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Luteolin

Synonyms: Luteoline, Luteolol, Digitoflavone

Luteolin (Luteoline, Luteolol, Digitoflavone) is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively.

Luteolin Chemical Structure

Luteolin Chemical Structure

CAS No. 491-70-3

Purity & Quality Control

Luteolin Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
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
CHO cells Function assay Agonist activity at rat DAT expressed in CHO cells, EC50=1.45 μM 20971650
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
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
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
RBL-2H3 cells Function assay Inhibitory activity against IL-4 production in RBL-2H3 cells was determined, IC50=3.7 μM 12951092
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 LNCAP cells Function assay Downregulation of prostate specific antigen secretion in human LNCAP cells, IC50=5 μM 25019478
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
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 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
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
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
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
K562 cells Growth inhibition assay 5 days Growth inhibition of K562 cells by XTT assay after 5 days, IC50=14.65 μM 17411092
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 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 U937 cells Proliferation assay 72 h Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=20 μM 17158054
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
human THP1 cells Function assay 20 μM 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
MDA-MB-231 cells Function assay 5 μM 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
HL60 cells Proliferation assay 30 μM 48 h Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay 18258440
Click to View More Cell Line Experimental Data

Biological Activity

Description Luteolin (Luteoline, Luteolol, Digitoflavone) is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively.
Targets
PDE2 [1]
(Cell-free assay)		 PDE5 [1]
(Cell-free assay)		 PDE4 [1]
(Cell-free assay)		 PDE3 [1]
(Cell-free assay)		 PDE1 [1]
(Cell-free assay)
6.4 μM(Ki) 9.5 μM(Ki) 11.1 μM(Ki) 13.9 μM(Ki) 15.0 μM(Ki)
In vitro
In vitro

Luteolin is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively. [1] Luteolin inhibits LPS-stimulated TNF-alpha production with an IC50 of less than 1 μM. Luteolin inhibites LPS-induced phosphorylation of Akt as well as IkappaBalpha. [2]
Experimental Result Images Methods Biomarkers Images PMID
Western blot FADD / PARP / Cleaved PARP Caspase-3 / Cleaved Caspase-3 / Caspase-8 / Cleaved Caspase-8 ERK / p-ERK / JNK / p-JNK / p38 / p-p38 / Bax / Bcl-2 p-VEGFR2 / p-mTOR / pS6K1 / p70S6K1 / pAKT / AKT / MMP-2 / MMP-9 p21 / Survivin / Cyclin D1 DNMT1 / DMNT3A / DNMT3B TET1 / TET2 / TET3 30992674
Immunofluorescence 5-hmC 30988303
Growth inhibition assay Cell viability 30992674
In Vivo
In vivo

LD50: Mice >2500mg/kg (i.g.) [3]

Chemical Information & Solubility

Molecular Weight 286.24 Formula

C15H10O6
CAS No. 491-70-3 SDF Download Luteolin SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 33 mg/mL ( (115.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Would you please suggest a suitable vehicle to dissolve Luteolin for in vivo i.p. use?

Answer:
Formula: 5% DMSO+40% PEG 300+5% Tween80+ddH2O, working Solution concentration: up to 7.5mg/ml, stable for 30min.

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