Structure–activity relationships of antibacterial peptides

Antimicrobial peptides play a crucial role in innate immunity, whose components are mainly peptide-based molecules with antibacterial properties. Indeed, the exploration of the immune system over the past 40 years has revealed a number of natural peptides playing a pivotal role in the defence mechanisms of vertebrates and invertebrates, including amphibians, insects, and mammalians. This review provides a discussion regarding the antibacterial mechanisms of peptide-based agents and their structure–activity relationships (SARs) with the aim of describing a topic that is not yet fully explored. Some growing evidence suggests that innate immunity should be strongly considered for the development of novel antibiotic peptide-based libraries. Also, due to the constantly rising concern of antibiotic resistance, the development of new antibiotic drugs is becoming a priority of global importance. Hence, the study and the understanding of defence phenomena occurring in the immune system may inspire the development of novel antibiotic compound libraries and set the stage to overcome drug-resistant pathogens. Here, we provide an overview of the importance of peptide-based antibacterial sources, focusing on accurately selected molecular structures, their SARs including recently introduced modifications, their latest biotechnology applications, and their potential against multi-drug resistant pathogens. Last, we provide cues to describe how antibacterial peptides show a better scope of action selectivity than several anti-infective agents, which are characterized by non-selective activities and non-targeted actions toward pathogens

Haemodynamic Response to a Standard Meal: Consideration on A Case of Significant Blood Pressure Peaks in a Diabetic Hypertensive Patient Treated with ARB and Comparison with Normal Age and Sex Matched Subjects

A standard meal is a stimulus that produces a response that consists in the redistribution of blood flow to the splanchnic district, potentially, affecting systemic blood pressure, this phenomenon was studied in animal models and in critic patient. Here we report a case of a diabetic hypertensive-in-treatment woman where two significant blood pressure peaks were recorded, during lunch and dinner, over an optimal 24/h blood pressure control. In the absence of previous normal reference values in the literature, we retrieved a series of n=10 age and sex matched subjects diagnosed normotensive on the mean of 24/h Ambulatory Blood Pressure Monitoring. We finally present our considerations on the normal response to a standard meal compared to what was found in the literature and in the present case, where an impaired control of resistance is hypothesised, and on the possible mechanisms supporting

Cascade reaction based synthetic strategies targeting biologically intriguing indole polycycles

Indole polycycles are common structural frameworks of biologically intriguing small molecules of natural and synthetic origin and therefore remain interesting and challenging synthetic targets. Cascade reactions wherein a number of reactions occur in a sequential manner in the same reaction apparatus are highly efficient chemical processes which quickly build up molecular complexity. Synthetic approaches based on cascade reactions are highly useful as they tend to avoid multiple reaction work-up steps as well as purifications of all intermediary products. Therefore, in the last decade, a number of cascade reaction based approaches to build various molecular scaffolds of biological interest have been reported. However, a relatively smaller number of cascade reaction based synthetic strategies have targeted the indole polycycles. In this article, we have summarized some interesting cascade reaction based synthesis designs leading to complex indole polycycles including some biologically intriguing and natural product inspired indole frameworks

Boosted Cross-Linking and Characterization of High-Performing Self-Assembling Peptides

Tissue engineering (TE) strategies require the design and characterization of novel biomaterials capable of mimicking the physiological microenvironments of the tissues to be regenerated. As such, implantable materials should be biomimetic, nanostructured and with mechanical properties approximating those of the target organ/tissue. Self-assembling peptides (SAPs) are biomimetic nanomaterials that can be readily synthesized and customized to match the requirements of some TE applications, but the weak interactions involved in the self-assembling phenomenon make them soft hydrogels unsuited for the regeneration of medium-to-hard tissues. In this work, we moved significant steps forward in the field of chemical cross-linked SAPs towards the goal of stiff peptidic materials suited for the regeneration of several tissues. Novel SAPs were designed and characterized to boost the 4-(N-Maleimidomethyl) cyclohexane-1-carboxylic acid 3-sulpho-N-hydroxysuccinimide ester (Sulfo-SMCC) mediated cross-linking reaction, where they reached G′ values of ~500 kPa. An additional orthogonal cross-linking was also effective and allowed to top remarkable G′ values of 840 kPa. We demonstrated that cross-linking fastened the pre-existing self-aggregated nanostructures, and at the same time, a strong presence of ß-structures is necessary for an effective cross-linking of (LKLK)3-based SAPs. Combining strong SAP design and orthogonal cross-linking reactions, we brought SAP stiffness closer to the MPa threshold, and as such, we opened the door of the regeneration of skin, muscle and lung to biomimetic SAP technology

