Posted by admin on Feb 28, 2021 in |
Heparin is a mixture of glycosaminoglycan (GAG) chains originating from the porcine intestinal mucosa. It is used therapeutically as an anticoagulant for the treatment and prevention of thrombosis. Glyco-saminoglycans such as heparin (H) and heparan sulfate (HS) are considered attractive therapeutic agents because they modulate many biological processes and have been implicated in numerous pathologies, including cardiovascular, cancer, inflammation, metabolic, and neurodegenerative diseases and viral infections. These biological functions are believed to be dependent on the interaction of these linear polysaccharides with key proteins such as growth factors, cytokines, proteases, adhesion proteins, lipid binding proteins, etc., which have a heparin-binding domain in common and are termed heparin binding proteins (HBPs). The variability in unfractionated heparin’s pharmacokinetic properties and pharmacological effects led to the development of low MW heparin (LMWH), which is a degraded product of heparin using chemical or enzymatic cleavage techniques. The most common form of LMWH in the U.S. is enoxaparin, which is produced by β-eliminative cleavage of the benzyl esters of porcine mucosal heparin under alkaline...
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Posted by admin on Feb 28, 2021 in |
The epidermal growth factor receptor (EGFR), which is a potential anticancer drug target, is over-expressed in non-small-cell lung cancer (NSCLC). The present study is an attempt to explore the human EGFR (protein data bank code: 1M17) inhibition potential of Lipinski compliant compounds possessing 2-arylquinazoli-4-one scaffold with chalcone structural motif; by docking analysis, using Auto Dock 4.0 and Discovery Studio Visualizer. Docking experiments were validated by docking the reported co-crystallized erlotinib confermer at the active site of a target protein. The root means square deviation (RMSD) calculated for the docked co-crystallized confermer by using UCSF chimera was 0.989Ao. Five compounds C21, C42, C47, C10, and C46, were found as the most potent in-silico EGFR inhibitors and their free energy of binding (BE) came in the range of -45.56 kJ/mol to -41.25 kJ/mol. Absorption and toxicity predictions of the compounds were done using ad met SAR, an online prediction tool. The BE of the reference compound afatinib was found to be -32.72 kJ/mol. The understanding of protein-legend interactions would give accurate...
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Posted by admin on Feb 28, 2021 in |
This study seeks to evaluate the nephroprotective activity of chloroform extract of Abrus precatorius against gentamycin-induced nephrotoxicity in rats. Albino rats of Wistar strain of both sexes were used for the study and grouped into five, containing 6 animals. The study was performed for 14 days. For induction of nephrotoxicity, gentamycin and paracetamol were used, and the plant extract was given for 14 days. Later the animals were sacrificed, and kidneys were collected for histopathological studies. Meanwhile, blood was collected for estimation of serum parameters. All the animals treated with plant extract had shown decreased serum creatinine levels. The urea levels were also altered when compared to those of control. The histopathology studies of the kidney tissues also supported the results that the plant has a protective effect of gentamycin induced nephrotoxicity. The results of the study explored that the chloroform extract of Abrus precatorius has nephroprotective activity. Further studies are needed to isolate the active ingredients that have the protective...
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Posted by admin on Feb 28, 2021 in |
Mutual prodrugs of fenbufen and propyphenazone were synthesized with the aim of getting better therapeutic index through avoidance of gastrointestinal problems and to check the efficiency of release of parent drug in the presence of spacer. These mutual pro-drugs were synthesized by direct esterification and by using glycine as a spacer. The title compounds (FP1 & FP2) were characterized by spectral methods and the release of the parent drug from the mutual pro-drug was studied in two different non-enzymatic buffer solutions at pH 1.2 and pH 7.4. The biological activity of the title compounds (FP1 & FP2) was determined by tail-flick method, carrageenan-induced paw edema method, and ulcerogenic potential. From the results obtained it was concluded that these compounds exhibit better biological activity and less gastro-intestinal side effects than parent drug fenbufen. Both mutual prodrugs (FP1 & FP2) exhibited 42 and 32% respectively hydrolysis profile in buffer solutions of pH 7.4 and showed almost negligible hydrolysis i.e., 4.6 and 5.9 % respectively at pH 1.2 over a period of...
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Posted by admin on Feb 28, 2021 in |
Diagnosis of oral ulcerative lesions might be quite challenging. Oral ulcerative lesions were categorized into three major groups as acute, chronic, and recurrent ulcers. Helicobacter pylori (H. pylori) have been found in the oral cavity and stomach, and its infection is one of the most frequent worldwide. There is a close relation between H. pylori infection in the oral cavity and the stomach. H. pylori etiologic agent in recurrent apthous stomatitis, Canker sores. Quercetin inhibits the H. Pylori. Monoammonium glycyrrhizinate (MAG) was recognized as a compound possessing antimicrobial properties; MAG tested many researchers using the agar diffusion method which, show significant antibacterial activities against gram-positive (Bacillus subtilis, Stap Hylococcus aureus) as well as gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa). The objective of the present investigation was to formulate and evaluate gel for mouth ulcer treatment of Quercetin and MAG. The concentration of carbopol p940 and propylene glycol were optimized using a central composite design for two factors. Formulations were evaluated for various parameters such as pH, viscosity, spreadability, drug...
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