In silico approaches to identify the potential inhibitors of glutamate carboxypeptidase II (GCPII) for neuroprotection.

To develop a potential inhibitor for glutamate carboxypeptidase II (GCPII) effective against all the eight common genetic variants reported, PyMOL molecular visualization system was used to generate models of variants using the crystal structure of GCPII i.e. 2OOT as a template.

Development and evaluation of PLGA polymer based nanoparticles of quercetin.

Quercetin is the most abundant antioxidant found in the human diet. Low aqueous solubility of quercetin limits its bioavailability and hence therapeutic effects. Therefore, the aim of the present study was to develop a poly lactide-co-glycolic acid (PLGA) polymer based nanoparticles of quercetin with a view to improve its aqueous solubility and examine the effect on its antioxidant and diuretic properties.

An Overview of the Regulatory and Developmental Strategies of Chronotherapeutics.

The pivotal idea toward the development of chronotherapeutics is synchronizing the in vivo drug bioavailability with the rhythms of the disease to optimize therapeutic outcomes and minimize side effects, which is contrary to the homeostatic theory of drug delivery. The advent of formulation technologies, marketing exclusivities of innovative products, and provisions/amendments in regulatory frameworks have led to the development of commercial chronotherapeutic products, but their numbers are few and are confined mainly to diseases of the cardiovascular system. A major bottleneck for its development would be the understanding of rhythmic variations of disease, but following regulatory pathways for commercial development has always been challenging.

A review on the strategies for oral delivery of proteins and peptides and their clinical perspectives.

In the modern world, a number of therapeutic proteins such as vaccines, antigens, and hormones are being developed utilizing different sophisticated biotechnological techniques like recombinant DNA technology and protein purification. However, the major glitches in the optimal utilization of therapeutic proteins and peptides by the oral route are their extensive hepatic first-pass metabolism, degradation in the gastrointestinal tract (presence of enzymes and pH-dependent factors), large molecular size and poor permeation. These problems can be overcome by adopting techniques such as chemical transformation of protein structures, enzyme inhibitors, mucoadhesive polymers and permeation enhancers.

Potential Health Benefits and Metabolomics of Camel Milk by GC-MS and ICP-MS.

None of the research reports reveals the metabolomics and elemental studies on camel milk. Recent studies showed that camel milk possesses anticancer and anti-inflammatory activity. Metabolomics and elemental studies were carried out in camel milk which showed us the pathways and composition that are responsible for the key biological role of camel milk.

Deleterious effects of incense smoke exposure on kidney function and architecture in male albino rats.

Context: Previous studies, including ours, have shown adverse effects of incense smoke on human health. However, the effect of incense smoke on kidney function and structure remains unknown.

Objective: To evaluate possible adverse effects of incense smoke on kidney function and architecture in albino rats after chronic exposure to Arabian incense.

Analysis of anti-neoplastic drug in bacterial ghost matrix, w/o/w double nanoemulsion and w/o nanoemulsion by a validated 'green' liquid chromatographic method.

The objective of the present investigation was to develop and validate a 'green' reversed phase high-performance liquid chromatography (RP-HPLC) method for rapid analysis of a cytotoxic drug 5-fluorouracil (5-FU) in bulk drug, marketed injection, water-in-oil (w/o) nanoemulsion, double water-in-oil-in-water (w/o/w) nanoemulsion and bacterial ghost (BG) matrix. The chromatography study was carried out at room temperature (25±1°C) using an HPLC system with the help of ultraviolet (UV)-visible detector. The chromatographic performance was achieved with a Nucleodur 150mm×4.

Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system.

Objective: The current studies were undertaken to enhance dissolution and bioavailability/pharmacokinetic profile of a newly approved anticancer drug ibrutinib (IBR) via encapsulation of drug into self-nanoemulsifying drug delivery system (SNEDDS).

Methods: Various SNEDDS formulations of IBR were developed by aqueous phase titration method using Capryol-PGMC (oil phase), Tween-20 (surfactant), Carbitol (cosurfactant) and water (aqueous phase). Developed SNEDDS of IBR was evaluated in vitro for various physicochemical properties and drug release profile.

Artificial neural network-based exploration of gene-nutrient interactions in folate and xenobiotic metabolic pathways that modulate susceptibility to breast cancer.

