Luteolin(Synonyms: 木犀草素; Luteoline; Luteolol; Digitoflavone)

Luteolin (Synonyms: 木犀草素; Luteoline; Luteolol; Digitoflavone) 纯度: 98.42%

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。

Luteolin(Synonyms: 木犀草素; Luteoline;  Luteolol;  Digitoflavone)

Luteolin Chemical Structure

CAS No. : 491-70-3

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生物活性

Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells[1][2][3].

IC50 & Target

Human Endogenous Metabolite

 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

286.24

Formula

C15H10O6

CAS 号

491-70-3

中文名称

木犀草素;檞片素;木樨草素

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
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (349.36 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-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。

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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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 MCE 网站选购。
参考文献
  • [1]. Ma L, et al. Luteolin exerts an anticancer effect on NCI-H460 human non-small cell lung cancer cells through the induction of Sirt1-mediated apoptosis. Mol Med Rep. 2015 Sep;12(3):4196-4202.

    [2]. Abu-Elsaad N, et al. Protection against nonalcoholic steatohepatitis through targeting IL-18 and IL-1alpha by luteolin. Pharmacol Rep. 2019 Aug;71(4):688-694.

    [3]. Xiuwen Tang, et al. Luteolin inhibits Nrf2 leading to negative regulation of the Nrf2/ARE pathway and sensitization of human lung carcinoma A549 cells to therapeutic drugs. Free Radic Biol Med. 2011 Jun 1;50(11):1599-609.