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151.
Structure-Photodynamic Activity Relationships of a Series of 4-Substituted Zinc Phthalocyanines 总被引:1,自引:0,他引:1
Philippe Margaron Marie-Josée Grégoire Vladimir asnár † Hasrat Ali Johan E. van Lier ‡ 《Photochemistry and photobiology》1996,63(2):217-223
Abstract— Radioiodinated zinc phthalocyanine including [125I]ZnPcI4 and differently sulfonated [65Zn]ZnPcS (ZnPcS4, ZnPcS3, ZnPcS2 and ZnPcS1.75, a mixture of adjacent di and 25% mono) were prepared in order to study cell uptake and release kinetics in EMT-6 cells. The same compounds were evaluated for their in vitro phototoxicity and the biological parameters were compared to partition coefficients to arrive at quantitative structure-activity relationships (QSAR). At 1 μM in 1% serum, at 37°C, all dyes showed rapid cell uptake during the first hour followed by a slow accumulation phase. After 24 h, the highest cellular concentration was observed with the lipophilic ZnPcI4, followed by the amphiphilic ZnPcS2 and ZnPcS1.75. The hydrophilic ZnPcS4 and ZnPcS3 showed lower uptake. Dye release from dyeloaded cells during incubation in dye-free medium could reach up to 60% and was shown to depend mainly on the amount of drug incorporated rather than the type of compound. These results suggest that care should be taken in interpreting dye toxicity data, which involve in vitro cell manipulations in dye-free medium, particularly during in vitro/in vivo protocols. The EMT-6 cell survival after 1 h or 24 h incubation with 1 μM dye in 1% serum followed by exposure to red light was assessed by means of the colorimetric 3-(4,5-dimethylthiazol-2-yl)-diphenyl-tetrazolium bromide (MTT) assay. Photocytotoxicities correlated inversely with the tendencies of the dyes to aggregate. Increased dye uptake by the cells also correlated with their activities, except for the lipophilic ZnPcI4, which showed the highest cell uptake but little phototoxicity. The QSAR between phototoxicity and the log of the partition coefficients (phosphate-buffered saline and n-octanol) gave a parabola with optimal partition values corresponding to the adjacent sulfonated ZnPcS2. 相似文献
152.
Janine Cossy Haja Rakotoarisoa Philippe Kahn Jean-Roger Desmurs 《Tetrahedron letters》1998,39(52):3240-9674
The synthesis of functionalized 2,2-disubstituted 2H-1-benzopyrans was achieved by condensing 2,3,5-trimethylhydroquinone (TMHQ) with ,β-unsaturated aldehydes or ,β-unsaturated acetals under acidic conditions. 相似文献
153.
Benjamin Ruiz Philippe Sistat Patrice Huguet Gérald Pourcelly Monica Araya-Farias Laurent Bazinet 《Journal of membrane science》2007
Electrodialysis (ED) is a membrane process used on a large scale. However, one of the common problems is fouling of ion-exchange membranes stacked in the cell. The use of pulsed power, consisting in applying a constant current density during a fixed time of application (Ton) followed by a pause duration (Toff), was demonstrated recently as an effective fouling mitigation method for electrodialysis. Up until now, no work has investigated the potential of electrodialysis using pulsed electric field on protein fouling. The aim of the present work was to study the influence of pulsed electric field (PEF) with a low frequency square shaped periodic signal (Ton = 10 s–Toff = 10 s, Ton = 10 s–Toff = 40 s) in comparison with dc current during electrodialysis of a casein solution at different current densities (10, 20 and 30 mA/cm2) on membrane fouling. It appeared from these results that PEF, under certain conditions of pulse, would avoid fouling on anion-exchange membranes. For 10 s–40 s pulsed electric field conditions, no fouling was observed with any density, while for 10 s–10 s PEF conditions, fouling appeared only at current density over 10 mA/cm2. dc current, whatever the current density conditions, led to a fouling on the diluate side of the AEM. Furthermore, when fouling occurred, magnitude layer thickness and dry weight increased with the applied current density. The nature of the fouling was identified as 97% protein. The protein fouling would be due to the dissociation of water molecules and/or heat increase at the anion-exchange membrane interface. The relaxation time of the pulse would limit both phenomena on the membrane. 相似文献
154.
