Mg/S@g-C3N4 nanosheets: A promising fluorescence sensor for selective Cu2+ detection in water.

This work describes the development of a novel fluorescence sensor based on magnesium/S@g-C3N4 nanosheets for selective detection of copper (Cu2+) ions in water. Mg/S@g-C3N4 nanosheets were prepared by the polycondensation technique and investigated by X-ray diffraction (XRD), ATR-FTIR spectroscopy, scanning electron microscopy (SEM), surface area (BET), and UV-Vis optical absorption measurements. XRD and ATR-FTIR analysis showed the characteristic peaks for S@g-C3N4. The broad full width at half maximum (0.056 radians) implies a smaller crystallite size, representing smaller Mg/S@g-C3N4 sheets. SEM micrograph showed non-exfoliated nanosheets with flake-like structures. The EDS mapping confirmed the presence of magnesium, carbon, nitrogen, and sulfur throughout the nanosheets. The Mg/S@g-C3N4 nanosheets possess a high surface area of 40 m2/g and mesopores within the nanosheets, with a size of 1.57 nm. The band gap of the Mg/S@g-C3N4 nanosheet was estimated to be 3.0 eV. The sensor exhibits a strong quenching response towards Cu2+ ions, with a decrease in fluorescence intensity as the concentration of Cu2+ increased from 1 µM to 20 µM. The Stern-Volmer quenching constant (KSV) showed a relatively high value of 185053 M-1. The estimated value of LOD by the Mg/S@g-C3N4 sensor for Cu2+ was 16.2 nM. The sensor offered high sensitivity and selectivity for Cu2+ detection over other heavy metals.

Thymus Vulgaris Oil Nanoemulsion: Synthesis, Characterization, Antimicrobial and Anticancer Activities.

Essential oil nanoemulsions have received much attention due to their biological activities. Thus, a thyme essential oil nanoemulsion (Th-nanoemulsion) was prepared using a safe and eco-friendly method. DLS and TEM were used to characterize the prepared Th-nanoemulsion. Our findings showed that the nanoemulsion was spherical and ranged in size from 20 to 55.2 nm. The micro-broth dilution experiment was used to evaluate the in vitro antibacterial activity of a Th-emulsion and the Th-nanoemulsion. The MIC50 values of the thymol nanoemulsion were 62.5 mg/mL against Escherichia coli and Klebsiella oxytoca, 250 mg/mL against Bacillus cereus, and 125 mg/mL against Staphylococcus aureus. Meanwhile, it emerged that the MIC50 values of thymol against four strains were not detected. Moreover, the Th-nanoemulsion exhibited promising antifungal activity toward A. brasiliensis and A. fumigatus, where inhibition zones and MIC50 were 20.5 ± 1.32 and 26.4 ± 1.34 mm, and 12.5 and 6.25 mg/mL, respectively. On the other hand, the Th-nanoemulsion displayed weak antifungal activity toward C. albicans where the inhibition zone was 12.0 ± 0.90 and MIC was 50 mg/mL. Also, the Th-emulsion exhibited antifungal activity, but lower than that of the Th-nanoemulsion, toward all the tested fungal strains, where MIC was in the range of 12.5-50 mg/mL. The in vitro anticancer effects of Taxol, Th-emulsion, and Th-nanoemulsion were evaluated using the standard MTT method against breast cancer (MCF-7) and hepatocellular carcinoma (HepG2). Additionally, the concentration of VEGFR-2 was measured, and the activities of caspase-8 (casp-8) and caspase-9 (casp-9) were evaluated. The cytotoxic effect was the most potent against the MCF-7 breast cancer cell line after the Th-nanoemulsion treatment (20.1 ± 0.85 µg/mL), and was 125.1 ± 5.29 µg/mL after the Th-emulsion treatment. The lowest half-maximal inhibitory concentration (IC50) value, 20.1 ± 0.85 µg/mL, was achieved when the MCF-7 cell line was treated with the Th-nanoemulsion. In addition, Th-nanoemulsion treatments on MCF-7 cells led to the highest elevations in casp-8 and casp-9 activities (0.66 ± 0.042 ng/mL and 17.8 ± 0.39 pg/mL, respectively) compared to those with Th-emulsion treatments. In comparison to that with the Th-emulsion (0.982 0.017 ng/mL), the VEGFR-2 concentration was lower with the Th-nanoemulsion treatment (0.672 ± 0.019ng/mL). In conclusion, the Th-nanoemulsion was successfully prepared and appeared in nanoform with a spherical shape according to DLS and TEM, and also exhibited antibacterial, antifungal, as well as anticancer activities.

