Posted by admin on Nov 30, 2019 in |
Alzheimer’s disease (AD) is a disorder of the central nervous system with progressive neurodegeneration, cognition, and memory loss. A major molecular hallmark of the disorder includes extracellular deposition of the Amyloid beta-peptide (Aβ) in senile plaques, the appearance of intracellular neurofibrillary tangles. The Aβ peptide is produced by sequential cleavage of the Amyloid precursor protein (APP) by α, β, and γ-secretase. The secretase β and γ generate a number of isoforms of peptides containing 36-43 amino acid residues in length. The mainly universal isoforms are Aβ(1-40) and Aβ(1-42). Aβ(1-42) C-terminal domain (29-42 amino acid residues) adopts β conformation, and the N-terminal domain (10-24 amino acid residues) facilitates a dynamic equilibrium between α- helix and β-strand. Thus Aβ polymerization requires unfolding of the native α-helical structure of Aβ. Stabilization of the Aβ central α- helix is an efficient step to foil the Aβ polymerization. Here we report test compounds which to bind and stabilize the 11-30 amino acid regions of Aβ(1-42) in α-helical conformation. On docking, the ligands with Aβ...
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Posted by admin on Nov 30, 2019 in |
Three novel metal complexes of 2-aminobenzonitrile (ABN) and octanoate ion (OC) with Mn2+, Co2+, and Ni2+ have been prepared by using microwave irradiation. The DNA-binding properties of the free ligand 2-aminobenzonitrile and its Mn2+, Co2+ and Ni2+ complexes have been investigated by fluorescence measurements. The results suggest that ABN, Mn2+, Co2+ and Ni2+ complexes both bind to DNA via an intercalative binding mode and the affinity for DNA is more strong in case of Mn2+, Co2+, and Ni2+ complexes when compared with ABN. The intrinsic binding constants (Kb) of the Mn2+, Co2+ and Ni2+ complexes and ligand with DNA were 2.75 × 104 M−1, 3.08 × 104 M−1, 3.80 × 104 M−1 and 1.96 × 104 M−1, respectively. Ni2+ complex is strongly bound to DNA compared to other complexes and the ligand. Furthermore, the free radical scavenging activity of the free ligand and their complexes has been determined by measuring their interaction with the stable free radical DPPH. The complexes have larger antioxidant activity as compared to the...
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Posted by admin on Nov 30, 2019 in |
The current study deals with anti-diabetic and pancreatic protective effects of Flemengia strobilifera extracts in a high-fat diet (HFD) and streptozotocin (STZ) induced type 2 diabetes model. Toluene extracts were orally administered at the dose of 10, 30 and 100 mg/kg and metformin was used as a standard anti-diabetic drug at 10 mg/kg dose orally. Blood glucose, lipid profiles, pancreatic oxidative stress parameters and oral glucose tolerance test (OGTT) were performed. Treatment with extracts resulted in a significant decrease in diabetes incidence with a marked reduction in the blood glucose levels dose dependent and time dependent. Glucose tolerance was greatly improved after treatment with plant extracts with high dose group producing effects similar to standard drug-mediated beneficial effects. Histopathological studies also indicated pancreatic beta-cell protective effects of Flemengia strobilifera extracts with increased beta-cell number and size. Our results demonstrate that Flemengia strobilifera can be a possible remedy to treat type 2 diabetes and associated...
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Posted by admin on Nov 30, 2019 in |
Background: Hypertension is associated with the flow of blood under high pressures, and is a risk factor for coronary heart disease. Methodology: We designed a prospective observational study that included 280 participants to investigate the effect of hypertension on the health-related quality of life (HRQOL) for hypertensive patients in the eastern province of KSA. To measure HRQOL, this study used EQ-5D-5L which consists of five dimensions that are further divided into five levels of severity. Results: Among the normotensive participants, 77%, 96%, 66%, 38%, and 44% were agreed as having no problem in terms of self-care, anxiety or depression, usual activities, mobility, and pain or discomfort respectively; whereas among the hypertensive participants, these were 36%, 79%, 20%, 21%, and 31% respectively. Conclusion: We concluded that health-related quality for hypertensive patients is significantly affected by HTN. Therefore, great attention must be paid to enhance their quality of life to avoid any future...
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Posted by admin on Nov 30, 2019 in |
The main objective of the study was to formulate tablets of Candesartan cilexetil using the crystal agglomerates for the enhancement in flow properties and solubility. The crystal agglomerates were prepared by polymer enriched bridging liquid (PEBL) technique. The process requires three solvent systems, the good solvent for the drug, the bad solvent and the bridging liquid. The hydrophilic polymer PVP K30 was incorporated in the bridging liquid. The addition of hydrophilic polymer increased the hydrophilicity and wettability of Candesartan cilexetil. The saturation solubility analysis, percentage yield, drug content, micromeritic properties, FTIR, DSC, XRD, SEM were carried out for the evaluation of crystal agglomerates. The tablets were prepared by direct compression using the formulated crystal agglomerates and were subjected to various in-vitro evaluations. The crystal agglomerates prepared by the PEBL technique showed 25 folds enhancement in the solubility. The FTIR analysis revealed the absence of incompatibility. The DSC analysis and XRD pattern showed a reduction in crystallinity. The SEM analysis revealed the porous and sphericity of the agglomerates. The tablets...
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