Experimental and DFT Approaches to Physico-Chemical Properties of Bioactive Resveratrol Analogues DOI Creative Commons
Borislav Kovačević, Ivana Šagud,

Katarina Marija Drmić

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(22), P. 5481 - 5481

Published: Nov. 20, 2024

Acetylcholinesterase and butyrylcholinesterase are two related enzymes that represent pharmacologically suitable targets in neurodegenerative disorders, given their physiological roles the body. The treatment of disorders currently includes common reversible cholinesterase inhibitors. Resveratrol analogues, as molecules focus, have shown very strong inhibition potential cholinesterases. In this research, experimental DFT approaches for p

Language: Английский

Resveratrol Activates Antioxidant Protective Mechanisms in Cellular Models of Alzheimer’s Disease Inflammation DOI Creative Commons
Clara Bartra, Yi Yuan, Kristijan Vuraić

et al.

Antioxidants, Journal Year: 2024, Volume and Issue: 13(2), P. 177 - 177

Published: Jan. 31, 2024

Resveratrol is a natural phenolic compound with known benefits against neurodegeneration. We analyzed in vitro the protective mechanisms of resveratrol proinflammatory monomeric C-reactive protein (mCRP). mCRP increases risk AD after stroke and we previously demonstrated that intracerebral induces AD-like dementia mice. Here, used BV2 microglia treated for 24 h presence or absence resveratrol. Cells conditioned media were collected analysis. Lipopolysaccharide (LPS) has also been implicated progression so LPS was as resveratrol-sensitive reference agent. at concentration 50 µg/mL activated nitric oxide pathway NLRP3 inflammasome pathway. Furthermore, induced cyclooxygenase-2 release cytokines. effectively inhibited these changes increased expression antioxidant enzyme genes Cat Sod2. As central defense, hub Sirt1 Nfe2l2 nuclear translocation signal transducer NF-ĸB. Proinflammatory by primary mixed glial cultures protected This work provides mechanistic insight into preventing agents.

Language: Английский

Citations

20

A Decade of Dedication: Pioneering Perspectives on Neurological Diseases and Mental Illnesses DOI Creative Commons
Masaru Tanaka, László Vécsei

Biomedicines, Journal Year: 2024, Volume and Issue: 12(5), P. 1083 - 1083

Published: May 13, 2024

Welcome to

Language: Английский

Citations

17

Targeting natural antioxidant polyphenols to protect neuroinflammation and neurodegenerative diseases: a comprehensive review DOI Creative Commons
Maroua Jalouli, Md. Ataur Rahman, Partha Biswas

et al.

Frontiers in Pharmacology, Journal Year: 2025, Volume and Issue: 16

Published: Jan. 24, 2025

Polyphenols, naturally occurring phytonutrients found in plant-based foods, have attracted significant attention for their potential therapeutic effects neurological diseases and neuroinflammation. These compounds possess diverse neuroprotective capabilities, including antioxidant, anti-inflammatory, anti-amyloid properties, which contribute to mitigating the progression of neurodegenerative conditions such as Alzheimer's Disease (AD), Parkinson's (PD), Dementia, Multiple Sclerosis (MS), Stroke, Huntington's (HD). Polyphenols been extensively studied ability regulate inflammatory responses by modulating activity pro-inflammatory genes influencing signal transduction pathways, thereby reducing neuroinflammation neuronal death. Additionally, polyphenols shown promise various cellular signaling pathways associated with viability, synaptic plasticity, cognitive function. Epidemiological clinical studies highlight polyphenol-rich diets decrease risk alleviate symptoms disorders Furthermore, demonstrated through regulation key Akt, Nrf2, STAT, MAPK, play critical roles neuroprotection body's immune response. This review emphasizes growing body evidence supporting combating neurodegeneration neuroinflammation, well enhancing brain health. Despite substantial promising hypotheses, further research investigations are necessary fully understand role establish them advanced targets age-related neuroinflammatory conditions.

