| Bioactivity | 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[1][2][3]. |
| Target | NF-κBAmyloid-β (Aβ)α4β2 nAChR |
| Invitro | Anatabine (600 μg/mL; 24 hours; SHSY-5Y cells) treatment shows an inhibition of p65 NF-κB phosphorylation[1].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[1].Anatabine dose dependently inhibits Aβ1-40 and Aβ1-42 with an approximate half maximal inhibitory concentration of 640 μg/mL for both Aβ1-40 and Aβ1-42 in 7W CHO cells. Anatabine inhibits sAPPβ secretion without impacting sAPPα suggesting that Anatabine is preventing the β-cleavage of amyloid precursor protein (APP)[1]. Western Blot Analysis[1] Cell Line: |
| In Vivo | Anatabine (0.5-2 mg/kg; intraperitoneal injection; daily; for 4 days; transgenic mouse) treatment significantly lowers brain soluble Aβ1-40 and Aβ1-42 levels in a transgenic mouse model of Alzheimer's disease[1]. Animal Model: |
| Name | Anatabine dicitrate |
| Formula | C22H28N2O14 |
| Molar Mass | 544.46 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Paris D, et al. Anatabine lowers Alzheimer's Aβ production in vitro and in vivo. Eur J Pharmacol. 2011 Nov 30;670(2-3):384-91. [2]. Xing H, et al. A Pharmacological Comparison of Two Isomeric Nicotinic Receptor Agonists: The Marine Toxin Isoanatabine and the Tobacco Alkaloid Anatabine. Mar Drugs. 2020 Feb 11;18(2). pii: E106. [3]. eo EJ, et al. Phytochemicals as inhibitors of NF-κB for treatment of Alzheimer's disease. Pharmacol Res. 2018 Mar;129:262-273. |