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Luteolin

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Chemical Structure| 491-70-3 同义名 : Luteoline;Luteolol;Salifazide;Flacitran;Cyanidenon 1470;CCRIS 3790;C.I. Natural Yellow 2;C.I. 75590;BRN 0292084;Digitoflavone
CAS号 : 491-70-3
货号 : A144892
分子式 : C15H10O6
纯度 : 98%
分子量 : 286.24
MDL号 : MFCD00017309
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(366.83 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PDE1

    PDE1, Ki:15.0 μM

  • PDE4

    PDE4, Ki:11.1 μM

  • PDE2

    PDE2, Ki:6.4 μM

  • PDE3

    PDE3, Ki:13.9 μM

  • PDE5

    PDE5, Ki:9.5 μM
描述 Phosphodiesterases (PDEs) comprise 11 enzyme families that hydrolyze adenosine 3′,5′ cyclic monophosphate and/or guanosine 3′,5′ cyclic monophosphate. Luteolin is a flavonoid that has been shown to inhibit PDE1-5 with IC50 values of around 20μM. The Ki values of luteolin against PDE1-5 were 15.0  3.9, 6.4  1.9, 13.9  4.2, 11.1  3.7 and 9.5  1.7μM, respectively. The EC50 (PDE4H) value of luteolin for displacing 2nM [3H]-rolipram binding on the high-affinity rolipram binding sites was 11.2 ± 1.5μM[9]. In RAW 264.7 cells, luteolin inhibited LPS-induced TNF-alpha release with an IC50 value of less than 1μM. Preincubation of cells with luteolin also inhibited LPS-induced phosphorylation of Akt and IkappaB-alpha[10]. Treatment with luteolin (10 – 30μmol/kg, s.c.) significantly and dose-dependently shortened the duration of xylazine/ketamine-induced anesthesia. Also, luteolin inhibited 5nM [3H]-flunitrazepam binding to rat cerebral cortex membranes with a Ki value of 60.1μM[9].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Agonist activity at rat DAT expressed in CHO cells, EC50=1.45 μM 20971650
HEK293 cells Function assay 24 h Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=2.3 μM 24955889
HEK293 FS cells Function assay Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=0.85 μM 20731357
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.49mL

0.70mL

0.35mL

17.47mL

3.49mL

1.75mL

34.94mL

6.99mL

3.49mL
参考文献

[1]Yu MC, Chen JH, et al. Luteolin, a non-selective competitive inhibitor of phosphodiesterases 1-5, displaced [3H] -rolipram from high-affinity rolipram binding sites and reversed xylazine/ketamine-induced anesthesia. Eur J Pharmacol. 2010 Feb 10;627(1-3):269-75.

[2]Xagorari A, Papapetropoulos A, et al. Luteolin inhibits an endotoxin-stimulated phosphorylation cascade and proinflammatory cytokine production in macrophages. J Pharmacol Exp Ther. 2001 Jan;296(1):181-7.

[3]Kotanidou A, Xagorari A, et al. Luteolin reduces lipopolysaccharide-induced lethal toxicity and expression of proinflammatory molecules in mice. Am J Respir Crit Care Med. 2002 Mar 15;165(6):818-23.

[4]Tambe R, Patil A, et al. Assessment of luteolin isolated from Eclipta alba leaves in animal models of epilepsy. Pharm Biol. 2017 Dec;55(1):264-268.

[5]Seelinger G, Merfort I, et al. Anti-carcinogenic effects of the flavonoid luteolin. Molecules. 2008 Oct 22;13(10):2628-51.

[6]Das M, Ram A, et al. Luteolin alleviates bronchoconstriction and airway hyperreactivity in ovalbumin sensitized mice. Inflamm Res. 2003 Mar;52(3):101-6.

[7]Pharmacokinetics of Luteolin and Metabolites in Rats

[8]Wei B, Lin Q, et al. Luteolin ameliorates rat myocardial ischaemia-reperfusion injury through activation of peroxiredoxin II. Br J Pharmacol. 2018 Aug;175(16):3315-3332.

[9]Yu MC, Chen JH, Lai CY, Han CY, Ko WC. Luteolin, a non-selective competitive inhibitor of phosphodiesterases 1-5, displaced [3H]-rolipram from high-affinity rolipram binding sites and reversed xylazine/ketamine-induced anesthesia. Eur J Pharmacol. 2010 Feb 10;627(1-3):269-75.

[10]Xagorari A, Papapetropoulos A, Mauromatis A, Economou M, Fotsis T, Roussos C. Luteolin inhibits an endotoxin-stimulated phosphorylation cascade and proinflammatory cytokine production in macrophages. J Pharmacol Exp Ther. 2001 Jan;296(1):181-7.