Laboratoire Of Biophotonique Et Pharmacologie

Illkirch-Graffenstaden, France

Laboratoire Of Biophotonique Et Pharmacologie

Illkirch-Graffenstaden, France
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Hallouard F.,University of Strasbourg | Hallouard F.,French National Center for Scientific Research | Anton N.,University of Strasbourg | Anton N.,French National Center for Scientific Research | And 14 more authors.
RSC Advances | Year: 2011

The context of the this research is the development of nanoparticulate systems exhibiting long circulation times in the blood pool, loaded with X-ray contrasting compounds, to be used as blood pool contrast agents in computed tomography. This study presents an original, new and simple formulation of radiopaque nano-emulsions composed of iodinated oil, formed by a spontaneous emulsification method. As a result, extremely monodisperse, iodinated nano-droplets were generated, ranging in size from 20 to 190 nm, presenting an iodine concentration of around 85 mg I/mL, and coated with a polyethylene glycol shell which ensured their stealth properties against the immune system in the blood stream. In vivo assays demonstrated a significant contrast effect, along with a long residence in the blood pool. This study highlights novel nano-formulations used as efficient contrast agents for preclinical X-ray imaging applications, along with simple and efficient alternatives for the generation of iodinated nano-emulsions. This journal is © The Royal Society of Chemistry 2011.

Rochel N.,Institute Of Genetique Et Of Biologie Moleculaire Et Cellulaire | Rochel N.,Institute National Of Sante Et Of Recherche Medicale U964 | Rochel N.,French National Center for Scientific Research | Rochel N.,University of Strasbourg | And 27 more authors.
Nature Structural and Molecular Biology | Year: 2011

Nuclear hormone receptors (NHRs) control numerous physiological processes through the regulation of gene expression. The present study provides a structural basis for understanding the role of DNA in the spatial organization of NHR heterodimers in complexes with coactivators such as Med1 and SRC-1. We have used SAXS, SANS and FRET to determine the solution structures of three heterodimer NHR complexes (RXR-RAR, PPAR-RXR and RXR-VDR) coupled with the NHR interacting domains of coactivators bound to their cognate direct repeat elements. The structures show an extended asymmetric shape and point to the important role played by the hinge domains in establishing and maintaining the integrity of the structures. The results reveal two additional features: the conserved position of the ligand-binding domains at the 5-2 ends of the target DNAs and the binding of only one coactivator molecule per heterodimer, to RXR's partner. © 2011 Nature America, Inc. All rights reserved.

Donato L.,CNRS Laboratory of Design and Application of Bioactive Molecules | Mourot A.,University of California at Berkeley | Davenport C.M.,University of California at Berkeley | Herbivo C.,CNRS Laboratory of Design and Application of Bioactive Molecules | And 7 more authors.
Angewandte Chemie - International Edition | Year: 2012

Rattling the cage: The two γ-aminobutyric acid (GABA) derivatives 1 and 2 exhibit efficient and rapid (<5à- 10 -6 s) GABA photorelease upon one-photon excitation combined with two-photon uncaging cross-section at λ=800 nm. Compounds 1 and 2 were successfully used for two-photon GABA release in intact brain tissue, thus offering attractive perspectives in chemical neurosciences. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Contal E.,CNRS Laboratory of Design and Application of Bioactive Molecules | Klymchenko A.S.,Laboratoire Of Biophotonique Et Pharmacologie | Mely Y.,Laboratoire Of Biophotonique Et Pharmacologie | Meunier S.,CNRS Laboratory of Design and Application of Bioactive Molecules | Wagner A.,CNRS Laboratory of Design and Application of Bioactive Molecules
Soft Matter | Year: 2011

Diacetylene amphiphile bearing terminal alkyne moiety form micelles which can be further photopolymerized. Herein we address the covalent grafting of a fluorescent label within the micelles by a "click" reaction. Fluorescence experiments revealed that micelles act for the label as a protective shield from the bulk water. © 2011 The Royal Society of Chemistry.

Specht A.,CNRS Laboratory of Design and Application of Bioactive Molecules | Bolze F.,Laboratoire Of Biophotonique Et Pharmacologie | Donato L.,CNRS Laboratory of Design and Application of Bioactive Molecules | Herbivo C.,CNRS Laboratory of Design and Application of Bioactive Molecules | And 6 more authors.
Photochemical and Photobiological Sciences | Year: 2012

Different photoremovable protecting groups in the o-nitrobenzyl, phenacyl, and 2-(o-nitrophenyl)propyl series with a donor-acceptor biphenyl backbone, known to display excellent two-photon absorption cross-sections, were investigated in order to develop efficient two-photon sensitive photoremovable protecting groups. The 2-(o-nitrophenyl)propyl series was a more versatile platform to increase the two-photon sensitivity of photoremovable protecting groups, leading to the p-alkoxy and p-bisalkylamino-4-nitro-[1,1′- biphenyl]-3-yl)propyl derivatives: PENB and EANBP respectively. Those two photoremovable protecting groups are to date the best caging groups for two-photon excitation at 800 and 740 nm respectively, offering attracting perspectives in chemical biology. © 2012 The Royal Society of Chemistry and Owner Societies.

