Armepavine

Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia^[1][2]. In Vitro:Armepavine (1-10 μM; 24 h) does not exert cytotoxic effects on HSC-T6 rat hepatic stellate cells^[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF-α-induced collagen deposition in HSC-T6 rat hepatic stellate cells, with significant inhibition at 10 μM^[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF^−α- and LPS-induced α-SMA protein expression in HSC-T6 rat hepatic stellate cells^[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF-α- and LPS-induced AP-1 transcriptional activity in HSC-T6 rat hepatic stellate cells, with significant effects at 10 μM for TNF-α and 3-10 μM for LPS^[1].
Armepavine (1-10 μM; 6 h) concentration-dependently inhibits TNF-α-induced IκBα phosphorylation and NFκB p65 nuclear translocation in HSC-T6 rat hepatic stellate cells^[1].
Armepavine (1-10 μM; 6 h) concentration-dependently inhibits TNF-α-induced NFκB transcriptional activity in HSC-T6 rat hepatic stellate cells, with significant effects at 1 and 10 μM^[1].
Armepavine (10 μM; 15-60 min) inhibits TNF-α-induced phosphorylation of p38, ERK1/2, and JNK1/2 in HSC-T6 rat hepatic stellate cells^[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF-α-induced mRNA expression of iNOS, collagen 1α2, TIMP-1, and α-SMA in HSC-T6 rat hepatic stellate cells^[1]. In Vivo:Armepavine (3-10 mg/kg; p.o.; twice daily; 3 weeks) exerts dose-dependent anti-hepatic fibrosis effects in bile duct-ligated rats, with the 10 mg/kg dose reducing fibrosis scores by 47% and collagen content to 4.38 mg/g liver, and the 3 mg/kg dose reducing fibrosis scores by 24% and hepatocyte necrosis scores by 68%^[1].