Phosphated crosslinked pectin as a potential excipient for specific drug delivery: preparation and physicochemical characterization

Pectin was chemically modified with different amounts of trisodium trimetaphosphate (STMP) in aqueous solution (pH = 12), thereby giving a material with reduced water solubility. The physiochemical characterization of this new material was carried out through Fourier transform infrared and thermogravimetric analyses. Phosphated pectin (Pect‐STMP) together with prebiotic (oligosaccharide) were incorporated into an aqueous dispersion of polymethacrylate (Eudragit^® RS 30 D) in order to obtain free films using a casting process (50 °C) on a Teflon plate. The free films were evaluated using water vapour transmission, average swelling index in simulated gastric fluid (SGF) and simulated intestinal fluid, scanning electron microscopy and a diffusion study with theophylline in buffer solution with and without pectinolytic enzyme. The results suggest that the new material can be used in the coating process for oral solid‐reservoir systems, to prevent the premature release of drugs in SGF (pH = 1.2). Furthermore, the presence of both Pect‐STMP and oligosaccharide favours the specific degradation of the pellicle by the action of the enzymes produced by colonic microflora. The material obtained in this work has the potential to be applied in devices for drug delivery in the colon, making possible modified release of drugs. Nevertheless, subsequent colon‐specific experiments in vivo need to be carried out in order to confirm the possible application of this new material. Copyright © 2009 Society of Chemical Industry     

Exploring the anticancer properties of essential oils from family Lamiaceae

Lamiaceae is among the largest families of flowering plants with about 250 genera and over 7,000 species distributed around the world. It is considered as the important source of essential oils, for example, menthol, geraniol, eucalyptol, camphor and thymol. Therefore, it is imperative to study these economically important compounds under in vitro conditions for their sustainable and enhanced production. In addition to proven biological activities, essential oils from this family have recently been evaluated for anticancer activities and considered as a source of anticancer drugs. Mechanisms involved in the essential oils-mediated antiproliferative activity include cell cycle arrest, apoptosis and DNA repair mechanisms. Essential oils also act in the reduction of tumors, inhibiting metastasis and as anti-multidrug resistance molecules. The aim of this review is to assess the anticancer properties of essential oils obtained from different members of family Lamiaceae. The available reports on active components of essential oils and their effect on cancer type and cell line have been discussed. Biotechnological studies to improve the production of essential oils have also been highlighted. Various methods have been adopted to obtain essential oils under in vitro conditions from different plant species of family Lamiaceae, and their production is affected by culture conditions, cultivation mode, utilization of nutrient media and plant growth regulators. The literature survey suggests that essential oils obtained from family Lamiaceae have perspective for the development of new alternatives for disease treatment and prevention.     

Fabrication of microstructures on different materials by diode-pumped solid state laser writing for microfluidics applications

Laser writing attached many attentions for fabrication micro-channels in microfluidics devices and lab-on-chip devices for biomedical applications. In this study, micro-channels were fabricated on different materials as masters using nanosecond diode-pumped solid state (DPSS) laser writing for imprinting on glass and polymer microfluidics devices. Good quality microstructures were fabricated on silicon, nickel alloy, cooper/brass and alumina, respectively by laser writing which proved that the nanosecond DPSS laser is suitable for rapid prototyping and rapid manufacturing of surface microstructures on different substrates as mask-less exposure system of imprinting.     

In situ activated 3,5-dinitrobenzoic acid covalent attached to nanostructured platform for NADH electrooxidation

The activation of 3,5-dinitrobenzoic acid (3,5-DNBA) in situ is proposed for electrocatalytic detection of NADH at low overpotentials. Thus, 3,5-DNBA was strategically connected to a nanostructured surface based on MWCNTs and PEI (an amine rich polymer). Then, R–NO/R–NHOH was electrogenerated in situ by cycling the potential between 0.15 and −0.55 V versus SCE. The formation of an intermediate charge transfer complex is proposed for the reaction between NADH and redox mediator. The apparent Michaelis–Menten constant (K_M) obtained by RDE voltammetry and amperometry was in good agreement, around 10⁻⁵ mol L⁻¹. The k_obs for the catalytic reaction evaluated by chronoamperometry and RDE voltammetry, was in good agreement and was found to be around 10⁴ L mol⁻¹ s⁻¹. The sensor provides a linear response range for NADH from 4.0 up to 42.0 μmol L⁻¹ with a sensitivity of 71 nA L μmol⁻¹, detection and quantification limits of 1.2 and 4.0 μmol L⁻¹ respectively, with a response time of 0.16 s.     

