Synthesis, characterization and antimicrobial activity of conjugates based on fluoroquinolon-type antibiotics and gelatin

Different fluoroquinolon-type antibiotics were conjugated to gelatin with the aim to synthesize biomacromolecules with antimicrobial properties. The covalent linkage of the antibiotic was performed by a radical process involving the residues in the side chains of gelatin able to undergo oxidative modifications. The conjugation of antibiotic moieties onto the protein structure was confirmed by FT-IR, UV–Vis, fluorescence, and calorimetric analyses. Biocompatibility tests were performed on human bone marrow mesenchymal stromal cells and the antibacterial properties of bioactive polymers were investigated by appropriate tests against Klebsiella pneumoniae and Escherichia coli. With regard to the tests conducted in the presence of E. coli, a minimum inhibitory concentration (MIC) ranging from 0.05 to 0.40 μg mL^?1 was recorded, while in the presence of K. pneumoniae this concentration varies from 0.10 to 1.60 μg mL^?1. In all the conjugates, the drug moieties retain their biological activity and the MIC values are lower than the resistance parameters of fluoroquinolon-type antibiotics versus Enterobacteriacae. The collected data suggest a broad range of applications, from biomedical to pharmaceutical and food science for all conjugates.     

Speed up of Video Enhancement based on Human Perception

This paper presents SUVEHP (speed up of video enhancement based on human perception), a human perception-based model oriented to reduce the computational time of digital video restoration. In particular, two specific hypothesis tests able to classify degraded frame regions are proposed. Classification is performed in agreement with regions visual significance in order to enable or inhibit motion compensated enhancement. The level of the proposed hypothesis tests is theoretically assessed. Moreover, extensive experimental results on video sequences affected by additive Gaussian noise show that SUVEHP speeds up some standard motion compensated denoisers up to 60%, preserving or even slightly increasing both the objective and subjective visual quality of the restored sequences.     

The Histamine H4 Receptor Participates in the Neuropathic Pain-Relieving Activity of the Histamine H3 Receptor Antagonist GSK189254

Growing evidence points to the histamine system as a promising target for the management of neuropathic pain. Preclinical studies reported the efficacy of H₃R antagonists in reducing pain hypersensitivity in models of neuropathic pain through an increase of histamine release within the CNS. Recently, a promising efficacy of H₄R agonists as anti-neuropathic agents has been postulated. Since H₃R and H₄R are both localized in neuronal areas devoted to pain processing, the aim of the study is to investigate the role of H₄R in the mechanism of anti-hyperalgesic action of the H₃R antagonist GSK189254 in the spared nerve injury (SNI) model in mice. Oral (6 mg/kg), intrathecal (6 µg/mouse), or intra locus coeruleus (LC) (10 µg/µL) administration of GSK189254 reversed mechanical and thermal allodynia in the ipsilateral side of SNI mice. This effect was completely prevented by pretreatment with the H₄R antagonist JNJ 10191584 (6 µg/mouse i.t.; (10 µg/µL intraLC). Furthermore, GSK189254 was devoid of any anti-hyperalgesic effect in H₄R deficient mice, compared with wild type mice. Conversely, pretreatment with JNJ 10191584 was not able to prevent the hypophagic activity of GSK189254. In conclusion, we demonstrated the selective contribution of H₄R to the H₃R antagonist-induced attenuation of hypernociceptive behavior in SNI mice. These results might help identify innovative therapeutic interventions for neuropathic pain.     

Open Questions in Cold Atmospheric Plasma Treatment in Head and Neck Cancer: A Systematic Review

Over the past decade, we witnessed a promising application of cold atmospheric plasma (CAP) in cancer therapy. The aim of this systematic review was to provide an exhaustive state of the art of CAP employed for the treatment of head and neck cancer (HNC), a tumor whose late diagnosis, local recurrence, distant metastases, and treatment failure are the main causes of patients’ death. Specifically, the characteristics and settings of the CAP devices and the in vitro and in vivo treatment protocols were summarized to meet the urgent need for standardization. Its molecular mechanisms of action, as well as the successes and pitfalls of current CAP applications in HNC, were discussed. Finally, the interesting emerging preclinical hypotheses that warrant further clinical investigation have risen. A total of 24 studies were included. Most studies used a plasma jet device (54.2%). Argon resulted as the mostly employed working gas (33.32%). Direct and indirect plasma application was reported in 87.5% and 20.8% of studies, respectively. In vitro investigations were 79.17%, most of them concerned with direct treatment (78.94%). Only eight (33.32%) in vivo studies were found; three were conducted in mice, and five on human beings. CAP showed pro-apoptotic effects more efficiently in tumor cells than in normal cells by altering redox balance in a way that oxidative distress leads to cell death. In preclinical studies, it exhibited efficacy and tolerability. Results from this systematic review pointed out the current limitations of translational application of CAP in the urge of standardization of the current protocols while highlighting promising effects as supporting treatment in HNC.     

