Evaluation of acetylcholinesterase and butyrylcholinesterase inhibitory activity of Huperzine-A; in silico and in vitro studies

The present study is focused on exploring the Acetylcholinesterase and Butyrylcholinesterase inhibitory activity of Huperzine-A in silico and in vitro. In this study, Huperzine-A-A was docked with Acetylcholinesterase and Butyrylcholinesterase. Docking studies revealed the excellent interaction of Huperzine-A-A with these targets. The result of present study provides insight for the in vitro studies. The in vitro studies the enzyme kinetics of Huperzine-A-A via Lineweaver brooks plot revealed the kinetics and non-competitive inhibitory nature of the later. Further studies on Huperzine-A-A are necessary to develop and establish its role on brain cholinergic system and cognitive deficits which may serve a stepping stone in CNS medication

Synergistic effect of folic acid and galantamine against experimentally induced oxidative stress in IMR 32 cells

286-292Galantamine is an active constituent obtained from Galanthus nivalis L., a traditional herb known for its pharmacological properties, particularly nootropic effect. Folic acid is a dietary supplement that enhances neuronal activity. Effect of galantamine and folic acid on human neuronal cells is well known. In the present study, we explored the protective effect of galantamine and folic acid, both independently as well as in combination, over antioxidant defence system and nootropic effects on human neuroblastoma cells IMR-32. The treatment galantamine, folic acid and their combination was given for 24 h and cytotoxicity study was carried out by trypan blue dye exclusion assay. Apoptosis and necrosis were observed using Propidium iodide (PI) and Hoechst double staining method. Biochemical assays viz. total protein, protein carbonyl, lipid peroxidation and glutathione were analyzed along with super oxide dismutase and catalase. Result of cytotoxicity showed dose dependent increase in percent viability and significant decrease was observed in apoptosis and necrosis. Moreover, exposure to Galantamine, Folic acid and their combination significantly decreased lipid peroxidation and protein carbonyl formation along with the enhancement in antioxidant defence mechanism. Findings of these dose reliant toxicity study of Galantamine , Folic acid and their combination suggest that these has higher potency when given together and shows synergistic effect. They also causes repair of human neuronal cells IMR-32 cells enhancing the cell viability and consumption of Galantamine and Folic acid together will help in prevention of CNS disorders and neurodegeneration