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04 décembre 19311931/12/04 (A60).Appartient à l’ensemble documentaire : PoitouCh

Media 1: Real-time image edge enhancement with a spiral phase filter and graphic processing unit

Originally published in Applied Optics on 01 July 2014 (ao-53-19-4297

Drug Molecule Diflunisal Forms Crystalline Inclusion Complexes with Multiple Types of Linear Polymers

Co-crystals between drug molecules and coformers have shown great potential to optimize the stability and dissolution profiles of drugs. However, most of the coformers studied so far are small molecules. Here, we use diflunisal (DIF) as the model drug, and show that it could form co-crystals with multiple types of linear polymers in the form of crystalline inclusion complexes (ICs). These drug-polymer ICs were thoroughly characterized with single-crystal and powder XRD, solid-state NMR, DSC, and TGA, and showed similar channel structures, but their thermal properties changed with the type and molecular weight (MW) of the guest polymers. In addition, a strategy is proposed to identify the drug candidates with the potential to form ICs with polymers, which may help to expand the range of drug-polymer co-crystals

Suppressed renal peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α) expression and activation after liver transplantation.

<p>Transplantation was performed as described in “Methods” and kidneys were collected 18 h after sham-operation (<b>Sham</b>) or liver transplantation (<b>LTX</b>). <b>A</b>, representative immunoblot images of PGC-1α; <b>B</b>, quantification of immunoblot images of PGC-1α by densitometry; <b>C</b>, PGC-1α mRNA detected by qPCR; <b>D</b>, representative immunoblot images of acetylated lysine residues (Ac-Lys) of immunoprecipitated (IP) PGC-1α; <b>E</b>, quantification of immunoblot images of Ac-Lys. Values are mean ± SEM. **p<0.01 vs sham (n = 3-4/group).</p

Increased renal mitophagy after liver transplantation.

<p>Transplantation was performed as described in “Methods” and kidneys were collected 18 h after sham-operation (<b>Sham</b>) or liver transplantation (<b>LTX</b>). <b>A</b>, representative immunoblot images of PTEN-induced putative kinase 1 (PINK-1) and microtubule-associated protein 1A/1B-light chain 3 (LC3); <b>B</b>, quantification of immunoblot images of PINK-1 by densitometry; <b>C</b>, quantification of immunoblot images of LC3 by densitometry. Values are mean ± SEM. **p<0.01 vs sham (n = 3-4/group).</p

Inhibited renal mitochondrial transcription factor A (Tfam) expression and decreased renal mitochondrial DNA (mtDNA) after liver transplantation.

<p>Transplantation was performed as described in “Methods” and kidneys were collected 18 h after sham-operation (<b>Sham</b>) or liver transplantation (<b>LTX</b>). <b>A</b>, representative immunoblot images of Tfam; <b>B</b>, quantification of immunoblot images of Tfam by densitometry; <b>C</b>, Tfam mRNA detected by qPCR; <b>D</b>, relative mitochondrial DNA copy number detected by qPCR. Values are mean ± SEM. **p<0.01 vs sham (n = 3-4/group).</p

Design, synthesis and biological evaluation of 3-fluoroalkenyloxindole ring-fused 3-trifluoromethyloxindoles obtained from indoline-2,3-diones and difluoromethylene phosphabetaine

<p></p> <p>A wide variety of multi-substituted 3-fluoroalkenyloxindole ring-fused 3-trifluoromethyloxindoles were obtained in good yields by the reaction of indoline-2,3-diones with difluoromethylene phosphabetaine. Their biological activities against human prostate cancer cells <b>PC-3</b> and human Breast cancer cells <b>MCF-7</b> have been preliminarily demonstrated, using MTT-based assays with the commercially available standard drug Paclitaxel as a positive control. Several compounds exhibited comparable <i>in vitro</i> inhibitory activities against human prostate cancer cells <b>PC-3</b> and human Breast cancer cells <b>MCF-7</b> to Paclitaxel. These results indicate that 3-fluoroalkenyloxindole ring-fused 3-trifluoromethyloxindoles may be potential lead compounds for further biological screening.</p

Combined ethanol and cholesterol feeding increases hepatic triglycerides and cholesterol but suppressed fatty acid synthase and carnitine palmitoyltransferase-1 expression.

<p>Mice were fed CTR, Chol, EtOH and EtOH+Chol diets for 3 months. Triglycerides (<b>A</b>) and cholesterol (<b>B</b>) in liver extracts were measured using commercial kits. FAS and Cpt1 were detected by immunoblotting (<b>C</b>, representative images). <b>D</b>, quantification of FAS immunoblots by densitometry. <b>E</b>, quantification of Cpt1 immunoblots. Values are means ± S.E.M. <b>a</b>, p < 0.05 vs CTR; <b>b</b>, p < 0.05 vs Chol; <b>c</b>, p < 0.05 vs EtOH (n = 3–4 per group).</p

Suppressed renal function after liver transplantation.

<p>Transplantation was performed as described in “Methods” and blood was collected 18 h after sham-operation (<b>Sham</b>) or liver transplantation (<b>LTX</b>). <b>A</b>: serum creatinine; <b>B</b>: blood urea nitrogen (BUN). Values are mean ± SEM. **p<0.01 vs sham (n = 4/group).</p

Renal injury after liver transplantation.

<p>Transplantation was performed as described in “Methods” and kidneys were collected 18 h after sham-operation (<b>Sham</b>) or liver transplantation (<b>LTX</b>). <b>A</b>, H&E-stained slides; black arrow, necrotic tubules; black double arrow head, loss of brush border; white arrow, hyaline cast formation; white double arrow head, infiltrated leukocytes and other cell debris in tubular lumen. <b>B</b>, representative immunoblot images of neutrophil gelatinase-associated lipocalin (NGAL) and cleaved caspase-3 (CC3); <b>C</b>, quantification of immunoblot images of NGAL by densitometry; <b>D</b>, quantification of immunoblot images of CC3 by densitometry. Values are mean ± SEM. **p<0.01 vs sham (n = 3-4/group).</p