The antiparasitic effect of the norditerpenoid yaretol on Trypanosoma cruzi

Chagas disease is caused by the intracellular parasite Trypanosoma cruzi. Approximately seven million people are infected worldwide, and more of 10,000 deaths occur annually. Due to the increase in migration from Latin America to the rest of the world, mainly the United States and Europe, Chagas disease has emerged in countries where it was unknown. The effect on the proliferation and viability of T. cruzi epimastigotes of the eight terpenes, AZ1: azorellolide, AZ2: mulinol, AZ3: stachytriol, AZ4:1α,10β,4β,5α-diepoxy-7β-germacran-6β-ol, AZ5:1β,10α,4β,5α-diepoxy-7β-germacran-6β- ol, AZ6: 1,2,3,3α,4,5,6,7,8,8α-decahydro-7-(1-hydroxy-1-methylethyl)-1,4- dimethylazulene-3α,8α-diol, AZ7: madreporanone, and AZ8: yaretol, previously isolated of the aerial parts from Azorella cryptantha were tested. The norditerpenoid yaretol inhibited epimastigotes proliferation, the IC50 value was 6.38 ± 0.47 μM, more effective than benznidazole (9.6 μM) and less cytotoxic in Vero cell line (8.87 μM) at 48 hs incubation. Studies to evaluate the effect of yaretol on other forms of the parasite are currently being performed

Convective drying of yellow discarded onion (Angaco INTA): Modelling of moisture loss kinetics and effect on phenolic compounds

The Angaco INTA onion variety is the most cultivated and its production, mostly is destined for export. Due to their high-quality standards of these markets, many onions are discarded. The drying process seems to be a promising solution that not only give added value to this product, but also extend shelf life. In this work, the influence of convective drying process, at 60 and 70 °C, on the kinetic behavior, antioxidant activity, phenolic and flavonoid contents of discarded onion slices were investigated. Considering that, the Angaco INTA onion is a variety genetically developed to have shorter cultivation times in this region; the phenolic compounds content in this onion variety, the drying kinetics and its influence on this content have never been studied. In this study, the phenolic compounds contributions to dehydrated product quality was evaluated, observing that the convective drying increased the total soluble phenolic and flavonoid contents and antioxidant properties for both temperatures, being highest at 70 °C. The rehydration ratios were similar to the slices dried at 60 and 70 °C. Several models were used for describing the obtained drying curve equation of onion slices, being the Midilli’s model the one that presented the best fit. Ficks’s model of water diffusion fitted all experimental data with acceptable correlation coefficients. Considering the achieved findings, 70 °C is the optimum temperature to produce the dehydrated Angaco INTA onion.Fil: Roman, María Celia. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Ingeniería Química; ArgentinaFil: Fabani, Maria Paula. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Luna, Lorena Celina. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Ingeniería Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Feresin, Gabriela Egly. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Mazza, German Delfor. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Patagonia Norte. Instituto de Investigación y Desarrollo en Ingeniería de Procesos, Biotecnología y Energías Alternativas. Universidad Nacional del Comahue. Instituto de Investigación y Desarrollo en Ingeniería de Procesos, Biotecnología y Energías Alternativas; ArgentinaFil: Rodriguez, Rosa. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Ingeniería Química; Argentin

Design and Development of Soap Herbal Tablet of Larrea divaricata (Cav.) with Antifungal Activity Against Candida albicans

In this present work soap herbal tablet of Larrea divaricata Cav. ethanolic extract (LdE) with antifungal activity against Candida albicans, was designed and developed. The chemical profile of main compounds and quantification of nordihydroguaiaretic acid (NDGA) in the LdE was performed by means of UPLC-MS/MS. Two formulations (F1 and F2) were prepared by direct compression with different concentrations of active herbal ingredient (AHI). The performance of three carriers for impregnating LdE was evaluated. TRI-CAFOS® 500 was selected as carrier after a comparative study by Scanning Electron Microscope with AEROSIL® 200 and AEROPERL® 300. StarLac® 90, a coprocessed lactose, was employed as binder. The soap herbal tablets quality parameters were evaluated in accordance with United States Pharmacopeia (USP-43) guidelines, weight variation, hardness, friability, disintegration test, foam stability test and microbiological assay against candida albicans were performed. The F1 (LdE + TRI-CAFOS®500 (LdET1) 62.8%, StarLac®90 0.1%, Microcrystalline cellulose 10%, vitamin E 0.1%, Betan F® 5%, Lactic acid 5%, Rose essence 0.1%, Low density Hyaluronic acid 1.5% and magnesium stearate 0.5%) showed optimal rheological properties, good biopharmaceutical parameters (Disintegration test (27.33s), Hardness (3.00Kp), Friability (0.92%), Foam stability (1.12)) and Minimum inhibitory concentration (MIC) 25 mg/ml for Candida albicans. Considering that there are no soap herbal tablets on the market, the present design can be used as a novel herbal cosmetic form of vaginal hygiene.Fil: Jofre, Maria de Los Angeles. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; ArgentinaFil: Favier, Laura Silvina. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; ArgentinaFil: Cianchino, Valeria Andrea. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; ArgentinaFil: Divizia, Maria Julia. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Ortiz, Javier Esteban. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Juan; Argentina. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; ArgentinaFil: Feresin, Gabriela Egly. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Juan; ArgentinaFil: Ortega, Claudia Alicia. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia; Argentin

