Emodin是一种具有抗肿瘤、抗菌和血管舒张活性的生物活性蒽醌类化合物。
Cas No.:518-82-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Emodin is a bioactive anthraquinone with anti-tumor, anti-bacterial, and vasorelaxant effects [1]. Emodin inhibits the adhesion of many tumor cells by suppressing lipid raft coalescence and interfering with integrin clustering and focal adhesion complex (FAC) formation [2]. Emodin has been widely used to down-regulate the expression of estrogen receptor α (ERα) and inhibit the proliferation of breast cancer cells[3].
In vitro, Emodin treatment for 72 hours significantly inhibited the proliferation of A549 cells, with an IC50 value of 16.85μg/ml, and caused the cells to shrink in size[4]. Treatment with 60µM Emodin for 48 hours significantly increased the p53 protein level in HepG2/C3A cells, activated the expression of Caspase-3, and induced cell arrest at the G2/M phase[5]. Treatment with 3µM Emodin for 5 days significantly inhibited apoptosis of human umbilical vein endothelial cells (HUVECs) induced by high glucose (22.2mM), reduced CCL5 expression, and prevented the activation of p38 MAPK and ERK1/2 caused by high glucose[6].
In vivo, Emodin treatment via intraperitoneal injection at a dose of 10mg/kg, every other day, for 10 days, inhibited the synovial inflammation and joint destruction in mice with collagen-induced arthritis (CIA), and reduced the production of pro-inflammatory cytokines in joint tissues and serum[7]. Oral administration of Emodin at the 100mg/kg dose twice daily for 35 days significantly improved the metabolic abnormalities in diet-induced obese (DIO) mice, and reduced serum insulin levels and lipid levels[8].
References:
[1] Monisha B A, Kumar N, Tiku A B. Emodin and its role in chronic diseases[J]. Anti-inflammatory nutraceuticals and chronic diseases, 2016: 47-73.
[2] Hsu S C, Chung J G. Anticancer potential of emodin[J]. BioMedicine, 2012, 2(3): 108-116.
[3] Huang P H, Huang C Y, Chen M C, et al. Emodin and aloe‐emodin suppress breast cancer cell proliferation through ERα inhibition[J]. Evidence‐based Complementary and Alternative Medicine, 2013, 2013(1): 376123.
[4] Li W Y, Ng Y F, Zhang H, et al. Emodin elicits cytotoxicity in human lung adenocarcinoma A549 cells through inducing apoptosis[J]. Inflammopharmacology, 2014, 22(2): 127-134.
[5] Shieh D E, Chen Y Y, Yen M H, et al. Emodin-induced apoptosis through p53-dependent pathway in human hepatoma cells[J]. Life sciences, 2004, 74(18): 2279-2290.
[6] Gao Y, Zhang J, Li G, et al. Protection of vascular endothelial cells from high glucose-induced cytotoxicity by emodin[J]. Biochemical Pharmacology, 2015, 94(1): 39-45.
[7] Hwang J K, Noh E M, Moon S J, et al. Emodin suppresses inflammatory responses and joint destruction in collagen-induced arthritic mice[J]. Rheumatology, 2013, 52(9): 1583-1591.
[8] Feng Y, Huang S, Dou W, et al. Emodin, a natural product, selectively inhibits 11β‐hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet‐induced obese mice[J]. British Journal of Pharmacology, 2010, 161(1): 113-126.
Emodin是一种具有抗肿瘤、抗菌和血管舒张活性的生物活性蒽醌类化合物[1]。Emodin通过抑制脂筏聚集、干扰整合素簇集和黏着斑复合物(FAC)的形成，从而抑制多种肿瘤细胞的黏附[2]。Emodin已被广泛用于下调雌激素受体α(ERα)的表达并抑制乳腺癌细胞的增殖[3]。
在体外，Emodin处理72小时显著抑制了A549细胞的增殖，IC50值为16.85µg/ml，并导致细胞体积缩小[4]。用60µM的Emodin处理HepG2/C3A细胞48小时，显著提高了p53蛋白水平，激活了Caspase-3的表达，并诱导细胞阻滞在G2/M期[5]。用3µM的Emodin处理人脐静脉内皮细胞(HUVECs) 5天，显著抑制了高糖(22.2mM)诱导的细胞凋亡，降低了CCL5表达，并阻止了高糖引起的p38 MAPK和ERK1/2的激活[6]。
在体内，每隔一天腹腔注射10mg/kg剂量的Emodin，连续10天，抑制了胶原诱导的关节炎(CIA)小鼠的滑膜炎症和关节破坏，并减少了关节组织和血清中促炎细胞因子的产生[7]。每日两次口服100mg/kg剂量的Emodin，连续35天，显著改善了饮食诱导肥胖(DIO)小鼠的代谢异常，并降低了血清胰岛素水平和血脂水平[8]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were grown in low-glucose Dulbecco's Modified Eagle Medium (DMEM) with 10% (v/v) fetal bovine serum (FBS), 100μg/ml streptomycin, and 100U/ml penicillin at 37°C in 5% CO2/atmosphere. 3000 A549 cells were seeded into each well of a 96-well plate for 24h, and were treated with different concentrations of Emodin (0, 5, 10, 15, 20, 25, and 30µg/ml) for different incubation periods (24, 48, and 72h), and then the cell viability was analyzed. |
Reaction Conditions | 0, 5, 10, 15, 20, 25, and 30µg/ml; 24, 48, and 72h |
Applications | Emodin treatment significantly decreased the cell viability of A549 cells in a dose-and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6J male mice |
Preparation Method | C57BL/6J male mice (3-4 weeks) were fed a formulated research diet containing 60% of the calories from fat for 12 weeks before and throughout the duration of the experiment. DIO mice were assigned to two groups and subjected to gavage treatment twice per day with vehicle (0.5% CMC) or Emodin 100mg/kg for 35 days. On the last day of treatment, 5h-fasted mice were anaesthetized with an i.p. injection of sodium pentobarbital (40mg/kg). Serum was collected for analysis. |
Dosage form | 100mg/kg; twice a day for 35 days; p.o. |
Applications | Emodin treatment significantly reduced serum insulin levels and lipid levels in DIO mice. |
References: | |
| Cas No. | 518-82-1 | SDF | |
| 别名 | 大黄素; Frangula emodin | ||
| 化学名 | 1,3,8-trihydroxy-6-methylanthracene-9,10-dione | ||
| Canonical SMILES | CC1=CC(O)=C2C(C(C3=CC(O)=CC(O)=C3C2=O)=O)=C1 | ||
| 分子式 | C15H10O5 | 分子量 | 270.24 |
| 溶解度 | ≥ 27 mg/mL in DMSO | 储存条件 | Store at 2-8°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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL |
| 5 mM | 740.1 μL | 3.7004 mL | 7.4008 mL |
| 10 mM | 370 μL | 1.8502 mL | 3.7004 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet