Aspulvinone O

Aspulvinone O is a selective inhibitor of glutamate oxaloacetate aminotransferase GOT1. Aspulvinone O inhibits glutamine metabolism and reduces NADPH production, thereby inducing oxidative stress and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cells. Aspulvinone O inhibits PDAC cell proliferation in vitro and tumor growth in xenograft models^[1][2]. In Vitro:Aspulvinone O (0.1-100 μM; 48 h) inhibits the proliferation of pancreatic ductal adenocarcinoma cell lines (SW1990, PANC-1, AsPC-1) with IC₅₀ of 20.54-26.80 μM, showing selectivity for cancer cells over normal cells^[1].
Aspulvinone O (10-40 μM; 48 h) arrests the cell cycle of SW1990 cells at the S phase and induces apoptosis^[1].
Aspulvinone O (10-40 μM; 24 h) reduces the levels of glutamine metabolic intermediates (OAA, malate) and the NADPH/NADP⁺ ratio^[1] in SW1990 cells^[1].
In Vivo:Aspulvinone O (2.5 mg/kg, 5 mg/kg; intraperitoneal injection; once daily; 14 days) significantly inhibits tumor growth in the SW1990 PDAC cell xenograft model of CB17/scid mice, reducing tumor weight by 40-60%, without obvious systemic toxicity^[1].