Language: Английский

Citations

3

Cholinesterase Inhibition and Antioxidative Capacity of New Heteroaromatic Resveratrol Analogs: Synthesis and Physico-Chemical Properties DOI Open Access
Milena Mlakić, Ilijana Odak, Danijela Barić

et al.

Published: June 24, 2024

The targeted compounds in this research, resveratrol analogs 1–14 were synthesized as mixtures of isomers by the Wittig reaction using heterocyclic triphenylphosphonium salts and various benzaldehydes. planned those possessing trans-configuration biologically active trans-resveratrol. pure obtained repeated column chromatography isolated yields depending on heteroaromatic ring. It was found that butyrylcholinesterase (BChE) more sensitive to than acetylcholinesterase (AChE), except for 6, methylated thiophene derivative with chlorine, which showed equal inhibition toward both enzymes. Compounds 5 8 achieved highest BChE IC50 values 22.9 24.8 μM, respectively. same AChE BChE, subunits better enzyme unmethylated ones. Two antioxidant spectrophotometric methods, DPPH CUPRAC, applied determine potential new analogs. Molecular docking these conducted visualize ligand-active site complexes' structure identify non-covalent interactions responsible complex's stability, influence inhibitory potential. As ADME properties are crucial developing drug product formulations, they have also been addressed work. genotoxicity is evaluated silico studies all synthesized.

Language: Английский

Citations

4

Computational Analysis of Stilbenes as Potential Multi-Targeted Therapeutics for Alzheimer’s Disease DOI Creative Commons
Seda Şirin

Osmaniye Korkut Ata Üniversitesi Fen Bilimleri Enstitüsü Dergisi, Journal Year: 2025, Volume and Issue: 8(1), P. 145 - 166

Published: Jan. 15, 2025

Purpose: The aim of this study is to compare 13 stilbenes and 5 FDA-approved drugs used in the treatment Alzheimer’s disease (AD) by ADME prediction molecular docking method. Cholinergic, amyloid, tau, oxidative stress inflammation hypotheses involved AD pathology were targeted docking. Materials Methods: SwissADME has been determine physicochemical, lipophilicity, water solubility, pharmacokinetics, drug-likeness medicinal chemistry properties (resveratrol, pterostilbene, oxyresveratrol, piceatannol, pinosylvin, isorhapontigenin, isorhapontin, astringin, piceid (polydatin), mulberroside A) (tacrine, donepezil, rivastigmine, galantamine, memantine). CBDOCK2 binding affinity target proteins (AChE, BuChE, APP, BACE, GSK-3β, CDK5, SOD, CAT, GPx, Cox-2, iNOS, IL-1β, TNF-α). Results: SWISS results showed that could be as natural products AD. indicated A best vina score (kcal/mol) followed galanthamine, resveratrol, tacrine, memantine. Conclusion: Our evaluated for using computational approaches. highlight its potential therapeutic effects on various pathology. More research needed validate these findings clinical practice.

Language: Английский

Citations

0

Role and therapeutic considerations of SIRT1 in epilepsy DOI
S Zeng, Xiangyi Huang,

Shun-Lin Qu

et al.

Neuroscience, Journal Year: 2025, Volume and Issue: 568, P. 109 - 115

Published: Jan. 15, 2025

Language: Английский

Citations

0

Cytotoxic Stilbenoids, Hetero- and Homodimers of Homoisoflavonoids from Prospero autumnale DOI Creative Commons
Hasan Kırmızıbekmez, Başak Aru, Jana Maříková

et al.

Journal of Natural Products, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 24, 2025

An activity-guided isolation study on the EtOH extract prepared from bulbs of Prospero autumnale yielded four new phenolic compounds, including a stilbenoid (1), homoisoflavonoid derivative (8), dimer (9), and an unprecedented homoisoflavone–stilbene heterodimer (10), together with six known (2–7) analogs. Their chemical structures were elucidated by spectroscopic analysis theoretical NMR ECD calculations. Compounds 9 10 are unique in their scaffolds. The vitro cytotoxic activity purified compounds was evaluated against eight tumor cell lines (HCT116, LoVo, DU145, PC3, HEP3B, HEPG2, MCF7, MDA-MB-231) one nontumor line (L929) MTS assay. 1, 2, 4, exhibited inhibition IC50 values ranging 8.2 to 37.6 μM. Cytotoxic death mechanisms further investigated, indicating variability apoptosis, necrosis, or cycle arrest.

Language: Английский

Citations

0

Separation of polyphenols by HILIC methods with diode array detection, charged aerosol detection and mass spectrometry: application to grapevine extracts rich in stilbenoids DOI
Karen Gaudin, Josep Valls,

Rémy Cordazzo

et al.

Journal of Chromatography A, Journal Year: 2024, Volume and Issue: 1736, P. 465422 - 465422

Published: Oct. 6, 2024

Language: Английский

Citations

1

Cholinesterase Inhibition and Antioxidative Capacity of New Heteroaromatic Resveratrol Analogs: Synthesis and Physico—Chemical Properties DOI Open Access
Milena Mlakić, Stanislava Talić, Ilijana Odak

et al.

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(13), P. 7401 - 7401

Published: July 5, 2024

The targeted compounds in this research, resveratrol analogs 1–14, were synthesized as mixtures of isomers by the Wittig reaction using heterocyclic triphenylphosphonium salts and various benzaldehydes. planned those possessing trans-configuration biologically active trans-resveratrol. pure obtained repeated column chromatography isolated yields depending on heteroaromatic ring. It was found that butyrylcholinesterase (BChE) more sensitive to than acetylcholinesterase (AChE), except for 6, methylated thiophene derivative with chlorine, which showed equal inhibition toward both enzymes. Compounds 5 8 achieved highest BChE IC50 values 22.9 24.8 μM, respectively. same AChE BChE, subunits better enzyme unmethylated ones. Two antioxidant spectrophotometric methods, DPPH CUPRAC, applied determine potential new analogs. molecular docking these conducted visualize ligand-active site complexes’ structure identify non-covalent interactions responsible complex’s stability, influence inhibitory potential. As ADME properties are crucial developing drug product formulations, they have also been addressed work. genotoxicity is evaluated silico studies all synthesized.

Language: Английский

Citations

0

Targeting Neurological Disorders with Stilbenes: Bridging the Preclinical-Clinical Gap DOI Creative Commons

Md. Zamshed Alam Begh,

Jishan Khan,

Mehrukh Zehravi

et al.

International Journal of Biological Sciences, Journal Year: 2024, Volume and Issue: 20(14), P. 5474 - 5494

Published: Jan. 1, 2024

Neurological disorders (NDs) encompass a range of debilitating conditions that affect the nervous system, including prevalent illnesses such as Alzheimer's disease, Parkinson's and ischemic stroke. Despite significant ongoing studies, effective therapeutic strategies to halt or slow down progression these are still lacking. Stilbenes, class natural polyphenols, have shown potential candidates for due their capacity protect system. Preclinical studies provided strong evidence stilbenes can regulate many cellular pathways implicated in neurodegeneration, with resveratrol being well-studied compound has ability reduce oxidative damage, promote neurogenesis, enhance mitochondrial function - crucial maintaining brain health. In preclinical animal models, initial research also promise additional substances piceatannol pterostilbene. Furthermore, clinical explored benefits NDs. promising results research, use trials is currently limited, most focusing on resveratrol. Although several demonstrated beneficial impact supplementation health degenerative consequences, other investigations yielded ambiguous findings, underscoring urgent need more comprehensive precisely planned research. This study delves into neuroprotective agents It emphasizes our understanding effectiveness specific patient groups.

Language: Английский

Citations

0