UN MODELLO ALLE DIFFERENZE FINITE DI UN PANNELLO FOTOVOLTAICO ACCOPPIATO A MATERIALE A CAMBIAMENTO DI FASE

La diffusione commerciale dei dispositivi fotovoltaici presenta negli ultimi anni un trend di crescita significativa a livello internazionale. Numerose ricerche sono state svolte al fine di incrementare l\u2019efficienza di conversione elettrica dei pannelli fotovoltaici e tra le soluzioni indagate \ue8 stato sperimentato l\u2019impiego di materiali a cambiamento di fase (MCF) per ridurre i picchi di temperatura di funzionamento. Nel lavoro \ue8 stato sviluppato un algoritmo di calcolo in grado di fornire l\u2019andamento temporale della temperatura di un pannello fotovoltaico accoppiato a materiale a cambiamento di fase (Sistema PV-MCF). La determinazione della distribuzione di temperature che interessano un sistema PV-MCF \ue8 stata affrontata con il metodo delle differenze finite in geometria monodimensionale. Sono state definite le equazioni di conservazione dell\u2019energia per ogni punto nodale in cui \ue8 stato discretizzato il sistema fisico, differenziandole per i nodi \u201cinterni\u201d e per i nodi \u201csuperficiali\u201d. Le equazioni alle differenze finite sono state formulate esplicitamente rispetto alla variabile temporale e sono state codificate in un apposito software. Il confronto con alcune soluzioni analitiche largamente impiegate nella bibliografia di settore ha permesso di verificare la correttezza e la validit\ue0 dell\u2019approccio sviluppato

Total synthesis of natural disaccharide sambubiose

A practical and robust synthetic method to obtain the natural disaccharide sambubiose (2O-β-D-xylopyranosyl-D-glucopyranose) is reported, exploring the key step in the synthesis, i.e., stereoselective O-glycosylation. Specifically, the best combinations of glycoside donors and acceptors were identified, stereospecific control of the reaction was achieved by screening several catalysts and protection/deprotection steps were evaluated and improved. The best result was obtained by coupling allyl 3,5,6-tri-O-benzyl-β-D-glucofuranoside with 2,3,4-tri-O-acetyl-Dxylopiranosyl-α-trichloro acetimidate in the presence of trimethylsilyl triflate as a catalyst giving the corresponding protected target compound as a correct single isomer. The latter was transformed accordingly into the desired final product by deprotection steps (deallylation, deacetylation, and debenzylation). Sambubiose was synthesized into a satisfactory and higher overall yield than previously reported and was also characterized

Regression analysis to design a solar thermal collector for occasional use

Optimal design of a solar thermal system is necessary to minimize payback time and to diffuse renewable energy use for Domestic Hot Water production in residential areas. More accurate design is crucial in the case of seasonal or occasional use of the system; indeed, the standard criteria generally applied to a design system for continuous use, can lead to considerable over-sizing. To speed up the design phase and to help the planner in the identification of the best solution without any complex evaluation or long computational time, it would be interesting to have available a simpler method than the standard procedures, but one that is reliable and accurate for the evaluation of the best configuration, taking into account occasional use, seasonal and monthly domestic hot water demand, orientation and primary flow rate. To this end, the authors investigated a methodology for the identification of some empirical correlations based on the analysis of data coming from a parametric simulation; in this way the identified correlations can indicate, with high reliability, the optimal design knowing only well-known parameters. In detail, the data output was extracted and processed to evaluate the best design configurations under any operative conditions. Determination of the best configuration identifies the operative parameters that maximize the Solar Fraction of the plant and minimize the auxiliary energy. To highlight the reliability of this methodology, in this work, the authors describe a case study of the Sicilian region proposing a set of simple, reliable correlations that allow the determination of the best tilt angle for monthly or seasonal use. Following the same steps the procedure can be replicate in any context and in any conditions