Tryptanthrin 是一种吲哚喹唑啉，可以是产自靛蓝植物的生物碱。Tryptanthrin 是一种口服有效的细胞白三烯 (LT) 生物合成抑制剂。Tryptanthrin 具有抗癌活性。Tryptanthrin 可抑制 NOS1、COX-2、NF-κB 的表达水平，调节 IL-2、IL-10、TNF-α 的表达水平。
| 生物活性 | Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearingplants. Tryptanthrin is a potent and orally active cellularLeukotriene (LT) biosynthesisinhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1,COX-2, andNF-κBand regulates the expression levels ofIL-2,IL-10, and TNF-α[1][2]. |
| IC50& Target[1] | IL-2 | nNOS | IL-6 | IL-10 | IL-12 |
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体外研究
(In Vitro) | Tryptanthrin (0-60 μM; 24, 48 and 72 h) inhibits the proliferation and colony formation of MCF-7 cells[1].
Tryptanthrin (6.25-25 μM; 48 h; MCF-7 cells) reverses EMT-associated E-cadherin, MMP-2 and Snail[1].
Tryptanthrin (0-30 μM; 15 min; MCF-7 cells) reduces Leukotriene (LT)-formation in human neutrophils with an IC50value of 0.6 μM[2].
Cell Viability Assay[1] | Cell Line: | MCF-7 cells | | Concentration: | 0-60 μM | | Incubation Time: | 24, 48 and 72 hours | | Result: | Increased the inhibition rates of MCF-7 cells in a dose- and time- dependent manner. |
Western Blot Analysis[1] | Cell Line: | MCF-7 cells | | Concentration: | 6.25, 12.5, and 25 μM | | Incubation Time: | 48 hours | | Result: | Increased the E-cadherin protein levels and markedly upregulated the protein expression levels of MMP-2 and Snail in MCF-7 cells induced by TGF-β1. |
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体内研究
(In Vivo) | Tryptanthrin (25-100 mg/kg; i.g.; daily, for 13 d; Female Bal b/c mice with 4T1 xenograft) inhibits tumor growth and regulates IL-2, IL-6, IL-10, IL-12 and TNF-α levels in tumor-bearing mice[1].
Tryptanthrin (10 mg/kg; p.o.; male Wistar Han rats) inhibits LTB4formation in vivo[2].
| Animal Model: | Female Bal b/c mice with 4T1 xenograft[1] | | Dosage: | 25, 50, and 100 mg/kg | | Administration: | Oral gavage; daily, for 13 days | | Result: | Inhibited tumor growth in a dose-dependent manner. |
| Animal Model: | Male Wistar Han rats (220–230 g)[2] | | Dosage: | 10 mg/kg | | Administration: | Oral administration; once | | Result: | Reduced LTB4pleural levels by 46%.
Reduced PGE2levels (by 42%), exudate volume (by 80%) and the number of infiltrating cells (by 41%).
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| Formula | |
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| 结构分类 | - Alkaloids
- Indole Alkaloids
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| 来源 | - Plants
- Polygonaceae
- Polygonum tinctoriumAit.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 7.14 mg/mL(28.76 mM;Need ultrasonic) 配制储备液 | 1 mM | 4.0284 mL | 20.1418 mL | 40.2836 mL | | 5 mM | 0.8057 mL | 4.0284 mL | 8.0567 mL | | 10 mM | 0.4028 mL | 2.0142 mL | 4.0284 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。-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: 0.71 mg/mL (2.86 mM); Suspended solution; Need ultrasonic
此方案可获得 0.71 mg/mL (2.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 7.1 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: 0.67 mg/mL (2.70 mM); Suspended solution; Need ultrasonic
此方案可获得 0.67 mg/mL (2.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 6.7 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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