Tangeretin
(Synonyms: 桔皮素; Tangeritin; NSC53909; NSC618905) 目录号 : GN10797
Tangeretin是一种从柑橘皮中提取的天然多甲氧基黄酮化合物，是Notch-1的抑制剂。
Cas No.:481-53-8
Sample solution is provided at 25 µL, 10mM.
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Tangeretin is a naturally polymethoxylated flavone compound extracted from the citrus peel and acts as a Notch-1 inhibitor[1]. Tangeretin exhibits antitumor properties in several types of cancerous cell lines[2] and targets some hallmarks of cancer, such as antiproliferative, apoptotic, anti-inflammatory, anti-metastatic, anti-angiogenic, antioxidant, regulatory expression of tumor-suppressor genes, and epigenetic modulation[3].
Tangeretin (20μM; 24h) inhibits ROS generation and GSH depletion induced by t-BHP in HepG2 cells[4]. Tangeretin (45μM; 48h) treatment increases G2/M arrest and apoptosis by modulating PTEN and cell-cycle regulated genes such as cyclin-D mRNA and protein expressions[5].
Tangeretin (100mg/kg) pre-treatment significantly alleviated liver damage, inhibited cisplatin-induced lipid profile aberrations (total cholesterol and triglycerides) and diminished histopathologic structural damage in rat liver tissues[6]. Tangeretin (100mg/kg; 3d; i.g.) inhibits human respiratory syncytial virus (RSV) replication and RSV-induced lung inflammation in mouse[7].
References:
[1]. Liu LL, Li FH, Zhang Y, et al. Tangeretin has anti-asthmatic effects via regulating PI3K and Notch signaling and modulating Th1/Th2/Th17 cytokine balance in neonatal asthmatic mice. Braz J Med Biol Res. 2017 Jul 20;50(8):e5991. doi: 10.1590/1414-431X20175991. PMID: 28746467; PMCID: PMC5520220.
[2]. Arafa EA, Shurrab NT, Buabeid MA. Therapeutic Implications of a Polymethoxylated Flavone, Tangeretin, in the Management of Cancer via Modulation of Different Molecular Pathways. Adv Pharmacol Pharm Sci. 2021 Mar 5;2021:4709818. doi: 10.1155/2021/4709818. PMID: 33748757; PMCID: PMC7954633.
[3]. de Luna FCF, Ferreira WAS, Casseb SMM, de Oliveira EHC. Anticancer Potential of Flavonoids: An Overview with an Emphasis on Tangeretin. Pharmaceuticals (Basel). 2023 Aug 30;16(9):1229. doi: 10.3390/ph16091229. PMID: 37765037; PMCID: PMC10537037.
[4]. Liang F, Fang Y, Cao W, et al. Attenuation of tert-Butyl Hydroperoxide (t-BHP)-Induced Oxidative Damage in HepG2 Cells by Tangeretin: Relevance of the Nrf2-ARE and MAPK Signaling Pathways. J Agric Food Chem. 2018 Jun 27;66(25):6317-6325. doi: 10.1021/acs.jafc.8b01875. Epub 2018 Jun 14. PMID: 29871486.
[5]. Ma LL, Wang DW, Yu XD, et al. Tangeretin induces cell cycle arrest and apoptosis through upregulation of PTEN expression in glioma cells. Biomed Pharmacother. 2016 Jul;81:491-496. doi: 10.1016/j.biopha.2016.04.006. PMID: 27261630.
[6]. Omar HA, Mohamed WR, Arab HH, et al. Tangeretin Alleviates Cisplatin-Induced Acute Hepatic Injury in Rats: Targeting MAPKs and Apoptosis. PLoS One. 2016 Mar 31;11(3):e0151649. doi: 10.1371/journal.pone.0151649. PMID: 27031695; PMCID: PMC4816535.
[7]. Xu JJ, Liu Z, Tang W, et al. Tangeretin from Citrus reticulate Inhibits Respiratory Syncytial Virus Replication and Associated Inflammation in Vivo. J Agric Food Chem. 2015 Nov 4;63(43):9520-7. doi: 10.1021/acs.jafc.5b03482. Epub 2015 Oct 26. PMID: 26468759.
Tangeretin是一种从柑橘皮中提取的天然多甲氧基黄酮化合物，是Notch-1的抑制剂[1]。Tangeretin在多种癌细胞系中表现出抗肿瘤特性[2]，并针对癌症的多个特征发挥作用，例如抗增殖、促凋亡、抗炎、抗转移、抗血管生成、抗氧化、调控抑癌基因表达以及表观遗传调控等[3]。
Tangeretin（20μM；24小时）在HepG2细胞中可以抑制由t-BHP诱导的ROS生成和GSH耗竭[4]。Tangeretin（45μM; 48h）通过调控PTEN和细胞周期相关基因，比如cyclin-D的mRNA和蛋白质的表达来增加G2/M期阻滞和凋亡[5]。
Tangeretin（100mg/kg）预处理可以显著减轻了肝损伤，抑制顺铂诱导的脂质谱异常（总胆固醇和甘油三酯），并减少大鼠肝组织的组织病理学结构损伤[6]。Tangeretin（100mg/kg; 3d; i.g.）可以抑制人类呼吸道合胞病毒（RSV）的复制和RSV引起的小鼠肺部炎症[7]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were pretreated with Tangeretin (0−20μM) for 24h and then exposed to t-BHP for another 3h. Then MTT assay was used for the determination of cytotoxicity. |
Reaction Conditions | 20μM; 24h |
Applications | Tangeretin markedly protected HepG2 cells from t-BHP-induced cytotoxicity. |
| Animal experiment [2]: | |
Animal models | Adult male Wistar Rats |
Preparation Method | Rats received Tangeretin for 7 days and a single dose of cisplatin (7.5mg/kg) on the 2nd day of the experiment day, 1 hour after the dose of Tangeretin. Animals were sacrificed and blood samples were collected to separate serum. The collected serum was used for the colorimetric estimation of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) by measuring the amount of pyruvate or oxaloacetate produced by forming 2,4-dinitrophenylhydrazone. |
Dosage form | 100mg/kg/day; 7d; oral |
Applications | Tangeretin pretreatment significantly alleviated the development of cisplatin-induced liver tissue damage. |
References: | |
| Cas No. | 481-53-8 | SDF | |
| 别名 | 桔皮素; Tangeritin; NSC53909; NSC618905 | ||
| 化学名 | 5,6,7,8-tetramethoxy-2-(4-methoxyphenyl)chromen-4-one | ||
| Canonical SMILES | COC1=CC=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C(=C3OC)OC)OC)OC | ||
| 分子式 | C20H20O7 | 分子量 | 372.38 |
| 溶解度 | ≥ 37.2mg/mL in DMSO | 储存条件 | Store at RT |
| 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 | 2.6854 mL | 13.4271 mL | 26.8543 mL |
| 5 mM | 0.5371 mL | 2.6854 mL | 5.3709 mL |
| 10 mM | 0.2685 mL | 1.3427 mL | 2.6854 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。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet