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Epiberberine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Epiberberine图片
CAS NO:6873-09-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议

产品介绍
Epiberberine 是一种从黄连中分离出来的生物碱,是一种有效的 AChE 和 BChE 抑制剂,以及一种非竞争性 BACE1 抑制剂,IC50 分别为 1.07、6.03 和 8.55 μM。
Cas No.6873-09-2
别名表小檗碱
Canonical SMILESCOC1=C(C=C2C(=C1)CC[N+]3=C2C=C4C=CC5=C(C4=C3)OCO5)OC
分子式C20H18NO4
分子量336.36
溶解度≥ 12.7mg/mL in DMSO
储存条件Store at 2-8℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 8.55 μM for BACE1

Epiberberine is a natural bioactive protoberberine alkaloid from Coptidis Rhizoma. Coptidis Rhizoma and its isolated alkaloids are found to possess a variety of activities including antioxidant and neuroprotective activities.

In vitro: Among six protoberberine alkaloids from Coptidis Rhizoma exhibiting predominant cholinesterases (ChEs) inhibitory effects, only epiberberine and groenlandicine exerted good, non-competitive BACE1 inhibitory activities with IC50 values of 8.55 and 19.68 μM, respectively, as compared with a positive control, quercetin. In addition, epiberberine also showed potent AChE and BChE inhibitory effects [1].

In vivo: In rats, epiberberine could parallelly shift the dose-response curves of Clo and BHT-920 to the normal without changing the maximal effect. The pA2 values of epiberberine were found to be 6.5 and 6.8 respectively. Epiberberine was also found to antagonize the contractile response of isolated rabbit aortic strips to Meth competitively. Epiberberine given to anesthetized rats intravenously was shown to be able to temporarily decrease blood pressure and gradually accelerate heart rate. The heart rate persistently and constantly increased in spite of blood pressure restoration. These results suggested epiberberine possessed poor α-blocking action [2].

Clinical trial: N/A

References:
[1] Jung HA,Min BS,Yokozawa T,Lee JH,Kim YS,Choi JS. Anti-Alzheimer and antioxidant activities of Coptidis Rhizoma alkaloids. Biol Pharm Bull.2009 Aug;32(8):1433-8.
[2] Wang JL,Fang DC.  Effect of epiberberine on alpha-adrenoceptors. Yao Xue Xue Bao.1990;25(4):289-92.