Microwave-assisted oxidation of silibinin: A simple and preparative method for the synthesis of improved radical scavengers

A new and preparative oxidation of silibinin has been developed to give access to two different silibinin derivatives known for their enhanced antioxidant properties. Conventional heating methods were compared with results obtained from microwave (MW) heating. The base-catalysed oxidation of silibinin under MW heating is a very efficient method for the preparation of 2,3-dehydrosilybin and a related silybin rearrangement product. This latter compound shows enhanced radical scavenging properties. Optimised conditions were used to prepare 2,3-dehydrosilybins A and B from optically pure silybins A and B. An efficient, preparative purification method was also developed to enable isolation of different products in high purity. © 2013 Elsevier Ltd. All rights reserved

Phosphodiester Silybin Dimers Powerful Radical Scavengers: A Antiproliferative Activity on Different Cancer Cell Lines

Silibinin is the main biologically active component of silymarin extract and consists of a mixture 1:1 of two diastereoisomeric flavonolignans, namely silybin A (1a) and silybin B (1b), which we call here silybins. Despite the high interest in the activity of this flavonolignan, there are still few studies that give due attention to the role of its stereochemistry and, there is still today a strong need to investigate in this area. In this regard, here we report a study concerning the radical scavenger ability and the antiproliferative activity on different cell lines, both of silybins and phosphodiester-linked silybin dimers. An efficient synthetic strategy to obtain silybin dimers in an optical pure form (6aa, 6ab and 6bb) starting from a suitable building block of silybin A and silybin B, obtained by us from natural extract silibinin, was proposed. New dimers show strong antioxidant properties, determined through hydroxyl radical (HO°) scavenging ability, comparable to the value reported for known potent antioxidants such as quercetin. A preliminary screening was performed by treating cells with 10 and 50 µM concentrations for 48 h to identify the most sensitive cell lines. The results show that silibinin compounds were active on Jurkat, A375, WM266, and HeLa, but at the tested concentrations, they did not interfere with the growth of PANC, MCF-7, HDF or U87. In particular, both monomers (1a and 1b) and dimers (6aa, 6ab and 6bb) present selective anti-proliferative activity towards leukemia cells in the mid-micromolar range and are poorly active on normal cells. They exhibit different mechanisms of action in fact all the cells treated with the 1a and 1b go completely into apoptosis, whereas only part of the cells treated with 6aa and 6ab were found to be in apoptosis

Relationship between gastric pouch and GERD after laparoscopic sleeve gastrectomy

open9noAims and objectives Laparoscopic Sleeve Gastrectomy (LSG) is considered safe and effective even as conversion procedure after primary bariatric operations. The correlation between gastric pouch volumes and gastro-esophageal reflux disease's (GERD) symptoms (heartburn, reflux, regurgitation) remains unclear (1, 2). With this study we want to assess a correlation between the gastric remnant size and GERD.openPomerri, F.; Romanucci, G.; Barbiero, G.; Zuliani, M.; Ortu, V.; Miotto, D.; Albanese, A.; Prevedello, L.; Foletto, M.Pomerri, Fabio; Romanucci, G.; Barbiero, G.; Zuliani, M.; Ortu, V.; Miotto, Diego; Albanese, A.; Prevedello, L.; Foletto, M

Exploring the therapeutic potential of Aloin: unraveling neuroprotective and anticancer mechanisms, and strategies for enhanced stability and delivery

: We investigate the therapeutic potential of Aloin A and Aloin B, two natural compounds derived from Aloe vera leaves, focusing on their neuroprotective and anticancer properties. The structural differences between these two epimers suggest that they may exhibit distinct pharmacological properties. Our investigations revealed that both epimers are not stable in aqueous solution and tend to degrade rapidly, with their concentration decreasing by over 50% within approximately 12 h. These results underscore the importance of addressing issues such as the need for encapsulation into effective drug delivery systems to enhance stability. ThT fluorescence experiments showed that neither compound was able to inhibit Aβ amyloid aggregation, indicating that other mechanisms may be responsible for their neuroprotective effects. Next, an equimolar mixture of Aloin A and Aloin B demonstrated an ability to inhibit proteasome in tube tests, which is suggestive of potential anticancer properties, in accordance with antiproliferative effects observed in neuroblastoma SH-SY5Y and HeLa cell lines. Higher water stability and increased antiproliferative activity were observed by encapsulation in carbon dot nanoparticles, suggesting a promising potential for further in vivo studies

Defensome against Toxic Diatom Aldehydes in the Sea Urchin Paracentrotus lividus

Many diatom species produce polyunsaturated aldehydes, such as decadienal, which compromise embryonic and larval development in benthic organisms. Here newly fertilized Paracentrotus lividus sea urchins were exposed to low concentration of decadienal and the expression levels of sixteen genes, implicated in a broad range of functional responses, were followed by Real Time qPCR in order to identify potential decadienal targets. We show that at low decadienal concentrations the sea urchin Paracentrotus lividus places in motion different classes of genes to defend itself against this toxic aldehyde, activating hsp60 and two proteases, hat and BP10, at the blastula stage and hsp56 and several other genes (14-3-3ε, p38 MAPK, MTase, and GS) at the prism stage. At this latter stage all genes involved in skeletogenesis (Nec, uni, SM50 and SM30) were also down-expressed, following developmental abnormalities that mainly affected skeleton morphogenesis. Moreover, sea urchin embryos treated with increasing concentrations of decadienal revealed a dose-dependent response of activated target genes. Finally, we suggest that this orchestrated defense system against decadienal represents part of the chemical defensome of P. lividus affording protection from environmental toxicants

Wavelength-shifting fibers for calorimetric measurements in a long base line neutrino oscillation experiment

Abstract The NOE Collaboration has proposed a calorimeter to measure the energy of the final states of ν interaction events. The properties of long scintillator bars with wavelength-shifting fiber readout have been studied to develop a calorimeter design option. Various prototypes have been exposed to a cosmic rays stand. The total measured light yield in the middle of a 6 m -long fiber is about 15 photoelectrons. With this photon collection performance, it has been simulated that the calorimeter can achieve 17%/ E and 50%/ E resolutions for electrons and pions, respectively

Oncoplastic and reconstructive surgery in SENONETWORK Italian breast centers: lights and shadows

Highlights: • Despite the significance of oncoplastic procedure, an italian database is lacking. • Senonetwork established a multidisciplinary survey to assess their safety and efficacy. • Reconstructive outcomes were positive across low and high-volume centers. • After mastectomy, implant-based techniques are common. DTI reconstruction is advantageuos. • This contributes to the global understanding of effective strategies against breast cancer

Phytotoxic effects of mediterranean plants extracts on lettuce, tomato and onion as possible additive in irrigation drips

The study aimed to identify the mixtures of natural products to be added to the drippers (used in drip irrigation) during their preparation, so that the slow release of phytotoxic substances with the passage of water reduces or eliminates the intrusion of roots in the drippers. In field studies, we selected five phytotoxic plant species [Vetch villosa Roth., Brassica juncea L., Secale cereale L., Juncus effusus L. and Vallisneria natans L.] and their hydroalcoholic extracts were tested on two dicotyledons [Lactuca sativa L. cv Cavolo di Napoli and Lycopersicon esculentum L.] and one monocotyledon, Allium cepa L. We determined the structure of the main components of each extract. The Vetch villosa extract was most inhibitory. Further studies are required to determine whether to use the extract as such or one or more of its individual components can be used as possible additive in subsurface irrigation drip