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Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.

Anatabine (600 μg/mL; 24 hours; SHSY-5Y cells) treatment shows an inhibition of p65 NF-κB phosphorylation.
Anatabine (500-1000μg/mL; 30 minutes; SHSY-5Y cells) treatment fully prevents the increase in BACE-1 mRNA levels induced by TNF-α. After 24 hours, Anatabine treatment shows a dose-dependent inhibition of BACE-1 protein levels.
Anatabine dose dependently inhibits Aβ_1-40 and Aβ_1-42 with an approximate half maximal inhibitory concentration of 640 μg/mL for both Aβ_1-40 and Aβ_1-42 in 7W CHO cells. Anatabine inhibits sAPPβ secretion without impacting sAPPα suggesting that Anatabine is preventing the β-cleavage of amyloid precursor protein (APP).

Anatabine (0.5-2 mg/kg; intraperitoneal injection; daily; for 4 days; transgenic mouse) treatment significantly lowers brain soluble Aβ_1-40 and Aβ_1-42 levels in a transgenic mouse model of Alzheimer's disease.

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