69 research outputs found

    1-[2-(2,4-Dichloro­phenyl)­pent­yl]-1H-1,2,4-triazole

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    The title compound, C13H15Cl2N3, also known as penconazole, crystallizes as a racemate. The dihedral angle between the benzene and triazole rings is 24.96 (13)°. In the crystal structure, mol­ecules are linked into chains running parallel to the c axis by inter­molecular C—H⋯N hydrogen-bonding inter­actions

    Rottlerin Inhibits ROS Formation and Prevents NFκB Activation in MCF-7 and HT-29 Cells

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    Rottlerin, a polyphenol isolated from Mallotus Philippinensis, has been recently used as a selective inhibitor of PKC δ, although it can inhibit many kinases and has several biological effects. Among them, we recently found that Rottlerin inhibits the Nuclear Factor κB (NFκB), activated by either phorbol esters or H2O2. Because of the redox sensitivity of NFκB and on the basis of Rottlerin antioxidant property, we hypothesized that Rottlerin could prevent NFκB activation acting as a free radicals scavenger, as other natural polyphenols. The current study confirms the antioxidant property of Rottlerin against the 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) in vitro and against oxidative stress induced by H2O2 and by menadione in culture cells. We also demonstrate that Rottlerin prevents TNFα-dependent NFκB activation in MCF-7 cells and in HT-29 cells transfected with the NFκB-driven plasmid pBIIX-LUC, suggesting that Rottlerin can inhibit NFκB via several pathways and in several cell types

    Divergent effects of quinolinic aminoxyls on mitochondrial ultrastructure and localisation in osteosarcoma 143 B cells

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    In the present study we have shown that quinolinic aromatic aminoxyls are very efficient in protecting lipids of endoplasmic reticulum membranes against hydroperoxide- induced oxidation. The efficacy of these aminoxyls as protectors of lipids was much higher than the water-soluble 4-OH-TEMPO. We have also shown that QAL causes distinct changes of the morphology of mitochondria: from filamentous to granular enlarged structure via the folding of the former. QAL induces also perinuclear clustering of mitochondria. C-QAL as well as 4-OH-TEMPO treated cells revealed filamentous and scattered pattern of mitochondria. Antioxidant activity of QAL as well as morphological changes of mitochondrial raise the possibility that this drug can affect cell physiology via changes of mitochondrial function

    2,2-Diphenyl­benzo[c]quinoline-1-ox­yl

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    In the title compound, C25H18NO, a stable phenanthridinic nitroxide, the ring containing the nitroxide function assumes a twist-boat conformation and the dihedral angle formed by adjacent benzene rings is 21.78 (5)°. The phenyl substituents at position 2 are approximately orthogonal to each other, forming a dihedral angle of 81.04 (4)°. The crystal structure is stabilized by an intra­molecular C—H⋯O hydrogen bond and by C—H⋯π inter­actions

    Sunscreens Cause Coral Bleaching by Promoting Viral Infections

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    Background: Coral bleaching (i.e., the release of coral symbiotic zooxanthellae) has negative impacts on biodiversity and functioning of reef ecosystems and their production of goods and services. This increasing world-wide phenomenon is associated with temperature anomalies, high irradiance, pollution, and bacterial diseases. Recently, it has been demonstrated that personal can products, including sunscreens, have an impact on aquatic organisms similar to that of other contaminants. Objectives: Our goal was to evaluate the potential impact of sunscreen ingredients on hard corals and their symbiotic algae. Methods: In situ and laboratory experiments were conducted in several tropical regions (the Atlantic, Indian, and Pacific Oceans, and the Red Sea) by supplementing coral branches with aliquots of sunscreens and common ultraviolet filters contained in sunscreen formula. Zooxanthellae were checked for viral infection by epifluorescence and transmission electron microscopy analyses. Results: Sunscreens cause the rapid and complete bleaching of hard corals, even at extremely low concentrations. The effect of sunscreens is due to organic ultraviolet filters, which are able to induce the lyric viral cycle in symbiotic zooxanthellae with latent infections. Conclusions: We conclude that sunscreens, by promoting viral infection, potentially play an important role in coral bleaching in areas prone to high levels of recreational use by humans

    Modification of permeability transition pore arginine(s) by phenylglyoxal derivatives in isolated mitochondria and mammalian cells. Structure-function relationship of arginine ligands.

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    Methylglyoxal and synthetic glyoxal derivatives react covalently with arginine residue(s) on the mitochondrial permeability transition pore (PTP). In this study, we have investigated how the binding of a panel of synthetic phenylglyoxal derivatives influences the opening and closing of the PTP. Using both isolated mitochondria and mammalian cells, we demonstrate that the resulting arginine-phenylglyoxal adduct can lead to either suppression or induction of permeability transition, depending on the net charge and hydrogen bonding capacity of the adduct. We report that phenylglyoxal derivatives that possess a net negative charge and/or are capable of forming hydrogen bonds induced permeability transition. Derivatives that were overall electroneutral and cannot form hydrogen bonds suppressed permeability transition. When mammalian cells were incubated with low concentrations of negatively charged phenylglyoxal derivatives, the addition of oligomycin caused a depolarization of the mitochondrial membrane potential. This depolarization was completely blocked by cyclosporin A, a PTP opening inhibitor, indicating that the depolarization was due to PTP opening. Collectively, these findings highlight that the target arginine(s) is functionally linked with the opening/closing mechanism of the PTP and that the electric charge and hydrogen bonding of the resulting arginine adduct influences the conformation of the PTP. These results are consistent with a model where the target arginine plays a role as a voltage sensor

    3-Benzyl-3-hy­droxy-2-phenyl-3H-indole 1-oxide

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    The asymmetric unit of the title compound, C21H17NO2, contains two crystallographically independent mol­ecules of similar geometry. The indole ring systems form dihedral angles of 8.30 (5) and 9.58 (5)° with the attached phenyl rings, and 56.96 (5) and 57.68 (5)° with the aromatic rings of the respective benzyl groups. The mol­ecular conformations are stabilized by intra­molecular C—H⋯O hydrogen bonds. In the crystal structure, centrosymmetrically related pairs of mol­ecules are linked into dimers through pairs of inter­molecular O—H⋯O hydrogen bonds, generating 12-membered rings with R 2 2(12) motifs. The dimers are further linked into a three-dimensional network by C—H⋯O inter­actions
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