Arctigenin is a dibenzyl butyrolactone lignan agent with antiinflammatory and antioxidant properties. Studies describe arctigenin to potently block TNF- α production and NO secretion. MAP kinase studies show that arctigenin effectively inhibits the activity of MAP kinases and AP-1 activation through vigorous inhibition of MKK. Additional studies report that arctigenin acts as a potent inhibitor of PAC-1 activity. Arctigenin has also been shown to bind to kainic acid receptors and protect neurons from neurodegeneration induced by glutamate and inhibit HIV-1 integrase. Furthermore, this compound acts as an inhibitor of IκB phosphorylation. Arctigenin is an inhibitor of MEK-1 and Topo II.
溶解性:DMSO : 37.2 mg/mL (100 mM)
体外研究:
Arctigenin induces apoptosis in HT-29 colon cancer cells by regulating ROS and p38 MAPK pathways. It is a phytoestrogen that exerts a proliferative effect by binding to the ER. Treatment with arctigenin effectively downregulates ERα expression. Thus, arctigenin, mainly targets the mTOR pathway in ERα-positive MCF-7 human breast cancer cells, leading to autophagy-induced cell death and the downregulation of ERα expression. Arctigenin decreases BACE1 translation via dephosphorylation of eIF2α, causing the suppression of Aβ production, and initiates autophagy through both AMPK/Raptor signaling activation and AKT/mTOR pathway inhibition, resulting in enhanced Aβ clearance. Arctigenin suppresses BACE1 activity via inhibition of BACE1 translation.
体内研究:Treatment of arctigenin in mice highly decreases Aβ formation and senile plaques and efficiently ameliorates AD mouse memory impairment of APP/PS1 transgenic model mice.