Posted by admin on Dec 31, 2019 in |
Organophosphorus (OP) nerve agents blocks acetylcholinesterase and do not allow the degradation of acetylcholine. Post-treatment of organophosphate poisoning involves the treatment with oxime reactivators as an antidote, which will dephosphorylate the phosphate bond between enzyme and nerve agent. Due to CNS permeability failure of these oximes, the introduction of low molecular non-oximes has become a challenging role for reactivation of inhibited acetylcholinesterase. In-silico high-throughput structure-based virtual screening and docking by using LOPAC database targeting CNS for inhibited acetylcholinesterase reactivation. For the identification of an active site of AChE enzyme and high throughput virtual screening, Inventus™ software was being used. ADME analysis for the selection of leads which can follow up Lipinski rule of 5 and CNS parameters for permeation. Further docking studies of selected lead candidates was done using Schrodinger software. By taking various CNS parameters into consideration hits were selected. For further refinement docking was performed, and the best lead obtained with glide XP docking score -11.656 Kcal/mol. The best lead candidates passed CNS permeation parameters range and...
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Posted by admin on Dec 31, 2019 in |
Hardwickia binata belongs to family Fabaceae / Caesalpiniaceae and commonly known as ‘Anjan’. The present study includes phytochemical screening, FTIR and GC-MS analysis. Shade dried powdered leaves, seed and husk of H. binata extracted in petroleum ether, chloroform, ethyl acetate, acetone, methanol, ethanol, distilled water using Soxhlet apparatus and used for phytochemical analysis. Crude powder of plant used for FTIR analysis and ethanolic extracts was analyzed using GC-MS. The phytochemical screening of H. binata revealed the presence of carbohydrates, proteins, amino acids, steroids, glycosides, flavonoids, lipids, tannins, phenolic compounds, quinones, mucilage, volatile oils, fats, and fixed oils whereas alkaloids, emodins and resins were not detected in any extracts of leaves, seed, and husk. The majorities of compounds are present in acetone, methanol, ethanol and distilled water and glycosides, lipids and mucilage are present in all extracts. FTIR analysis showed the presence of alcohol, phenols, amines, amides, carboxylic acids, aromatics, alkenes, alkanes, aliphatic amines, esters, ethers, alkynes, alkyl halides in leaves, seed and husk; saturated aliphatic found in only seed...
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Posted by admin on Dec 31, 2019 in |
Introduction: Cutaneous adverse drug reactions (CADRs) associated with significant morbidity and mortality are probably the most frequent of all manifestations of drug sensitivity. Material and Methods: It was a prospective observational study where newly diagnosed patients with ADRs reporting to OPD of Dermatology, K.G.M.U, Lucknow and satisfying inclusion criteria were enrolled. The various study tools used were the suspected ADR reporting form (CDSCO), Naranjo’s causality scale, Modified Hartwig and Siegel severity scale and Dermatology Life Quality Index. Results: In a total of 124 patients recorded with CADRs, males (60.5%) were found more affected than females (39.5%). The most common age group found was 21-30 yrs (36.3%) followed by 31-40 yrs (25.8%) with a mean age ± SD 35.88 ± 13.87 range (18-78) years. The most common clinical pattern observed was Fixed Drug Eruption (FDE) (49.2%) followed by maculopapular rash (MPR) (36.3%). The incidence of Severe CADRs (SCADR) was 8.06%. Antimicrobial (50.8%) followed by unknown (17.7%), combinations (14.5%) and anti-epileptics (8.9%) were the most common drug groups suspected. On the...
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Posted by admin on Dec 31, 2019 in |
A selective and rapid LC-MS/MS spectrophotometric method has been developed and validated for the simultaneous determination of three ACE-inhibitors used in anti-hypertensive therapy, namely enalapril maleate, perindopril, and ramipril in human plasma using high-performance liquid chromatography-tandem mass spectrophotometry (LC-MS/MS) with electrospray ionization (ESI). Separation of analytes and internal standard; atorvastatin was performed on X-terra C8 (3.5 µm, 4.6 × 50 mm) column with a run time of 2 min. The mobile phase consisted of methanol: 20 mM ammonium formate, pH 6.3 ± 0.05 with formic acid (80:20, v/v). Analytes were extracted from human plasma using a simple protein precipitation technique with methanol, allowing fast analysis. The method was validated in terms of accuracy, precision, selectivity, recovery and stability as per FDA and EMA guidelines. The method showed linearity over the concentration range 4- 400 ng/mL, 2 – 200 ng/mL and 0.5 – 50 ng/mL for enalapril, perindopril and ramipril, respectively, applying weighted (1/X2) linear regression. The method is simple, fast, precise, accurate and suitable for its application for bioequivalence...
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Posted by admin on Dec 31, 2019 in |
Electron microscopic studies revealed variations in different cell organelles in steroidogenic cells of normal, regressing and pregnant caprine corpora lutea. Corpus luteum was comprised of two types of steroidogenic cells viz. small theca luteal cells and large granulosa luteal cells. In granulosa luteal cells, rough endoplasmic reticulum was most abundant in corpus luteum of pregnancy. The number of mitochondria, Golgi complex and secretory granules increased from normal to pregnancy category and decreased in regressing category. In theca luteal cells, smooth endoplasmic reticulum, number of mitochondria and Golgi complex were more in pregnancy. During regression, degenerating luteal cells with shrunken cytoplasm, dispersed nuclear membrane, apoptotic granules, increased number of lipid droplets, lysosomes, swollen mitochondria, irregular plasma membrane, disintegrating and vacuolated rough endoplasmic reticulum were observed. The degenerating luteal cells of regressing corpus luteum revealed the patches of chromatin material along the periphery of the uneven nuclear membrane and also within the nucleoplasm. These variations shall be discussed in relation to their physiological...
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