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<p>Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder, marked by cholinergic dysfunction, amyloid-β (Aβ) plaque deposition and oxidative stress. Nowadays, natural flavonoids have gained attention of altering the key pathological target of AD. The current investigation aimed to screen the potent flavonoids among the selected 10 flavonoids (apigenin, catechin, chrysin, diosmin, kaempferol, luteolin, myricetin, naringenin, quercetin and rutin) by investigating their inhibitory effect on Aβ aggregation, anticholinesterase activity (AChE) and oxidative stress, supported by computational analysis. Molecular docking study identified rutin (-5.17&#xa0;kcal/mol against AChE and − 10.29&#xa0;kcal/mol against Aβ), quercetin (-4&#xa0;kcal/mol against AChE and − 8.09&#xa0;kcal/mol against Aβ) and catechin (-5&#xa0;kcal/mol against AChE and − 9.4&#xa0;kcal/mol against Aβ) having superior binding affinities as compared to standard drug donepezil. In vitro, these flavonoids showed dose-dependent AChE inhibition, with IC<sub>50</sub> values 3.88, 3.66 and 3.38&#xa0;µg/mL respectively for catechin, quercetin and rutin. Rutin inhibited Aβ aggregation by 76.05%, quercetin by 72.25% and catechin by 65.2%. Additionally, glutathione reductase (GR) assay was also assessed in SH-SY5Y neuronal cells to evaluate the antioxidant enhancement by the selected flavonoids. Both in silico and in vitro findings suggested that rutin, quercetin and catechin exert neuroprotective effects to manage multifactorialAD by inhibiting the Aβ plaques aggregation, anticholinesterase and enhanced antioxidant property by GR activation. These results may suggestthem as promising candidates for the development of flavonoid-based drug delivery systems for the management of Alzheimer’s disease.</p>

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Neuroprotective potential of flavonoids against alzheimer’s disease: in silico and in vitro study

  • 期刊论文

  • 发表日期：

    2025年11月24日

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  • Bibhanwita Satpathy,
  • Tushar Kanti Rajwar,
  • Ajit Mishra,
  • Ivy Saha,
  • Rakesh Kumar Sahoo,
  • Jitu Halder,
  • Vineet Kumar Rai,
  • Ritu Mahanty,
  • Anindya Bagchi,
  • Sakti Ketan Prusty,
  • Deepak Pradhan,
  • Biswakanth Kar,
  • Goutam Ghosh,
  • Goutam Rath

摘要

Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder, marked by cholinergic dysfunction, amyloid-β (Aβ) plaque deposition and oxidative stress. Nowadays, natural flavonoids have gained attention of altering the key pathological target of AD. The current investigation aimed to screen the potent flavonoids among the selected 10 flavonoids (apigenin, catechin, chrysin, diosmin, kaempferol, luteolin, myricetin, naringenin, quercetin and rutin) by investigating their inhibitory effect on Aβ aggregation, anticholinesterase activity (AChE) and oxidative stress, supported by computational analysis. Molecular docking study identified rutin (-5.17 kcal/mol against AChE and − 10.29 kcal/mol against Aβ), quercetin (-4 kcal/mol against AChE and − 8.09 kcal/mol against Aβ) and catechin (-5 kcal/mol against AChE and − 9.4 kcal/mol against Aβ) having superior binding affinities as compared to standard drug donepezil. In vitro, these flavonoids showed dose-dependent AChE inhibition, with IC50 values 3.88, 3.66 and 3.38 µg/mL respectively for catechin, quercetin and rutin. Rutin inhibited Aβ aggregation by 76.05%, quercetin by 72.25% and catechin by 65.2%. Additionally, glutathione reductase (GR) assay was also assessed in SH-SY5Y neuronal cells to evaluate the antioxidant enhancement by the selected flavonoids. Both in silico and in vitro findings suggested that rutin, quercetin and catechin exert neuroprotective effects to manage multifactorialAD by inhibiting the Aβ plaques aggregation, anticholinesterase and enhanced antioxidant property by GR activation. These results may suggestthem as promising candidates for the development of flavonoid-based drug delivery systems for the management of Alzheimer’s disease.