Esculetin

Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities^[1]. In Vitro:Esculetin (40 μM, 24 h or 48 h) inhibits PDGF-BB-induced ASMC proliferation and migration^[1].
Esculetin (40 μM, 1 h) inhibits PDGF-BB-induced ECM secretion and activation of PI3K/Akt pathway in ASMC cells^[1].
Esculetin (100 μM, 36 h) induces pancreatic cancer cell (such as PANC-1 cells) apoptosis and loss of mitochondrial membrane potential by activation of caspases 3, 8 and 9^[2].
Esculetin (100 μM, 0-12 h) binds to KEAP1 and inhibits its interaction with Nrf2 in pancreatic cancer cells (in PANC-1 cells)^[2].
In Vivo:Esculetin (50 and 100 mg/kg/day, p.o., 7d) ameliorates skin lesion in Imiquimod (HY-B0180) (IMQ)-induced psoriatic mice^[3].
Esculetin (10 or 30 mg/kg, i.p., three times per week for 28 days) inhibits tumor growth and metastasis via Axin2 suppression in an HCT116-implanted orthotopic mouse model^[4].
Esculetin (oral gavage, 25 mg/kg for 35 days) inhibits acute restraint stress (ARS)-induced oxidative stress in mature adult mice by increasing antioxidant enzyme activities, the GSH/GSSG ratio, and cytochrome c oxidase activity in cortex^[5].