Theaflavin 3,3'-digallate
(Synonyms: 茶黄素-3,3'-双没食子酸; TF-3; ZP10) 目录号 : GC41573
Theaflavin 3,3'-digallate（茶黄素-3,3'-双没食子酸; TF-3; ZP10）是一种有效的寨卡病毒（ZIKV）蛋白酶抑制剂，IC50值为2.3μM。
Cas No.:30462-35-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | OVCAR-3 cells |
Preparation Method | OVCAR-3 cells were seeded into 96-well plates at a density of 2×104 per well in medium with 10% FBS. After overnight growth, cells were treated with 0-25µM of Theaflavin 3,3'-digallate for 24h. |
Reaction Conditions | 0-25µM; 24h |
Applications | Theaflavin 3,3'-digallate treatment for 24h dose-dependently inhibited the viability of OVCAR-3 cells, ranging from 100 to 48.3%. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice were randomly divided into five groups: control group, model group (LPS), DEX, low-concentration Theaflavin 3,3'-digallate, and high-concentration Theaflavin 3,3'-digallate groups. Mice in the control group and model group were intraperitoneally injected with 0.9% saline, and mice in the DEX, low-concentration Theaflavin 3,3'-digallate, and high-concentration Theaflavin 3,3'-digallate groups were intraperitoneally injected with DEX (5mg/kg) and Theaflavin 3,3'-digallate (20 and 40mg/kg) for nasal administration, respectively. One hour later, LPS or PBS (control group) was dripped into the nasal cavity. Mice were euthanized 6 hours later, and samples were collected for subsequent analysis. |
Dosage form | 20、40mg/kg; nasal administration |
Applications | Theaflavin 3,3'-digallate inhibited the serum concentrations of TNF-α and IL-6 in a dose-dependent manner and significantly reduced the ratio of lung wet weight to dry weight in LPS-challenged mice, indicating that Theaflavin 3,3'-digallate could improve severe pulmonary edema. |
References: | |
Theaflavin 3,3'-digallate (TF-3; ZP10) is a potent inhibitor of Zika virus (ZIKV) protease with an IC50 value of 2.3μM[1]. Theaflavin 3,3'-digallate is a polyphenolic compound with multiple biological activities such as anti-inflammatory, antioxidant, anti-tumor, and anti-angiogenic[2, 3].
In vitro, Theaflavin 3,3'-digallate (0-25μM) treated OVCAR-3 cells for 24h dose-dependently inhibited cell viability, ranging from 100% to 48.3%, and downregulated vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1-α (HIF-1α) to reduce angiogenesis[4]. Theaflavin 3,3'-digallate (0-50µM) treated platinum-resistant human ovarian cancer cell line A2780/CP70 cells for 24h, inhibited cell viability in a dose-dependent manner, ranging from 100% to 11.38%, induced G2 cell cycle arrest, reduced Akt phosphorylation without affecting total Akt protein expression, and reduced mouse double minute 2 (MDM2) protein levels[5].
In vivo, Theaflavin 3,3'-digallate (20, 40mg/kg) was intranasally administered to treat LPS-induced lung injury mice, inhibited the concentrations of TNF-α and IL-6 in serum in a dose-dependent manner, significantly reduced the ratio of lung wet weight to dry weight, and improved pulmonary edema in mice[6]. Theaflavin 3,3'-digallate (5mg/kg) was orally administered to mice with trinitrobenzene sulfonic acid (TNBS)-induced colitis, which inhibited the nuclear localization of NF-κB and the increase in cytoplasmic IκB kinase (IKK) activity, and retained NF-κB inhibitory protein (IκBα) in colon tissue, thereby improving colitis in mice[7].
References:
[1] Cui X, Zhou R, Huang C, et al. Identification of theaflavin-3, 3’-digallate as a novel Zika virus protease inhibitor[J]. Frontiers in pharmacology, 2020, 11: 514313.
[2] Ko H J, Lo C Y, Wang B J, et al. Theaflavin-3, 3′-digallate, a black tea polyphenol, stimulates lipolysis associated with the induction of mitochondrial uncoupling proteins and AMPK–FoxO3A–MnSOD pathway in 3T3-L1 adipocytes[J]. Journal of Functional Foods, 2015, 17: 271-282.