Synthesis, biological evaluation and molecular modeling studies of substitutedN-benzyl-2-phenylethanamines as cholinesterase inhibitors

In this work, we report the synthesis of a series of derivatives of N-benzyl-2-phenylethanamine which is the framework of norbelladine, the natural common precursor of the Amaryllidaceae alkaloids. These compounds were assessed in the inhibition of both AChE and BChE which are the enzymes responsible for the breakdown of acetylcholine and hence they constitute targets in the palliative treatment of Alzheimer's disease. In particular, brominated derivatives exhibited the lowest IC50 values against AChE. Interestingly, the presence of iodine in one of the aromatic rings highly increased the inhibition of BChE compared to its analogues, with an IC50 value similar to that of galantamine, which is the reference compound currently used in the treatment of AD. A possible mechanism of action for these compounds was determined by molecular modeling studies using combined techniques of docking and molecular dynamics simulations.Fil: Carmona Viglianco, Maria Florencia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Investigaciones en Tecnología Química. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia. Instituto de Investigaciones en Tecnología Química; ArgentinaFil: Zaragoza Puchol, José Daniel. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Juan; ArgentinaFil: Parravicini, Oscar. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis; ArgentinaFil: Garro, Adriana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis; ArgentinaFil: Enriz, Ricardo Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis; ArgentinaFil: Feresin, Gabriela Egly. Universidad Nacional de San Juan. Facultad de Ingeniería. Instituto de Biotecnología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Juan; ArgentinaFil: Kurina Sanz, Marcela Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Investigaciones en Tecnología Química. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia. Instituto de Investigaciones en Tecnología Química; ArgentinaFil: Orden, Alejandro Agustin. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Investigaciones en Tecnología Química. Universidad Nacional de San Luis. Facultad de Química, Bioquímica y Farmacia. Instituto de Investigaciones en Tecnología Química; Argentin

New short cationic antibacterial peptides. Synthesis, biological activity and mechanism of action

We report a theoretical and experimental study on a new series of small-sized antibacterial peptides. Synthesis and bioassays for these peptides are reported here. In addition, we evaluated different physicochemical parameters that modulate antimicrobial activity (charge, secondary structure, amphipathicity, hydrophobicity and polarity). We also performed molecular dynamic simulations to assess the interaction between these peptides and their molecular target (the membrane). Biophysical characterization of the peptides was carried out with different techniques, such as circular dichroism (CD), linear dichroism (LD), infrared spectroscopy (IR), dynamic light scattering (DLS), fluorescence spectroscopy and TEM studies using model systems (liposomes) for mammalian and bacterial membranes. The results of this study allow us to draw important conclusions on three different aspects. Theoretical and experimental results indicate that small-sized peptides have a particular mechanism of action that is different to that of large peptides. These results provide additional support for a previously proposed four-step mechanism of action. The possible pharmacophoric requirement for these small-sized peptides is discussed. Furthermore, our results indicate that a net +4 charge is the adequate for 9 amino acid long peptides to produce antibacterial activity. The information reported here is very important for designing new antibacterial peptides with these structural characteristics.Fil: Lima, Beatriz Viviana. Universidad Nacional de San Juan; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Juan; ArgentinaFil: Ricci, Maria. Természettudományi Kutatóközpont; HungríaFil: Garro, Adriana. Universidad Nacional de San Luis; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis; ArgentinaFil: Juhász, Tünde. Természettudományi Kutatóközpont; HungríaFil: Szigyártó, Imola Csilla. Természettudományi Kutatóközpont; HungríaFil: Papp, Zita I.. Szegedi Tudományegyetem; HungríaFil: Feresin, Gabriela Egly. Universidad Nacional de San Juan; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Juan; ArgentinaFil: Garcia de la Torre, Jose. Universidad de Murcia; EspañaFil: Lopez Cascales, Jose Javier. Universidad Politécnica de Cartagena; EspañaFil: Fülöp, Lívia. Szegedi Tudományegyetem; HungríaFil: Beke-Somfai, Tamás. Természettudományi Kutatóközpont; HungríaFil: Enriz, Ricardo Daniel. Universidad Nacional de San Luis; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones Biológicas de San Luis; Argentin