Ouedraogo S.,Institute Of Recherche En Science Of La Sante Irss Cnrst | Some N.,Institute Of Recherche En Science Of La Sante Irss Cnrst | Ouattara S.,University of Ouagadougou | Kini F.B.,Institute Of Recherche En Science Of La Sante Irss Cnrst | And 4 more authors.
African Journal of Traditional, Complementary and Alternative Medicines | Year: 2012

The authors report here the results of study on Parkia biglobosa seeds used in Burkina Faso for arterial hypertension treatment. Investigations were done on acute toxicity and vascular properties of fermented and roasted seeds. Acute toxicity test using mice, revealed by the intraperitoneal route a lethal dose 50 (LD50) of 1800 mg/kg and 1600 mg/kg of body weight for aqueous extract from roasted and fermented seeds respectively. According to the scale of Hodge and Sterner and that of the World Health Organization, such drugs would be classified lightly toxic. Oral administration (up to 3000 mg/kg) did not induce any death of animal. For the vascular properties, the effects of these products were tested on the aorta isolated from rats. The cumulative administration of extract from roasted and fermented seeds (0.1-10 mg/mL) in an organ bath induced a concentration-dependent relaxation of the aorta pre contracted by phenylephrine, with or without functional endothelium. The extracts (10 mg/mL) inhibited for 100% the contraction induced by phenylephrine. The EC50 values in presence and absence of endothelium were respectively of 5.37 ± 0.12 and 4.19 ± 1.02 mg/mL for fermented seeds; for roasted seeds these values were respectively, 5.39 ± 1.12 and 5.93 ± 0.95 mg/mL. Nevertheless, low concentration of roasted seeds (1-4 mg/mL) induced endothelium-dependent relaxation and this effect was inhibited by indomethacin (10-5M), and not by L-NAME (310-4M). These experimental results revealed a vasorelaxant effect of P. biglobosa seeds. P. biglobosa seems to act directly on the smooth muscle and via endothelium involving the generation of vasodilatating prostaglandins. This vasodilator effect would be in favor of an anti hypertensive property of P. biglobosa seeds.

Ihm S.-H.,Catholic University of Korea | Jang S.-W.,Catholic University of Korea | Kim O.-R.,Catholic University of Korea | Chang K.,Catholic University of Korea | And 4 more authors.
Atherosclerosis | Year: 2012

Background: Oxidative stress and endothelial dysfunction are closely associated with hypertension and insulin resistance (IR) in metabolic syndrome (MetS). It is still controversial whether green tea extract (GTE) may have blood pressure (BP) lowering effect. Decaffeinated GTE might be presumed to have strong antioxidative effect and BP-lowering effect as compared with catechins. Thus we investigated whether decaffeinated-GTE could attenuate hypertension and IR by improving endothelial dysfunction and reducing oxidative stress in a rat model of MetS. Methods and Results: 20 Otsuka Long-Evans Tokushima Fatty (OLETF) rats at 13 weeks old, MetS rats, were randomized into a saline treated group (OLETF; n = 10) and a group treated with decaffeinated-GTE (25 mg/kg/day) (GTE-OLETF; n = 10). Intraperitoneal glucose tolerance tests and BP measurements were performed at 13 and 25 weeks. Decaffeinated-GTE significantly reduced BP (OLETF vs. GTE-OLETF; 130 ± 7 vs. 121 ± 3 mmHg, p = 0.01), fasting/postprandial 2 h glucose (141 ± 18/159 ± 13 vs. 115 ± 7/132 ± 16 mg/dL, p = 0.009/0.002) and insulin levels (4.8 ± 2.3 vs. 2.4 ± 1.3 ng/mL, p < 0.001). Decaffeinated-GTE significantly reduced vascular reactive oxygen species (ROS) formation and NADPH oxidase activity, and improved endothelium dependent relaxation in the thoracic aorta of OLETF rats. Decaffeinated-GTE also suppressed the expression of p47 and p22phox (NADPH oxidase subunits) in the immunohistochemical staining, and stimulated phosphorylation of endothelial nitric oxide synthase (eNOS) and Akt in the immunoblotting of aortas. Conclusions: Decaffeinated-GTE reduced the formation of ROS and NADPH oxidase activity and stimulated phosphorylation of eNOS and Akt in the aorta of a rat model of MetS, which resulted in improved endothelial dysfunction and IR, and eventually lowered BP. © 2012.

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