Posted by admin on May 31, 2023 in |
Leukemia is a disease of cancer that affects blood-forming tissues i.e., bone marrow and lymph nodes, which is associated with uncontrolled growth of WBCs. These cells are unable to fight against infection and weaken the ability of bone marrow to make RBCs and platelets. When leukemic cells overproduce, they interfere in circulatory cells’ functioning, i.e., RBCs and platelets. Along this, leukemia’s pathogenesis is unique in relation to different malignant growths which ordinarily start in major organs and then spread in bone marrow. Different types of leukemia are discovered based on different classification systems with the two major leukemia types – acute and chronic. The work includes the 50-year history of leukemia-lymphoma cell lines, which is considered a key model system in biomedicine. The work involves finding suitable protein receptors for the available potent drugs. Protein receptors are the target sites where drug molecules bind, activate and start their response. FLT3 tyrosine kinase protein is taken as a receptor to study docking concerning ligands like Abacavir, Gabapentin, etc. Autodock and...
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Posted by admin on May 31, 2023 in |
Background: The infectious disease, COVID-19, caused by SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2), is hardly showing signs of waning as it is still ongoing as a pandemic. Objective: To figure out potential leads from Ocimum sanctum and Plectranthus amboinicus’s phytoconstituents against SARS-CoV-2. Methodology: Selected phytoconstituents of O. sanctum and P. amboinicus were targeted on the PDB protein sequences of SARS-CoV-2 like 6W02, 4M0W, and 7T9L and were subjected to docking simulations using Pymol and the Autodock Vina tool of version 1.5.6. Hydrogen bond interactions and the amino acid residues of the targeted protein sequences were analyzed. ADME and drug-likeness predictions of the best dock-scored phytochemicals were further screened using the online tool molinspiration. Result: Out of 14 phytochemicals, only 9 had significant interactive profiles, of which Carvacrol, Eugenol, Apigenin, Luteolin, and Rosmarinic acid could potentially inhibit the targets of coronavirus. Only these five chemicals obey the ADME limitations and drug-likeness LogP values. Apigenin and Rosmarinic acid had better interactions at the active site of all three protein targets....
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Posted by admin on May 31, 2023 in |
The oral bioavailability of lumefantrine (LUMF) is low and erratic owing to its low aqueous solubility and P-glycoprotein (P-gp) mediated efflux. The present investigation aims to develop amorphous solid dispersions (SD) of LUMF co-loaded with piperine (PIP), a P-gp and CYP3A4 inhibitor, to improve its dissolution and thereby oral bioavailability. LUMF-SDs were prepared by using Polyvinyl-pyrrolidone, grade Povidone K30 (PVP) as a polymeric carrier, at three different ratios with increasing concentrations of polymer, employing melt method. DSC, XRD and FTIR characterized the PIP-LUMF-PVPSD at ratio of 1:6:18demonstrating higher aqueous solubility of LUMF. The DSC thermogram and XRD diffractogram confirmed the loss of crystallinity of both LUMF and PIP in PIP-LUMF SD, resulting in improved dissolution. Moreover, the possible molecular interactions between LUMF and PIP and /or PVP were investigated by FTIR studies. Crystallinity being a function of time, the stability of LUMF-PIP-PVP SD exposed to stressed humidity and temperature conditions (40 °C/75% RH) for 90 days was validated by DSC and release studies. These findings suggest that the SD...
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Posted by admin on May 31, 2023 in |
This study focuses on preparing and evaluating polymeric nanoparticles made of pegylated PLGA. In this study, both double-emulsion solvent evaporation and single-emulsion solvent evaporation were employed to formulate the pegylated PLGA nanoparticles with PVA as the surfactant. For the encapsulation of the hydrophobic drug Resveratrol, formulations were successfully prepared and tested for their particle size, polydispersity index, zeta potential, drug loading and entrapment efficiency. Scanning electron microscopy was used to observe the morphology and surface characteristics of the nanoparticles. The results demonstrated successful fabrication of the Resveratrol loaded pegylated PLGA nanoparticles. PVA was demonstrated in the present study to be a promising surfactant for the encapsulation and delivery of poorly water-soluble compounds as pegylated PLGA nanoparticles with the desired particle size, morphology and drug loading. PLGA nanoparticles encapsulated with Resveratrol had been successfully used to deliver the drug to the target site by pegylated PLGA...
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Posted by admin on May 31, 2023 in |
Oxidative stress and cholinergic deficit are major culprits of cognitive impairment. Intake of green leafy vegetables – rich in antioxidant phytoconstituents- strongly correlates with memory-preserving capacity. Our earlier work showed that hydromethanol (HM) extract of Chenopodium album (a common leafy vegetable) had strong acetylcholinesterase inhibitory and antioxidant activity in-vitro. The objective of the present study was to isolate the bioactive fraction/constituent from HM extract of C. album and substantiate its memory-enhancing capacity with in-vitro and in-vivo evidence. The HM extract was fractionated by solvent portioning and column chromatography and the antioxidant and acetylcholinesterase inhibition by fractions and sub-fractions thus obtained were assessed by DPPH and Ellman assays, respectively. The fraction F6 showed best potential in-vitro. Subsequently, the anti-amnesic capacity of HM extract and F6 was assessed using a scopolamine-induced memory impairment mouse model. Morris Water Maze test was used to determine memory. Biochemical parameters and histopathological studies of brain were also evaluated to elucidate anti-amnesic mechanism. In-vivo studies confirmed that F6 protected against scopolamine-induced memory impairment and significantly reduced...
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