[3] Seo E J, Wu C F, Ali Z, et al. Both phenolic and non-phenolic green tea fractions inhibit migration of cancer cells[J]. Frontiers in Pharmacology, 2016, 7: 398.
[4] Gao Y, Rankin G O, Tu Y, et al. Theaflavin-3, 3'-digallate decreases human ovarian carcinoma OVCAR-3 cell-induced angiogenesis via Akt and Notch-1 pathways, not via MAPK pathways[J]. International journal of oncology, 2016, 48(1): 281-292.
[5] Tu Y, Kim E, Gao Y, et al. Theaflavin-3, 3'-digallate induces apoptosis and G2 cell cycle arrest through the Akt/MDM2/p53 pathway in cisplatin-resistant ovarian cancer A2780/CP70 cells[J]. International journal of oncology, 2016, 48(6): 2657-2665.
[6] Wu Y, Jin F, Wang Y, et al. In vitro and in vivo anti-inflammatory effects of theaflavin-3, 3′-digallate on lipopolysaccharide-induced inflammation[J]. European Journal of Pharmacology, 2017, 794: 52-60.
[7] Ukil A, Maity S, Das P K. Protection from experimental colitis by theaflavin‐3, 3′‐digallate correlates with inhibition of IKK and NF‐κB activation[J]. British journal of pharmacology, 2006, 149(1): 121-131.
Theaflavin 3,3'-digallate（茶黄素-3,3'-双没食子酸; TF-3; ZP10）是一种有效的寨卡病毒（ZIKV）蛋白酶抑制剂，IC50值为2.3μM[1]。Theaflavin 3,3'-digallate是一种多酚类化合物，具有抗炎、抗氧化、抗肿瘤、抗血管生成等多种生物活性[2, 3]。
在体外，Theaflavin 3,3'-digallate（0-25µM）处理OVCAR-3细胞24h，剂量依赖性地抑制了细胞活力，抑制范围为100%至48.3%，下调了血管内皮生长因子（VEGF）和缺氧诱导因子1-α（HIF-1α）来减少血管生成[4]。Theaflavin 3,3'-digallate（0-50µM）处理铂抗性人卵巢癌细胞系A2780/CP70细胞24h，剂量依赖性地抑制了细胞活力，抑制范围为100%至11.38%，诱导了G2细胞周期停滞，降低Akt的磷酸化而不影响总Akt蛋白表达，降低鼠双微体2（MDM2）的蛋白水平[5]。
在体内，Theaflavin 3,3'-digallate（20、40mg/kg）通过鼻腔给药治疗LPS诱导的肺损伤小鼠，剂量依赖性方式抑制了血清中TNF-α和IL-6的浓度, 显著降低了肺湿重与干重之比，改善了小鼠肺水肿[6]。Theaflavin 3,3'-digallate（5mg/kg）通过口服治疗三硝基苯磺酸（TNBS）诱导的结肠炎的小鼠，抑制了NF-κB核定位、胞质IκB激酶（IKK）活性的增加，并在结肠组织中保留了NF-κB抑制蛋白（IκBα），改善了小鼠结肠炎[7]。
| Cas No. | 30462-35-2 | SDF | |
| 别名 | 茶黄素-3,3'-双没食子酸; TF-3; ZP10 | ||
| Canonical SMILES | O=C1C2=C(O)C(O)=CC([C@@H]3[C@H](OC(C4=CC(O)=C(O)C(O)=C4)=O)CC(C(O)=CC(O)=C5)=C5O3)=C2C=C([C@H]6OC(C=C(O)C=C7O)=C7C[C@H]6OC(C8=CC(O)=C(O)C(O)=C8)=O)C=C1O | ||
| 分子式 | C43H32O20 | 分子量 | 868.7 |
| 溶解度 | DMF: 25 mg/ml,DMF:PBS(pH 7.2)(1:6): 0.14 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml | 储存条件 | Store at -20°C, sealed storage, away from moisture and 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 | 1.1511 mL | 5.7557 mL | 11.5115 mL |
| 5 mM | 0.2302 mL | 1.1511 mL | 2.3023 mL |
| 10 mM | 0.1151 mL | 0.5756 mL | 1.1511 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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