表小檗碱

• 常用名: 表小檗碱
• 英文名: Epiberberine
• CAS号: 6873-09-2
• 分子量: 336.36
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₁₈NO₄+
• 熔点: 260ºC
• 闪点: N/A

表小檗碱用途

Epiberberine 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 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[3]有潜在治疗作用[1]。在 3T3-L1 细胞分化早期,Epiberberine 能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路[3]。

表小檗碱名称

• 中文名: 表小檗碱
• 英文名: Epiberberine

表小檗碱生物活性

• 描述: Epiberberine 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 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[3]有潜在治疗作用[1]。在 3T3-L1 细胞分化早期,Epiberberine 能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路[3]。
• 相关类别:
  信号通路 >> 神经信号通路 >> 疼痛
  信号通路 >> 神经信号通路 >> β-分泌
  天然产物 >> 生物碱
  研究领域 >> 代谢疾病
  研究领域 >> 神经疾病
• 靶点实验:

  IC50: 1.07 μM (AChE), 6.03 μM (BChE), 8.55 μM (BACE1)[2]

• 体外研究: Epiberberine(0,12.5,25或50μM)剂量依赖性地抑制3T3-L1脂肪细胞中的细胞甘油三酯积累,IC50为52.8μM[2]。 Epiberberine(12.5-50μM)抑制3T3-L1脂肪细胞分化早期的Raf/MEK1/ERK1/2和AMPKα/ Akt通路[2]。 Epiberberine(0.2,1,5μg/ mL)以浓度依赖性方式抑制HepG2细胞中的葡萄糖摄取[3]。
• 体内研究: Epiberberine(225 mg/kg,每日口服40天)可降低KK-Ay小鼠的体重,食物消耗,水分摄入量和尿量[3]。
• 参考文献:

  [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.

表小檗碱物理化学性质

• 熔点: 260ºC
• 分子式: C₂₀H₁₈NO₄+
• 分子量: 336.36
• PSA: 40.80000
• LogP: -0.99
• InChIKey: FPJQGFLUORYYPE-UHFFFAOYSA-N
• SMILES: COc1cc2c(cc1OC)-c1cc3ccc4c(c3c[n+]1CC2)OCO4
• 储存条件: 2-8C

表小檗碱靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

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表小檗碱英文别名

• HMS2229E04
• Benz(a)-1,3-benzodioxolo(4,5-g)quinolizinium,11,12-dihydro-8,9-dimethoxy
• GNF-Pf-2355
• epiberberinium
• 8,9-dimethoxy-11,12-dihydro-[1,3]dioxolo[4,5-h]isoquino[2,1-b]isoquinolinylium
• 8,9-Dimethoxy-11,12-dihydro[1,3]dioxolo[4,5-h]isoquinolino[2,1-b]isoquinolin-13-ium
• pseudo-Epiberberin
• Epiberberin