Caracterización de aceite de semilla de girasol extraído enzimáticamente así como de los residuos proteínicos

Sunflower seed oil was enzymatically extracted with six different enzymes: cellulase, hemicellulase, animal proteinase, acid proteinase, pectinase and pectinex under the following conditions: substrate concentration in phosphate buffer (0.5M, pH 5) 30%, enzyme concentration 2% (E/S), temperature 50°C and time 3 hours. The obtained oils were analyzed for physicochemical properties and fatty acid profiles. The protein residues were analyzed for amino acid compositions. The results showed that the enzymatic extraction with cellulase or hemicellulase could maintain good oil quality of the extracted oils as their levels of linoleic and oleic acids recorded similar values to those of the control oil extracted with organic solvents. Also the level of iodine value was in the same level of control. On the other hand, the use of proteases in the enzymatic extraction of sunflower seed oil caused some reductions in the levels of the unsaturated fatty acids as well as the iodine value. The pectinases showed a similar trend to that of the proteinase with the least recovery of linoleic acid among the different oils under study. Similarly, the use of cellulases did not change the amino acid composition of the protein residue as compared to the control, in the contrary to the extraction with the proteinases which caused reduction of some amino acids from the protein residues especially lysine, leucine, iso-leucine, alanine, arginine and aspartic. In that respect the use of pectinases behaved similar to cellulases.Aceite de semilla de girasol fue extraído enzimáticamente con seis enzimas diferentes: celulasa, hemicelulasa, proteinasa animal, proteinase acida, pectinasa y pectinex bajo las condiciones siguientes: concentración de sustrato en tampón fosfato (0,5M, pH 5) 30%, concentración enzimática 2% (E/S), temperatura 50°C y tiempo 3 horas. Los aceites obtenidos fueron analizados por sus propiedades fisicoquímicas y perfiles de ácidos grasos. Los residuos proteínicos fueron analizados por sus composiciones en aminoácidos. Los resultados mostraron que la extracción enzimática con celulasa o hemicelulasa podían proporcionar buena calidad en los aceites, ya que sus niveles de ácidos linoleico y oleico registraron valores similares a los del aceite control extraído con disolventes orgánicos. También el valor de índice de iodo fue similar al del control. Por otro lado, el uso de proteasas en la extracción enzimática de aceite de semilla de girasol causó algunas reducciones en los niveles de ácidos grasos insaturados, así como en el índice de iodo. Las pectinasas mostraron una tendencia similar a la de las proteinases con la menor obtención de ácido linoleico entre los diferentes aceites en estudio. Del mismo modo, el uso de celulasas no cambió la composición de aminoácidos del residuo proteínico comparado con el control, por el contrario la extracción con proteinasas causó una disminución de algunos aminoácidos, especialmente lisina, leucina, isoleucina, alanina, arginina y aspártico. A este respecto, el uso de pectinasa se portó de manera análoga al de celulasas

Physiol Rep

Obliterative bronchiolitis is the principal long-term problem for lung transplant patients. One of the simplest and most reproducible animal models of obliterative bronchiolitis is heterotopic tracheal transplantation in subcutaneous tissue, where the graft is not primarily vascularized. We demonstrate here the rapid graft revascularization and the kinetics of expression of its angiogenic and lymphatic factors. We performed iso- and allotracheal transplantations harvested on day 0-21. The number of functional blood vessels, quantified after intravenous biotinylated dextran administration, increased from D0 (0 for both iso- and allografts) to D21 (44 +/- 8 vessels/mm(2) in isografts and 22 +/- 3 in allografts, P < 0.001 for both vs. D0). VEGF mRNA expression assessed by qPCR peaked on D1 (4.3-fold increase in isografts and 4.0-fold in allografts, P < 0.0001 for both vs. D0), but receded thereafter. Angiopoietin-1, involved in the maturation of the neoformed vessels, increased later on, by 6.2-fold (P < 0.05) in isografts and 11.5-fold in allografts (P < 0.001) by D21, and angiopoietin-2 by 7.8-fold in isografts (P < 0.05) and 13.8-fold in allografts (P < 0.01). Although always present in the iso- and allografts, there were significantly more and larger LYVE1(+) lymphatic vessels at D21 in allografts than in isografts. Thus, we demonstrate that tracheal grafts are rapidly revascularized by functional blood and lymphatic vessels, due to early VEGF and subsequent angiopoietins expression, which is a new advantage of this model, in addition to its ease of use, reproducibility, and viability in the absence of immunosuppressive treatment

An optimized derivative of an endogenous CXCR4 antagonist prevents atopic dermatitis and airway inflammation

Aberrant CXCR4/CXCL12 signaling is involved in many pathophysiological processes such as cancer and inflammatory diseases. A natural fragment of serum albumin, named EPI-X4, has previously been identified as endogenous peptide antagonist and inverse agonist of CXCR4 and is a promising compound for the development of improved analogues for the therapy of CXCR4-associated diseases. To generate optimized EPI-X4 derivatives we here performed molecular docking analysis to identify key interaction motifs of EPI-X4/CXCR4. Subsequent rational drug design allowed to increase the anti-CXCR4 activity of EPI-X4. The EPI-X4 derivative JM#21 bound CXCR4 and suppressed CXCR4-tropic HIV-1 infection more efficiently than the clinically approved small molecule CXCR4 antagonist AMD3100. EPI-X4 JM#21 did not exert toxic effects in zebrafish embryos and suppressed allergen-induced infiltration of eosinophils and other immune cells into the airways of animals in an asthma mouse model. Moreover, topical administration of the optimized EPI-X4 derivative efficiently prevented inflammation of the skin in a mouse model of atopic dermatitis. Thus, rationally designed EPI-X4 JM#21 is a novel potent antagonist of CXCR4 and the first CXCR4 inhibitor with therapeutic efficacy in atopic dermatitis. Further clinical development of this new class of CXCR4 antagonists for the therapy of atopic dermatitis, asthma and other CXCR4-associated diseases is highly warranted

Author response: Myopalladin knockout mice develop cardiac dilation and show a maladaptive response to mechanical pressure overload

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Design, Synthesis and Biological Evaluation of Arylpyridin-2-yl Guanidine Derivatives and Cyclic Mimetics as Novel MSK1 Inhibitors. An Application in an Asthma Model

Mitogen‐ and Stress‐Activated Kinase 1 (MSK1) is a nuclear kinase, taking part in the activation pathway of the pro‐inflammatory transcription factor NF‐kB and is demonstrating a therapeutic target potential in inflammatory diseases such as asthma, psoriasis and atherosclerosis. To date, few MSK1 inhibitors were reported. In order to identify new MSK1 inhibitors, a screening of a library of low molecular weight compounds was performed, and the results highlighted the 6phenylpyridin‐2‐yl guanidine (compound 1a, IC50~18 μM) as a starting hit for structure‐activity relationship study. Derivatives, homologues and rigid mimetics of 1a were designed, and all synthesized compounds were evaluated for their inhibitory activity towards MSK1. Among them, the noncytotoxic 2‐aminobenzimidazole 49d was the most potent at inhibiting significantly: (i) MSK1 activity, (ii) the release of IL‐6 in inflammatory conditions in vitro (IC50~2 μM) and (iii) the inflammatory cell recruitment to the airways in a mouse model of asthma