Coronaridine
(Synonyms: 狗牙花定碱) 目录号 : GC64816
Coronaridine是一种TCF/β-catenin抑制剂，IC50值为5.8μM。
Cas No.:467-77-6
Sample solution is provided at 25 µL, 10mM.
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Coronaridine is an inhibitor of TCF/β-catenin, with an IC50 value of 5.8μM[1]. Coronaridine has been widely used in neurological function studies and in development of congeners[2].
In vitro, Coronaridine showed potent cytotoxic activity in the laryngeal carcinoma cell line Hep-2, with an IC50 value of 54.47µg/mL) after 24h treatment[3]. Coronaridine treatment (10μg/ml; 24h) exhibited potent antileishmanial activity, suppressing promastigote and amastigote growth[4].
In vivo, Coronaridine treatment (72mg/kg; p.o.) for 25 minutes produced a sedative effect and reduced spontaneous activity in Male CD-1 albino mice [5].
References:
[1] Ohishi K, Toume K, Arai M A, et al. Coronaridine, an iboga type alkaloid from Tabernaemontana divaricata, inhibits the Wnt signaling pathway by decreasing β-catenin mRNA expression[J]. Bioorganic & medicinal chemistry letters, 2015, 25(18): 3937-3940.
[2] Arias H R, Tae H S, Micheli L, et al. Coronaridine congeners decrease neuropathic pain in mice and inhibit α9α10 nicotinic acetylcholine receptors and CaV2. 2 channels[J]. Neuropharmacology, 2020, 175: 108194.
[3] Rizo W F, Ferreira L E, Colnaghi V, et al. Cytotoxicity and genotoxicity of coronaridine from Tabernaemontana catharinensis A. DC in a human laryngeal epithelial carcinoma cell line (Hep-2)[J]. Genetics and molecular biology, 2013, 36: 105-110.
[4] Delorenzi J C, Attias M, Gattass C R, et al. Antileishmanial activity of an indole alkaloid from Peschiera australis[J]. Antimicrobial Agents and chemotherapy, 2001, 45(5): 1349-1354.
[5] Arias H R, Tae H S, Micheli L, et al. Coronaridine congeners decrease neuropathic pain in mice and inhibit α9α10 nicotinic acetylcholine receptors and CaV2. 2 channels[J]. Neuropharmacology, 2020, 175: 108194.
Coronaridine是一种TCF/β-catenin抑制剂，IC50值为5.8μM [1]。Coronaridine被广泛应用于神经功能研究以及衍生物的开发[2]。
在体外，Coronaridine在喉癌细胞系Hep-2中表现出显著的细胞毒活性，24小时处理后的IC50值为54.47µg/mL[7]。以10μg/mL的浓度处理24小时，Coronaridine展现出强效的抗利什曼原虫活性，可抑制前鞭毛体和无鞭毛体的生长[4]。
在体内，口服给药72mg/kg剂量的Coronaridine 25分钟后，可在雄性CD-1白化小鼠体内产生镇静作用并减少小鼠自发活动[5]。
| Cell experiment [1]: | |
Cell lines | Hep-2 cells |
Preparation Method | Hep-2 cells (2×104 cells/mL) were incubated with 15.62, 31.25, 62.5, and 125µg/mL Coronaridine, respectively, for 6 hours at 37°C in a 5% CO2 atmosphere. Minor modifications were made to the alkaline comet assay. Three hundred cells were randomly selected from three replicate slides, for a total of=900 cells, and each Coronaridine concentration was analyzed. The cells were scored for damage and divided into five categories to calculate the DNA damage index. Doxorubicin 0.2μg/mL was used as a positive control, and 1% dimethyl sulfoxide was used as a solvent control. |
Reaction Conditions | 15.62, 31.25, 62.5, and 125µg/mL; 6h |
Applications | Coronaridine treatment increased DNA damage in Hep-2 cell line in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male CD-1 albino mice |
Preparation Method | Male CD-1 albino mice weighing approximately 22 to 25g at the beginning of the experiment were used in all experiments. Ten mice were housed in each cage (26 ×41cm). Animals were fed a standard laboratory diet and tap water AD libitum and maintained at 23±1°C on a 12-h day-night cycle with light at 7 am. Neuropathic pain was produced in mice (n=10/group) intermittently by intraperitoneal (i.p.) injection of 2.4mg/kg oxaliplatin (dissolved in 5% glucose solution) on days 1-3, 6-10, and 13-14. On day 15, a coronary contrast agent (Coronaridine) that induces antineuropathic pain was administered (p.o.) at the highest dose (72mg/kg), and a hole-plate test was performed 25 minutes later. The device consisted of a 40cm square plane with 16 flush cylindrical holes (3cm in diameter) distributed in a 4×4 equispaced grid. Each mouse was placed in the center of the plate and allowed to move freely for 5min at a time. Two light beams passed from the midpoint of the plane to the midpoint on opposite sides, thus dividing the plane into four equal quadrants, automatically signaling the movement of the animal across the plate surface for a total time of 5min (i.e., spontaneous activity). Miniature photocells were present in each of the 16 wells, and the mice were recorded for a total of 5min of hole exploration time. Higher or lower exploratory activity compared with control animals indicates anxiolytic or anxiogenic activity of the drug, respectively. |
Dosage form | 72mg/kg for 25min; p.o. |
Applications | Coronaridine treatment decreased locomotor activity and reduced spontaneous mobility in mice. |
References: | |
| Cas No. | 467-77-6 | SDF | Download SDF |
| 别名 | 狗牙花定碱 | ||
| 分子式 | C21H26N2O2 | 分子量 | 338.44 |
| 溶解度 | 储存条件 | 4°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 | 2.9547 mL | 14.7737 mL | 29.5473 mL |
| 5 mM | 0.5909 mL | 2.9547 mL | 5.9095 mL |
| 10 mM | 0.2955 mL | 1.4774 mL | 2.9547 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)
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