Taxifolin
(Synonyms: (-)-二氢槲皮素; (-)-Dihydroquercetin) 目录号 : GN10304
Taxifolin是一种酪氨酸酶抑制剂，并具有显著的胶原酶抑制活性，其IC50值为193.3μM。
Cas No.:480-18-2
Sample solution is provided at 25 µL, 10mM.
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Taxifolin is a tyrosinase inhibitor and has significant collagenase inhibitory activity, with an IC50 value of 193.3μM[1]. As a ubiquitous bioactive constituent of foods and herbs, Taxifolin is also an important natural compound with antifibrotic activity and a free radical scavenger with antioxidant capacity[2][3]. Taxifolin showed promising pharmacological activities in various diseases, including inflammation, tumors, microbial infections, oxidative stress, cardiovascular and neurodegenerative diseases[4][5].
In vitro, administration of Taxifolin(10-100μM; 48h) to human colorectal cancer HCT116 and HT29 cells induced cytotoxicity in a dose- and time-dependent manner, resulting in cell growth arrest, alterations in molecules controlling the G2 phase of the cell cycle, apoptosis in a concentration-dependent manner, and decreased expression of β-catenin, AKT, and Survivin genes and proteins[6]. Taxifolin inhibited the proliferation and migration of B16F10 melanoma cells at 200 and 400μM, and of A375 cells at 100 and 200μM after treatment for 48h[7].
In vivo, treatment of Taxifolin(60mg/kg; i.p.) suppressed tumor growth and metastasis in mouse models without causing significant toxicity[7]. In DSS-induced mice, Taxifolin(200mg/kg; p.o.; daily for 7 consecutive days) treatment decreased weight loss and diarrhea score, increased colon length, significantly upregulated the expression of GPR41 and GPR43 in the colon, inhibited the expression of TNF-α, IL-1β, and IL-6 in colon tissue, reversed the fecal metabolic pattern altered by DSS, and significantly increased fecal levels of butyric acid and isobutyric acid[8].
References:
[1] Angelis, A., Hubert, J., Aligiannis, N., Michalea, R., Abedini, A., Nuzillard, J. M., Gangloff, S. C., Skaltsounis, A. L., & Renault, J. H. (2016). Bio-Guided Isolation of Methanol-Soluble Metabolites of Common Spruce (Picea abies) Bark by-Products and Investigation of Their Dermo-Cosmetic Properties. Molecules (Basel, Switzerland), 21(11), 1586.
[2] Yang, P., Xu, F., Li, H. F., Wang, Y., Li, F. C., Shang, M. Y., Liu, G. X., Wang, X., & Cai, S. Q. (2016). Detection of 191 Taxifolin Metabolites and Their Distribution in Rats Using HPLC-ESI-IT-TOF-MS(n). Molecules (Basel, Switzerland), 21(9), 1209.
[3] Ren, L., Guo, H. N., Yang, J., Guo, X. Y., Wei, Y. S., & Yang, Z. (2021). Dissecting Efficacy and Metabolic Characteristic Mechanism of Taxifolin on Renal Fibrosis by Multivariate Approach and Ultra-Performance Liquid Chromatography Coupled With Mass Spectrometry-Based Metabolomics Strategy. Frontiers in pharmacology, 11, 608511.
[4] Sunil, C., & Xu, B. (2019). An insight into the health-promoting effects of taxifolin (dihydroquercetin). Phytochemistry, 166, 112066.
[5] Yang, R., Yang, X., & Zhang, F. (2023). New Perspectives of Taxifolin in Neurodegenerative Diseases. Current neuropharmacology, 21(10), 2097–2109.
Razak, S., Afsar, T., Ullah, A., Almajwal, A., Alkholief, M., Alshamsan, [6] A., & Jahan, S. (2018). Taxifolin, a natural flavonoid interacts with cell cycle regulators causes cell cycle arrest and causes tumor regression by activating Wnt/ β -catenin signaling pathway. BMC cancer, 18(1), 1043.
[7] Xu, L., Zhang, L., Zhang, S., Yang, J., Zhu, A., Sun, J., Kalvakolanu, D. V., Cong, X., Zhang, J., Tang, J., & Guo, B. (2024). Taxifolin inhibits melanoma proliferation/migration impeding USP18/Rac1/JNK/β-catenin oncogenic signaling. Phytomedicine : international journal of phytotherapy and phytopharmacology, 123, 155199.
[8] Li, W., Zhang, L., Xu, Q., Yang, W., Zhao, J., Ren, Y., Yu, Z., & Ma, L. (2022). Taxifolin Alleviates DSS-Induced Ulcerative Colitis by Acting on Gut Microbiome to Produce Butyric Acid. Nutrients, 14(5), 1069.
