Epiberberine chloride 是从黄连中得到的生物碱，为有效的 AChE 和 BChE 抑制剂，和非竞争性的 BACE1 抑制剂，IC50 值分别为 1.07，6.03 和 8.55 μM。Epiberberine chloride 具有抗氧化作用，能够清除 ONOO- (IC50，16.83 μM)，对阿尔滋海默症和糖尿病有潜在治疗作用。在 3T3-L1 细胞分化早期，Epiberberine chloride 能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路。
CAS：889665-86-5
分子式：C20H18ClNO4
分子量：371.81
纯度：98%
存储：Store at -20°C

Background:

Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO- scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease[1]. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways[2]. Epiberberine has the potential effect in the research of diabetic disease[3].

Epiberberine (0, 12.5, 25, or 50 μM) dose-dependently inhibits cellular triglyceride accumulation in 3T3-L1 adipocytes, with an IC50 of 52.8 μM[2]. Epiberberine (12.5-50 μM) suppresses the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways in the early stage of 3T3-L1 adipocyte differentiation[2].Epiberberine (0.2, 1, 5 μg/mL) inhibits glucose uptake in HepG2 cells in a concentration-dependent manner[3].

Epiberberine (225 mg/kg, p.o. daily for 40 days) reduces body weight, food consumption, water intake, and urinary output of KK-Ay mice[3].

[1]. Jung HA, et al. Anti-Alzheimer and antioxidant activities of Coptidis Rhizoma alkaloids. Biol Pharm Bull. 2009 Aug;32(8):1433-8. [2]. Choi JS, et al. Anti-adipogenic effect of epiberberine is mediated by regulation of the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Arch Pharm Res. 2015 Dec;38(12):2153-62. [3]. Ma H, et al. Antihyperglycemia and Antihyperlipidemia Effect of Protoberberine Alkaloids From Rhizoma Coptidis in HepG2 Cell and Diabetic KK-Ay Mice. Drug Dev Res. 2016 Jun;77(4):163-70.