Yazar "Bahadori, Fatemeh" seçeneğine göre listele

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    Anticholinesterase and Antioxidant Activities of Natural Abietane Diterpenoids with Molecular Docking Studies
    (Bentham Science Publ Ltd, 2020) Topcu, Gulacti; Akdemir, Atilla; Kolak, Ufuk; Ozturk, Mehmet; Boga, Mehmet; Bahadori, Fatemeh; Cakmar, Seda Damla Hatipoglu
    Background: Alzheimer's Disease (AD) is one of the most prevalent causes of dementia in the world, and no drugs available that can provide a complete cure. Cholinergic neurons of the cerebral cortex of AD patients are lost due to increased activity of cholinesterase enzymes. Objective: Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) are the two major classes of cholinesterases in the mammalian brain. The involvement of oxidative stress in the progression of AD is known. Thus, the objective of this study is to determine strong ChE inhibitors with anti-oxidant activity. Methods: In this study, 41 abietane diterpenoids have been assayed for antioxidant and anticholinesterase (both for AChE and BuChE) properties in vitro, which were previously isolated from Salvia species, and structurally determined by spectroscopic methods, particularly intensive 1D- and 2D-NMR and mass experiments. Molecular modeling studies were performed to rationalize the in vitro ChE inhibitory activity of several abietane diterpenoids compared with galantamine. Results: Thirteen out of the tested 41 abietane diterpenoids exhibited at least 50% inhibition on either AChE or BuChE. The strongest inhibitory activity was obtained for Bractealine against BuChE (3.43 mu M) and AChE (33.21 mu M) while the most selective ligand was found to be Hypargenin E against BuChE enzyme (6.93 mu M). A full correlation was not found between anticholinesterase and antioxidant activities. The results obtained from molecular modelling studies of Hypargenin E and Bractealine on AChE and BuChE were found to be in accordance with the in vitro anti-cholinesterase activity tests. Conclusion: Abietane diterpenoids are promising molecules for the treatment of mild-moderate AD.
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    Öğe
    Inhibition of Amyloid Aggregation Using Optimized Nano-Encapsulated Formulations of Plant Extracts with High Metal Chelator Activities
    (Bentham Science Publ Ltd, 2020) Kazdal, Fatma; Bahadori, Fatemeh; Celik, Burak; Ertas, Abdulselam; Topcu, Gulacti
    Background: The role of Fe+2, Cu+2 and Zn+2 in facilitating aggregation of Amyloid beta (A beta) and consequently, the progression of Alzheimer's disease (AD) is well established. Objective: Development of non-toxic metal chelators is an emerging era in the treatment of AD, in which complete success has not been fully achieved. The purpose of this study was to determine plant extracts with high metal chelator and to encapsulate them in nano-micellar systems with the ability to pass through the Blood Brain Barrier (BBB). Methods: Extracts of 36 different Anatolian plants were prepared, total phenolic and flavonoid contents were determined, and the extracts with high content were examined for their Fe+2, Cu+2 and Zn+2 chelating activities. Apolipoprotein E4 (Apo E) decorated nano-formulations of active extracts were prepared using Poly (Lactide-co-Glycolide) (PLGA) (final product ApoEPLGA) to provide BBB penetrating property. Results: Verbascum jlavidum aqueous extract was found as the most active sample, incubation of which, with A beta before and after metal-induced aggregation, resulted in successful inhibition of aggregate formation, while re-solubilization of pre-formed aggregates was not effectively achieved. The same results were obtained using ApoEPLGA. Conclusion: An optimized metal chelator nano-formulation with BBB penetrating ability was prepared and presented for further in vivo studies.