Pyronaridine as a Bromodomain-Containing Protein 4-N-Terminal Bromodomain (BRD4-BD1) Inhibitor: In Silico Database Mining, Molecular Docking, and Molecular Dynamics Simulation.

BRD4 (bromodomain-containing protein 4) is an epigenetic reader that realizes histone proteins and promotes the transcription of genes linked to cancer progression and non-cancer diseases such as acute heart failure and severe inflammation. The highly conserved N-terminal bromodomain (BD1) recognizes acylated lysine residues to organize the expression of genes. As such, BD1 is essential for disrupting BRD4 interactions and is a promising target for cancer treatment. To identify new BD1 inhibitors, a SuperDRUG2 database that contains more than 4600 pharmaceutical compounds was screened using in silico techniques. The efficiency of the AutoDock Vina1.1.2 software to anticipate inhibitor-BRD4-BD1 binding poses was first evaluated based on the co-crystallized R6S ligand in complex with BRD4-BD1. From database screening, the most promising BRD4-BD1 inhibitors were subsequently submitted to molecular dynamics (MD) simulations integrated with an MM-GBSA approach. MM-GBSA computations indicated promising BD1 binding with a benzonaphthyridine derivative, pyronaridine (SD003509), with an energy prediction (ΔGbinding) of -42.7 kcal/mol in comparison with -41.5 kcal/mol for a positive control inhibitor (R6S). Pharmacokinetic properties predicted oral bioavailability for both ligands, while post-dynamic analyses of the BRD4-BD1 binding pocket demonstrated greater stability for pyronaridine. These results confirm that in silico studies can provide insight into novel protein-ligand regulators, specifically that pyronaridine is a potential cancer drug candidate.

Antimicrobial, Antibiofilm, and Anticancer Activities of Syzygium aromaticum Essential Oil Nanoemulsion.

In the current study, clove oil nanoemulsion (CL-nanoemulsion) and emulsion (CL-emulsion) were prepared through an ecofriendly method. The prepared CL-nanoemulsion and CL-emulsion were characterized using dynamic light scattering (DLS) and a transmission electron microscope (TEM), where results illustrated that CL-nanoemulsion droplets were approximately 32.67 nm in size and spherical in shape, while CL-nanoemulsion droplets were approximately 225.8 nm with a spherical shape. The antibacterial activity of CL-nanoemulsion and CL-emulsion was carried out using a microbroth dilution method. Results revealed that the preferred CL-nanoemulsion had minimal MIC values between 0.31 and 5 mg/mL. The antibiofilm efficacy of CL-nanoemulsion against S. aureus significantly decreased the development of biofilm compared with CL-emulsion. Furthermore, results illustrated that CL-nanoemulsion showed antifungal activity significantly higher than CL-emulsion. Moreover, the prepared CL-nanoemulsion exhibited outstanding antifungal efficiency toward Candida albicans, Cryptococcus neoformans, Aspergillus brasiliensis, A. flavus, and A. fumigatus where MICs were 12.5, 3.12, 0.78, 1.56, and 1.56 mg/mL, respectively. Additionally, the prepared CL-nanoemulsion was analyzed for its antineoplastic effects through a modified MTT assay for evaluating apoptotic and cytotoxic effects using HepG2 and MCF-7 cell lines. MCF-7 breast cancer cells showed the lowest IC50 values (3.4-fold) in CL-nanoemulsion relative to that of CL-emulsion. Thus, CL-nanoemulsion induces apoptosis in breast cancer cells by inducing caspase-8 and -9 activity and suppressing VEGFR-2. In conclusion, the prepared CL-nanoemulsion had antibacterial, antifungal, and antibiofilm as well as anticancer properties, which can be used in different biomedical applications after extensive studies in vivo.

