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.
Wedelolactone/蟛蜞菊内酯 细胞实验
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.
Wedelolactone/蟛蜞菊内酯 动物实验
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
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
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