In the current study, an artificial neural network (ANN)-based breast cancer prediction model was developed from the data of folate and xenobiotic pathway genetic polymorphisms along with the nutritional and demographic variables to investigate how micronutrients modulate susceptibility to breast cancer. The developed ANN model explained 94.2% variability in breast cancer prediction.

Antioxidant Potential and In Situ Analysis of Major and Trace Element Determination of Ood-saleeb, a Known Unani Herbal Medicine by ICP-MS.

The intention of the present research work was to investigate the antioxidant activity and trace element analysis of Ood-saleeb, a known herbal medicine. Preliminary screening of phytochemicals showed that the extract of Ood-saleeb had flavonoids and phenolics. The significant activities in all antioxidant assays were observed in the extract of Ood-saleeb in comparison with the standard antioxidant with respect to dose of Ood-saleeb.

Copper-Induced Inactivation of Camel Liver Glutathione S-Transferase.

Glutathione S-transferases (GSTs) are multifunctional enzymes and play an important role in detoxification of xenobiotics and protection against oxidative stress. Camel liver glutathione transferase (cGST) was recently isolated and characterized in our lab. In this study, we have evaluated the effect of monovalent, divalent, and trivalent cations on its activity and stability.

Solubility and thermodynamic behavior of vanillin in propane-1,2-diol+water cosolvent mixtures at different temperatures.

The solubilities of bioactive compound vanillin were measured in various propane-1,2-diol+water cosolvent mixtures at T=(298-318)K and p=0.1 MPa. The experimental solubility of crystalline vanillin was determined and correlated with calculated solubility.

Dissolution thermodynamics and solubility of silymarin in PEG 400-water mixtures at different temperatures.

An isothermal method was used to measure the solubility of silymarin in binary polyethylene glycol 400 (PEG 400) + water co-solvent mixtures at temperatures T = 298.15-333.15 K and pressure p = 0.

Ultrastructural changes, increased oxidative stress, inflammation, and altered cardiac hypertrophic gene expressions in heart tissues of rats exposed to incense smoke.

Incense smoke exposure has recently been linked to cardiovascular disease risk, heart rate variability, and endothelial dysfunction. To test the possible underlying mechanisms, oxidative stress, and inflammatory markers, gene expressions of cardiac hypertrophic and xenobiotic-metabolizing enzymes and ultrastructural changes were measured, respectively, using standard, ELISA-based, real-time PCR, and transmission electron microscope procedures in heart tissues of Wistar rats after chronically exposing to Arabian incense. Malondialdehyde, tumor necrosis alpha (TNF)-α, and IL-4 levels were significantly increased, while catalase and glutathione levels were significantly declined in incense smoke-exposed rats.

Quantification of glycyrrhizin in anti-stress herbal formulations by validate HPTLC method: a rational paradigm towards quality control of herbals.

In the present study an analytical method of high-performance thin-layer chromatography (HPTLC) has been developed for quantification of glycyrrhizin for marketed antistressliquorice root capsules (LRC) and herbal tea (HT). Chromatography was performed by using mobile phase ethyl acetate (EA): glacial acetic acid (GAA): Methanol (MeOH): water (H(2)O) in proportion of 6:2:2:1, v/v/v/v. The developed plate was scanned and quantified densitometrically at absorption maxima 254nm.

Removal of alizarin red from aqueous solution by ethyl acetate green nanoemulsions.

The objective of the present study was to develop ethyl acetate (EA) green nanoemulsions for removal of alizarin red (AR) from water. Developed formulations were characterized in terms of thermodynamic stability, self-nanoemulsification efficiency, droplet size, polydispersity, viscosity, refractive index and per cent transmittance. Adsorption studies were performed by mixing small amounts of green nanoemulsions (1 ml) with relatively large amounts of AR solution (10 ml).

Development and validation of UHPLC-MS/MS assay for rapid determination of a carvone Schiff base of isoniazid (CSB-INH) in rat plasma: application to pharmacokinetic study.

In this study, a fast UHPLC-MS/MS method was developed and validated for the determination of a novel potent carvone Schiff base of isoniazid (CSB-INH) in rat plasma using carbamazepine as an internal standard (IS). After a single-step protein precipitation by acetonitrile, CSB-INH and IS were separated on an Acquity BEH(TM) C18 column (50 × 2.1 mm, 1.

Cloning and Expression Profiling of the Polycomb Gene, Retinoblastoma-related Protein from Tomato Solanum lycopersicum L.

Cell cycle regulation mechanisms appear to be conserved throughout eukaryotic evolution. One of the important proteins involved in the regulation of cell cycle processes is retinoblastoma-related protein (RBR), which is a negative regulator of cell cycle progression, controlling the G1/S transition in plants and animals. In this study, we present the cloning and genomic structure of a putative SlRBR gene in the tomato Solanum lycopersicum L.

Surface-adsorbed reverse micelle-loaded solid self-nanoemulsifying drug delivery system of talinolol.

The aim of present investigation was to develop surface-adsorbed reverse-micelle-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) of talinolol in order to enhance its in vitro dissolution rate, which in turn enhance the bioavailability. SNEDDS were prepared using aqueous phase titration method. Thermodynamically stable formulations were characterized in terms of droplet size, viscosity, % transmittance, drug content and surface morphology.

Rapid Analysis of Glibenclamide Using an Environmentally Benign Stability-Indicating RP-HPLC Method.

An environmentally benign RP-HPLC approach for rapid analysis of glibenclamide in pure form, developed nanoemulsion and commercial tablets was developed and validated in present investigation. The green chromatographic identification was performed on Lichrosphere 250 X 4.0 mm RP C8 column having a 5 μm packing as a stationary phase using a combination of ethanol: methanol (50:50 % v/v) as a mobile phase, at a flow rate of 1.

Whole serum 3D LC-nESI-FTMS quantitative proteomics reveals sexual dimorphism in the milieu intérieur of overweight and obese adults.

Linking gender-specific differences to the molecular etiology of obesity has been largely based on genomic and transcriptomic evidence lacking endophenotypic insight and is not applicable to the extracellular fluid compartments, or the milieu intérieur, of the human body. To address this need, this study profiled the whole serum proteomes of age-matched nondiabetic overweight and obese females (n = 28) and males (n = 31) using a multiplex design with pooled biological and technical replicates. To bypass basic limitations of immunodepletion-based strategies, subproteome enrichment by size-exclusion chromatography (SuPrE-SEC) followed by iTRAQ 2D-LC-nESI-FTMS analysis was used.

Vitamin D receptor gene polymorphisms are associated with obesity and inflammosome activity.

To explore the mechanisms underlying the suggested role of the vitamin D/vitamin D receptor (VDR) complex in the pathogenesis of obesity we performed genetic and immunologic analyses in obese and non-obese Saudi individuals without other concomitant chronic diseases. Genomic DNA was genotyped for gene single nucleotide polymorphisms (SNPs) of VDR by allelic discrimination in 402 obese (body mass index -BMI≥30 kg/m2) and 489 non-obese (BMI<30 kg/m2) Saudis. Q-PCR analyses were performed using an ABI Prism 7000 Sequence Detection System.

Gender-dependent associations between socioeconomic status and metabolic syndrome: a cross-sectional study in the adult Saudi population.

Background: To determine the gender-dependent association of socio-economic status variables with the prevalence of metabolic syndrome (MetS) in the adult Saudi population.

Methods: A total of 9164 adult Saudis (aged 18-70 years) were included in this cross-sectional study. Marital status, income, education, and occupation were used as socio-economic indicators while behavioral factor like physical exercise was also taken into account.

Association of VDR-gene variants with factors related to the metabolic syndrome, type 2 diabetes and vitamin D deficiency.

The prevalence of metabolic syndrome (MetS) is rising alarmingly in the Saudi Arabian population. This study was conducted to assess the association between vitamin D receptor (VDR) polymorphisms and genetic susceptibility to components of the metabolic syndrome, type 2 diabetes mellitus (T2DM), and vitamin D deficiency in the Saudi Arabian population. Five-hundred-seventy Saudi individuals (285 MetS and 285 controls) were enrolled in this cross-sectional study.

Induction of CYP1A1, CYP1A2, CYP1B1, increased oxidative stress and inflammation in the lung and liver tissues of rats exposed to incense smoke.

Incense smoke is increasingly being recognized as a potential environmental contaminant and is linked to malignant and non-malignant respiratory diseases. The detoxification of environmental contaminants including polycyclic aromatic hydrocarbons (PAHs) involves the induction of cytochrome P-450 family enzymes (CYPs) by PAHs. However, the detoxification of PAHs also results in the generation of reactive and unstable intermediary metabolites which are implicated in the oxidative stress, DNA damage, and inflammation.