Nanoparticle-laden contact lens for controlled release of vancomycin with enhanced antibiotic efficacy.

Vancomycin is the last resort antibiotic for the treatment of severe bacterial keratitis. Its clinical application is limited due to its hydrophilicity and high molecular weight. To overcome this, this study aims to develop nanoparticles-laden contact lens for controlled ocular delivery of vancomycin. Polyvinyl alcohol (PVA) was used as encapsulant material. The nanoparticles had a negative surface charge and an average size of 147.6 nm. A satisfactory encapsulation efficiency (61.24%) was obtained. The release profile was observed to be slow and sustained, with a release rate of 1.29 µL mg-1 h-1 for 48 h. Five out of 6 test bacteria were suppressed by vancomycin nanoparticles-laden contact lens. Vancomycin is generally ineffective against Gram-negative bacteria and unable to pass through the outer membrane barrier. In this study, vancomycin inhibited Proteus mirabilis and Pseudomonas aeruginosa. Nano-encapsulation enables vancomycin to penetrate the Gram-negative cell wall and further destroy the bacterial cells. On Hohenstein challenge test, all test bacteria exhibited significant reduction in growth when exposed to vancomycin nanoparticles-laden contact lens. This study created an effective and long-lasting vancomycin delivery system via silicone hydrogel contact lenses, by using PVA as encapsulant. The antibiotic efficacy and vancomycin release should be further studied using ocular in vivo models.

SuperNatural inhibitors to reverse multidrug resistance emerged by ABCB1 transporter: Database mining, lipid-mediated molecular dynamics, and pharmacokinetics study.

An effective approach to reverse multidrug resistance (MDR) is P-glycoprotein (P-gp, ABCB1) transport inhibition. To identify such molecular regulators, the SuperNatural II database, which comprises > 326,000 compounds, was virtually screened for ABCB1 transporter inhibitors. The Lipinski rule was utilized to initially screen the SuperNatural II database, identifying 128,126 compounds. Those natural compounds were docked against the ABCB1 transporter, and those with docking scores less than zosuquidar (ZQU) inhibitor were subjected to molecular dynamics (MD) simulations. Based on MM-GBA binding energy (ΔGbinding) estimations, UMHSN00009999 and UMHSN00097206 demonstrated ΔGbinding values of -68.3 and -64.1 kcal/mol, respectively, compared to ZQU with a ΔGbinding value of -49.8 kcal/mol. For an investigation of stability, structural and energetic analyses for UMHSN00009999- and UMHSN00097206-ABCB1 complexes were performed and proved the high steadiness of these complexes throughout 100 ns MD simulations. Pharmacokinetic properties of the identified compounds were also predicted. To mimic the physiological conditions, MD simulations in POPC membrane surroundings were applied to the UMHSN00009999- and UMHSN00097206-ABCB1 complexes. These results demonstrated that UMHSN00009999 and UMHSN00097206 are promising ABCB1 inhibitors for reversing MDR in cancer and warrant additional in-vitro/in-vivo studies.

Large-scale sonochemical fabrication of a Co3O4-CoFe2O4@MWCNT bifunctional electrocatalyst for enhanced OER/HER performances.

