class I antibodies, cell proliferation and survival pathways are activated and this is thought to contribute to the development of antibody-mediated rejection. Crosslinking of HLA class I molecules by anti-HLA antibodies also triggers reorganization of the cytoskeleton, which induces the formation of F-actin stress fibers. HLA class I induced stress fiber formation is not well understood.The present study examines the protein composition of the cytoskeleton fraction of ECs treated with HLA class I antibodies and compares it to other agonists known to induce alterations of the cytoskeleton in endothelial cells. Analysis by tandem mass spectrometry revealed unique cytoskeleton proteomes for each treatment group. Using annotation tools a candidate list was created that revealed 12 proteins, which were unique to the HLA class I stimulated group. Eleven of the candidate proteins were phosphoproteins and exploration of their predicted kinases provided clues as to how these proteins may contribute to the understanding of HLA class I induced antibody-mediated rejection. Three of the candidates, eukaryotic initiation factor 4A1 (eIF4A1), Tropomyosin alpha 4-chain (TPM4) and DDX3X, were further characterized by Western blot and found to be associated with the cytoskeleton. Confocal microscopy analysis showed that class I ligation stimulated increased eIF4A1 co-localization with F-actin and paxillin.Colocalization of eIF4A1 with F-actin and paxillin following HLA class I ligation suggests that this candidate protein could be a target for understanding the mechanism(s) of class I mediated antibody-mediated rejection. This proteomic approach for analyzing the cytoskeleton of ECs can be applied to other agonists and various cells types as a method for uncovering novel regulators of cytoskeleton changes

Investigation of the activity of new derivatives of 1,3-diazinone-4 and their acyclic precursors with respect to bacteria of the genus Proteus

The present paper provides a study of the activity of the new 1,3-diazinon-4 derivatives and their acyclic precursors under the laboratory cipher PYaTd1, PYaTs2, PYaTs3 and PYaTs4 against microorganisms of the genus Proteus, which is of high importance at the moment as the growing resistance of the Proteus to previously highly active antibiotics dictates the need to search for effective antimicrobial agents that meet modem safety requirement

Aktywność antywirusowa i cytotoksyczna antrachinonów wyizolowanych z liści Cassia roxburghii Linn.

The cytotoxic activity of petroleum ether extract of the leaves of Cassia roxburghii Linn. against HCT-116 and MCF-7 cell lines resulted with IC50=34.9 and 38.04 μg/ml, respectively, while against HepG-2 showed no activity. A bioassay guided-fractionation approach was conducted to isolate and identify the active cytotoxic principles. Further chromatographic separation and purification of the petroleum ether extract resulted in the isolation of two anthraquinones identified as aloe-emodin acetate and aloe-emodin, along with stigmasterol, β-sitosterol and palmitic acid. The structure elucidation of isolated compounds was performend using 1D, 2D-NMR and HR-MS. Furthermore, the cytotoxicity of aloe-emodin acetate and aloe-emodin were evaluated and resulted with IC50=153.30 and 70.02 μg/ml against HCT-116 and with 93.20 and 53.20 μg/ml against MCF-7, respectively, while against HepG-2 showed no activity. Moreover, the antiviral activity of the two isolated anthraquinones was tested against influenza virus-A, and resulted with IC50=10.23 as well as 2.00 and with CC50=1.32 and 0.47 μg/ml, respectively.Aktywność cytotoksyczna wyciągu benzynowego z liści Cassia roxburghii Linn. przeciwko liniom komórkowym HCT-116 i MCF-7 wynosiła odpowiednio IC50=34.9 i 38,04 μg/ ml, natomiast nie wykazano aktywności przeciwko HepG-2. Przeprowadzono biologiczne frakcjonowanie w celu wyizolowania i identyfikacji aktywnych związków o działaniu cytotoksycznym. Późniejsza separacja chromatograficzna i oczyszczenie wyciągu benzynowego zaowocowało wyizolowaniem dwóch antrachinonów oznaczonych jako octan aloe-emodyny i aloe-emodyna, a także stigmasterolu, β-sitosterolu i kwasu palmitynowego. Określenie struktury wyizolowanych składników przeprowadzono przy użyciu 1D, 2D-NMR i HR-MS. Określono także cytotoksyczność octanu aloe-emodyny i aloe-emodyny, której wartość wyniosła odpowiednio IC50=153,30 i 70,02 μg/ml przeciwko HCT-116 oraz odpowiednio 93,20 i 53,20 μg/ml przeciwko MCF-7. Nie wykazano aktywności przeciwko HepG-2. Testowano też aktywność przeciwwirusową dwóch wyizolowanych antrachinonów przeciwko wirusowi grypy typu A. Wyniosła ona odpowiednio IC50=10,23 oraz 2,00 przy CC50=1,32 i 0,47 μg/ml