Gamabufotalin (CS-6), a above bufadienolide of Chansu, has been acclimated for blight analysis due to its adorable metabolic adherence and beneath adverse effect. However, the basal apparatus of CS-6 complex in anti-tumor action charcoal ailing understood.
The biological functions of gamabufotalin (CS-6) were advised by migration, antecedents accumulation and apoptosis assays in NSCLC cells. The nuclear localization and alternation amid transcriptional co-activator p300 and NF-κB p50/p65 and their bounden to COX-2 apostle were analyzed afterwards analysis with CS-6. Molecular advancing abstraction was acclimated to simulate the alternation of CS-6 with IKKβ. The in vivo anti-tumor ability of CS-6 was aswell analyzed in xenografts nude mice. Western blemish was acclimated to ascertain the protein announcement level.
Gamabufotalin (CS-6) acerb suppressed COX-2 announcement by inhibiting the phosphorylation of IKKβ via targeting the ATP-binding site, thereby abrogating NF-κB bounden and p300 application to COX-2 promoter. In addition, CS-6 induced apoptosis by activating the cytochrome c and caspase-dependent apoptotic pathway. Moreover, CS-6 clearly down-regulated the protein levels of COX-2 and phosphorylated p65 NF-κB in bump tissues of the xenograft mice, and inhibited bump weight and size.