Herein, we have prepared a mixed-phase Co3O4-CoFe2O4@MWCNT nanocomposite through a cheap, large-scale, and facile ultrasonication route followed by annealing. The structural, morphological, and functional group analyses of the synthesized catalysts were performed by employing various characterization approaches such as X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). The resultant samples were tested for bifunctional electrocatalytic activity through various electrochemical techniques: cyclic voltammetry (CV), linear sweep voltammetry (LSV), and electrochemical impedance spectroscopy (EIS). The prepared Co3O4-CoFe2O4@MWCNT nanocomposite achieved a very high current density of 100 mA cm-2 at a lower (290 mV and 342 mV) overpotential (vs. RHE) and a smaller (166 mV dec-1 and 138 mV dec-1) Tafel slope in the oxygen evolution reaction (OER) and hydrogen evolution reaction (HER), respectively, compared to Co3O4-CoFe2O4. The excellent electrochemical activity of the as-prepared electrocatalyst was attributed to the uniform incorporation of Co3O4-CoFe2O4 over MWCNTs which provides high redox active sites, a greater surface area, better conductivity, and faster charge mobility. Furthermore, the enhanced electrochemical active surface, low charge-transfer resistance (Rct), and higher exchange current density (J0) of the Co3O4-CoFe2O4@MWCNT ternary composite are attributed to its superior behavior as a bifunctional electrocatalyst. Conclusively, this study demonstrates a novel and large-scale synthesis approach for bifunctional electrocatalysts with a high aspect ratio and abundance of active sites for high-potential energy applications.

Heavy metals biosensor based on defective one-dimensional phononic crystals.

In recent years, the detection of water pollution with low levels of heavy metals has attracted the great attention of many researchers as a result of the imminent danger of this type of pollution to all mankind. Meanwhile, we introduce a theoretical approach based on the one-dimensional phononic crystals (1D-PnCs) with a central defect layer as a novel platform for the highly sensitive detection of heavy metal pollution in freshwater. Therefore, the creation of a resonant peak in the transmittance spectrum related to this defect layer is highly conceivable. In this regard, the detection of cadmium chloride (CdCl2) as a dangerous, toxic, and extremely hazardous heavy metal could be investigated based on the small displacement in the position of this resonant peak with the changes in the CdCl2 concentration. Notably, any change in CdCl2 concentration has a direct impact on its acoustic properties. The theoretical framework of our research study is essentially based on the 2 × 2 transfer matrix method and the acoustic properties of the constituent materials as well. The optimization of all sensor parameters represents the mainstay of this study to get the best sensor performance. In this regard, the proposed sensor has a remarkably high sensitivity (S = 1904.25 Hz/ppm) over a concentration range of 0 - 10000 ppm. In addition, the sensor has a high quality factor (QF), and figure of merit of 1771.318, and 73529410-5 (ppm-1), respectively. Finally, we believe this sensor could be a key component of a feasible platform for detecting low concentrations of different heavy metal ions in freshwater.

Unveiling the non-polar [3+2] cycloaddition reactions of cyclic nitrones with strained alkylidene cyclopropanes within a molecular electron density theory study.

The role of cyclopropane substitution on the ethylene in zw-type [3+2] cycloaddition (32CA) reactions of cyclic nitrones has been studied within Molecular Electron Density Theory (MEDT) at the ωB97X-D/6-311G(d,p) computational level. Electron Localization Function (ELF) analysis of the ethylenes shows that the presence the cyclopropane only slightly increases the electron density in the C-C bonding region. Analysis of the Conceptual DFT reactivity indices indicates that the presence of the cyclopropane does not produce any remarkable change in the reactivity of these strained ethylenes. The marginal electrophilic character of ethylene makes the zw-type 32CA reactions of non-polar character. The presence of the cyclopropane in the ethylene decreases the activation enthalpy of the 32CA reactions by only 1.7 and 2.6 kcal mol-1, and also decreases the ortho regioselectivity. The loss of the strain present in the cyclopropane is responsible for the reduction of the activation enthalpy and the increase of the reaction enthalpy in these non-polar 32CA reactions. The presence of the cyclopropane does not cause any change, neither in the transition state structure (TS) geometries nor in their electronic structure. The very low global electron density transfer (GEDT) computed at the TSs confirms the non-polar character of these 32CA reactions. The ortho regioselectivity experimentally observed in these non-polar 32CA reactions is determined by the most favorable two-center interaction between the less electronegative C1 carbon of nitrone and the non-substituted methylene C5 carbon of the ethylenes.

