Enoxolone
(Synonyms: 甘草次酸) 目录号 : GC13955
An anti-inflammatory and immunomodulatory compound
Cas No.:471-53-4
Sample solution is provided at 25 µL, 10mM.
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Glycyrrhetinic acid (enoxolone) is a major component of a plant called licorice. It has been found to have both antiviral and antifungal activities. It is able to carboxilate the replication of DNA and inhibits the production of microbial toxins and enzymes [1] [2]. In rats, 18β-Glycyrrhetinic acid potently inhibited 11β-hydroxysteroid dehydrogenase (11β-HSD) activity of hepatic and renal homogenates with IC50 values of 0.09 μm and 0.36 μm, respectively [3].
Before glucocorticoids bind the mineralocorticoid receptor (MR), the selectivity of MR for aldosterone can be exerted by enzymes, and hence competing glucocorticoids is inactivated. 11β-HSD-1 and 11β-HSD-2 and 11β-HSD-3 are three of the enzymes. 11β-HSD-1 has bidirectional activity and a Km value in the micromolar range. It is NADP+-dependent. 11β-HSD-2 exhibits only oxidase activity and has a Km in the nanomolar range. It is NAD+-dependent. In the kidney, it colocalizes with the MR [4].
JEG-3 cell line was derived from a human choriocarcinoma. In this cell line, the enzyme activity of 11β-HSD-3 was inhibited by glycyrrhetinic acid [4].
In rats, 3 h after the administration of glycyrrhetinic acid at concentration of 200 mg/kg, p.o. significantly inhibited 11β-HSD activity in the kidney and the liver. In addition, glycyrrhetinic acid slightly increased the circulating corticosterone level. In differential inhibitory effects on 11β-HSD isozyme activity, the 11-, 24- and 30-positions of glycyrrhetinic acid may play important roles. This had been showed by Data [3].
References:
[1]. Salari MH, Sohrabi N, Kadkhoda Z, et al. Antibacterial Effects of Enoxolone on Periodontopathogenic and Capnophilic Bacteria Isolated from Specimens of Periodontitis Patients. Iranian Biomedical Journal, 2003, 7(1):39-42.
[2]. Bahmani M, Rafieian-Kopaei M, Jeloudari M, et al. A review of the health effects and uses of drugs of plant licorice (Glycyrrhiza glabra L.) in Iran. Asian Pacific Journal of Tropical Disease, 2015, 5: 127-29.
[3]. Shimoyama Y, Hirabayashi K, Matsumoto H, et al. Effects of glycyrrhetinic acid derivatives on hepatic and renal 11beta-hydroxysteroid dehydrogenase activities in rats. J Pharm Pharmacol, 2003, 55(6):811-7.
[4]. Gomez-Sanchez EP, Cox D, Foecking M, et al. 11 beta-hydroxysteroid dehydrogenases of the choriocarcinoma cell line JEG-3 and their inhibition by glycyrrhetinic acid and other natural substances. Steroids, 1996, 61(3):110-5.
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Cell experiment: |
Primary microglia cultures are used in this study. For treatment assay, microglia are incubated with complete DMEM and stimulated with or without 100 ng/mL IFN-γ in the presence or absence of 18β-Glycyrrhetinic acid (25 μM and 50 μM) at 37°C in a humidified incubator with 5% CO2. For cell migration assay, the isolated primary microglia that seeded in complete DMEM medium are stimulated with or without IFN-γ (100 ng/mL), and treated with different doses of 18β-Glycyrrhetinic acid, 24 h later, the microglia culture supernatants are collected and added to the lower chambers of Transwell inserts[2]. |
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Animal experiment: |
Healthy Wistar rats (male, 200±20 g) are used and divided into five groups with 10 individuals for each group randomly. Animals in normal control (NC) group receive distilled water for 6 days and 0.5% CMC-Na for the last 3 days. Rats in Triptolide model group (TP), 18β-Glycyrrhetinic acid low-dose group (GAL+TP), and 18β-Glycyrrhetinic acid high-dose group (GAH+TP) receive distilled water, 18β-Glycyrrhetinic acid (50 mg/kg, p.o., dissolved in distilled water), or 18β-Glycyrrhetinic acid (100 mg/kg, p.o., dissolved in distilled water) for consecutive 6 days, respectively, and liver injury is induced by TP (2.4 mg/kg, p.o., suspended in 0.5% CMC-Na) for the last 3 days. Animals in the above three groups receive TP 6 hours after distilled water or 18β-Glycyrrhetinic acid treatment on the last 3 days[3]. |
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References: [1]. Huang RY, et al. 18β-Glycyrrhetinic acid suppresses cell proliferation through inhibiting thromboxane synthase in non-small cell lung cancer. PLoS One. 2014 Apr 2;9(4):e93690. |
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| Cas No. | 471-53-4 | SDF | |
| 别名 | 甘草次酸 | ||
| 化学名 | (2S,4aS,6aS,6bR,8aR,10S,12aS,12bR,14bR)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-icosahydropicene-2-carboxylic acid | ||
| Canonical SMILES | CC([C@]1([H])CC[C@]23C)([C@](O)([H])CC[C@@]1([C@@]2([H])C(C=C4[C@]5([H])C[C@](CC[C@](CC[C@]43C)5C)(C(O)=O)C)=O)C)C | ||
| 分子式 | C30H46O4 | 分子量 | 470.68 |
| 溶解度 | ≥ 19.3mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.1246 mL | 10.6229 mL | 21.2459 mL |
| 5 mM | 0.4249 mL | 2.1246 mL | 4.2492 mL |
| 10 mM | 0.2125 mL | 1.0623 mL | 2.1246 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet