Sodium bicarbonate‐gelled chitosan beads as mechanically stable carriers for the covalent immobilization of enzymes

The poor mechanical stability of chitosan has long impeded its industrial utilization as an immobilization carrier. In this study, the mechanical properties of chitosan beads were greatly improved through utilizing the slow rate of the sodium bicarbonate‐induced chitosan gelation and combining it with the chemical cross‐linking action of glutaraldehyde (GA). The GA‐treated sodium bicarbonate‐gelled chitosan beads exhibited much better mechanical properties and up to 2.45‐fold higher observed activity of the immobilized enzyme (β‐D‐galactosidase (β‐gal)) when compared to the GA‐treated sodium tripolyphosphate (TPP)‐gelled chitosan beads. The differences between the sodium bicarbonate‐gelled and the TPP‐gelled chitosan beads were proven visually and also via scanning electron microscopy, elemental analysis, and differential scanning calorimetry. Moreover, the optimum pH, the optimum temperature, the apparent K_m, and the apparent V_max of the β‐gals immobilized onto the two aforementioned types of chitosan beads were determined and compared. A reusability study was also performed. This study proved the superiority of the sodium bicarbonate‐gelled chitosan beads as they retained 72.22 ± 4.57% of their initial observed activity during the 13^th reusability cycle whereas the TPP‐gelled beads lost their activity during the first four reusability cycles, owing to their fragmentation. © 2017 American Institute of Chemical Engineers Biotechnol. Prog., 34:347–361, 2018     

Evaluation of nanoselenium and nanogold activities against murine intestinal schistosomiasis

Nanomedicine is one of the most important methods used to treat human diseases including parasitic diseases. Schistosomiasis is a major parasitic disease that affects human health in tropical regions. Whilst Praziquantel is the main classic antischistosomal drug, new drugs are required due to the poor effect of the drug on the parasite juveniles and immature worms, and the emergence of drug resistant strains of Schistosoma. The present study aimed to examine the curative roles of both gold and selenium nanoparticles on jejunal tissues of mice infected with Schistosoma mansoni. Transmission electron microscopy was used for characterization of nanoparticles. Gold nanoparticles of 1 mg/kg mice body weight and selenium nanoparticles 0.5 mg/kg body weight were inoculated separately into mice infected with S. mansoni. The parasite induced a significant decrease in glutathione levels; however, the levels of nitric oxide and malondialdehyde were significantly increased. Additionally, the parasite introduced deteriorations in histological architecture of the jejunal tissue. Treatment of mice with metal nanoparticles reduced the levels of body weight changes, oxidative stress and histological impairment in the jejunal tissue significantly. Therefore, our results revealed the protective role of both selenium and gold nanoparticles against jejunal injury in mice infected with S. mansoni.     

Carbon metabolism in in vitro cultures of date palm: the role of carboxylases (PEPC and RubisCO)

While describing major trends of carbon metabolism during the initiation and expression of somatic embryogenesis in date palm (Phoenix dactylifera L., cv. Deglet Nour), we have investigated the role of two carboxylases, namely PEPC (Phosphoenolpyruvate carboxylase, EC 4.1.1.31) and RubisCO (Ribulose 1,5-bisphosphate carboxylase/oxygenase, EC 4.1.1.39), in embryogenic and non-embryogenic cultures. The detection of PEPC activity on polyacrylamide native gels after electrophoresis revealed the presence of 3 active isoforms in crude extracts from the embryogenic (E) callus strain, whereas only a single band was present in the non-embryogenic (NE) one. The level of PEPC specific capacity was of the same order (3.9 ± 1.2 μmol CO₂ h⁻¹ mg⁻¹ TSP) in both types of cultures. Further changes in carboxylase (PEPC and RubisCO) activities during the growth and development of somatic embryo–derived plantlets were also analysed. The PEPC/RubisCO ratio was found to progressively decrease (from 17.7 to 0.2) throughout the in vitro development of plantlets, due to a substantial depletion of PEPC activity, which decreased from 5.3 to 1.2 μmol CO₂ h⁻¹ mg⁻¹ TSP. Concomitantly, RubisCO assumed greater importance (from 0.3 to 5.3 μmol CO₂ h⁻¹ mg⁻¹ _TSP ) and became the main route for inorganic carbon fixation. Western blot analysis using polyclonal antibodies raised against PEPC and RubisCO purified from tobacco leaves confirmed this trend in terms of relative enzyme abundance. This revised version was published online in June 2006 with corrections to the Cover Date.     

