Columbianadin
(Synonyms: 二氢欧山芹醇当归酸酯) 目录号 : GN10123
A coumarin with diverse biological activities
Cas No.:5058-13-9
Sample solution is provided at 25 µL, 10mM.
Columbianadin, a natural coumarin from, is known to have various biological activities including anti-inflammatory and anti-cancer effects.
Columbianadin (CBN) effectively suppresses the growth of colon cancer cells. Low concentration (up to 25 μM) of Columbianadin induces apoptosis, and high concentration (50 μM) of Columbianadin induces necroptosis. The induction of apoptosis by Columbianadin is correlated with the modulation of caspase-9, caspase-3, Bax, Bcl-2, Bim and Bid, and the induction of necroptosis is related with RIP-3, and caspase-8. In addition, Columbianadin induces the accumulation of ROS and imbalance in the intracellular antioxidant enzymes such as SOD-1, SOD-2, catalase and GPx-1. Columbianadin shows the most effective growth inhibitory activity against human colorectal cancer cells. Accordingly, further study is performed using HCT116 cells to give the detailed growth-inhibitory mechanism of action mediated by Columbianadin. The cells treated with various concentrations of Columbianadin (0-100 μM) exhibit a dose- and time-dependent growth inhibition with an IC50 value of 47.2 and 32.4 μM after 48 and 72 h incubation, respectively. Treatment of various concentrations (12.5, 25, and 50 μM) of Columbianadin for 48 h in HCT116 cells decreases the number of cells and increases the floating cells. Apparent morphological changes with round-shape and dying cells are also observed at 25 and 50 μM Columbianadin -treated cells[1].
The analysis method is successfully applied to a tissue distribution study of Columbianadin (CBN) and Columbianetin (CBT) after intravenous administration of Columbianadin to rats. The results of this study indicated that Columbianadin can be detected in all of the selected tissues after i.v. administration. Columbianadin is distributed to rat tissues rapidly and can be metabolized to CBT in most detected tissues. Of the detected tissues, heart had the highest uptake of Columbianadin, which suggests that heart might be one of the main target tissues of Columbianadin [2].
References:
[1]. Kang JI, et al. Columbianadin Inhibits Cell Proliferation by Inducing Apoptosis and Necroptosis in HCT116 Colon Cancer Cells. Biomol Ther (Seoul). 2016 May 1;24(3):320-7.
[2]. Zhang YB, et al. Tissue distribution study of columbianadin and its active metabolite columbianetin in rats. Biomed Chromatogr. 2016 Feb;30(2):256-62.
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Cell experiment: |
The effect of Columbianadin on the cell proliferation is evaluated by SRB cellular protein-staining method. The cells are seeded in 96-well plates with various concentrations of Columbianadin and incubated at 37°C in a humidified incubator with 5% CO2 for 48 and 72 h. The cells are fixed with 10% trichloroacetic acid (TCA) solution for 30 min at 4°C, washed 5 times with tap water, and dried in the air. The cells are stained with 0.4% SRB in 1% acetic acid solution for 1 h at room temperature. After washing out the unbound dye and drying, the stained cells are dissolved in 10 mM Tris buffer (pH 10.0), and the absorbance is measured at 515 nm. Cell viability is calculated by comparing to the absorbance of the vehicle-treated control group. The IC50 values are calculated by non-linear regression analysis using the Table Curve 2D v5.01 software[1]. |
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Animal experiment: |
Rats[2] For tissue distribution study, 20 male Sprague-Dawley rats (200±10 g) are divided into four groups (n=5 per group), and Columbianadin is i.v. administered to overnight fasted rats at a single dose of 20 mg/kg. The rats in the four groups are sacrificed by decapitation at 10, 30, 60 and 120 min. Then the tissues of liver, lung, kidney, spleen, heart, stomach, intestine, brain, testis and muscle are removed and washed. Each tissue sample is weighted and stored at -20 °C until analysis. |
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References: [1]. Kang JI, et al. Columbianadin Inhibits Cell Proliferation by Inducing Apoptosis and Necroptosis in HCT116 Colon Cancer Cells. Biomol Ther (Seoul). 2016 May 1;24(3):320-7. |
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| Cas No. | 5058-13-9 | SDF | |
| 别名 | 二氢欧山芹醇当归酸酯 | ||
| 化学名 | 2-[(8S)-2-oxo-8,9-dihydrofuro[2,3-h]chromen-8-yl]propan-2-yl (Z)-2-methylbut-2-enoate | ||
| Canonical SMILES | CC=C(C)C(=O)OC(C)(C)C1CC2=C(O1)C=CC3=C2OC(=O)C=C3 | ||
| 分子式 | C19H20O5 | 分子量 | 328.35 |
| 溶解度 | ≥ 32.8mg/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 | 3.0455 mL | 15.2277 mL | 30.4553 mL |
| 5 mM | 0.6091 mL | 3.0455 mL | 6.0911 mL |
| 10 mM | 0.3046 mL | 1.5228 mL | 3.0455 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet