Withanone 是来自Withania somnifera根的活性成分，在减轻认知功能障碍方面具有多功能的神经保护作用。在神经元样细胞中，Withanone 可以抑制NMDA诱导的兴奋性毒性。
| 生物活性 | Withanone is an active constituent fromWithania somniferaroots with multifunctional neuroprotective effect in alleviating cognitive dysfunction. Withanone affords protection againstN-methyl-D-aspartate (NMDA)-induced excitotoxicity in Neuron-like cells[1][2]. |
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体外研究
(In Vitro) | Withanone (5-20 μM; Neuro2a cells) treatment significantly reverses the cell death induced by NMDA in N2a cells[1].
Withanone (5-20 μM; Neuro2a cells) treatment significantly normalizes Bax and Bcl-2 levels[1].
Attenuation of NMDA-induced intracellular calcium releases by Withanone in N2a cells[1].
Withanone attenuates NMDA-induced Reactive Oxygen Species generation in N2a cells and induces attenuation of mitochondrial membrane motential loss[1].
Withanone treatment down-regulates the expression of cytochrome c[1].
Withanone treatment decteases the Malondialdehyde levels in NMDA-induced excitotoxicity[1].
Withanone shows promise in Alzheimer's disease (AD) treatment because of cognitive benefits and more importantly, mechanisms of action with respect to the fundamental pathophysiology of the disease, not limited to the inhibition of AChE, but also include the modification of Aβ processing, protection against oxidative stress and anti-inflammatory effects. Withanone (24 hours) treatment shows significant protective effect against amyloid β (Aβ) toxicity in Aβ induced toxicity in PC-12 cells[2].
Cell Viability Assay[1] | Cell Line: | Neuro2a (N2a) cells | | Concentration: | 5 μM, 10 μM, 20 μM | | Incubation Time: | | | Result: | Attenuated NMDA-Induced cell death in N2a cells. |
Western Blot Analysis[1] | Cell Line: | Neuro2a (N2a) cells | | Concentration: | 5 μM, 10 μM, 20 μM | | Incubation Time: | | | Result: | Normalized NMDA-induced alterations in Bax and Bcl-2. |
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体内研究
(In Vivo) | Withanone (5-20 mg/kg; oral administration; daily; for 21 days; male Wistar rats) treatment shows significant improvement in the cognitive skill by inhibiting amyloid β-42 and attenuates the elevated levels of pro-inflammatory cytokines like TNF α, IL-1β, IL-6, MCP-1, Nitric oxide, lipid peroxidation and both β- and γ- secretase enzymatic activity. Administration of Withanone also significantly reverses the decline in acetyl choline and Glutathione (GSH) activity[1].
| Animal Model: | Male Wistar rats (20-24 weeks; 320-360 g) received ICV injection of STZ[1] | | Dosage: | 5 mg/kg, 10 mg/kg and 20 mg/kg | | Administration: | Oral administration; daily; for 21 days | | Result: | Showed significant improvement in the cognitive skill by inhibiting amyloid β-42 and attenuated the elevated levels of pro-inflammatory cytokines like TNF alpha, IL-1β, IL-6, MCP-1, Nitric oxide, lipid peroxidation and both β- and γ- secretase enzymatic activity. Also significantly reversed the decline in acetyl choline and Glutathione (GSH) activity. |
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| 来源 | - Plants
- Solanaceae
- Withania somnifera
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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