CdO-supported ZrO2heterojunctions: facile synthesis and rapid visible-light oxidation of atrazine herbicide with superb recyclability.

The advancement in ceramic oxide-based photocatalysis has got much attention recently for environmental issues. Atrazine (AZ) is one of the major used herbicides in agricultural and related industries. This work familiarizes a polymeric-assisted sol-gel preparation of high surface area zirconium oxide (ZrO2) supported with cadmium oxide nanoparticles at minor content (0.5-2.0 wt%). Exploration of the synthesized heterostructures revealed the enhancement of visible-light absorbance and reduction of bandgap energy to 2.76 eV keeping the same crystalline form and high surface area of 170 m2g‒1. The prepared photocatalysts were used to degrade AZ in water at a concentration of 231.8µM (50 ppm). The 1.5%-introduced CdO to ZrO2revealed the best-performed photocatalyst for complete oxidation of AZ within 40 at an optimized dose of 1.6 g l-1. This novel ceramic photocatalyst showed a chemical and structural ability to keep 98.5% of its initial efficiency after five regenerated cycles. The construction of p-n heterojunction between the p-type ZrO2and the n-type CdO contributed to the comprehensive photocatalytic competence toward the efficient charge separation and photooxidation process.

Adsorption of Magenta Dye on PbO Doped MgZnO: Interpretation of Statistical Physics Parameters Using Double-Layer Models.

This article reports the synthesis of PbO doped MgZnO (PbO@MgZnO) by a co-precipitation method, followed by an ultrasonication process. PbO@MgZnO demonstrates a significant adsorption capability toward Magenta Dye (MD). The greatest adsorption capability was optimized by varying parameters such as pH, MD concentration, and adsorbent dose. The kinetics study illustrates that the adsorption of MD on PbO@MgZnO follows the pseudo-second-order. The isotherm study revealed that Langmuir is best fitted for the adsorption, but with little difference in the R2 value of Langmuir and Freundlich, the adsorption process cloud be single or multi-layer. The maximum adsorption capacity was found to be 333.33 mg/g. The negative ΔG refers to the spontaneity of MD adsorption on PbO@MgZnO. The steric parameters from statistical physics models also favor the multi-layer adsorption mechanism. As a function of solution temperature, the parameter n pattern has values of n = 0.395, 0.290, and 0.280 for 298, 308, and 318 K, respectively (i.e., all values were below 1). Therefore, horizontal molecule positioning and multiple locking mechanisms were implicated during interactions between MD and PbO@MgZnO active sites.

Mesopores silica nanotubes-based sensors for the highly selective and rapid detection of Fe2+ ions in wastewater, boiler system units and biological samples.

Mesopores silica nanotubes (MSNTs)-based chemical sensors for the rapid detection and of highly selective Fe2+ ions have been prepared. The novel nanosensors were prepared via immobilization of 1,10-phenanthroline-5-amine (PA) and bathophenanthroline (BP) onto the MSNTs. The resultant PA and BP sensors display high sensitivity for detection the Fe2+ ions in tap water, river water, sea water, two units in simple cycle power station, and biological samples. More interestingly, upon meeting ultra-trace amount of Fe2+ ions, a red complex appears at once. Color changes can be seen from the naked eye and tracked with a smartphone or spectrophotometric techniques. The response time that is necessary to achieve a stable signal was less than 15 s. The Univariate (Univar) calibration technique had been utilized for the determination of figures of merits. The detection limit obtained from the digital image analysis was 19 ppb (7.04 × 10-7 M) for Fe2+ ions, while the obtained from the spectrophotometric method was 6.7 ppb (2.48 × 10-7 M). Therefore, the two sensors had been successfully used in the determination of Fe2+ in several real samples with high sensitivity and selectivity. In addition, they can be used as a simple, rapid, and portable method to detect and quantify the pre rust in any cooler system.