Influenza virus NS1 protein binds cellular DNA to block transcription of antiviral genes

Influenza NS1 protein is an important virulence factor that is capable of binding double-stranded (ds) RNA and inhibiting dsRNA-mediated host innate immune responses. Here we show that NS1 can also bind cellular dsDNA. This interaction prevents loading of transcriptional machinery to the DNA, thereby attenuating IAV-mediated expression of antiviral genes. Thus, we identified a previously undescribed strategy, by which RNA virus inhibits cellular transcription to escape antiviral response and secure its replication. (C) 2016 Elsevier B.V. All rights reserved.Peer reviewe

ZNF366 is an estrogen receptor corepressor that acts through CtBP and histone deacetylases

The regulation of gene expression by estrogen receptor-α (ERα) requires the coordinated and temporal recruitment of diverse sets of transcriptional co-regulator complexes, which mediate nucleosome remodelling and histone modification. Using ERα as bait in a yeast two-hybrid screen, we have identified a novel ERα-interacting protein, ZNF366, which is a potent corepressor of ERα activity. The interaction between ZNF366 and ERα has been confirmed in vitro and in vivo, and is mediated by the zinc finger domains of the two proteins. Further, we show that ZNF366 acts as a corepressor by interacting with other known ERα corepressors, namely RIP140 and CtBP, to inhibit expression of estrogen-responsive genes in vivo. Together, our results indicate that ZNF366 may play an important role in regulating the expression of genes in response to estrogen

Palynology of the Jagüel Formation (Maastrichtian–Danian) in northwestern Río Negro, Neuquén Basin, Argentina: paleobiogeographic inferences

The palynology of the Jagüel Formation at Cerro Azul locality Río Negro province; in the Neuquén Basin, was studied. The distribution of palynomorphs (spores, pollen grains, chlorophytes, and miscellaneous forms) across the outcrops allowed the definition of three palynological associations: A1 (upper Maastrichtian), A2 and A3 (Danian). The palynological results, together with micro- and invertebrate fossils found in this locality contributed to the paleoenvironmental reconstruction of this unit. A1 is deposited in mixed (coastal) to shallow marine environments with low energy associated to freshwater bodies. Whereas it is interpreted that A2 and A3 are deposited in coastal lagoons near shallow and internal platform marine environments. The largest number of palm pollen grains of Proxapertites and other angiosperms Retitrescolpites baculatus and Striatopollis for the Danian of Argentina has been registered here. These associations shared species with Maastrichtian and Danian palynofloras of the Colorado and western Neuquén basins. Species with affinities from northern latitudes of South America and Africa, and a few other species distributed more widely (cosmopolitan) and from southern regions (Argentina, Chile, Antarctica, New Zealand) predominate in the Danian. Therefore, we can confirm that the palynofloras of the Jagüel Formation are part of the Mixed Floristic Realm.Fil: Perez Pincheira, Egly Veronica. Provincia de Entre Ríos. Centro de Investigaciones Científicas y Transferencia de Tecnología a la Producción. Universidad Autónoma de Entre Ríos. Centro de Investigaciones Científicas y Transferencia de Tecnología a la Producción. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Centro de Investigaciones Científicas y Transferencia de Tecnología a la Producción; ArgentinaFil: Di Pasquo Lartigue, Maria. Provincia de Entre Ríos. Centro de Investigaciones Científicas y Transferencia de Tecnología a la Producción. Universidad Autónoma de Entre Ríos. Centro de Investigaciones Científicas y Transferencia de Tecnología a la Producción. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Centro de Investigaciones Científicas y Transferencia de Tecnología a la Producción; Argentin