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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Picroside II
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
39012-20-9
- 规格：
10mg/5mg
| 规格： | 10mg | 产品价格： | ￥130.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥90.0 |
Picroside II 具有抗炎和抗细胞凋亡的活性。Picroside II 是一种抗氧化剂，具有神经保护活性。
| 基本信息 | |
| CAS | No.39012-20-9 |
| 中文名称 | 胡黄连苷II |
| 英文名称 | Picroside II |
| 别名 | 6-Vanilloylcatalpol |
| 分子式 | C23H28O13 |
| 分子量 | 512.46 |
| 溶解性 | Soluble in DMSO |
| 纯度 | HPLC≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 254-247-6 |
| MDL | MFCD00135962 |
| SMILES | OC1=CC=C(C(OC(C2C3(CO)O2)C4C3C(OC5C(O)C(O)C(O)C(CO)O5)OC=C4)=O)C=C1OC |
| 靶点 | NF-kB |
| 通路 | NF-κB |
| 背景说明 | Picroside II 具有抗炎和抗细胞凋亡的活性。Picroside II 是一种抗氧化剂,具有神经保护活性。 |
| 生物活性 | Picroside II is an antioxidant with oral activity that can reduce the production of ROS and protect the blood-brain barrier (BBB) after CI/R injury， offering neuroprotective effects. Picroside II has antioxidant， immune-regulating， antiviral properties， and inhibits apoptosis. Picroside II alleviates the inflammatory response in sepsis by suppressing the activation of the NLRP3 inflammasome and NF-κB pathways[1][2][3][4][5]. |
| In Vitro | Picroside II decreased the levels of alanine aminotransferase and aspartate aminotransferase in the serum resulting from acute-liver injured mice induced with D-GalN and LPS; it also reduced the content of MDA， and thus， enhanced the activity of SOD. Picroside II 10 mg/kg was found to protect hepatocytes against Apoptosis in a dose-dependent manner; it up-regulated the expression of Bcl-2 genes， thus increased the Bcl-2/Bax ratio.[1]。RT-PCR[1]:Cell Line:Primary rat hepatocytes;Concentration:5， 10， 20 μM;Incubation Time: 24 h;Result:Upregulated bcl-2.Cell Viability Assay[2]:Cell Line:HepG2;Concentration: 0， 3， 10， 30， 100， 300 μM;Incubation Time: 24 h;Result:Showed the inhibition rate of cell growth was 24%.Western Blot Analysis[2]:Cell Line:HepG2;Concentration: 10 μM;Incubation Time:20h;Result:Increased expression of SREBP-1 protein.RT-PCR[2]:Cell Line:HepG2;Concentration:10 μM;Incubation Time: 20 h;Result:Down-regulated the expression of FATP5 and increased the expression of SCD mRNA. |
| 细胞实验 | Picroside II could significantly prevent liver toxicity in the three models of liver damage. It decreased the high levels of ALT and AST in serum induced by the administration of CCl(4)， D-GalN and AP， reduced the cellular damage of liver markedly， and appeared to be even more potent than the positive control drug of biphenyl dimethyl dicarboxylate pilules (DDB). In groups treated with different doses of picroside II， compared to the model group， the content of MDA in serum decreased evidently， whereas the content of SOD and GSH-Px increased in a dose-dependent manner， and the difference was statistically significant. Further， in the study of AP model， picroside II inhibited AP-induced liver toxicity in mice， enhanced the activity of ATPase， improved the swelling extent of mitochondria and helped to maintain a normal balance of energy metabolism.[5]。Animal Model: DGalN and LPS(HY-D1056)-induced acute liver injury in mice[1];Dosage:0， 5， 10， 20 mg/kg; administered 10 min before and 4 h after D-GalN and LPS administration;Administration:i.g.Result:Reduced the levels of alanine aminotransferase and aspartate aminotransferase in the serum， decreased MDA content， had a dose-dependent effect on hepatocyte apoptosis， and upregulated the expression of the bcl-2 gene.Animal Model:Sepsis mouse model[3];Dosage: 20 mg/kg; four times injected (2 h， 14 h， 26 h and 38 h after CLP)Administration:Intravenous injection (i.v.)Result:Improved survival， reduced sepsis-related infiltration and attenuated lung injury， enhanced bacterial clearance， reduced IL-6， IL-1β， and TNF-α levels， inhibited splenic lymphocyte apoptosis， reduced p-NF-κB (p65) expression， and reduced IL-1β and caspase-1 levels.Animal Model:Rats with cerebral ischemia-reperfusion injury[4];Dosage:20 mg/kg; single dose;Administration:Intraperitoneal injection (i.p.);Result:Reduced the nervous system score， neuronal injury， BBB damage， ROS content and NADPH oxidase activity， down-regulated the protein levels of Rac-1， Nox2， ROCK， MLCK and MMP-2， and up-regulated the expression of claudin-5.Animal Model: Mouse model of liver injury induced by CCl4， D-GalN and AP[5];Dosage:5， 10， 20mg/kg; daily; 7 days;Administration:i.g.Result: Reduced the high levels of ALT and AST in serum caused by CCl4， D-GalN and AP， significantly alleviated liver cell damage， reduced MDA， and increased SOD and GSH-Px content in a dose-dependent manner， inhibited AP-induced liver toxicity in mice， enhanced ATPase activity， and improved mitochondrial swelling. |
| 数据来源文献 | [1]. Hua Gao， et al. Inhibitory effect of picroside II on hepatocyte apoptosis. Acta Pharmacol Sin. 2005 Jun;26(6):729-36. [2]. Hiteshi Dhami-Shah， et al. Picroside II attenuates fatty acid accumulation in HepG2 cells via modulation of fatty acid uptake and synthesis. Clin Mol Hepatol. 2018 Mar;24(1):77-87. [3]. Huang Y， et al. Picroside II protects against sepsis via suppressing inflammation in mice. Am J Transl Res. 2016 Dec 15;8(12):5519-5531. eCollection 2016. [4]. Zhai L， et al. Picroside II protects the blood-brain barrier by inhibiting the oxidative signaling pathway in cerebral ischemia-reperfusion injury. PLoS One. 2017 Apr 7;12(4):e0174414. [5]. Hua Gao， et al. Anti-lipid peroxidation and protection of liver mitochondria against injuries by picroside II. World J Gastroenterol. 2005 Jun 28;11(24):3671-4. |
| 单位 | 瓶 |
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IP0730 胡黄连苷II 抑制剂/拮抗剂/激动剂 索莱宝
￥90 - 130
