Posted by admin on Jul 31, 2023 in |
Enzyme Alanine racemase is well known for performing the predominating role in mycobacterium cell wall synthesis. D-alanine provided by Alanine racemase serves as a peptidoglycan precursor, utterly vital for maintaining the growth and integrity of the cell wall. The lipid-rich mycobacterium cell wall is prevalent amidst prokaryotes with immense potential of becoming a therapeutic target for new drug discovery. The imperative role of Alanine racemase in mycobacterium cell wall synthesis implies that its inhibition is of utmost priority in dealing with various pathogenic infections. Interference with metabolic processes, lack of specificity, and cellular toxicity caused by several known inhibitors prompted renewed efforts by researchers to discover new and improved inhibitors with better therapeutic indexes. This paper provides an overview of the updated status of reported Alanine racemase inhibitors based on shreds of evidence in literature so that more precise inhibitors could be explored, designed, and identified to rationalize the overall drug discovery process, which will be true serendipity for the...
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Posted by admin on Jul 31, 2023 in |
Rheumatoid arthritis (RA) causes joint disability due to pannus formation, synovitis, joint erosion, joint destruction and cartilage damage. Disease-modifying antirheumatic drugs (DMARDs) and nonsteroidal anti-inflammatory drugs (NSAIDs) prevent the disease progression but suffer the disadvantage of severe adverse drug reactions. An extensive literature search revealed reports of 176 phytoconstituents having anti-inflammatory and/or anti-arthritic activity. Their binding affinities to TLR-4 and NLRP3 receptors were predicted by molecular docking using target proteins of TLR4-MD2 (PDB ID: 3FXI) and chain A and chain B of NLRP3 (PDB ID: 6NPY). Docking score results revealed that 11 phytoconstituents with promising inhibition of TLR4-MD2 along with 27 phytoconstituents inhibiting binding to Chain A of NLRP3 and 65 phytoconstituents binding to Chain B of NLRP3 proteins were identified through an extra precision (XP) docking study by comparing standard antagonists of TLR4 such as Resatorvid and standard antagonists of NLRP3, i.e., MCC950 and Anakinra. Further, we analyzed the pharmacokinetic properties (absorption, distribution, metabolism, excretion, and toxicity) of selected phytoconstituents using pKCSM. Thus, this study reveals that the...
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Posted by admin on Jul 31, 2023 in |
It is an ornamental shrub native to Madagascar and the Philippines, widely distributed in India. Euphorbia milii Des Moul is widely used in folk medicine to treat warts (South Brazil), cancer and hepatitis in (China). The present study seeks to evaluate the methanolic aerial extract of Euphorbia milii Des Moul (MAEEM) for its anti-diabetic effect against streptozotocin–nicotinamide induced type 2 diabetic model in Albino Wistar rats. Oral glucose tolerance test, Phytochemical screening and Acute toxicity study were carried out. Graded doses of MAEEM (100mg/kg, 200mg/kg and 400mg/kg) were administered to diabetic rats for 21 days. The activity was evaluated by using some biochemical parameters such as blood glucose levels, serum lipid profiles, liver profile markers (AST, ALP, ALT), and renal profile markers (serum creatinine, blood urea). Type-2 diabetes significantly altered these parameters, while oral administration of the MAEEM significantly ameliorated...
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Posted by admin on Jul 31, 2023 in |
Eslicarbazepine acetate is a chemical compound that has found medical use as a partial seizure drug. Monitoring of heavy metals (As, Mn, Cd, Cr, V, Mo, Cu, and Sb) in-process, intermediates, and final drug substances is an important activity in the pharmaceutical industry because of the potential for toxicity and the risk of serious health hazards even at very low doses. This research article established and validated an easy and rapid analytical method for determining eight heavy metals in Eslicarbazepine acetate. Drugs must first be processed through acid digestion using microwave radiation before being analyzed for these elemental impurities. The % RSD of the LOQ solution was found to be < 20.0 for all the elements. The analytical method seems linear, with a correlation coefficient > 0.99. Eslicarbazepine acetate sample amounts spiked at three different concentrations, resulting in acceptable percentage recoveries of heavy metal ions ranging from 70% to 150%. Individually, precision and robustness for all conditions met the acceptable limits. Heavy metal analysis by ICP-MS is a powerful...
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Posted by admin on Jul 31, 2023 in |
Mikania micrantha Kunth is a noxious weed of Asteraceae, which is the biggest enemy of biodiversity right now, but we cannot disregard the plant’s therapeutic potential. This study evaluated the antioxidant and antibacterial properties of leaves and flowers from Mikania micrantha Kunth. Antibacterial screening was done by agar well diffusion method using Gentamicin (4mg/ml stock) as a standard antibiotic. The active extract’s minimum inhibitory concentration (MIC) was determined using the broth dilution method. The antioxidant activity was evaluated by DPPH method using Ascorbic acid as standard. The results showed that leaf and flower is antioxidant property correlates with their total phenol and flavonoid content. The flower extract exhibited highest antioxidant properties with IC50 value of 60.44 μg/ml. Leaf extract showed very strong antibacterial properties against wound infection-causing bacteria like Staphylococcus aureus MTCC 87 and Streptococcus pyogens MTCC 437. Minimum inhibitory concentration (MIC) of the active extract against Staphylococcus aureus MTCC 87, Streptococcus pyogens MTCC 437 was 400μg/ml and 800μg/ml, respectively. The result of this study indicates that the flower...
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