Exploring the anti-biofilm activity of cinnamic acid derivatives in Candida albicans

Some compounds, characterized by phenylethenyl moiety, such as methyl cinnamate and caffeic acid phenethyl ester, are able to inhibit C. albicans biofilm formation. On these bases, and as a consequence of our previous work, we synthesized a series of cinnamoyl ester and amide derivatives in order to evaluate them for the activity against C. albicans biofilm and planktonically grown cells. The most active compounds 7 and 8 showed ⩾50% biofilm inhibition concentrations (BMIC50) of 2 μg/mL and 4 μg/mL respectively, against C. albicans biofilm formation; otherwise, 7 showed an interesting activity also against mature biofilm, with BMIC50 of 8 μg/m

New N,N-dimethylcarbamate inhibitors of acetylcholinesterase: design synthesis and biological evaluation

A series of N,N-dimethylcarbamates containing a N,N-dibenzylamino moiety was synthesized and tested to evaluate their ability to inhibit Acetylcholinesterase (AChE). The most active compounds 4 and 8, showed 85 and 69% of inhibition at 50 mM, respectively. Furthermore, some basic SAR rules were outlined: an alkyl linker of six methylene units is the best spacer between the carbamoyl and dibenzylamino moieties; electron-withdrawal substituents on aromatics rings of the dibenzylamino group reduce the inhibitory power. Compound 4 produces a slow onset inhibition of AChE and this is not due to the carbamoylation of the enzyme, as demonstrated by the time-dependent inhibition assay of AChE with compound 4 and by MALDI-TOF MS analysis of trypsinized AChE inhibited by compound 4. Instead, compound 4 could act as a slow-binding inhibitor of AChE, probably because of its high conformational freedom due to the linear alkyl chain

Vulnerability of demersal fish assemblages to trawling activities: a traits-based index

Reducing the impact on vulnerable species through changes in fishing practices, such as the spatial or temporal avoidance of certain areas, is key to increase the ecological sustainability of fisheries. However, it is often hampered by the availability of sufficiently detailed data and robust indicators. Existing trawl surveys are a cost-effective data source to assess the vulnerability of fishing areas based on the quantities of vulnerable species caught. We developed a biological traits-based approach to the vulnerability of demersal assemblages using commercial trawl catch data. An expert-based approach identified a set of biological traits that are expected to condition the species' response to trawling impact and are combined to produce the vulnerability index ranked into four levels (low, moderate, high, and very high vulnerability). The approach was tested in four southern European fishing grounds showing evidence of over-exploitation, through catches being dominated by species of relatively low vulnerability to fishing impacts. The general distribution of species' biomass amongst vulnerability groups was highly homogenous across case studies, despite local differences in fishing fleet structure, target species and fishing depths. Within all areas the species with moderate vulnerability dominated and, in most instances, species of "very high" vulnerability were not recorded. Nevertheless, differences emerged when comparing the proportions of highly vulnerable species in the catches. Variability in vulnerability level of the catch was also observed at small spatial scales, which was principally explained by differences in habitat type and depth and, secondarily, by fishing effort. In fine mud in the shallower areas there was a higher presence of low vulnerable fauna. Furthermore, vulnerable organisms decreased in their presence in sandier substrates on the continental shelf. The spatial heterogeneity in assemblage vulnerability composition encourages the potential for adoption of this index in the spatial management of fishing grounds aiming at ensuring a sustainable exploitation by mitigating trawl impacts on the most vulnerable components of the demersal assemblages.MINOUW Horizon 2020 (Project ID: 634495); H2020-Marie Skłodowska-Curie Action MSCA-IF-2016 (Project ID: 743545)info:eu-repo/semantics/publishedVersio

Pedicularis L. Genus. Systematics, botany, phytochemistry, chemotaxonomy, ethnopharmacology, and other

In this review, the relevance of the plant species belonging to the Pedicularis L. genus has been considered from different points of view. Particular emphasis was given to phytochemistry and ethnopharmacology, since several classes of natural compounds have been reported within this genus and many of its species are well known to be employed in the traditional medicines of many Asian countries. Some important conclusions on the chemotaxonomic and chemosystematic aspects of the genus have also been provided for the first time. Actually, this work represents the first total comprehensive review on this genus

Right diaphragmatic injury and lacerated liver during a penetrating abdominal trauma: case report and brief literature review.

INTRODUCTION: Diaphragmatic injuries are rare consequences of thoracoabdominal trauma and they often occur in association with multiorgan injuries. The diaphragm is a difficult anatomical structure to study with common imaging instruments due to its physiological movement. Thus, diaphragmatic injuries can often be misunderstood and diagnosed only during surgical procedures. Diagnostic delay results in a high rate of mortality. METHODS: We report the management of a clinical case of a 45-old man who came to our observation with a stab wound in the right upper abdomen. The type or length of the knife used as it was extracted from the victim after the fight. CT imaging demonstrated a right hemothorax without pulmonary lesions and parenchymal laceration of the liver with active bleeding. It is observed hemoperitoneum and subdiaphragmatic air in the abdomen, as a bowel perforation. A complete blood count check revealed a decrease in hemoglobin (7 mg/dl), and therefore it was decided to perform surgery in midline laparotomy. CONCLUSION: In countries with a low incidence of inter-personal violence, stab wound diaphragmatic injury is particularly rare, in particular involving the right hemidiaphragm. Diaphragmatic injury may be underestimated due to the presence of concomitant lesions of other organs, to a state of shock and respiratory failure, and to the difficulty of identifying diaphragmatic injuries in the absence of high sensitivity and specific diagnostic instruments. Diagnostic delay causes high mortality with these traumas with insidious symptoms. A diaphragmatic injury should be suspected in the presence of a clinical picture which includes hemothorax, hemoperitoneum, anemia and the presence of subdiaphragmatic air in the abdomen

