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Chemical Structure| 529-53-3 Chemical Structure| 529-53-3

Structure of Scutellarein
CAS No.: 529-53-3

Chemical Structure| 529-53-3

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Scutellarin is cytotoxic to cancer cells and could induce DNA damage, metabolic suppression and mitochondrial reactive oxygen species. It has has antioxidant, anti-inflammatory, and antiproliferative biological activities that can be can be found in scutellaria lateriflora.

Synonyms: 4',5,6,7-Tetrahydroxyflavone; 6-Hydroxyapigenin

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Product Citations

Product Citations

Krueger, Nadine ; Kronenberger, Thales ; Xie, Hang ; Rocha, Cheila ; Poehlmann, Stefan ; Su, Haixia , et al.

Abstract: The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has forced the development of direct-acting antiviral drugs due to the coronavirus disease 2019 (COVID-19) pandemic. The main protease of SARS-CoV-2 is a crucial enzyme that breaks down polyproteins synthesized from the viral RNA, making it a validated target for the development of SARS-CoV-2 therapeutics. New chem. phenotypes are frequently discovered in natural goods. In the current study, we used a fluorogenic assay to test a variety of natural products for their ability to inhibit SARS-CoV-2 Mpro. Several compounds were discovered to inhibit Mpro at low micromolar concentrations It was possible to crystallize robinetin together with SARS-CoV-2 Mpro, and the X-ray structure revealed covalent interaction with the protease's catalytic Cys145 site. Selected potent mols. also exhibited antiviral properties without cytotoxicity. Some of these powerful inhibitors might be utilized as lead compounds for future COVID-19 research.

Keywords: COVID-19 ; antivirals ; coronavirus ; covalent drugs ; dynamic light scattering ; inhibitors ; main protease ; natural products

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Product Details of Scutellarein

CAS No. :529-53-3
Formula : C15H10O6
M.W : 286.24
SMILES Code : O=C1C=C(C2=CC=C(O)C=C2)OC3=C1C(O)=C(O)C(O)=C3
Synonyms :
4',5,6,7-Tetrahydroxyflavone; 6-Hydroxyapigenin
MDL No. :MFCD00017692
InChI Key :JVXZRQGOGOXCEC-UHFFFAOYSA-N
Pubchem ID :5281697

Safety of Scutellarein

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MG63 cells 0-300 µM 48 hours SCU significantly inhibited OS cell proliferation Drug Des Devel Ther. 2025 Jan 6;19:51-64
143B cells 0-300 µM 48 hours SCU significantly inhibited OS cell proliferation Drug Des Devel Ther. 2025 Jan 6;19:51-64
BEAS-2B cells 12.5–50 µM 1 hour pretreatment followed by 24 hours LPS stimulation Reduced intracellular ROS accumulation, inhibited NADPH oxidase activity, downregulated transcription and translation of pro-inflammatory cytokines IL-6, CCL2, and CXCL8 Antioxidants (Basel). 2024 Jun 12;13(6):710
Huh-7 cells 25, 50, 100, 150, 200 µM 24 and 48 hours To evaluate the effect of SCU on Huh-7 cell viability, results showed SCU significantly decreased cell viability in a dose- and time-dependent manner. Int J Mol Sci. 2021 Aug 17;22(16):8841
Hep3B cells 0, 100, 200, 300, 400, 500, 600 µM 24 hours SCU significantly inhibited Hep3B cell proliferation and induced G2/M phase cell cycle arrest. Nutrients. 2019 Jan 24;11(2):263
T84 cells 0, 20, 40, 60, 80 µM 24 hours Scutellarein significantly inhibited the viability and clone formation ability of T84 cells and induced apoptosis. IC50 value was 39.6 µM. Int J Mol Med. 2020 Apr;45(4):1059-1072
SW480 cells 0, 20, 40, 60, 80 µM 24 hours Scutellarein significantly inhibited the viability and clone formation ability of SW480 cells and induced apoptosis. IC50 value was 40 µM. Int J Mol Med. 2020 Apr;45(4):1059-1072
CL-40 cells 0, 20, 40, 60, 80 µM 24 hours Scutellarein significantly inhibited the viability and clone formation ability of CL-40 cells and induced apoptosis. IC50 value was 40.9 µM. Int J Mol Med. 2020 Apr;45(4):1059-1072
Primary rat hepatocytes 80 µM 24 hours To investigate the protective effect of Scutellarein on THP-induced hepatotoxicity, results showed that Scutellarein significantly improved hepatocyte viability and inhibited inflammatory response. Int J Mol Med. 2023 Jul;52(1):55
HT1080 human fibrosarcoma cells 10 and 50 µM 24 hours To evaluate the inhibitory effect of Scutellarein on the proliferation of HT1080 cells. The results showed that Scutellarein significantly suppressed the proliferation rate of HT1080 cells. Int J Mol Med. 2015 Jan;35(1):31-8
HT-29 cells 10 µM 24 hours Scu attenuated the IL-1β-downregulated expression levels of E-cadherin, occludin, and ZO-1, while reduced IL-1β-upregulated IL-6 and IL-8 mRNA levels. Moreover, Scu inhibited the phosphorylation and nuclear translocation of NF-κB and suppression of NF-κB phosphorylation abolished IL-1β-disrupted epithelial barrier integrity and IL-1β-upregulated proinflammatory mediators expression in HT-29 cells. Front Pharmacol. 2024 Oct 21;15:1479441
PC12 cells 1-100 µM 3 hours Evaluate the protective effect of Scutellarein on H2O2-induced cytotoxicity in PC12 cells, results showed Scutellarein had significant dose-dependent protective effects. Int J Mol Sci. 2011;12(11):8208-16
HT1080 human fibrosarcoma cells 10 and 50 µM 36 hours To evaluate the effect of Scutellarein on the invasion of HT1080 cells. The results showed that Scutellarein significantly reduced the invasion ability of HT1080 cells. Int J Mol Med. 2015 Jan;35(1):31-8
RAW264.7 cells 25, 50, 75 µM 48 hours Investigate the effect of SCU on LPS-induced inflammation, finding that SCU suppresses iNOS expression in a dose-dependent manner but does not affect COX-2 expression. Molecules. 2022 Jun 12;27(12):3782
HepG2 cells 25, 50, 100 µM 48 hours To evaluate the effect of SCU on HepG2 cell migration and proliferation, results showed SCU significantly inhibited cell migration and proliferation, and induced G2/M phase cell cycle arrest. Int J Mol Sci. 2021 Aug 17;22(16):8841
HaCaT cells 25, 50, 100 µM 48 hours To evaluate the effect of SCU on HaCaT cell viability, results showed no significant effect at 25, 50, 100 μM concentrations within 48 hours. Int J Mol Sci. 2021 Aug 17;22(16):8841
HT1080 human fibrosarcoma cells 10 and 50 µM 6 hours To evaluate the effect of Scutellarein on the migration of HT1080 cells. The results showed that Scutellarein significantly reduced the migration ability of HT1080 cells. Int J Mol Med. 2015 Jan;35(1):31-8
Rat liver microsomes 30 µM 90 min To study the metabolic stability of Scutellarin in male and female rat liver microsomes. Results showed that the metabolic clearance rate (CLint) of Scutellarin was significantly higher in male rats than in female rats (P<0.01). Acta Pharmacol Sin. 2011 May;32(5):655-63

