Cirsimaritin
(Synonyms: 蓟黄素) 目录号 : GC31120
Cirsimaritin是一种存在于植物中的二甲氧基黄酮，具有抗癌潜力，并显示出显著的抗菌、抗氧化、解痉作用，同时还可抑制环氧合酶-1。
Cas No.:6601-62-3
Sample solution is provided at 25 µL, 10mM.
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Cirsimaritin is a dimethoxy flavonoid found in plants, it has anticancer potential and shows potent antimicrobial, antioxidant, antispasmodic, activity, and also inhibits cyclooxygenase-1[1-3].
Cirsimaritin significantly decreased cell proliferation in the NCIH-520 cell line, with an IC50 value of 23.29 ± 3.51µM[4]. Cirsimaritin(0–120µg/mL; 20h) inhibited interleukin-6, tumor necrosis factor-α, and NO production in a concentration-dependent manner in lipopolysaccharide (LPS)-stimulated RAW264.7 cells[5]. Cirsimaritin(5-20µg/mL) reduced viral titers and influenza A virus (IAV) RNA and protein synthesis in a dose-dependent manner[6].
Cirsimaritin(10mg/kg; i.g)ffectively prevented DSS-induced colon inflammation in mice by mitigating mucosal damage and inflammatory cell infiltration. It significantly downregulated proinflammatory cytokines such as MMP9, NF-κB, COX-2, and iNOS. Additionally, cirsimaritin reversed DSS-induced effects, including weight loss, colon shortening, tissue damage, increased inflammatory cells, and elevated cytokine secretion[7]. Treatment with cirsimaritin(0.5-1mg/kg; p.o; 8 weeks) reduced the severity of liver injury in the experimental mouse model of metabolic dysfunction-associated fatty liver disease (MAFLD) by inhibiting hepatic steatosis, oxidative stress, inflammation, and liver fibrosis[8].
References:
[1]. Benali T, Jaouadi I, et,al. The Current State of Knowledge in Biological Properties of Cirsimaritin. Antioxidants (Basel). 2022 Sep 19;11(9):1842. doi: 10.3390/antiox11091842. PMID: 36139916; PMCID: PMC9495358.
[2]. Ben Sghaier M, Skandrani I, et,al. Flavonoids and sesquiterpenes from Tecurium ramosissimum promote antiproliferation of human cancer cells and enhance antioxidant activity: a structure-activity relationship study. Environ Toxicol Pharmacol. 2011 Nov;32(3):336-48. doi: 10.1016/j.etap.2011.07.003. Epub 2011 Jul 12. PMID: 22004952.
[3]. Nyiligira E, Viljoen AM, et,al. Phytochemistry and in vitro pharmacological activities of South African Vitex (Verbenaceae) species. J Ethnopharmacol. 2008 Oct 28;119(3):680-5. doi: 10.1016/j.jep.2008.07.004. Epub 2008 Jul 16. PMID: 18678237.
[4]. Pathak G, Singh S, et,al. Cirsimaritin, a lung squamous carcinoma cells (NCIH-520) proliferation inhibitor. J Biomol Struct Dyn. 2021 Jun;39(9):3312-3323. doi: 10.1080/07391102.2020.1763198. Epub 2020 May 13. PMID: 32362196.
[5]. Shin MS, Park JY, et,al. Anti-inflammatory effects and corresponding mechanisms of cirsimaritin extracted from Cirsium japonicum var. maackii Maxim. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3076-3080. doi: 10.1016/j.bmcl.2017.05.051. Epub 2017 May 17. PMID: 28554870.
[6]. sYan H, Wang H, et,al. Cirsimaritin inhibits influenza A virus replication by downregulating the NF-κB signal transduction pathway. Virol J. 2018 May 21;15(1):88. doi: 10.1186/s12985-018-0995-6. PMID: 29783993; PMCID: PMC5963025.
[7]. Alqudah A, Qnais E, et,al. Cirsimaritin Alleviates Dextran Sodium Sulfate-Induced Acute Colitis in Experimental Animals: A Therapeutic Approach for Inflammatory Bowel Disease. Prev Nutr Food Sci. 2024 Mar 31;29(1):31-39. doi: 10.3746/pnf.2024.29.1.31. PMID: 38576881; PMCID: PMC10987388.