Derivative emission spectrofluorimetry: Application to the analysis of newly approved FDA combination of ibuprofen and famotidine in tablets

A new combination of ibuprofen (NSAID) and famotidine (H₂ receptor antagonist) was recently approved by the FDA. It was formulated to relief pain while decreasing the risk of ulceration, which is a common problem for patients receiving NSAID. A rapid and simple derivative emission spectrofluorimetric method is proposed for the simultaneous analysis of this combination in their pharmaceutical preparation. The method is based upon measurement of the native fluorescence intensity of the two drugs at λ_ex = 233 nm in acetonitrile. The emission data were differentiated using the first (D1) derivative technique. The plots of derivative fluorescence intensity versus concentration were rectilinear over a range of 2–35 and 0.4–8 µg/mL for both ibuprofen (IBU) and famotidine (FAM), respectively. The method was sensitive as the limits of detection were 0.51 and 0.12 µg/mL and limits of quantitation were 1.70 and 0.39 µg/mL, for IBU and FAM respectively. The proposed derivative emission spectrofluorimetric method was successfully applied for the determination of the two drugs in their synthetic mixtures and tablets with good accuracy and precision. The proposed method was validated as per ICH guidelines. Copyright © 2014 John Wiley & Sons, Ltd.     

Management of Citrus sinensis peels for protection and treatment against gastric ulcer induced by ethanol in rats

Abstract

Introduction: Stomach ulcer is one of the most prevalent disorders worldwide. The study was aimed to isolate and characterize the major polymethoxylated flavonoids in Citrus sinensis peels petroleum ether extract and investigate its protective and curative effect on gastric ulcer.

Material and methods: Some spectral analyses were used for identification of the isolated compounds from the petroleum ether extract of Citrus sinensis peels. One oral dose (0.5?ml/100?g b.wt.) of absolute ethanol was orally given to rats after starvation for 24?h to induce gastric ulcer. To explore the protective and curative role of the plant extract, it was orally (250?mg/kg b.wt.) given for 1 week either before or post-ulcer induction. A reference drug, ranitidine (100?mg/kg b.wt.), was also evaluated. Stomach acidity, gastric volume, lesion counts, glutathione (GSH), superoxide dismutase (SOD), malondialdehyde (MDA), succinate dehydrogenase (SDH), lactate dehydrogenase (LDH), acid phosphatase (AP), interlukin-10 (IL-10) and prostaglandin E2 (PGE2) were estimated. Stomach histopathological features were monitored.

Results: Nine polymethoxy flavonoids were identified from the extract. Treatment with C. sinensis peels extract recorded amelioration in all parameters.

Conclusion: Citrus sinensis petroleum ether peels extract had protective and curative effects against gastric ulcer. Therefore, the extract recorded anti-secretory, anti-ulcerative, anti-inflammatory, and antioxidant effects. Its healing action exceeded its protective role due to its richness in polymethoxylated flavonoids     

Lichenochemical Screening and Antioxidant Capacity of Four Tunisian Lichen Species

