Use of imidazo[1,5-a]quinoline scaffold as the pharmacophore in the design of bivalent ligands of central benzodiazepine receptors.

The imidazo[1,5-a]quinoline scaffold of central benzodiazepine receptor (CBR) ligands was used as the pharmacophore in the design of bivalent ligands bearing spacers showing variable length and different physicochemical features. The newly designed compounds were synthesized along with the corresponding reference monovalent compounds bearing the corresponding spacers terminated with a tert-butoxycarbonyl group. The novel compounds were tested in binding assays with different CBR preparations such as the cerebral cortex from male CD-1 albino mice or the human recombinant α1β3γ2 and α2β3γ2 γ-aminobutyric acid type A receptors (GABARs) stably expressed in mouse L(tk-) cells.

The roles of geometry and viscosity in the mobilization of coarse sediment by finer sediment.

In rivers, the addition of finer sediment to a coarser riverbed is known to increase the mobility of the coarser fraction. Two mechanisms have been suggested for this: a geometric mechanism whereby smaller sizes smooth the bed, increasing near-bed velocity and thus mobility of the larger sizes, and a viscous mechanism whereby a transitionally smooth turbulent boundary layer forms, rendering the coarser grains more mobile. Here, we report on experiments using two sediment mixtures to better understand these proposed mechanisms.

Contingency enables the formation of social expectations about an artificial agent.

What environmental regularities support infant communicative learning from social interactions? We propose that infants allocate their attention toward and learn from external events that are contingent on their own behaviors. We tested the robustness of the influence of contingency on communicative learning by using a non-biological stimulus, a remote-controlled car, as the social partner. The car approached infants and produced a speech sound either contingently to infants' vocalizations or on a yoked schedule.

Reactivity of a Morita-Baylis-Hillman Adduct Derivative Bearing a Triphenylamine Moiety with Lysine Models.

The reactivity of Morita-Baylis-Hillman Adduct (MBHA) derivative 7 was studied with different primary amine derivatives such as n-butylamine, Nα-acetyl-L-lysine methyl ester, and a poly-(L-lysine) derivative as lysine models to obtain information about the possible reactions in complex protein environments. MBHA derivative 7 reacted with n-butylamine or Nα-acetyl-L-lysine methyl ester producing monoadducts 9a or 9c, which showed bright emission features in the green region at 526-535 nm with photoluminescence quantum yield values in solutions of 73 % and 51 %, respectively. Based on these results, MBHA derivative 7 can be considered an interesting new fluorogenic probe potentially useful in the labelling of basic amino acid residues.

Cross-Linked Hyaluronan Derivatives in the Delivery of Phycocyanin.

An easy and viable crosslinking technology, based on the "click-chemistry" reaction copper(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (click-crosslinking), was applied to graft copolymers of medium molecular weight (i.e., 270 kDa) hyaluronic acid () grafted with ferulic acid () residues bearing clickable propargyl groups, as well as caffeic acid derivatives bearing azido-terminated oligo(ethylene glycol) side chains.

A Facile Access to Green Fluorescent Albumin Derivatives.

A Morita-Baylis-Hillman Adduct (MBHA) derivative bearing a triphenylamine moiety was found to react with human serum albumin (HSA) shifting its emission from the blue to the green-yellow thus leading to green fluorescent albumin (GFA) derivatives and enlarging the platform of probes for aggregation-induced fluorescent-based detection techniques. A possible interaction of MBHA derivative 7 with a lipophilic pocket within the HSA structure was suggested by docking studies. DLS experiments showed that the reaction with HSA induce a conformational change of the protein contributing to the aggregation process of GFA derivatives.

A tri(ethylene glycol)-tethered Morita-Baylis-Hillman dimer in the formation of macrocyclic crown ether-paracyclophane hybrid structures.

A Morita-Baylis-Hillman acetate was dimerized by a click-chemistry Copper(i)-Catalysed Azide-Alkyne Cycloaddition (CuAAC) reaction employing a tri(ethylene glycol) diazide derivative to obtain a dimeric MBHA derivative. The reaction of this dimeric MBHA derivative with -butylamine afforded a photoisomerizable macrocyclic crown ether-paracyclophane hybrid architecture that is potentially useful in a large variety of applications as well as those already well-known for crown ethers.

Ferulated Poly(vinyl alcohol) based hydrogels.

New graft copolymers were prepared by reaction of poly (vinyl alcohol) (PVA) with mono-imidazolide or bis-imidazolide derivatives of ferulic acid (FA) with the formation of ester bonds. The obtained graft copolymers, thanks to the crosslinking capability of FA, formed in water strong gels as verified by rheological analyses. The resulting hydrogels were characterized to evaluate their applicability as wound dressing.

Curiosity constructs communicative competence through social feedback loops.

One of the most important challenges for a developing infant is learning how best to allocate their attention and forage for information in the midst of a great deal of novel stimulation. We propose that infants of altricial species solve this challenge by learning selectively from events that are contingent on their immature behavior, such as babbling. Such a contingency filter would focus attention and learning on the behavior of social partners, because social behavior reliably fits infants' sensitivity to contingency.

Grain shape effects in bed load sediment transport.