Dating of newly formed minerals in geothermal fields through Th series short lived isotopes: Check on mineral of known age and implications to fluid-rock interactions

The ²²⁸Th/²²⁸Ra activity ratio can provide a tool for age measurements of newly formed minerals, down to about 15 yr. A general discussion of the method is followed by an experimental check on an aphthitalite brine, crystallized from a geothermal well at Cesano (Rome) in July, 1978 (the real age is 85 ± 5 months). It yielded an age of 75 + 8/-5 months through alpha-spectrometry activity measurements, and 85 ± 3 months through gamma-spectrometry activity measurements. A residence time of the fluid in the rock ranging from 3 to 10 centuries has been estimated by comparing the Ra isotopic composition of the fluid with the U/Th ratio of the wall rocks, according to a model proposed by Cherdyntsev (1971).     

Dimensioning of membrane bioreactors for municipal wastewater treatment.

A basic procedure is proposed for dimensioning membrane bioreactors that is generally applicable. It evaluates the required membrane surface with particular consideration of loading combinations and hydraulic loading characteristics; it also takes into account ranges of minimum temperatures and corresponding fluxes as given by suppliers. The procedures, while likely to require further improvement, should make MBR design more transparent and aid the comparison of design variants.     

Photoresponsive optically active polymers—a review

Photoresponsive macromolecules are of interest both as novel organic materials for applications in photodevices and as models for photomodulated biological processes. The presence in polymer chains of photosensitive groups and of chiral groups capable of inducing optical activity into the polymer is very useful for the analysis of photomodulated structural variations and allows storage of the light effect in the form of chiral information. Polypeptides bearing photochromic groups in the side chains are very convenient as the chiroptical properties of the peptide chromophore can be correlated to the backbone conformation. Thus polymers of L-aspartic acid, L-glutamic acid and L-lysine with azobenzene or stilbene groups attached covalently to the side chains are discussed in terms of photoinduced conformational changes and chiroptical information storage in the spectral region of the peptide and of the photoresponsive chromophore. Optically active photochromic macromolecules with hydrocarbon backbone, such as copolymers of (—)-menthyl acrylate with vinyl or acryloyl derivatives of azobenzene, stilbene and indolinospirobenzopyran, also show in some cases photodependence of chiroptical properties with evidence of at least local conformational changes as a consequence of light irradiation which can be used for chiral information.     

Identification of Aminoimidazole and Aminothiazole Derivatives as Src Family Kinase Inhibitors

Src family kinases (SFKs) are a family of non‐receptor tyrosine kinases (TKs) implicated in the regulation of many cellular processes. The aberrant activity of these TKs has been associated with the growth and progression of cancer. In particular, c‐Src is overexpressed or hyperactivated in a variety of solid tumors and is most likely a strong promoting factor for the development of metastasis. Herein, the synthesis of new 4‐aminoimidazole and 2‐aminothiazole derivatives and their in vitro biological evaluation are described for their potential use as SFK inhibitors. Initially, 2‐aminothiazole analogues of dasatinib and 4‐aminoimidazole derivatives were synthesized and tested against the SFKs Src, Fyn, Lyn, and Yes. Five hits were identified as the most promising compounds, with K_i values in the range of 90–480 nm . A combination of molecular docking, homology modeling, and molecular dynamics were then used to investigate the possible binding mode of such compounds within the ATP binding site of the SFKs. Finally, the antiproliferative activities of the best candidates were evaluated against SH‐SY5Y and K562 cell lines. Compound 3 b [2‐(4‐{2‐methyl‐6‐[(5‐phenylthiazol‐2‐yl)amino]pyrimidin‐4‐yl}piperazin‐1‐yl)ethanol] was found to be the most active inhibitor.     

Ascorbate Peroxidase and Catalase Activities and Their Genetic Regulation in Plants Subjected to Drought and Salinity Stresses

Hydrogen peroxide (H₂O₂), an important relatively stable non-radical reactive oxygen species (ROS) is produced by normal aerobic metabolism in plants. At low concentrations, H₂O₂ acts as a signal molecule involved in the regulation of specific biological/physiological processes (photosynthetic functions, cell cycle, growth and development, plant responses to biotic and abiotic stresses). Oxidative stress and eventual cell death in plants can be caused by excess H₂O₂ accumulation. Since stress factors provoke enhanced production of H₂O₂ in plants, severe damage to biomolecules can be possible due to elevated and non-metabolized cellular H₂O₂. Plants are endowed with H₂O₂-metabolizing enzymes such as catalases (CAT), ascorbate peroxidases (APX), some peroxiredoxins, glutathione/thioredoxin peroxidases, and glutathione sulfo-transferases. However, the most notably distinguished enzymes are CAT and APX since the former mainly occurs in peroxisomes and does not require a reductant for catalyzing a dismutation reaction. In particular, APX has a higher affinity for H₂O₂ and reduces it to H₂O in chloroplasts, cytosol, mitochondria and peroxisomes, as well as in the apoplastic space, utilizing ascorbate as specific electron donor. Based on recent reports, this review highlights the role of H₂O₂ in plants experiencing water deficit and salinity and synthesizes major outcomes of studies on CAT and APX activity and genetic regulation in drought- and salt-stressed plants.