Luteolin | Luteoline;Luteolol;Salifazide;Flacitran;Cyanidenon 1470;CCRIS 3790;C.I. Natural Yellow 2;C.I. 75590;BRN 0292084;Digitoflavone | Plant Standard | Lipoxygenase Inhibitor | PDE

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木犀草素 /Luteolin {[allProObj[0].p_purity_real_show]}

货号：A144892 同义名： Luteoline;Luteolol

Luteolin 是一种天然黄酮，具有抗氧化、抗炎和抗癌活性。Luteolin 在研究中主要用于探索其在肿瘤抑制、心血管健康和神经保护方面的作用。

Luteolin 化学结构
CAS号：491-70-3

Luteolin 3D分子结构
CAS号：491-70-3

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Luteolin 纯度/质量文件产品仅供科研

货号：A144892 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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PDE 亚型比较

产品名称	PDE ↓ ↑	PDE1 ↓ ↑	PDE10A ↓ ↑	PDE2 ↓ ↑	PDE3 ↓ ↑	PDE4 ↓ ↑	PDE5 ↓ ↑	PDE6 ↓ ↑	其他靶点	纯度
Doxofylline	✔									99+%
Deltarasin	+++ PDEδ , Kd: 38 nM									99+%
7-(2,3-Dihydroxypropyl)theophylline	✔									98%
Aminophylline	+ PDE, IC50: 0.12 mM									98+%
Anagrelide HCl	✔									99%+
Irsogladine	✔								mAChR,AChR	98%
PF-8380	+++ Autotaxin, IC50: 2.8 nM									99%+
Dipyridamole	✔									98%
Balipodect			++++ PDE10A, IC50: 0.3 nM							99%+
PF-2545920			++++ PDE10A, IC50: 0.37 nM							97%
Luteolin		+ PDE1, Ki: 15.0 μM		++ PDE2, Ki: 6.4 μM	+ PDE3, Ki: 13.9 μM	+ PDE4, Ki: 11.1 μM	+ PDE5, Ki: 9.5 μM			98%
Milrinone				++ PDE2, IC50: 5.2 μM	++ PDE3, IC50: 2.1 μM				ATPase	98%
Pimobendan					++ PDE3, IC50: 0.32 μM					98%
Cilostazol					++ PDE3, IC50: 0.2 μM					98%
Fenspiride HCl					+ PDE3, pIC50: 3.44	+ PDE4, pIC50: 4.16				98%
(S)-(+)-Rolipram						++ PDE4, IC50: 0.75 μM				98%
Apremilast						+++ PDE4, IC50: 74 nM				98%
GSK256066						++++ PDE4B, IC50: 3.2 pM				98+%
Roflumilast						++++ PDE4A1, IC50: 0.7 nM PDE4A4, IC50: 4.3 nM				99%
Rolipram						+++ PDE4B, IC50: 130 nM				99%+
Cilomilast						+++ LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM				98+%
Avanafil							++++ PDE5, IC50: 1 nM			98%
Vardenafil HCl Trihydrate							++++ PDE5, IC50: 0.7 nM			98%
Tadalafil							++++ PDE5, IC50: 1.8 nM			98%
Icariin							++ PDE5, IC50: 0.432 μM			98%
Sildenafil							✔	+++ PDE6, IC50: 33 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Luteolin 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 K_i 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 (PDE4_H) 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 [3^H]-flunitrazepam binding to rat cerebral cortex membranes with a K_i value of 60.1μM^[9].

Luteolin 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
HL60 cells	30 μM	Proliferation assay	48 h	Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay	18258440

Luteolin 动物研究

Dose

Mice: 0.2 mg/kg - 1 mg/kg^[3] (i.p.), 5 mg/kg - 20 mg/kg^[4] (i.p.); 0.1 mg/kg - 0.3 mg/kg^[5] (i.g.); 0.1 mg/kg - 10 mg/kg^[6] (p.o.) Rat: 50 mg/kg^[7] (i.v.); 5 mg/kg - 20 mg/kg^[8] (i.p.)

Administration

i.p., i.g., p.o., i.v.