Taxifolin是一种酪氨酸酶抑制剂，并具有显著的胶原酶抑制活性，其IC50值为193.3μM[1]。作为一种广泛存在于食物和草药中的生物活性成分，Taxifolin也是一种具有抗纤维化活性的重要天然化合物，同时它还是一种自由基清除剂，具有抗氧化能力[2][3]。Taxifolin在多种疾病（包括炎症、肿瘤、微生物感染、氧化应激、心血管疾病和神经退行性疾病）中显示出良好的药理活性[4][5]。
在体外实验中，对人结直肠癌HCT116和HT29细胞给予Taxifolin（10-100μM；作用48小时），以剂量和时间依赖的方式诱导细胞毒性，以浓度依赖的方式导致细胞生长停滞、细胞周期G2期调控分子的改变、并诱导细胞凋亡，以及降低β-catenin、AKT和Survivin基因和蛋白的表达[6]。此外，Taxifolin在200和400μM浓度下抑制了B16F10黑色素瘤细胞的增殖和迁移，在100和200μM浓度下抑制了A375细胞的增殖和迁移，处理时间为48小时[7]。
在体内实验中，Taxifolin（60mg/kg；腹腔注射）治疗抑制了小鼠模型中的肿瘤生长和转移，且未引起显著毒性[7]。在DSS诱导的小鼠模型中，Taxifolin（200mg/kg；口服；连续7天每天给药）治疗减轻了体重下降和腹泻评分，增加了结肠长度，显著上调了结肠中GPR41和GPR43的表达，抑制了结肠组织中TNF-α、IL-1β和IL-6的表达，逆转了DSS诱导的粪便代谢模式的改变，并显著提高了DSS处理小鼠粪便中丁酸和异丁酸的水平[8]。
| Cell experiment [1]: | |
Cell lines | HCT116 and HT29 cell lines |
Preparation Method | Two human colorectal cancer cell lines HCT116 and HT29 were grown in a 5% CO2 atmosphere at 37°C in medium containing RPMI medium 1640, 10% fetal bovine serum and 1% penicillin/streptomycin. Taxifolin and β-catenin inhibitor (FH535) suspended in DMSO was applied for cell treatment. Cells with 70% confluency were induced with Taxifolin and β-catenin inhibitor at 10-100μM for 48h in cell culture medium and the dilution of DMSO applied for each treatment was 0.1% (V/V). Cell viability assay, proliferation assay and cell cycle analysis were performed according to protocols. Cells were collected for western blot and PCR analysis. |
Reaction Conditions | 10–100μM; 48h |
Applications | Taxifolin induced cytotoxicity in a dose- and time-dependent manner, resulting in cell growth arrest, alterations in molecules controlling the G2 phase of the cell cycle, apoptosis in a concentration-dependent manner, and decreased expression of β-catenin, AKT, and Survivin genes and proteins. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice were randomly divided into 3 groups (n = 7/group): control group, DSS group, and DSS + Taxifolin group. Experimental colitis was induced by replacing the drinking water with 5% DSS for 7 days (from day 1 to day 7). While mice in the control group were orally administered ddH2O. Meanwhile, mice in the DSS + Taxifolin group were orally administered 150µL Taxifolin (200mg/kg in ddH2O) daily for 7 consecutive days (days 8–14). Mice in the control and DSS groups were given 150µL ddH2O (10mL/kg) per day. Disease severity, including the degree of body weight (BW) reduction and diarrhea severity, was recorded daily to assess colitis. Fresh feces were collected for 16S rRNA sequencing. After the mice were sacrificed, colon contents were collected for SCFA Quantification. colon tissue RNA were extraction for PCR. |
Dosage form | 200mg/kg/day for 7 consecutive days; p.o. |
Applications | Taxifolin decreased weight loss and diarrhea score, increased colon length, significantly upregulated the expression of GPR41 and GPR43 in the colon, inhibited the expression of TNF-α, IL-1β, and IL-6 in colon tissue, reversed the fecal metabolic pattern altered by DSS, and significantly increased fecal levels of butyric acid and isobutyric acid. |
References: | |
| Cas No. | 480-18-2 | SDF | |
| 别名 | (-)-二氢槲皮素; (-)-Dihydroquercetin | ||
| 化学名 | (2R,3R)-2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-2,3-dihydrochromen-4-one | ||
| Canonical SMILES | C1=CC(=C(C=C1C2C(C(=O)C3=C(C=C(C=C3O2)O)O)O)O)O | ||
| 分子式 | C15H12O7 | 分子量 | 304.25 |
| 溶解度 | ≥ 13.8mg/mL in DMSO | 储存条件 | -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 | 3.2868 mL | 16.4339 mL | 32.8677 mL |
| 5 mM | 0.6574 mL | 3.2868 mL | 6.5735 mL |
| 10 mM | 0.3287 mL | 1.6434 mL | 3.2868 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: >99.50%
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