Genetic markers associated to arbuscular mycorrhizal colonization in durum wheat

In this work we investigated the variability and the genetic basis of susceptibility to arbuscular mycorrhizal (AM) colonization of wheat roots. The mycorrhizal status of wild, domesticated and cultivated tetraploid wheat accessions, inoculated with the AM species Funneliformis mosseae, was evaluated. In addition, to detect genetic markers in linkage with chromosome regions involved in AM root colonization, a genome wide association analysis was carried out on 108 durum wheat varieties and two AM fungal species (F. mosseae and Rhizoglomus irregulare). Our findings showed that a century of breeding on durum wheat and the introgression of Reduced height (Rht) genes associated with increased grain yields did not select against AM symbiosis in durum wheat. Seven putative Quantitative Trait Loci (QTLs) linked with durum wheat mycorrhizal susceptibility in both experiments, located on chromosomes 1A, 2B, 5A, 6A, 7A and 7B, were detected. The individual QTL effects (r2) ranged from 7 to 16%, suggesting a genetic basis for this trait. Marker functional analysis identified predicted proteins with potential roles in host-parasite interactions, degradation of cellular proteins, homeostasis regulation, plant growth and disease/defence. The results of this work emphasize the potential for further enhancement of root colonization exploiting the genetic variability present in wheat

Leucosceptosides A and B. Two phenyl-ethanoid glycosides with important occurrence and biological activities

In this review paper, the occurrence in the plant kingdom, the chemophenetic value and the biological activities associated with two specific phenyl-ethanoid glycosides, i.e., leucosceptoside A and leucosceptoside B, were reported. This is the first work ever conducted on such a subject. Analysis of the literature data clearly led to three important conclusions: leucosceptoside A is much more common in plants than leucosceptoside B; leucosceptoside A exerts more biological activities than leucosceptoside B even if nothing can be generally concluded about which one is actually the most potent; neither of these compounds can be used as a chemophenetic marker. These three aspects and more are discussed in more depth in this work

The microRNA-Processing Enzyme Dicer Is Essential for Thyroid Function

Dicer is a type III ribonuclease required for the biogenesis of microRNAs (miRNAs), a class of small non-coding RNAs regulating gene expression at the post-transcriptional level. To explore the functional role of miRNAs in thyroid gland function, we generated a thyrocyte-specific Dicer conditional knockout mouse. Here we show that development and early differentiation of the thyroid gland are not affected by the absence of Dicer, while severe hypothyroidism gradually develops after birth, leading to reduced body weight and shortened life span. Histological and molecular characterization of knockout mice reveals a dramatic loss of the thyroid gland follicular architecture associated with functional aberrations and down-regulation of several differentiation markers. The data presented in this study show for the first time that an intact miRNAs processing machinery is essential for thyroid physiology, suggesting that deregulation of specific miRNAs could be also involved in human thyroid dysfunctions

Experimental study and computational modelling of cruzain cysteine protease inhibition by dipeptidyl nitriles

Chagas disease affects millions of people in Latin America. This disease is caused by the protozoan parasite Trypanossoma cruzi. The cysteine protease cruzain is a key enzyme for the survival and propagation of this parasite lifecycle. Nitrile-based inhibitors are efficient inhibitors of cruzain that bind by forming a covalent bond with this enzyme. Here, three nitrile-based inhibitors dubbed Neq0409, Neq0410 and Neq0570 were synthesized, and the thermodynamic profile of the bimolecular interaction with cruzain was determined using isothermal titration calorimetry (ITC). The result suggests the inhibition process is enthalpy driven, with a detrimental contribution of entropy. In addition, we have used hybrid Quantum Mechanical/Molecular Mechanical (QM/MM) and Molecular Dynamics (MD) simulations to investigate the reaction mechanism of reversible covalent modification of cruzain by Neq0409, Neq0410 and Neq0570. The computed free energy profile shows that the nucleophilic attack of Cys25 on the carbon C1 of inhibitiors and the proton transfer from His162 to N1 of the dipeptidyl nitrile inhibitor take place in a single step. The calculated free energy of the inhibiton reaction is in agreement with covalent experimental binding. Altogether, the results reported here suggests that nitrile-based inhibitors are good candidates for the development of reversible covalent inhibitors of cruzain and other cysteine proteases

Nor-lignans. Occurrence in plants and biological activities. A review

In this review article, the occurrence of nor-lignans and their biological activities are explored and described. Nor-lignans have proven to be present in several different families also belonging to chemosystematically distant orders as well as to have many different beneficial pharmacological activities. This review article represents the first one on this argument and is thought to give a first overview on these compounds with the hope that their study may continue and increase, after this