Pharmacokinetics

Animal	Rats^[7]
Dose	50 mg/kg
Administration	p.o. or i.v.
F	4.10% (p.o.)
Vd_area	27.58 L (i.v.)
CL	2.14 L/h/kg (i.v.)
AUC_0→last	0.87 h·μg/ml (p.o.) 20.55 h·μg/ml (i.v.)
AUC_0→∞	0.96 h·μg/ml (p.o.) 23.39 h·μg/ml (i.v.)

Luteolin 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.

Luteolin 实验方案

计算器

存储液制备

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

Luteolin 技术信息

CAS号	491-70-3
分子式	C₁₅H₁₀O₆
分子量	286.24

别名	Luteoline;Luteolol;Salifazide;Flacitran;Cyanidenon 1470;CCRIS 3790;C.I. Natural Yellow 2;C.I. 75590;BRN 0292084;Digitoflavone
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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

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
HL60 cells	30 μM	Proliferation assay	48 h	Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay	18258440
human H9 cells		Function assay	3 days	Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=10 μM	8158164
human H9 cells		Cytotoxicity assay	3 days	Cytotoxicity against human H9 cells after 3 days, IC50=16 μM	8158164
human HT-29 cells		Function assay	10 mins	Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay, EC50=7.24 μM	24900447
human HT-29 cells		Function assay	10 mins	Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins, IC50=18.6 μM	24900447
human LNCAP cells		Function assay		Downregulation of prostate specific antigen secretion in human LNCAP cells, IC50=5 μM	25019478
human mast cells		Function assay		Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=4.5 μM	22257213
human MV4-11 cells		Cytotoxicity assay	72 h	Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=1.76 μM	23411073
human RS4:11 cells		Cytotoxicity assay	72 h	Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=7.25 μM	23411073
human THP1 cells	20 μM	Function assay	1 h	Downregulation of TPA-induced NOX2 mRNA expression in human THP1 cells at 20 uM incubated for 1 hr prior to TPA challenge measured after 24 hrs by RT-PCR analysis	23786520
human U2OS cells		Function assay	5 h	Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay, EC50=3.2 μM	24900447
human U937 cells		Proliferation assay	72 h	Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=20 μM	17158054
K562 cells		Growth inhibition assay	5 days	Growth inhibition of K562 cells by XTT assay after 5 days, IC50=14.65 μM	17411092
MDA-MB-231 cells	5 μM	Function assay	16 h	Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay	25190466
MDCK cells		Cytotoxicity assay		Cytotoxicity against MDCK cells by MTT assay, CC50=12.44 μM	18640042
mouse B16-4A5 cells		Function assay	72 h	Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs, IC50=14 μM	20189399
mouse HT22 cells		Function assay	3 h	Neuroprotective activity in mouse HT22 cells assessed as t-BOOH-induced toxicity at 40 uM preincubated for 3 hrs followed by t-BOOH induction measured after 9 hrs by MTT assay	24245939
mouse RAW264.7 cells		Function assay	2 h	Inhibition of NO production in LPS-stimulated mouse RAW264.7 cells pre-incubated for 2 hrs before LPS stimulation for 24 hrs by Griess assay method, IC50=0.21 μM	25176187
NCI-H460 cells		Function assay	2-20 h	Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation after 2 to 20 hrs relative to fumitremorgin C, IC50=8.9 μM	21275386
rat H9c2 cells		Function assay	24 h	Cytoprotective activity against doxorubicin-induced cytotoxicity in rat H9c2 cells assessed as cell viability after 24 hrs by MTT assay, EC50=5.53 μM	20932762
RBL-2H3 cells		Function assay		Inhibitory activity against IL-4 production in RBL-2H3 cells was determined, IC50=3.7 μM	12951092

木犀草素 /Luteolin {[allProObj[0].p_purity_real_show]}

Luteolin 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Luteolin 质控信息

Luteolin 生物活性

Luteolin 细胞研究

Luteolin 动物研究

Luteolin 参考文献

Luteolin 实验方案

Luteolin 技术信息

最近浏览的产品

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摩尔计算器

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总药量计算器

工作液计算器

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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

木犀草素 /Luteolin {[allProObj[0].p_purity_real_show]}

Luteolin 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Luteolin 质控信息

Luteolin 生物活性

Luteolin 细胞研究

Luteolin 动物研究

Luteolin 参考文献

Luteolin 实验方案

Luteolin 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Luteolin 纯度/质量文件产品仅供科研