Santolina pinnata Viv. Exerts Promising Antitumor Activity against Breast Cancer Cells and Anti-Inflammatory Effects in LPS-Stimulated RAW 264.7 Cells

Cancer is one of the largest causes of mortality in the world, and due to its incidence, the discovery of novel anticancer drugs is of great importance. Many successful anticancer drugs used in clinical practices are derived from natural products. The genus Santolina is a group of species distributed in the Mediterranean area and used in traditional medicine for their biological properties. The aim of this work was to investigate, for the first time, the multi-target biological potential of Italian Santolina pinnata in relation to their chemical profile, by which an interesting natural source of valuable phytochemicals endowed with anticancer and anti-inflammatory features could be assessed. n-Hexane (EHSP) and methanol (EMSP) extracts were investigated by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) and ultra-high-performance liquid chromatography (UHPLC), respectively. Anti-proliferative activity was analyzed on MCF-7 and MDA-MB-231 breast cancer cells, as well as on non-tumorigenic MCF-10A cells, by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. Apoptotic death was assessed by comet assay. Cell motility and invasive features were examined in highly invasive MDA-MB-231 by wound-healing scratches, while, in both breast cancer cell lines, by gel-zymography experiments. The anti-inflammatory potential was analyzed by nitric oxide (NO) production and the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) staining experiments in bacterial lipopolysaccharides (LPS) which stimulated RAW 264.7 cells. EHSP and EMSP extracts exhibited anticancer activity against breast cancer cells, promoting apoptotic death, as well as decreasing cell migration and invasive behaviours. The highest activity (IC₅₀ of 15.91 μg/mL) was detected against MDA-MB-231 cells, a highly invasive breast cancer cell line. Both extracts were also able to promote anti-inflammatory effects (IC₅₀ values ranging from 27.5 to 61.14 μg/mL), as well as to reduce NO levels by inducing inhibitory effects on NF-κB nuclear translocation in LPS-stimulated RAW 264.7 cells. The different biological behaviours found between the extracts could be related to their different chemical compositions. Herein, the multi-target biological potential of S. pinnata in inducing antitumor and anti-inflammatory effects was comprehensively demonstrated. These findings will provide important stepping-stones for further investigations and may lead to the development of highly effective S. pinnata extract-based treatments for breast cancer and inflammatory processes.     

Compact high gain erbium-ytterbium doped waveguide amplifier fabricated by Ag-Na ion exchange

A report is presented on an erbium-ytterbium doped waveguide amplifier fabricated by Ag-Na ion-exchange in a commercial phosphate glass substrate. The 31 mm-long active waveguide provides a maximum internal gain of 5.3 dB/cm at 1534 nm. The amplifier was fully characterised in terms of gain spectrum, noise figure, pump efficiency and gain saturation.     

Structure–property relationships in crosslinked networks from cis-1,4-polybutadiene and methacrylic acid. Preliminary results

In this paper we report preliminary results obtained analyzing structural data and mechanical properties of a composite system prepared vulcanizing mixtures of cis polybutadiene and methacrylic acid with different acid amount. The structure was investigated by the small angle x-ray scattering, while the physicomechanical properties were analyzed carrying out stress and birefringence measurements as function of the strain at constant temperature.     

Permeation of carbon dioxide in a thermotropic liquid-crystalline polyester

The transport properties of a thermotropic liquid crystalline polyester have been analyzed using carbon dioxide as permeant. Carbon dioxide, in the analyzed range of temperature and pressure, gives some information on the phase organization of the system. The structural model compatible with the transport behavior assumes the presence of a disordered phase within the well-ordered liquid crystalline domains. The same structural model was previously suggested on the basis of the transport behavior of methylene chloride vapors in nematic and smectic liquid-crystalline polymers.     

Ethanol increases apolipoprotein B mRNA editing in rat primary hepatocytes and McArdle cells

Symptomatic and asymptomatic astrovirus infection was prospectively determined in a 3-year birth cohort of Mayan infants. Stool samples from 271 infants and 268 older siblings were tested for astrovirus, adenovirus 40/41, rotavirus and Salmonella, Shigella and Campylobacter species. Concurrent diarrhea, vomiting, fever, or anorexia were noted. Astrovirus was detected in 164 infants (61%) and 20 siblings (7%). Rotavirus (4%) and adenovirus 40/41 (13%) were isolated less frequently. Of all diarrheal episodes reported at a visit, 26% (78/305) were associated with astrovirus; 17% (78/452) of astrovirus infections were associated with diarrhea and 9% with other symptoms. Only diarrhea was associated with astrovirus infection (odds ratio, 1.4; 95% confidence interval [CI], 1.07-1.92; P = .01). Of infants with astrovirus, 70% shed at multiple visits over a period of 2-17 weeks (median, 5). The point prevalence of astrovirus infection was significantly higher among infants than siblings (relative risk, 6.18; 95% CI, 3.93-9.72; P < .0001, chi2). Astrovirus was identified throughout the year, peaked in March and May, and decreased in September. In this population, astrovirus was the most common enteric pathogen isolated; symptomatic infection was prevalent among infants.