Intense Visible-Light Absorption in SrRuO3/C3N4 Heterostructures for the Highly Efficient Reduction of Hg(II).

Strontium ruthenium oxide (SrRuO3) is recognized as a metallic itinerant ferromagnet and utilized as a conducting electrode in heterostructure oxides with unforeseen optical characteristics, including remarkably low-reflection and high-absorption visible-light spectrum compared to classical metals. By coupling mesoporous SrRuO3 nanoparticles (NPs) with porous g-C3N4 nanosheets for the first time, we evidence remarkably promoted visible light absorption and superior photocatalytic performances for Hg(II) reduction under illumination with visible light. The photocatalytic performance of g-C3N4 increased upon boosting the SrRuO3 percentage to 1.5%, and this (1.5% SrRuO3/g-C3N4 heterostructure) is considered the optimum condition to obtain a high photocatalytic efficiency of about 100% within 50 min. It was promoted 3.68 and 5.75 times compared to SrRuO3 and g-C3N4, respectively. Also, a Hg(II) reduction rate of 1.5% SrRuO3/g-C3N4 was enhanced3.84- and 6.28-fold than those of pure SrRuO3 NPs and g-C3N4, respectively. Such a high photocatalytic performance over SrRuO3/g-C3N4 photocatalysts was explained by the characteristics of SrRuO3 NPs incorporated on porous g-C3N4 layers, which demonstrate strong absorption of visible light with a narrow band gap, a large photocurrent density of ∼9.07 mA/cm2, well-dispersed and small particle sizes, and cause facile diffusion of HCOOH and Hg(II) ions and electrons. The present work provides a dramatic novel approach to the challenge of constructing visible-light photosensitive photocatalysts for wastewater remediation.

CoAl2O4-g-C3N4 Nanocomposite Photocatalysts for Powerful Visible-Light-Driven Hydrogen Production.

There is no doubt that the rate of hydrogen production via the water splitting reaction is profoundly affected to a remarkable degree based on the isolation of photogenerated electrons from holes. The precipitation of any cocatalysts on the substrate surfaces (including semiconductor materials) provides significant hindrance to such reincorporation. In this regard, a graphite-like structure in the form of mesoporous g-C3N4 formed in the presence of a template of mesoporous silica has been synthesized via the known combustion method. Hence, the resulting g-C3N4 nanosheets were decorated with varying amounts of mesoporous CoAl2O4 nanoparticles (1.0-4.0%). The efficiencies of the photocatalytic H2 production by CoAl2O4-doped g-C3N4 nanocomposites were studied and compared with those of pure CoAl2O4 and g-C3N4. Visible light irradiation was carried out in the presence of glycerol as a scavenger. The results showed that the noticeable photocatalytic enhancement rate was due to the presence of CoAl2O4 nanoparticles distributed on the g-C3N4 surface. The 3.0% CoAl2O4-g-C3N4 nanocomposite had the optimum concentration. This photocatalyst showed extremely high photocatalytic activities that were up to 22 and 45 times greater than those of CoAl2O4 and g-C3N4, respectively. This photocatalyst also showed 5 times higher photocatalytic stability than that of CoAl2O4 or g-C3N4. The presence of CoAl2O4 nanoparticles as a cocatalyst increased both the efficiency and productivity of the CoAl2O4-g-C3N4 photocatalyst. This outcome was attributed to the mesostructures being efficient charge separation carriers with narrow band gaps and high surface areas, which were due to the presence of CoAl2O4.

Anticryptosporidial effect of pomegranate peels water extract in experimentally infected mice with special reference to some biochemical parameters and antioxidant activity.

