bisabolol and 1-1-diphenyl-2-picrylhydrazyl

Alzheimer's disease (AD) is a multifaceted neurodegenerative disorder affecting the elderly people. For the AD treatment, there is inefficiency in the existing medication, as these drugs reduce only the symptoms of the disease. Since multiple pathological proteins are involved in the development of AD, searching for a single molecule targeting multiple AD proteins will be a new strategy for the management of AD. In view of this, the present study was designed to synthesize and evaluate the multifunctional neuroprotective ability of the sesquiterpene glycoside α-bisabolol β-D-fucopyranoside (ABFP) against multiple targets like acetylcholinesterase, oxidative stress and β-amyloid peptide aggregation induced cytotoxicity. In silico computational docking and simulation studies of ABFP with acetylcholinesterase (AChE) showed that it can interact with Asp74 and Thr75 residues of the enzyme. The in vitro studies showed that the compound possess significant ability to inhibit the AChE enzyme apart from exhibiting antioxidant, anti-aggregation and disaggregation properties. In addition, molecular dynamics simulation studies proved that the interacting residue between Aβ peptide and ABFP was found to be involved in Leu34 and Ile31. Furthermore, the compound was able to protect the Neuro2 a cells against Aβ

Topics: Acetylcholinesterase; Amyloid beta-Peptides; Animals; Biphenyl Compounds; Cell Line; Cell Survival; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Fucose; Mice; Models, Molecular; Molecular Structure; Monocyclic Sesquiterpenes; Picrates; Protein Aggregates; Structure-Activity Relationship

This study describes the chemical composition and the antibacterial, antifungal and antioxidant activities of the essential oil extracted from aerial parts of the Algerian Eryngium tricuspidatum L., obtained by hydrodistillation and analysed by using the combination of gas chromatography (GC) and GC/mass spectrometry. A total of 63 compounds were identified accounting for 93.1% of the total oil. Chemical composition of oil was characterised by a high proportion of oxygenated sesquiterpenes (49.6%) among which α-bisabolol (32.6%) was the predominant compound. The sesquiterpene hydrocarbons represent the second major fraction (31.9%) with α-curcumene (6.5%) being the predominant one. Antibacterial and antifungal activities of the oil were tested using the micro-well determination of minimum inhibitory concentration (MIC) assay against eleven bacteria and two Candida species. It was found that the aerial parts of E. tricuspidatum exhibited interesting antibacterial and anticandidal activities (MIC = 9 μg/mL against several strains of bacteria and MIC = 4.6 μg/mL against Candida albicans). The antioxidant effect of this oil was evaluated using the 2,2-diphenyl-l-1-picrylhydrazil (DPPH) and ferric reducing antioxidant power (FRAP) assays. Results revealed significant activities (DPPH method: IC₅₀ = 510 μg/mL; FRAP assay: reducing power of oil increases from 0.0188 at 5 μg/mL to 0.5016 at 1000 μg/mL).

Topics: Algeria; Anti-Bacterial Agents; Anti-Infective Agents; Antifungal Agents; Antioxidants; Biphenyl Compounds; Candida albicans; Eryngium; Free Radical Scavengers; Gas Chromatography-Mass Spectrometry; Microbial Sensitivity Tests; Monocyclic Sesquiterpenes; Oils, Volatile; Picrates; Plant Oils; Sesquiterpenes