Theaflavin 3,3'-digallate (TF-3) 是有效的寨卡病毒 (ZIKV) 蛋白酶抑制剂,IC50为 2.3 μM。Theaflavin 3,3'-digallate 直接与 ZIKVpro 结合 (Kd=8.86 μM) 并抑制 ZIKV 复制。Theaflavin 3,3'-digallate 抑制 gp41 和 NS2B-3 蛋白酶的活性,并具有抗HSV和HIV-1病毒活性。Theaflavin 3,3'-digallate 是红茶中的典型色素,一种有效的抗肿瘤剂。
生物活性 | Theaflavin 3,3'-digallate (TF-3) is a potentZika virus (ZIKV) proteaseinhibitor with anIC50of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity againstHSVandHIV-1[1]. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent[2]. |
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体外研究 (In Vitro) | Theaflavin 3,3'-digallate (TF-3; 6.25, 12.5, 25 μM; 24 hours) markedly reduces viral RNA copy numbers and NS3, U87 MG protein expression in a dose-dependent manner[1]. Theaflavin 3,3'-digallate inhibits dose-dependently ZIKV replication in Vero E6 cells (EC50=7.65 μM). Theaflavin 3,3'-digallate has minor cytotoxicity up to 40 μM in Vero E6 cells. Theaflavin 3,3'-digallate can inhibit the post-entry events of the ZIKV replication cycle from gene transcription and translation levels[1]. Theaflavin 3,3'-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50of 17.26 μM[2].
Western Blot Analysis[1] Cell Line: | Vero E6 cells | Concentration: | 6.25, 12.5, 25 μM | Incubation Time: | 24 hours | Result: | Markedly reduced NS3, U87 MG protein expression in a dose-dependent manner. |
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来源 | - Plants
- Theaceae
- Camellia sinensis(L.) O. Ktze.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(115.11 mM;Need ultrasonic) 配制储备液 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 |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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