Bed load sediment transport, in which wind or water flowing over a bed of sediment causes grains to roll or hop along the bed, is a critically important mechanism in contexts ranging from river restoration to planetary exploration. Despite its widespread occurrence, predictions of bed load sediment flux are notoriously imprecise. Many studies have focused on grain size variability as a source of uncertainty, but few have investigated the role of grain shape, even though shape has long been suspected to influence transport rates.

The 2015 landslide and tsunami in Taan Fiord, Alaska.

Glacial retreat in recent decades has exposed unstable slopes and allowed deep water to extend beneath some of those slopes. Slope failure at the terminus of Tyndall Glacier on 17 October 2015 sent 180 million tons of rock into Taan Fiord, Alaska. The resulting tsunami reached elevations as high as 193 m, one of the highest tsunami runups ever documented worldwide.

Prokineticin-2 and ghrelin robustly influence the sexual and ingestive behaviors of female Syrian hamsters.

Prokineticins are involved in many physiological processes including circadian rhythms, neurogenesis, angiogenesis, and cancer. Recently, they have been found to play a role in regulating food intake. Historically, proteins that increase feeding behavior in mammals decrease reproductive behavior to prevent pregnancy and lactation when food is scarce.

The Effect of the Menstrual Cycle on Body Composition Determined by Contact-Electrode Bioelectrical Impedance Analyzers.

Bioelectrical impedance analysis (BIA) is a noninvasive and relatively inexpensive method of assessing body composition. Manufacturers of BIA technology recommend to avoid testing women when they perceive to be retaining water during the menstrual cycle. The purpose of the present investigation was to examine the effect of the menstrual cycle on body composition determined by contact-electrode BIA analyzers.

Functional distribution of synapsin I in human sperm.

Proteins known to function during cell-cell communication and exocytosis in neurons and other secretory cells have recently been reported in human sperm. Synapsins are a group of proteins that have been very well characterized in neurons, but little is known about synapsin function in other cell types. Based upon previous findings and the known function of synapsin, we tested the hypothesis that synapsin I was present in human sperm.

Flow in bedrock canyons.

Bedrock erosion in rivers sets the pace of landscape evolution, influences the evolution of orogens and determines the size, shape and relief of mountains. A variety of models link fluid flow and sediment transport processes to bedrock incision in canyons. The model components that represent sediment transport processes are increasingly well developed.

[Bilateral pneumothorax complicating cavitary pulmonary metastases in angiosarcoma].

Metastatic pulmonary angiosarcomas are a common complication of a rare condition. Generally, they are presented as peripheral solid nodules, infiltrates, and pleural effusions. We report the case of a 65 year-old man with bilateral recurrent pneumothorax secondary to metastatic cavitary lesions from angiosarcoma of the scalp.

[Hemophagocytic syndrome. Report of four cases].

Hemophagocytic syndrome (HS) is a severe hyper inflammatory condition whose cardinal symptoms are prolonged fever, cytopenia, hepatosplenomegaly, and hemophagocytosis by activated, morphologically benign macrophages. The clinical course resembles sepsis, sharing similar physiopathological features. We report four patients with the syndrome.

Multiplexed methylation profiles of tumor suppressor genes and clinical outcome in lung cancer.

Background: Changes in DNA methylation of crucial cancer genes including tumor suppressors can occur early in carcinogenesis, being potentially important early indicators of cancer. The objective of this study was to examine a multiplexed approach to assess the methylation of tumor suppressor genes as tumor stratification and clinical outcome prognostic biomarkers for lung cancer.

Methods: A multicandidate probe panel interrogated DNA for aberrant methylation status in 18 tumor suppressor genes in lung cancer using a methylation-specific multiplex ligation-dependent probe amplification assay (MS-MLPA).

[Pulmonary tumor embolism: Report of two cases].

Dyspnea and hypoxemia in a patient with cancer may have several causes, including infections, thromboembolism, metastases, and pulmonary injuries by drugs. We report a 47-year-old female with breast cancer and a 70-year-old male with urinary bladder cancer who were admitted for dyspnea, hypoxemia and pulmonary hypertension. Chest X rays and CT scans were normal.

Hamster sperm-associated alpha-L-fucosidase functions during fertilization.

Sperm-associated alpha-L-fucosidases have been identified in diverse organisms. Their wide phylogenetic distribution and known properties support the likelihood that L-fucose and alpha-L-fucosidase have fundamental function(s) during gamete interaction. This is consistent with the substantial evidence in the literature documenting the importance of carbohydrate moieties during fertilization.

Analysis of survival in 400 surgically resected non-small cell lung carcinomas: towards a redefinition of the T factor.

Introduction: The tumor, node, metastasis (TNM) system has been recognized internationally as the standard for staging disease extension, but despite the improvements of the 1997/2002 international staging system, there may be marked differences in postoperative 5-year survival rates within each stage. There is controversy about the impact of tumor size itself as a variable unrelated to stage.The objective of this study was to analyze the influence of tumor size on the survival in patients with surgically resected non-small cell lung carcinoma (NSCLC).

Stabilization of membrane-associated alpha-L-fucosidase by the human sperm equatorial segment.

Previous reports from this laboratory documented the existence of two novel isoforms of alpha-L-fucosidase in human semen and showed that membrane-associated alpha-L-fucosidase is cryptically held within the acrosomal compartment and enriched within the sperm equatorial segment. The occurrence of these novel isoforms is provocative. Sperm proteins potentially involved in sperm-egg interactions must maintain their functional integrity as they travel through the female reproductive tract.