Introduction: Cerebral ischemia arise due to insufficient/ interrupted blood supply to brain and is accompanied by pathologies like degradation of extracellular matrix resulting in blood brain barrier disruption, intra cranial haemorrhage, activation of astroglial cells and hence death of neurons. In addition, oxidative stress and inflammation is common to all neurodegenerative diseases enhancing the harmful consequences of diseases. Matrix Metalloproteinases (MMP) are normally involved in extracellular matrix remodelling and are regulated while injury and inflammation in tissue. Over expression of MMP2 and MMP9 results in progression of ischemic conditions by extracellular matrix degradation thus compromising the structural integrity of Blood Brain Barrier (BBB) proving them a potent targets for the disease. Violacein (source: Chromobacterium violaceum), purple pigment from microbial origin is a bisindole have high anti-inflammatory, anti-oxidant, anti-bacterial, anticancer and anti-parasitic properties. Present study is to study the effective potential of violacein against cerebral ischemia.
Background: Brain cancer prevalence is increasing at an explosive pace. Aquaporins (AQPs) the integral membrane water channel proteins are diversely distributed in body and maintain osmotic gradient across cell's plasma membrane. Past researches proved that AQP1, AQP4, AQP5 and AQP9 are majorly found in brain and are overexpressed in malignant conditions elevating progression, metastasis, angiogenesis, and associated edema. Allicin a plant origin compound found in garlic (Allium sativum), has anticancer, antioxidant, antiinflammatory, antifungal and antibacterial properties. Although much literature is present for allicin in treating cancer, inhibition of AQPs in brain cancer has never caught much attention. In this study we performed molecular docking to reveal structural inhibition of AQP1, 4, 5 and 9 by allicin and also analysed molecular and ADMET properties and bioavailability scores of allicin for its consideration as target specific drug.Methods and findings: Molecular docking was performed for analysing inhibition potential of allicin for AQP1, 4, 5 and 9 by using Autodock 4.0. The ADMET properties were analysed using Swiss ADME and Protox web portal. The molecular properties and bioavailability were checked by Molinspiration web based tool. Our results of docking for AQP1, AQP4, AQP5 and AQP9 with allicin gave binding energies of -4.76 kcal/mol, -4.89 kcal/mol, -4.19 kcal/mol and -4.78 kcal/mol respectively with 1 hydrogen bonds in each interaction. Conclusion:Brain aquaporins inhibition by allicin can be a potent target specific treatment for brain cancers.
Objectives: Cefquinome is a fourth generation cephalosporin with broad spectrum antimicrobial activity. It is commonly used against respiratory tract diseases, acute mastitis, calf septicemia and foot rot in livestock. Clean-up step in sample preparation is invariably required for avoiding interferences in assay from other components. It is envisaged to prepare molecular imprinted based polymer with desired selectivity for cefquinome. Method: Imprinted polymer was synthesized over the surface of magnetite using methacrylate (monomer) acid and ethyleneglycoldimethacrylate (crosslinker) in the presence of cefquinome (imprint molecule). Magnetite was prepared by co-precipitation of 1.98 g FeCl 2 .4H 2 O and 5.41 g FeCl 3 .6H 2 O. Magnetic non-imprinted polymer was prepared similarly in absence of cefquinome. Selectivity in different solvent was calculated from partition coefficient values in imprinted and non-imprinted polymers. Result: Selectivity of imprinted polymer over non-imprinted polymer was dependent on nature of solvent and pH. Binding of cefquinome was highly selective in acetonitrile. Imprinted polymer lacks selectivity in methanol and 1M NaCl. Ionic interaction between quinolinium ion in cefquinome and carboxylate anion in polymer appears to be major force for recognition of cefquinome by imprinted polymer. Prepared polymer extracted cefquinome from milk, honey, egg and water and extraction efficiency was in the range of 74-93.7%. Conclusion: Selectivity of magnetic imprinted polymer must be determined in different solvents and this will enable selecting binding and elution conditions during extraction of imprint molecule.
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