Cryptosporidiosis is a zoonotic disease caused by a well-known parasitic protozoan called Cryptosporidium. Infection in livestock causes important economic losses among farm animals and its control has a global concern. In this study, internal white and external red layers were separated from pomegranate peels (Punica granatum) then; they were grinded to reach Nano form. Anticryptosporidial effect of their water extracts was investigated in experimentally infected mice. Also, their antioxidant activity, biochemical and histopathological changes were studied. Briefly, hot aqueous extracts of pomegranate peels were prepared regarding its good sensory attributes at concentration of 10% W/V. Analysis of total phenolics, individual phenolics by HPLC-DAD and antioxidant activities have been done. Forty-five mice were divided into five groups each one containing nine mice. The first group was healthy mice and the 2nd one was infected orally with 104 Cryptosporidium parvum (C. parvum) oocysts/mice and not treated. The other 3 groups were infected and orally treated with Nitazoxanide (NTZ) for the 3rd group, pomegranate red peel extract for the 4th group and pomegranate white peel extract for the 5th group. Blood samples were collected after 1 and 2 weeks post treatment for protein profile, liver enzymes and antioxidant activity evaluation. After 3 weeks, all animals were sacrificed and ileal tissues were embedded in paraffin for histopathological examination. The results showed that pomegranate peel extracts were rich in phenolic compounds, had high antioxidant activity and therapeutic effect on C. parvum in experimentally infected mice. Red peel extract diminished C. parvum oocysts count significantly in experimentally infected mice than white peel and NTZ treatments. Also, the histopathological examination revealed that red peel treated mice ileal sections showed a great enhancement in the shape and structure of villi towards normal structure than other treated groups. Most of the measured biochemical parameters after 2 weeks' treatment with red pomegranate peel and NTZ were enhanced in their concentrations towards the healthy normal status. In conclusion, this study showed the effectiveness of Nano-form of pomegranate white and red peel extracts against C. parvum oocysts. Pomegranate red peel extract was found to have antioxidant activity that could significantly enhance the serum biochemical parameters and oxidative stress towards the healthy normal status. Furthermore, it is suggested that pomegranate peel should be separated and used in the daily animal diet or as a functional beavarage for human as accepted from the panelists to give protective effects against this parasite as well as to improve health benefits.

Glucosamine modulates propranolol pharmacokinetics via intestinal permeability in rats.

Propranolol (PROP) undergoes extensive first-pass metabolism by the liver resulting in a relatively low bioavailability (13-23%); thus, multiple oral doses are required to achieve therapeutic effect. Since some studies have reported that glucosamine (GlcN) can increase the bioavailability of some drugs, therefore, it is aimed to study whether GlcN can change the pharmacokinetic parameters of PROP, thus modulating its bioavailability. When PROP was orally co-administered with GlcN (200mg/kg) to rats, PROP area under curve (AUC) and maximum concentration (Cmax) were significantly decreased by 43% (p<0.01) and 33% (p<0.05), respectively. In line with the in vivo results, in silico simulations confirmed that GlcN decreased rat intestinal effective permeability (Peff) and increased PROP clearance by 50%. However, in situ single pass intestinal perfusion (SPIP) experiments showed that GlcN significantly increased PROP serum levels (p<0.05). Furthermore, GlcN decreased PROP disposition/distribution into cultured hepatocytes in concentration dependent manner. Such change in the interaction pattern between GlcN and PROP might be attributed to the environment of the physiological buffer used in the in vitro experiments (pH7.2) versus the oral administration and thus, enhanced PROP permeability. Nevertheless, such enhancement was not detected when everted gut sacks were incubated with both drugs at the same pH in vitro. In conclusion, GlcN decreased PROP serum levels in rats in a dose-dependent manner. Such interaction might be attributed to decreased intestinal permeability and enhanced clearance of PROP in the presence of GlcN. Further investigations are still warranted to explain the in vitro inhibitory action of GlcN on PROP hepatocytes disposition and the involvement of GlcN in the intestinal and hepatic metabolizing enzymes of PROP at different experimental conditions.

Preparation of Chito-Oligomers by Hydrolysis of Chitosan in the Presence of Zeolite as Adsorbent.

