Epiberberine-chloride

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Name:Epiberberine chloride; 
Cat. No. :CS-6060
CAS No. :889665-86-5
Formula:C20H18ClNO4
M. Wt. : 371.81
Solubility:DMSO: 7.4 mg/mL (Need ultrasonic)

Epiberberine chloride, a natural alkaloid, is a BACE1 inhibitor, which also exhibits inhibition activity on CYP2D6 and aldose reductase, alpha-adrenoceptors, acetylcholinesterase (AChE), butyrylcholinesterase, and b-site amyloid precursor protein cleaving enzyme 1.In Vitro: Epiberberine has inhibitory effects on adipocyte differentiation and significantly decreases lipid accumulation by downregulating an adipocyte-specific transcription factor, sterol regulatory element-binding protein-1 (SREBP-1). Furthermore, epiberberine markedly suppresses the differentiation-mediated phosphorylation of components of both the Raf/mitogen-activated protein kinase 1 (MEK1)/extracellular signal-regulated protein kinase 1/2 (ERK1/2) and AMP-activated protein kinase-α1 (AMPKα)/Akt pathways. In addition, gene expression of fatty acid synthase (FAS) is significantly inhibited by treatment with epiberberine during adipogenesis. The anti-adipogenic effect of epiberberine is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during 3T3-L1 adipocyte differentiation. Moreover, the anti-adipogenic effects of epiberberine are not accompanied by modulation of β-catenin[2]. Epiberberine shows significant inhibition on CYP2D6 with IC50 value of 35.22 μM, but has no obvious inhibiting effect on the activities of CYP3A4, CYP1A2, CYP2E1 and CYP2C9[3]. In Vivo: Epiberberine (23.35, 46.70 or 70.05 mg/kg/day) dose-and time-dependently reduces body weight gain of dyslipidemia hamster. The high dose of epiberberine (EBBR(H)) remarkably reduces the weight of epididymal adipose tissue, perirenal adipose tissue and liver by 17.1%, 31.9%, 18.4%, respectively[1].

Yang XY, et al. [Identification of metabolites of epiberberine in rat liver microsomes and its inhibiting effects on CYP2D6]. Zhongguo Zhong Yao Za Zhi. 2014 Oct;39(19):3855-9. 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. Zou ZY, et al. Epiberberine reduces serum cholesterol in diet-induced dyslipidemia Syrian golden hamsters via network pathways involving cholesterol metabolism. Eur J Pharmacol. 2016 Mar 5;774:1-9.