The phenolic composition and antioxidant capacity of four Tunisian lichen species, Cladonia rangiformis, Flavoparmelia caperata, Squamarina cartilaginea and Xanthoria parietina, were determined in order to provide a better understanding of their lichenochemical composition. Powdered material of F. caperata was the richest in total phenolic content (956.68 μg GAE g⁻¹ DW) and S. cartilaginea in proanthocyanidin content (77.31 μg CE g⁻¹ DW), while the acetone extract of X. parietina showed the highest flavonoid content (9.56 μg CE g⁻¹ DW). The antioxidant capacity of all lichen extracts and crude material was evaluated by DPPH^. scavenging, iron-chelating, and iron-reducing powers. Results showed that methanol extracts of S. cartilaginea had the highest DPPH^. antioxidant capacity (IC₅₀=0.9 μg mL⁻¹) and the highest iron-reducing power was attributed to the acetone extract of this species. All extracts of all species were further screened by Fourier-transform infrared spectroscopy (FT-IR) and nuclear resonance spectroscopy (NMR); results showed an abundance of phenols, aromatic compounds, and fatty acids. Overall, our results showed that the investigated species are a rich source of potentially bioactive compounds with valuable properties.     

Impact of priming on global soil carbon stocks

Fresh carbon input (above and belowground) contributes to soil carbon sequestration, but also accelerates decomposition of soil organic matter through biological priming mechanisms. Currently, poor understanding precludes the incorporation of these priming mechanisms into the global carbon models used for future projections. Here, we show that priming can be incorporated based on a simple equation calibrated from incubation and verified against independent litter manipulation experiments in the global land surface model, ORCHIDEE. When incorporated into ORCHIDEE, priming improved the model's representation of global soil carbon stocks and decreased soil carbon sequestration by 51% (12 ± 3 Pg C) during the period 1901–2010. Future projections with the same model across the range of CO₂ and climate changes defined by the IPCC‐RCP scenarios reveal that priming buffers the projected changes in soil carbon stocks — both the increases due to enhanced productivity and new input to the soil, and the decreases due to warming‐induced accelerated decomposition. Including priming in Earth system models leads to different projections of soil carbon changes, which are challenging to verify at large spatial scales.     

Brain Barrier Breakdown as a Cause and Consequence of Neuroinflammation in Sepsis

The blood-brain barrier (BBB) and the blood-cerebrospinal fluid barrier (BCSFB) are important for the maintenance of brain homeostasis. During sepsis, peripheral production of proinflammatory cytokines and reactive oxygen species are responsible for structural alterations in those brain barriers. Thus, an increasing permeability of these barriers can lead to the activation of glial cells such as microglia and the production of cytotoxic mediators which in turn act on the brain barriers, damaging them further. Thereby, in this review, we try to highlight how the brain barrier’s permeability is not only a cause but a consequence of brain injury in sepsis.     

Tablet formulation containing meloxicam and β-cyclodextrin: Mechanical characterization and bioavailability evaluation

The purpose of this research was to evaluate β-cyclodextrin (β-CD) as a vehicle, either singly or in blends with lactose (spray-dried or monohydrate), for preparing a meloxicam tablet. Aqueous solubility of meloxicam in presence of β-CD was investigated. The tablets were prepared by direct compression and wet granulation techniques. The powder blends and the granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, disintegration time, and in vitro dissolution studies. The effect of β-CD on the bioavailability of meloxicam was also investigated in human volunteers using a balanced 2-way crossover study. Phase-solubility studies indicated an A_L-type diagram with inclusion complex of 1∶1 molar ratio. The powder blends and granules of all formulations showed satisfactory flow properties, compressibility, and drug content. All tablet formations prepared by direct compression or wet granulation showed acceptable mechanical properties. The dissolution rate of meloxicam was significantly enhanced by inclusion of β-CD in the formulations up to 30%. The mean pharmacokinetic parameters (C_max, K_e, and area under the curve [AUC]_0−∞) were significantly increased in presence of β-CD. These results suggest that β-CD would facilitate the preparation of meloxicam tablets with acceptable mechanical properties using the direct compression technique as there is no important difference between tablets prepared by direct compression and those prepared by wet granulation. Also, β-CD is particularly useful for improving the oral bioavailablity of meloxicam.