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c nude mice HT1080 cell-induced fibrosarcoma model Intraperitoneal injection 0.05 and 0.5 µg/g 20 days To evaluate the inhibitory effect of Scutellarein on the development of fibrosarcoma. The results showed that Scutellarein significantly reduced the volume and weight of the tumors. Int J Mol Med. 2015 Jan;35(1):31-8
BALB/c nude mice Colon cancer-bearing model Intraperitoneal injection 0.5 µg/g Once daily for 20 days Scutellarein significantly inhibited tumor volume and Ki-67 expression, alleviating pathological changes in tumor tissues. Int J Mol Med. 2020 Apr;45(4):1059-1072
BALB/c nude mice Osteosarcoma xenograft model Intraperitoneal injection 0.5 μg/g Every 2 days until tumor volume reached about 60 mm3 SCU significantly inhibited osteosarcoma growth Drug Des Devel Ther. 2025 Jan 6;19:51-64
SD rats THP-induced hepatotoxicity model Gavage 100 mg/kg Once a week for 6 weeks To investigate the protective effect of Scutellarein on THP-induced hepatotoxicity, results showed that Scutellarein significantly alleviated liver inflammation and liver function damage. Int J Mol Med. 2023 Jul;52(1):55
Rats Middle cerebral artery occlusion (MCAO) model Intragastric administration 100, 50, 25 mg/kg Administered for 6 consecutive days, MCAO surgery performed on the 7th day To evaluate the protective effect of Scutellarein on focal cerebral ischemia/reperfusion, results showed that Scutellarein dose-dependently reduced neurological deficit scores and cerebral infarction volume, with better efficacy than Scutellarin Molecules. 2012 Sep 6;17(9):10667-74
Galleria mellonella larvae A. baumannii infection model Injection in the left second proleg 20 mg/kg Administered 2 hours post-infection, monitored for at least 5 days Scu significantly increased the survival rate of larvae by about 35% Microb Cell Fact. 2024 Oct 8;23(1):269
ICR mice LPS-induced acute lung injury model Intraperitoneal injection 25, 50, 100 mg/kg Single administration, evaluated 6 h post-LPS stimulation Significantly reduced IL-6, CCL2, and TNF-α levels in BALF, attenuated lung pathological damage, and inhibited neutrophil infiltration Antioxidants (Basel). 2024 Jun 12;13(6):710
Sprague-Dawley rats Pharmacokinetic model of oral and intravenous administration of Scutellarin Oral and intravenous 400 mg/kg (oral), 40 mg/kg (intravenous) Single dose To study the pharmacokinetics and excretion characteristics of Scutellarin and its metabolite Scutellarein in rats. Results showed that plasma concentrations of Scutellarin were significantly higher in female rats than in male rats (P<0.05) after oral administration, and a large amount of Scutellarin was metabolized into Scutellarein in the gastrointestinal tract and excreted in feces, leading to its extremely low oral bioavailability. Acta Pharmacol Sin. 2011 May;32(5):655-63
C57BL/6 mice DSS-induced colitis model Intragastric gavage 5 mg/kg, 10 mg/kg, 20 mg/kg Once daily for 7 days Scu significantly decreased the DAI score, improved colon shortening, ameliorated the pathological score in DSS-treated mice with better efficacy than the positive drug, 5-aminosalicylic acid. Scu also inhibited the expression levels of cytokines (Il-1β, Tnf-α, Il-1α, Il-6, and Cxcl1) as well as barrier proteins (E-cadherin, Occludin, and ZO-1) in colon tissues of DSS mice. Front Pharmacol. 2024 Oct 21;15:1479441

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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