Posted by admin on May 31, 2024 in |
Background: NCp7 is a nucleocapsid protein of HIV-1, a retrovirus causing AIDS in human beings. It is a small protein of 72 amino acids that plays an important role in being a chaperone protein involved in viral development. HIV has shown resistance to drugs engineered to treat its infections. Objectives: In this study, a Structure-Activity Relationship analysis of two distinct derivatives based on point pharmacophore was carried out to obtain an NCp7 inhibitor of better performance. Materials and Methods: A Pharmacophore and 3D-QSAR modeling of Pyridinioalkanoyl thioesters and Benzamide-based thiolcarbamates derivatives was performed. Results: A four-point hypothesis of HHRR pharmacophoric feature was determined. A 3D-QSAR model was built which was validated through regression analysis. Molecular docking often lead compounds showed that the compound ZINC65398698 possesses a higher affinity towards NCp7 protein and binds well whereas other leads possessed only moderate binding affinity. The ADME/T prediction of all the ten lead compounds showed accepted values of biophysical properties. As ZINC65398698 showed higher binding affinity, a molecular dynamics simulation was performed...
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Posted by admin on May 31, 2024 in |
Nano composites of reduced graphene oxide (rGO) and silver nanoparticles (AgNps) were prepared in this work, adopting green reaction conditions. Aloe vera plant extract was used as the stabilizing agent in the AgNps system and graphite precursor has been chosen for rGO preparation adopting mild hydrothermal and sonication methods. AgNps and AgNp–rGO Nano composites are characterized using UV-VIS SPR; powder XRD, HR-TEM and FE-SEM measurements. The catalytic ability of AgNp–rGO nano composites in the as-synthesized form has been confirmed by following the oxidative degradation of the two therapeutically potential drugs such as sodium diclofenac (NaDF) and ranitidine hydrochloride (RHCl) under visible light irradiation in aqueous medium at 25°C. Reaction kinetic parameters and the oxidant peroxo monosulfate (Na2S2O5) effect in presence of AgNp–rGO nano-composites as the catalyst under visible light irradiation exhibited remarkable catalytic behavior in presence of visible light for the degradation of the two drug both in presence and absence of oxidant. However presence of oxidant enhanced the speed of drug degradations with AgNp–rGO nano composites and visible...
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Posted by admin on May 31, 2024 in |
Microbial chitosanase has received greater attention for producing chitooligosaccharides. In this study, chitooligosaccharide hydrolysate was developed using the chitosanase enzyme, and its bioactivity was evaluated. Marine muddy samples proved to be a source of isolating novel chitosan-degrading bacteria when compared to the other samples collected. A chitosan-degrading marine bacterium was isolated, and the characterization of its extracellular enzyme, chitosanase, was studied. The molecular characterization and 16S rDNA sequence evolutionary relatedness of the isolate were carried out. The organism was identified as Brevidomonas diminuta, and its sequence was deposited. The production of chitosanase enzyme was significantly induced by the chitosan substrate, while it reached its peak after 72 hours. pH and temperature have been verified to be ideal for enzyme synthesis at 6.5 and 30 °C, respectively. Utilizing a culture medium containing xylose as the substrate at a level ranging from 1.0 to 1.5% significantly enhanced the enzyme production. The molecular weight of the enzyme, 43 KDa, was ascertained through SDS-PAGE. The pathogen’s growth was suppressed by the chitooligosaccharide hydrolysate...
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Posted by admin on May 31, 2024 in |
Background & Objectives: Emblica officinalis Gaertn is a widely used medicinal plant with antidiabetic activity. This study was aimed to improve oral glucose tolerance, hepatoprotective and nephroprotective effect of linagliptin by given combination of aqueous fruit extract of Emblica officinalis on streptozotocin induced diabetic rats. Materials & Methods: Diabetes was produced on Wister albino rats by the intraperitoneal administration of streptozotocin (45 mg/kg BW). Linagliptin (5mg/70kg BW), E. officinalis (200 mg/kg BW) and fixed dose combination therapy of linagliptin (2.5 mg /70kg BW) with E. officinalis (100 mg/kg BW) were administered orally once daily for four weeks. Results: The result showed that both linagliptin and aqueous fruit extract of E. officinalis significantly increased oral glucose tolerance but combination therapy increased glucose utilization more significantly in comparison with linagliptin in glucose induced rats. Treatment with linagliptin and E. officinalis significantly restored liver function indices as measured by liver to body weight ratio, serum alanin transaminase, serum aspartate transaminase, serum alkaline phosphatase, serum Ɣ- glutamyl transferase, albumin and globulin and also...
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Posted by admin on May 31, 2024 in |
An increasing airflow limitation that is not entirely reversible is a hallmark of chronic obstructive pulmonary disease (COPD). In patients with COPD, the present study investigated the effectiveness and safety of formoterol/tiotropium bromide vs formoterol/glycopyrronium in fixed combinations. In conjunction with formoterol, the long-acting anti-muscarinic drug glycopyrrolate has recently received approval for the maintenance treatment of chronic obstructive pulmonary disease. Studies on the combination of long-acting beta 2 agonist and glycopyrrolate, particularly in patients from India, are scarce. Therefore, it was thought interesting to compare the safety and effectiveness of formoterol/tiotropium fixed dose combinations to formoterol/glycopyrrolate fixed dose combinations in GOLD Grade 3 COPD patients. In the COPD patients of GOLD Grade 3, the efficacy and safety of formoterol/glycopyrrolate and formoterol/tiotropium was studied. A total of 68 patients was assessed by using the Spirometry, the COPD Assessment Test score, and the Symptom score. The assessment of the effectiveness of treatment was done on days zero (before the therapeutic intervention) and at intervals of two weeks up to 12 weeks....
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