Document Type
Article
Source of Publication
Journal of Inflammation Research
Publication Date
1-1-2022
Abstract
Introduction: Several studies revealed that alcohol utilization impairs memory in adults; however, the underlying mechanism is still unclear. The production of inflammatory markers and reactive oxygen species (ROS) plays a major role in neurodegeneration, which leads to memory impairment. Therefore, targeting neuroinflammation and oxidative distress could be a useful strategy for abrogating the hallmarks of ethanol-induced neurodegeneration. Moreover, several studies have demonstrated multiple biological activities of thiazolidine derivatives including neuroprotection. Methods: In the current study, we synthesized ten (10) new thiazolidine-4-carboxylic acid derivatives (P1-P10), characterized their synthetic properties using proton nuclear magnetic resonance (1 H-NMR) and carbon-13 NMR, and further investigated the neuropro-tective potential of these compounds in an ethanol-induced neuroinflammation model. Results: Our results suggested altered levels of antioxidant enzymes associated with an elevated level of tumor necrosis factor-alpha (TNF-α), nuclear factor-κB (p-NF-κB), pyrin domain-containing protein 3 (NLRP3), and cyclooxygenase-2 (COX-2) in ethanol-treated animals. Ethanol treatment also led to memory impairment in rats, as assessed by behavioral tests. To further support our notion, we performed molecular docking studies, and all synthetic compounds exhibited a good binding affinity with a fair bond formation with selected targets (NF-κB, TLR4, NLRP3, and COX-2). Discussion: Overall, our results revealed that these derivatives may be beneficial in reducing neuroinflammation by acting on different stages of inflammation. Moreover, P8 and P9 treatment attenuated the neuroinflammation, oxidative stress, and memory impairment caused by ethanol.
DOI Link
ISSN
Publisher
Informa UK Limited
Volume
15
First Page
3643
Last Page
3660
Disciplines
Medicine and Health Sciences
Keywords
ethanol, molecular docking, neuroinflammation, neuroprotective, oxidative stress, thiazolidine
Scopus ID
Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License
Recommended Citation
Naz, Shagufta; Al Kury, Lina Tariq; Nadeem, Humaira; Shah, Fawad Ali; Paracha, Rehan Zafar; Imran, Muhammad; Li, Shupeng; and Ullah, Aman, "Synthesis, In Silico and Pharmacological Evaluation of New Thiazolidine-4-Carboxylic Acid Derivatives Against Ethanol-Induced Neurodegeneration and Memory Impairment" (2022). All Works. 5259.
https://zuscholars.zu.ac.ae/works/5259
Indexed in Scopus
yes
Open Access
yes
Open Access Type
Gold: This publication is openly available in an open access journal/series