Luteolin (Luteoline), 一种黄酮类化合物，也是一种有效的Nrf2抑制剂。Luteolin 具有抗炎和抗癌特性，可在人类多种癌细胞系 (包括非小肺癌细胞) 中诱导细胞凋亡和细胞周期停滞，并抑制细胞转移和血管生成。
| 生物活性 | Luteolin (Luteoline), a flavanoid compound, is a potentNrf2inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction ofapoptosisand cell cycle arrest, and the inhibition of metastasis and angiogenesis, in severalcancercell lines, including human non-small lungcancercells[1][2][3]. |
体外研究
(In Vitro) | Luteolin (0-160 μM; 24 hours; NCI-H460 cells) treatment inhibits the viability of NCI-H460 cells in a concentration-dependent manner[1].
Luteolin (20-80 μM; 24 hours; NCI-H460 cells) treatment causes an accumulation of cells in the S phase[1].
Luteolin (320-580 μM; 48 hours; NCI-H460 cells) treatment induces apoptosis[1].
Luteolin (20-80 μM; 24 hours; NCI-H460 cells) treatment increases the protein expression levels of apoptotic regulatory proteins, including the Bax/Bcl-2 ratio, in a concentration-dependent manner, however, only 80 μM Luteolin inhibits the expression of Bad. Luteolin also decreases the expression of Sirt1 in the NCI-H460 cell line in a concentration-dependent manner[1].
Cell Viability Assay[1] | Cell Line: | NCI-H460 cells | | Concentration: | 0 μM, 20 μM, 40 μM, 80 μM and 160 μM | | Incubation Time: | 24 hours | | Result: | Inhibited the viability of NCI-H460 cells in a concentration-dependent manner. |
Cell Cycle Analysis[1] | Cell Line: | NCI-H460 cells | | Concentration: | 20 μM, 40 μM, 80 μM | | Incubation Time: | 24 hours | | Result: | Induced cell cycle arrest in the S phase. |
Apoptosis Analysis[1] | Cell Line: | NCI-H460 cells | | Concentration: | 320 μM, 440 μM, 580 μM | | Incubation Time: | 48 hours | | Result: | Apoptotic fraction was markedly increased. |
Western Blot Analysis[1] | Cell Line: | NCI-H460 cells | | Concentration: | 20 μM, 40 μM, 80 μM | | Incubation Time: | 24 hours | | Result: | Increased the protein expression levels of apoptotic regulatory proteins and decreased the expression of Sirt1 in the NCI-H460 cell line in a concentration-dependent manner. |
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体内研究
(In Vivo) | Luteolin (10-100 mg/kg; oral gavage; daily; for 12 weeks; adult male Wistar rats) has an antioxidant effect and can also protect against non-alcoholic steatohepatitis through targeting the pro-inflammatory IL-1 and Il-18 pathways in rats with a high carbohydrate/high fat diet[2].
| Animal Model: | Adult male Wistar rats (200-220 g)[2] | | Dosage: | 10 mg/kg, 25 mg/kg, 50 mg/kg or 100 mg/kg | | Administration: | Oral gavage; daily; for 12 weeks | | Result: | Significantly reduced ALT and AST activity and reduced levels of bilirubin, hyaluronic acid and malondialdehyde. Shows an antioxidant activity such as a significant increase in reduced glutathione. IFN-γ, TNF-α, IL-1α and IL-18 levels decreased significantly. |
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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 : ≥ 100 mg/mL(349.36 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.4936 mL | 17.4679 mL | 34.9357 mL | | 5 mM | 0.6987 mL | 3.4936 mL | 6.9871 mL | | 10 mM | 0.3494 mL | 1.7468 mL | 3.4936 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: ≥ 2.08 mg/mL (7.27 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.27 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (7.27 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.27 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (7.27 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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