An increasing interest has recently been shown to use chitin/chitosan oligomers (chito-oligomers) in medicine and food fields because they are not only water-soluble, nontoxic, and biocompatible materials, but they also exhibit numerous biological properties, including antibacterial, antifungal, and antitumor activities, as well as immuno-enhancing effects on animals. Conventional depolymerization methods of chitosan to chito-oligomers are either chemical by acid-hydrolysis under harsh conditions or by enzymatic degradation. In this work, hydrolysis of chitosan to chito-oligomers has been achieved by applying adsorption-separation technique using diluted HCl in the presence of different types of zeolite as adsorbents. The chito-oligomers were retrieved from adsorbents and characterized by differential scanning calorimetry (DSC), liquid chromatography/mass spectroscopy (LC/MS), and ninhydrin test.

Influence of glucosamine on the bioactivity of insulin delivered subcutaneously and in an oral nanodelivery system.

The aim of the work reported herein was to study the effect of glucosamine HCl (GlcN·HCl) on the bioactivity (BA) of insulin, administered via subcutaneous (SC) and oral routes, in adult male Sprague Dawley rats. The oral insulin delivery system (insulin-chitosan reverse micelle [IC-RM]) was prepared by solubilizing insulin-chitosan (13 kDa) polyelectrolyte complex in a RM system consisting of oleic acid, PEG-8 caprylic/capric glycerides, and polyglycerol-6-dioleate. The BA of insulin in vivo was evaluated by measuring blood glucose level using a blood glucose meter; the results revealed that the extent of hypoglycemic activity of SC insulin was GlcN·HCl dose dependent when they were administered simultaneously. A significant reduction in blood glucose levels (P<0.05) was found for the insulin:GlcN·HCl at mass ratios of 1:10 and 1:20, whereas lower ratios (eg, 1:1 and 1:4) showed no significant reduction. Furthermore, enhancement of the action of SC insulin was achieved by oral administration of GlcN·HCl for 5 consecutive days prior to insulin injection (P<0.05). For oral insulin administration via the IC-RM system, the presence of GlcN·HCl increased the hypoglycemic activity of insulin (P<0.05). The relative BA were 6.7% and 5.4% in the presence and absence of GlcN·HCl (ie, the increase in the relative BA was approximately 23% due to incorporating GlcN·HCl in the IC-RM system), respectively. The aforementioned findings offer an opportunity to incorporate GlcN·HCl in oral insulin delivery systems in order to enhance a reduction in blood glucose levels.

Prasugrel Hydrochloride.

A comprehensive profile of prasugrel HCl is reported herein with 158 references. A full description including nomenclature, formulae, elemental analysis, and appearance is included. Methods of preparation for prasugrel HCl, its intermediates, and derivatives are fully discussed. In addition, the physical properties, analytical methods, stability, uses and applications, and pharmacology of prasugrel HCl are also discussed.

Influence of glutathione on the bioactivity of subcutaneously or orally administered insulin to rats.

The effect of reduced (GSH) and oxidized (GSSG) glutathione on the bioactivity of insulin was studied. A polyelectrolyte complex (PEC) of insulin with low molecular weight chitosan (13 kDa) was prepared and characterized. The PEC was then solubilized, in the presence and absence of GSH and GSSG, in a reverse micelle consisting of oleic acid and two surfactants (PEG-8 caprylic/capric glycerides and polyglycerol-6-dioleate). The in vitro and in vivo performances of the reverse micelle formulations (RMFs) were evaluated in rats. At pH 6.5 the association efficiency of the PEC was 76.2%. In vitro insulin release from the RMs was negligible at pH 1.2 and was markedly increased at pH 6.8. The hypoglycemic activity of insulin in the PEC was reduced when administered via the subcutaneous route, regardless of the GSH content. On the other hand, the presence of GSSG significantly enhanced hypoglycemia. When the RMF was administered via the oral route, the presence of GSH had no effect on the hypoglycemic activity of insulin compared with the GSH free system. However, the presence of GSSG in the oral preparation increased the hypoglycemic activity of insulin; probably by inhibiting insulin degradation, thereby prolonging its effect. Thus, incorporation of GSSG in the RMF reduces blood glucose levels in rats and protects insulin from degradation.