Nicolas P. Cheval Barbara Hoffmann Anna Dikova Fatih Sirindil Philippe Bertus Aurélien Blanc Jean-Marc Weibel Patrick Pale 《Tetrahedron》2018,74(50):7111-7119
Vinyl nosylates, readily obtained from β-dicarbonyl derivatives, could be efficiently engaged in Sonogashira cross-coupling reactions, either cocatalyzed by copper or silver salts. The para-nitrobenzenesulfonate (nosylate) group allows this coupling to be performed under very mild conditions (room temperature). These new leaving group and mild conditions could be applied to the synthesis of acetylenic coumarinyl derivatives and to the total synthesis of an acetylenic monoterpene natural product, named cleviolide. 相似文献
155.
156.
Philippe Rukimbira 《Journal of Geometry》2016,107(1):125-135
On a Riemannian manifold, any parallel form is preserved by the flow of any Killing vector field with constant magnitude. As a consequence, on a 2n+1-dimensional K-contact manifold, there are no nontrivial parallel forms except of degrees 0 and 2n+1. Flat contact metrics on 3-manifolds are characterized by reducible holonomy. 相似文献
157.
Dolorès Edmont Yvon Buisson Philippe Treillard Christophe Plisson Jacques Chenault 《合成通讯》2013,43(2):217-225
A high yielding N-amination of quinolones at low temperature via the use of O-mesitylenesulfonylhydroxylamine is reported. 相似文献
158.
Anne-Catherine Huet Monique Bienenmann-Ploum Ursula Vincent Philippe Delahaut 《Analytical and bioanalytical chemistry》2013,405(24):7733-7751
This article presents a review of the current trends in the analysis of coccidiostats in various matrices, focusing principally on screening and rapid methods. Coccidiosis is an infectious disease having a high negative impact on the animal industry. Drugs are therefore necessary to prevent and/or to combat this disease. However, it is also of crucial importance that these veterinary drugs do not enter the human food chain. European legislation has therefore established the boundaries for the use of coccidiosats and has also addressed the unavoidable problem of cross-contamination of the feed, mainly caused by the use of the same production lines. Consequently there is a need for analytical methods and/or analytical strategies for the monitoring and control of the residues of anticoccidials, both in feed and in the resulting matrices for human consumption. In the frame of the European collaborative project CONffIDENCE, such attempts to establish the required analytical tools were made, which required beforehand a review of the state of the art in this domain. Aiming at this objective, in this review we consider the most interesting publications since 2000. In essence, both a rapid approach with mainly immunoassays and chromatographic methods were developed. To date, the obstacle to routine use of the first approach has been its inability to detect more than two compounds simultaneously, but recent developments in flow cytometry have made it possible to detect six coccidiostats at once. On the other hand, an increasingly popular approach for detecting multiple coccidiostats simultaneously is liquid chromatography coupled with tandem mass spectrometry. There remains a need to adapt these analytical methods to legislative requirements. 相似文献
159.
Maxime Guitet Pinglu Zhang Filipa Marcelo Coralie Tugny Jesús Jimnez‐Barbero Olivier Buriez Christian Amatore Virginie Mouris‐Mansuy Jean‐Philippe Goddard Louis Fensterbank Yongmin Zhang Sylvain Roland Mickaël Mnand Matthieu Sollogoub 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2013,125(28):7354-7359
160.
Sabine Beernaerts Marie Gerard Philippe Debongnie Jean-Paul Barthelemy Luc Pussemier Alfred Copin 《International journal of environmental analytical chemistry》2013,93(6):469-480
A monitoring study was carried out in 1998-1999 on a medium-sized (c. 4580 km2) watershed of the Dyle (or Dijle) river in central Belgium, composed of both rural and urbanized areas. This watershed may be considered as representative of a large part of the country. Samples were taken each month from seven sites along the course of the river, plus one from its major affluent the Demer. The eight molecules monitored were the main herbicides used on the major crops in the area, plus some used in nonagricultural sectors. The concentrations found were mostly in the 0-3 μg/L range, with some peaks between 3 and 14 μg/L. The averages over all spring and summer samples analyzed ranged from 0.14 (bentazone) to 1.54 μg/L (diuron). Time and space specific patterns could be observed. 相似文献