Swerchirin

Swerchirin is an orally active, plant-derived xanthone that acts as an inhibitor of the Raf/MEK/ERK signaling pathway. Swerchirin downregulates the expression of phosphorylated MEK and phosphorylated ERK, induces mitochondrial apoptosis and cell cycle arrest, regulates Bcl-2 family proteins, triggers cytochrome c release, activates caspases, and drives PARP cleavage. Swerchirin reduces blood glucose levels in rat models under fasting, fed, glucose-loaded conditions, and following treatment with Tolbutamide (HY-B0401). Swerchirin can be used in research related to ovarian cancer, liver injury, and diabetes^[1][2][3]. In Vitro:Swerchirin (10-40 μM; 48 h) potently inhibits the viability of human ovarian cancer SKOV3 cells in a concentration-dependent manner, with an IC₅₀ of 20 μM^[1].
Swerchirin (10-40 μM; 24 h) induces G₂/M cell cycle arrest in human ovarian cancer SKOV3 cells in a concentration-dependent manner in vitro^[1].
Swerchirin (10-40 μM; 6-72 h) reduces the mitochondrial membrane potential of human ovarian cancer SKOV3 cells in a concentration-dependent manner in vitro^[1].
Swerchirin (10-40 μM; 48 h) induces apoptosis in human ovarian cancer SKOV3 cells in a concentration-dependent manner^[1].
Swerchirin (10-40 μM) regulates the expression of apoptosis-related proteins in human ovarian cancer SKOV3 cells in a concentration-dependent manner, upregulating pro-apoptotic proteins and downregulating the anti-apoptotic protein Bcl-2^[1].
Swerchirin (10-40 μM) inhibits the Raf/MEK/ERK signaling pathway in human ovarian cancer SKOV3 cells in vitro in a concentration-dependent manner by downregulating the expression of phosphorylated MEK and phosphorylated ERK^[1]. In Vivo:Swerchirin (3-50 mg/kg; p.o.; single administration 1 hour prior to acetaminophen treatment) exhibits hepatoprotective activity against Acetaminophen (HY-66005)-induced liver injury in male Swiss mice, reducing Acetaminophen-induced elevation of serum ALT by 80.0%^[2].
Swerchirin (5-250 mg/kg; p.o.; single administration) produces a dose-dependent, sustained hypoglycemic effect in fed male CF albino rats, with an ED₅₀ of 23.1 mg/kg for achieving a 40% hypoglycemic effect that lasts up to 7 h^[3].
Swerchirin (50 mg/kg; p.o.; single administration) reduces blood glucose by 39% in fasted male CF albino rats at 3 h and maintains blood glucose levels below baseline for 24 h^[3].
Swerchirin (50 mg/kg; p.o.; single administration) inhibits the post-glucose-load blood glucose peak and delays blood glucose recovery in glucose-loaded male CF albino rats^[3].
Swerchirin (20 mg/kg; p.o.; single dose) enhances the hypoglycemic effect of Tolbutamide in pretreated male CF albino rats, with the maximum hypoglycemic effect observed at 4 h^[3].