ANATABINE DICITRATE
ANATABINE DICITRATE 用途与合成方法
NF-κB
Amyloid-β (Aβ)
α4β2 nAChR
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).
Western Blot Analysis
| Cell Line: | SHSY-5Y cells |
| Concentration: | 600 μg/mL |
| Incubation Time: | 24 hours |
| Result: | An inhibition of p65 NF-κB phosphorylation was observed. |
RT-PCR
| Cell Line: | SHSY-5Y cells |
| Concentration: | 500 μg/mL, 1000 μg/mL |
| Incubation Time: | 30 minutes |
| Result: | Fully prevented the increase in BACE-1 mRNA levels induced by TNF-α. |
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.
| Animal Model: | Transgenic mice overexpressing the human APP695sw mutation and the presenilin-1 mutation M146L (Tg PS1/APPsw) (50 week-old) |
| Dosage: | 0.5 mg/kg, 2 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 4 days |
| Result: | Significantly lowered brain soluble Aβ 1-40 and Aβ 1-42 levels in a transgenic mouse model of Alzheimer's disease. |