[8]. Che DN, Shin JY, et,al. Ameliorative effects of Cirsium japonicum extract and main component cirsimaritin in mice model of high-fat diet-induced metabolic dysfunction-associated fatty liver disease. Food Sci Nutr. 2021 Sep 1;9(11):6060-6068. doi: 10.1002/fsn3.2548. PMID: 34760237; PMCID: PMC8565240.
Cirsimaritin是一种存在于植物中的二甲氧基黄酮，具有抗癌潜力，并显示出显著的抗菌、抗氧化、解痉作用，同时还可抑制环氧合酶-1[1-3]。
Cirsimaritin显著抑制了NCIH-520细胞系的增殖，其IC50值为23.29 ± 3.51µM[4]。在脂多糖(LPS)刺激的RAW264.7细胞中，Cirsimaritin(0–120µg/mL; 20h)以浓度依赖的方式抑制了白介素-6（IL-6）、肿瘤坏死因子-α(TNF-α)和一氧化氮(NO)的产生[5]。此外，Cirsimaritin(5–20µg/mL)以剂量依赖的方式降低了病毒滴度，并抑制了甲型流感病毒(IAV)的RNA和蛋白质合成[6]。
Cirsimaritin(10mg/kg; i.g)通过缓解粘膜损伤和炎性细胞浸润，有效预防了DSS诱导的小鼠结肠炎症。它显著下调了MMP9、NF-κB、COX-2和iNOS 等促炎性细胞因子的表达。此外，Cirsimaritin逆转了DSS诱导的体重减轻、结肠缩短、组织损伤、炎性细胞增加以及细胞因子分泌升高等效应[7]。在代谢功能障碍相关脂肪性肝病(MAFLD)实验性小鼠模型中，Cirsimaritin(0.5-1mg/kg; p.o; 8 weeks)通过抑制肝脂肪变性、氧化应激、炎症及肝纤维化，降低了肝损伤的严重程度[8]。
| Cell experiment [1]: | |
Cell lines | NCIH-520 cell line |
Preparation Method | Cells were cultured in high glucose DMEM or RPMI media and supplemented with 1% Ab/Am and 10% FBS and placed in a CO2 incubator at 37 ℃ temperature in 95% humidity. Cells were seeded in a sterile 96-well flat-bottom cell culture plates with approximately 2 × 103 cells/well in each well, and the plates were incubated for 24h in CO2 incubator. After 24h of incubation, cells were treated with different concentrations of cirsimaritin, ranging from 0.1-100μM and followed by incubation for 24h. |
Reaction Conditions | 0.1-100μM; 24h |
Applications | Cirsimaritin significantly decreased cell proliferation in the NCIH-520 cell line, with an IC50 value of 23.29 ± 3.51µM. |
| Animal experiment [2]: | |
Animal models | Male Swiss albino mice |
Preparation Method | Mice were given a regimen of cirsimaritin, which was administered at a daily dose of 10mg/kg body weight (BW) through gavage, before they were exposed to DSS (4% DSS in their drinking water for 6 days). |
Dosage form | 10mg/kg; i.g |
Applications | Cirsimaritin maintains BW (body weight) and reduces DAI (disease activity index) in mice with DSS (dextran sulfate sodium)-induced colitis. |
References: | |
| Cas No. | 6601-62-3 | SDF | |
| 别名 | 蓟黄素 | ||
| Canonical SMILES | O=C1C=C(C2=CC=C(O)C=C2)OC3=CC(OC)=C(OC)C(O)=C13 | ||
| 分子式 | C17H14O6 | 分子量 | 314.29 |
| 溶解度 | DMSO : 22.73 mg/mL (72.32 mM; Need ultrasonic) | 储存条件 | Store at -20°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 | 3.1818 mL | 15.9089 mL | 31.8177 mL |
| 5 mM | 0.6364 mL | 3.1818 mL | 6.3635 mL |
| 10 mM | 0.3182 mL | 1.5909 mL | 3.1818 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)
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