Posted by admin on Sep 30, 2016 in |
In this study, homology modeling and molecular docking studies were performed to explore structural features and binding mechanism of synthesized benzimidazole derivatives as ubiquitin inhibitors. A homology modeling procedure was employed to construct a 3D model of ubiquitin protein by using MODELLER9.15. For this procedure, the X-ray crystal structure of Gumby / fam105b in Complex with linear Di-ubiquitin (PDB ID: 4KSL) at 2.83 Å resolution was used as template. The predicted model was analyzed by PROCHECK. The 3D structure of predicted model shows 93.9% of amino acids in most favored region. The predicted model was used for molecular docking studies by using Autodock4.2. All the synthesized benzimidazole derivatives show good binding energy and interactions with the model. Compound one shows three interactions with Asp348, Leu297 and...
Read More
Posted by admin on Sep 30, 2016 in |
Curcuminoids are dietary phytochemicals obtained from dried rhizomes of turmeric plant (Curcuma longa). Curcuminoids are mixture of curcumin, demethoxy curcumin and bisdemethoxy curcumin in which curcumin is a major constituent. Several polymorphic forms of curcumin were reported. The present study relates to the preparation of different solid forms of curcuminoids and to study the influence of other constituents of curcuminoids on the polymorphic behaviour of curcumin. The developed solid forms were characterized by various spectral methods like Fourier Transform Infrared Spectroscopy (FTIR), Powder X- ray diffraction (PXRD), Differential Scanning Calorimetry (DSC) and Scanning Electron microscopy (SEM). On crystallization from ethanol and upon melt crystallization, curcuminoids underwent transformation into an amorphous form. Grinding did not affect the polymorphic nature of curcuminoids. These findings suggest that curcuminoids undergo polymorphic modifications very similar to...
Read More
Posted by admin on Sep 30, 2016 in |
Nanoparticles (NPs) have been extensively studied during the past few decades due to their well-recognised applicability. Thus, the present study was aimed to fabricate Carvedilol (CVD) a β-adrenoceptor antagonist, as NPs aiming towards the optimal physicochemical characteristics and improved solubility. The prepared NPs demonstrated a linear increase in the mean particle size from253 ± 19 to 598 ± 21 nm and entrapment efficiency (%EE) from 58.6% to 91.1%, when drug-to-polymer mass ratio was increased from 1:1 to 1:5. In vitro release studies showed significant variation in the rate and extent of CVD release from polymeric matrix at various pHs of release media (pH 1.2, pH 6.8 and distilled water) and drug-to-polymer mass ratios. The present study highlighted the optimal formulation conditions to fabricate CVD-loaded NPs with best physicochemical characteristics, improved solubility of incorporated drug and explored the prospects of manipulation and optimisation of the NPs for intended...
Read More
Posted by admin on Sep 30, 2016 in |
Most of the drug discovered in past decade belongs to biopharmaceutical classification system (BCS) class II. The solubility of these drugs is the limiting factor for oral bioavailability. The drug can be present in solution in a supersaturated state; however, it has a tendency to crystallize out. In this paper, we aim to study the effect of molecular weight of Polyvinylpyrrolidone (PVP) (PVP K12, PVP K29 and PVP K90) and Hydroxypropyl methyl cellulose (HPMC) (HPMC E5, HPMC E15 and HPMC E50) as potential antiprecipitant on weakly acidic drug-Indomethacin (INDO). Supersaturation assay was carried out by solvent shift and solvent casting method. These are non-formulated methods and to access their ability to generate supersaturation, spray dried solid dispersions (SD) were prepared. Supersaturation assay revealed that the ability to generate and maintain the supersaturation are concentration dependent for PVP. As the molecular weight increases the supersaturation produced is increased in PVP and decreased for HPMC polymers. On stability, PVP solvent casts are affected the most. SD were prepared and found out...
Read More
Posted by admin on Sep 30, 2016 in |
Metabolic syndrome (MS) is a multi-factorial disorder with insulin resistance as a major characteristic. Adiponectin, an adipocyte derived cytokine, can regulate glucose levels and lipid homeostasis by its insulin sensitizer properties. Low circulating levels of serum adiponectin has been reported as a risk factor for the development of MS. The aim of this case control study was to investigate the association of serum adiponectin concentration, insulin resistance and various risk factors with MS among Tunisian participants. We designed a case-control study involving 100 patients with MS (84 females and 16 males, mean age 54±11 years) and 100 healthy controls (60 females and 40 males, mean age 51±10 years). Serum total cholesterol and triglyceride were determined by enzymatic methods. Insulin resistance was calculated using the homeostasis model assessment (HOMA-IR) = fasting insulin (uU/ml) x fasting plasma glucose (mmol/l)/22.5 and serum adiponectin levels were measured by enzyme-linked immunosorbent assay. Interestingly, 72% of the subjects with MS had high blood pressure. Compared with controls, patients had significantly higher levels of triglycerides (1.64±0.88...
Read More
