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Chemical Structure| 524-12-9 Chemical Structure| 524-12-9

Structure of Wedelolactone
CAS No.: 524-12-9

Chemical Structure| 524-12-9

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Wedelolactone, a natural compound derived from Chinese herbal medicine Eclipta prostrate L, is an anti-cancer agent for breast and prostate carcinomas in vitro and in vivo targeting multiple cellular proteins including androgen receptors, 5-lipoxygenase and topoisomerase IIα.

Synonyms: IKK Inhibitor II

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Product Details of Wedelolactone

CAS No. :524-12-9
Formula : C16H10O7
M.W : 314.25
SMILES Code : O=C1C2=C(OC3=CC(O)=C(O)C=C32)C4=C(O)C=C(OC)C=C4O1
Synonyms :
IKK Inhibitor II
MDL No. :MFCD07778564
InChI Key :XQDCKJKKMFWXGB-UHFFFAOYSA-N
Pubchem ID :5281813

Safety of Wedelolactone

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PC3 cells 10-30 µM 24 hours WDL dramatically decreases c-Myc protein levels Mol Cancer Ther. 2016 Nov;15(11):2791-2801.
LNCaP cells 30 µM 4-16 hours WDL significantly reduces c-Myc mRNA levels Mol Cancer Ther. 2016 Nov;15(11):2791-2801.
NRK-52E rat renal tubular epithelial cells 30 μmol/L 2 hours Wedelolactone inhibited Ang II-induced expression of TGF-β, fibronectin, and collagen I Acta Pharmacol Sin. 2019 Jun;40(6):790-800.
RAW 264.7 cells 0.1, 1, 10 μM 12 h pretreatment followed by 20 h LPS stimulation To investigate the anti-inflammatory effects of WEL on LPS-induced responses, results showed WEL significantly inhibited the protein expression levels of iNOS and COX-2, as well as the production of downstream products including NO, PGE2, and TNF-α. J Biomed Sci. 2013 Oct 31;20(1):84.
Human alveolar epithelial cell MLE-12 10 μM 48 hours Wedelolactone significantly inhibited TGF-β1-induced abnormal expressions of EMT markers (α-SMA, Vimentin, Col I, and E-cadherin) and suppressed the EMT process of alveolar epithelial cells by activating AMPK. Front Pharmacol. 2019 Mar 5;10:151.
Primary mouse lung fibroblasts (PLFs) 10 μM 48 hours Wedelolactone significantly inhibited TGF-β1-induced α-SMA overexpression and suppressed the transdifferentiation of lung fibroblasts by activating AMPK. Front Pharmacol. 2019 Mar 5;10:151.
BMDMs 5, 10, 20, 40 μM 45 minutes Inhibited NLRP3 inflammasome activation, reduced IL-1β production Front Pharmacol. 2021 Jun 3;12:655531.
LX-2 cells 10, 20, 40 μM Inhibited TGF-β1/Smad signaling pathway, reduced expression and phosphorylation of Smad3 Front Pharmacol. 2021 Jun 3;12:655531.
THP-1 macrophages 10, 20, 40 μM 1 hour Wedelolactone dose-dependently inhibited nigericin-induced caspase-1 p10 and mature IL-1β secretion Cell Prolif. 2020 Sep;53(9):e12868.
BMDM macrophages 10, 20, 40 μM 1 hour Wedelolactone dose-dependently inhibited ATP-induced caspase-1 p20 and mature IL-1β release Cell Prolif. 2020 Sep;53(9):e12868.
J774A.1 macrophages 10, 20, 40 μM 1 hour Wedelolactone dose-dependently inhibited ATP-induced caspase-1 p20 and mature IL-1β release Cell Prolif. 2020 Sep;53(9):e12868.
RAW264.7 cells 5 μg/mL 24 hours Inhibited cleavage of Caspase 11 and GSDMD, reduced release of IL-1α and IL-1β MedComm (2020). 2024 Jun 14;5(6):e610.
J774A.1 cells 5 μg/mL 24 hours Inhibited cleavage of Caspase 11 and GSDMD, reduced release of IL-1α and IL-1β MedComm (2020). 2024 Jun 14;5(6):e610.
MH-S cells 30 μM 24 hours Inhibited caspase-11 activation and GSDMD cleavage induced by HDM/Curdlan stimulation Respir Res. 2024 Mar 8;25(1):119.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J male mice MSU-induced peritonitis and arthritis model Intraperitoneal injection 20 mg/kg Single dose, evaluated after 6 hours Wedelolactone significantly reduced MSU-induced IL-1β production and neutrophil migration into the peritoneal cavity, and decreased caspase 1 (p20) and IL-1β expression in joint tissues Cell Prolif. 2020 Sep;53(9):e12868.
MRL/lpr mice Systemic lupus erythematosus model Intraperitoneal injection 10 mg/kg Once daily for 9 weeks Inhibited Caspase 11/GSDMD pathway, alleviated lupus symptoms MedComm (2020). 2024 Jun 14;5(6):e610.
C57BL/6J mice Unilateral ureteral obstruction (UUO) model Oral gavage 30 mg/kg/day Once daily for 7 days Wedelolactone significantly alleviated renal fibrosis in UUO mice, improved histological changes, and suppressed caspase-1 activation, IL-1β maturation, TGF-β, fibronectin, and collagen I expression Acta Pharmacol Sin. 2019 Jun;40(6):790-800.
Balb/c nude mice LNCaP prostate cancer xenograft model Oral gavage 200 mg/kg/day Five days a week for four weeks WDL significantly inhibits tumor growth and reduces c-Myc and its target protein levels Mol Cancer Ther. 2016 Nov;15(11):2791-2801.
ICR and C57/BL6 mice Bleomycin (BLM)-induced pulmonary fibrosis model Intragastric administration 2 mg/kg or 10 mg/kg Once daily for 14 days Wedelolactone (10 mg/kg) significantly attenuated BLM-induced inflammatory cell infiltration, pro-inflammatory factor expression, and collagen deposition in lung tissues, and improved pulmonary fibrosis by activating AMPK and inhibiting the TGF-β1/Raf-MAPK signaling pathway. Front Pharmacol. 2019 Mar 5;10:151.
C57BL/6 mice BDL-induced hepatic fibrosis model Gavage 20 mg/kg Once daily for 14 days Alleviated hepatic injury and fibrosis, inhibited TGF-β/Smad-mediated activation of HSCs Front Pharmacol. 2021 Jun 3;12:655531.
BALB/c mice Footpad injection model Intraperitoneal injection 80 µM Single dose Wedelolactone, as a caspase-11 inhibitor, significantly reduced neutrophil infiltration and senescence markers γH2AX/p16INK4a expression in V Tn-induced chronic wounds, promoting wound healing. Int J Mol Sci. 2023 May 8;24(9):8453
C57BL/6 mice HDM-induced asthma model Intragastric administration 20 mg/kg Administered during sensitization and effector phase Alleviated airway inflammation aggravated by Curdlan, reducing inflammatory cell infiltration and mucus production Respir Res. 2024 Mar 8;25(1):119.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.91mL

3.18mL

1.59mL

31.82mL

6.36mL

3.18mL

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

References

 

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