Scutellarin
(Synonyms: 野黄芩苷) 目录号 : GN10624
Scutellarin是一种具有多种生物活性的黄酮。
Cas No.:27740-01-8
Sample solution is provided at 25 µL, 10mM.
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Scutellarin is a flavonoid with multiple biological activities[1]. Scutellarin can prevent endothelial dysfunction and prevent atherosclerosis through antioxidant activity[2]. Scutellarin has anti-HIV-1IIIB, HIV-1(74V) and HIV-1KM018 activities with EC50 of 26μM, 253μM and 136μM, respectively[3].
In vitro, Scutellarin (0-210μM) treated human renal cancer cells (ACHN and 786-O cells) for 24-72h inhibited cell proliferation in a dose- and time-dependent manner, induced cell apoptosis and cell cycle arrest at the G0/G1 phase, and increased the expression of phosphatase and tensin homolog (PTEN)[4]. Scutellarin (50μM) pre-treated BV-2 cells for 30min inhibited the production of NO, TNFα, IL-1β and ROS induced by lipopolysaccharide (LPS), and inhibited LPS-induced nuclear translocation and DNA binding activity of nuclear factor κB (NF-κB)[5].
In vivo, Scutellarin (30, 60mg/kg/day) was orally treated for 3 weeks in mice with H1975-Luciferase cell xenografts, which significantly inhibited the growth of transplanted tumors in mice, upregulated the levels of LC3-II and p-ERK1/2 in mouse lung tissue, and downregulated the level of p-AKT[6]. Scutellarin (5mg/kg) was intravenously injected to treat doxorubicin (DOX)-induced cardiac toxicity in rats, significantly reducing serum lactate dehydrogenase (LDH) activity, lipid peroxide (MDA) levels, and cardiac troponin T (cTnT) concentrations, and significantly reducing cardiac tissue damage[7].
References:
[1] Wang Z L, Wang S, Kuang Y, et al. A comprehensive review on phytochemistry, pharmacology, and flavonoid biosynthesis of Scutellaria baicalensis[J]. Pharmaceutical biology, 2018, 56(1): 465-484.
[2] Mo J, Yang R, Li F, et al. Scutellarin protects against vascular endothelial dysfunction and prevents atherosclerosis via antioxidation[J]. Phytomedicine, 2018, 42: 66-74.
[3] Zhang G H, Wang Q, Chen J J, et al. The anti-HIV-1 effect of scutellarin[J]. Biochemical and Biophysical Research Communications, 2005, 334(3): 812-816.
[4] Deng W, Han W, Fan T, et al. Scutellarin inhibits human renal cancer cell proliferation and migration via upregulation of PTEN[J]. Biomedicine & Pharmacotherapy, 2018, 107: 1505-1513.
[5] Wang S, Wang H, Guo H, et al. Neuroprotection of Scutellarin is mediated by inhibition of microglial inflammatory activation[J]. Neuroscience, 2011, 185: 150-160.
[6] Sun C Y, Li C Y, Li X F, et al. Scutellarin induces apoptosis and autophagy in NSCLC cells through ERK1/2 and AKT Signaling Pathways in vitro and in vivo[J]. Journal of Cancer, 2018, 9(18): 3247.
[7] Sun X P, Wan L L, Yang Q J, et al. Scutellarin protects against doxorubicin-induced acute cardiotoxicity and regulates its accumulation in the heart[J]. Archives of pharmacal research, 2017, 40: 875-883.
Scutellarin是一种具有多种生物活性的黄酮[1]。Scutellarin能够防止血管内皮功能障碍，并通过抗氧化来预防动脉粥样硬化[2]。Scutellarin具有抗HIV-1IIIB，HIV-1(74V)和 HIV-1KM018的活性，EC50分别为26μM，253μM和136μM[3]。
在体外，Scutellarin（0-210μM）处理人肾癌细胞（ACHN和786-O细胞）24-72h，以剂量和时间依赖性方式抑制了细胞增殖，诱导了细胞凋亡和细胞周期停滞在 G0/G1期，增加了磷酸酶和张力蛋白同源物（PTEN）的表达[4]。Scutellarin（50μM）预处理BV-2细胞30min，抑制了脂多糖（LPS）诱导的NO、TNFα、IL-1β和ROS的产生，抑制了LPS诱导的核转位和核因子κB（NF-κB）的DNA结合活性[5]。
在体内，Scutellarin（30, 60mg/kg/day）通过口服治疗H1975-Luciferase细胞异种移植小鼠3周，显著抑制了小鼠体内移植瘤的生长，上调了小鼠肺组织中LC3-II和p-ERK1/2的水平，下调了p-AKT水平[6]。Scutellarin（5mg/kg）通过静脉注射治疗阿霉素（DOX）诱导的大鼠心脏毒性，显著降低了血清中乳酸脱氢酶（LDH）活性、脂质过氧化物（MDA）水平、心肌肌钙蛋白T（cTnT）浓度，显著减少了心脏组织的损伤[7]。
| Cell experiment []: | |
Cell lines | ACHN、786-O cells |
Preparation Method | ACHN and 786-O cells were seeded into 96-well plates at the concentration of 5×103 cells per well and cultured to 70–80% confluence, cells were treated with different concentrations (0, 30, 60, 90, 120, 150, 180, and 210μM) of Scutellarin dissolved in DMSO for 24, 48, 72h at the indicated time point, 10μl of CCK-8 solution was added into each well and incubated for 2h. |
Reaction Conditions | 0, 30, 60, 90, 120, 150, 180, 210μM; 24, 48, 72h |
Applications | Scutellarin inhibites cell proliferation in dose- and time- dependent manner. |
| Animal experiment []: | |
Animal models | BALB/c nude mice |
Preparation Method | Mice were subcutaneously injected with 4×106 H1975-Luciferase cells (stably expressing fluorescence). When tumor reached approximately 100mm3, mice were randomly divided into three groups (n=8): the vehicle; the low dose Scutellarin (30mg/kg); the high dose Scutellarin (60mg/kg). At this point, Scutellarin was dissolved in PBS, and was orally administered to each mouse once a day for three weeks. The tumor dimensions were measured using digital calliper every 3 days. Before treatment or after the last administration, the tumor size was monitored by in vivo bioluminescence imaging. After 3 weeks, all mice were humanely sacrificed and the tumors were resected for protein quantitation analysis. |
Dosage form | 30, 60mg/kg/day for 3 weeks; p.o. |
Applications | Scutellarin suppressed tumor growth in mouse xenograft model. Scutellarin treatment could up-regulate LC3-II and p-ERK1/2 level, and down-regulate p-AKT. |
References: | |
| Cas No. | 27740-01-8 | SDF | |
| 别名 | 野黄芩苷 | ||
| 化学名 | (2S,3S,4S,5R,6S)-6-[5,6-dihydroxy-2-(4-hydroxyphenyl)-4-oxochromen-7-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid | ||
| Canonical SMILES | C1=CC(=CC=C1C2=CC(=O)C3=C(C(=C(C=C3O2)OC4C(C(C(C(O4)C(=O)O)O)O)O)O)O)O | ||
| 分子式 | C21H18O12 | 分子量 | 462.37 |
| 溶解度 | ≥ 46.2mg/mL in DMSO | 储存条件 | Store at 2-8°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1628 mL | 10.8139 mL | 21.6277 mL |
| 5 mM | 0.4326 mL | 2.1628 mL | 4.3255 mL |
| 10 mM | 0.2163 mL | 1.0814 mL | 2.1628 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet