Fisetin
(Synonyms: 漆黄素) 目录号 : GN10030
Fisetin是一种天然黄酮醇，存在于许多水果和蔬菜中，具有多种生物活性。
Cas No.:528-48-3
Sample solution is provided at 25 µL, 10mM.
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Fisetin is a natural flavonol found in many fruits and vegetables with multiple biological activities[1]. Fisetin is a strong antioxidant and can be used as an effective anti-aging agent[2]. Fisetin can be used as a chemotherapeutic agent for various cancers and as a neuroprotectant[3].
In vitro, treatment of human retinoblastoma Y79 cell line with Fisetin (25, 50, 100µM) for 24-72h inhibited cell viability and proliferation, cell invasion and migration, and intracellular vascular endothelial growth factor receptor (VEGFR) expression in a time- and dose-dependent manner[4]. Treatment of glioma cells (T98G and BEAS-2B cells) with Fisetin (1-500μM) for 24h and 48h inhibited cell proliferation and induced cell apoptosis and necrosis in a time- and dose-dependent manner[5]. Fisetin (0-40μM) treated A549 cells for 24-72h, inhibited cell proliferation in a time- and dose-dependent manner, led to cell cycle arrest, and inhibited cell adhesion, invasion, and migration[6].
In vivo, Fisetin (10, 20mg/kg) was orally treated for 10 days in mice with acute otitis media, significantly downregulated the mRNA levels of IL-1β, TNF-α, IL-6, and VEGF in mouse serum and middle ear tissue in a dose-dependent manner, upregulated the protein levels of SOD1, SOD2, HO-1, and Nrf2, and improved the inflammatory damage of the middle ear in mice[7]. Fisetin (223mg/kg) was treated with 4T1 breast tumor model mice by intraperitoneal injection for 3 weeks, inhibited the growth of 4T1 cell-derived in situ breast tumors, and promoted tumor cell apoptosis[8].
References:
[1] Antika L D, Dewi R M. Pharmacological aspects of fisetin[J]. Asian Pacific Journal of Tropical Biomedicine, 2021, 11(1): 1-9.
[2] Yousefzadeh M J, Zhu Y I, McGowan S J, et al. Fisetin is a senotherapeutic that extends health and lifespan[J]. EBioMedicine, 2018, 36: 18-28.
[3] Khan N, Syed D N, Ahmad N, et al. Fisetin: a dietary antioxidant for health promotion[J]. Antioxidants & redox signaling, 2013, 19(2): 151-162.
[4] Wang L, Chen N, Cheng H. Fisetin inhibits vascular endothelial growth factor induced angiogenesis in retinoblastoma cells[J]. Oncology Letters, 2020, 20(2): 1239-1244.
[5] Pak F, Oztopcu-Vatan P. Fisetin effects on cell proliferation and apoptosis in glioma cells[J]. Zeitschrift für Naturforschung C, 2019, 74(11-12): 295-302.
[6] Wang J, Huang S. Fisetin inhibits the growth and migration in the A549 human lung cancer cell line via the ERK1/2 pathway[J]. Experimental and Therapeutic Medicine, 2018, 15(3): 2667-2673.
[7] Li P, Chen D, Huang Y. Fisetin administration improves LPS-induced acute otitis media in mouse in vivo[J]. International journal of molecular medicine, 2018, 42(1): 237-247.
[8] Sun X, Ma X, Li Q, et al. Anti cancer effects of fisetin on mammary carcinoma cells via regulation of the PI3K/Akt/mTOR pathway: In vitro and in vivo studies[J]. International Journal of Molecular Medicine, 2018, 42(2): 811-820.
Fisetin是一种天然黄酮醇，存在于许多水果和蔬菜中，具有多种生物活性[1]。Fisetin是一种强抗氧化剂，能够作为有效的抗衰老剂[2]。Fisetin可作为多种癌症的化疗剂，也可作为神经保护剂[3]。
在体外，Fisetin（25, 50, 100µM）处理人视网膜母细胞瘤Y79细胞系24-72h，以时间和剂量依赖性方式抑制了细胞活力和增殖，抑制了细胞侵袭和迁移，抑制了细胞内血管内皮生长因子受体（VEGFR）的表达[4]。Fisetin（1-500μM）处理胶质瘤细胞（T98G和BEAS-2B细胞）细胞24h和48h，均以时间和剂量依赖性方式抑制了细胞增殖，诱导了细胞凋亡和坏死[5]。Fisetin（0-40μM）处理A549 细胞24-72h，以时间和剂量依赖性方式抑制了细胞增殖，导致了细胞周期停滞，抑制了细胞粘附、侵袭和迁移[6]。
在体内，Fisetin（10、20mg/kg）通过口服治疗急性中耳炎小鼠10天，以剂量依赖性方式显著下调了小鼠血清和中耳组织中IL-1β、TNF-α、IL-6和VEGF的mRNA水平，上调了SOD1、SOD2、HO-1和Nrf2的蛋白质水平，改善了小鼠的中耳炎症损伤[7]。Fisetin（223mg/kg）通过腹腔注射治疗4T1乳腺肿瘤模型小鼠3周，抑制了4T1细胞来源的原位乳腺肿瘤的生长，促进了肿瘤细胞凋亡[8]。
| Cell experiment [1]: | |
Cell lines | Y79 cells |
Preparation Method | The Y79 cells in the logarithmic growth phase were harvested, digested with 0.25% trypsin, added to RPMI-1640 medium containing 10% serum to prepare a cell suspension of 1×108/ml, plated in 96-well cell culture plates with 90µL per well, and incubated for 24h until the cells grew into a monolayer. Subsequently, 10µl of Fisetin were added at final concentrations of 25, 50 and 100µM with 100µg/ml VEGF. The negative control comprised an equal volume of DMSO with 100µg/ml VEGF. Fisetin was added to the cells for 24, 48 and 72h. The cell viability was determined by CCK-8 method, and the proliferation inhibition rate was calculated. |
Reaction Conditions | 25, 50, 100µM; 24, 48, 72h |
Applications | Fisetin inhibited Y79 cell viability and proliferation in a time- and dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | After LPS exposure for 24h, 36 mice with acute otitis media were randomly divided into two groups. Eighteen mice after LPS treatment were given low dose of 10mg/kg of Fisetin dissolved in 5% DMSO in PBS by intragastric administration every day for 10 days, and the other 18 mice a were given high dose of 20mg/kg of Fisetin dissolved in 5% DMSO in PBS through intragastric administration every day for 10 days. Finally, the mice were sacrificed and the eyeball blood and Middle ear lavage fluids (MELF) was collected for following research. |
Dosage form | 10、20mg/kg/day for 10 days; p.o. |
Applications | Fisetin administration significantly downregulated the mRNA levels of IL-1β, TNF-α, IL-6, and VEGF in the serum and middle ear tissues of mice in a dose-dependent manner, and upregulated the protein levels of SOD1, SOD2, HO-1, and Nrf2. |
References: [1]Wang L, Chen N, Cheng H. Fisetin inhibits vascular endothelial growth factor induced angiogenesis in retinoblastoma cells[J]. Oncology Letters, 2020, 20(2): 1239-1244. [2]Li P, Chen D, Huang Y. Fisetin administration improves LPS-induced acute otitis media in mouse in vivo[J]. International journal of molecular medicine, 2018, 42(1): 237-247. | |
| Cas No. | 528-48-3 | SDF | |
| 别名 | 漆黄素 | ||
| 化学名 | 2-(3,4-dihydroxyphenyl)-3,7-dihydroxychromen-4-one | ||
| Canonical SMILES | C1=CC(=C(C=C1C2=C(C(=O)C3=C(O2)C=C(C=C3)O)O)O)O | ||
| 分子式 | C15H10O6 | 分子量 | 286.05 |
| 溶解度 | ≥ 10.3mg/mL in DMSO | 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 | 3.4959 mL | 17.4795 mL | 34.9589 mL |
| 5 mM | 0.6992 mL | 3.4959 mL | 6.9918 mL |
| 10 mM | 0.3496 mL | 1.7479 mL | 3.4959 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%
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