Inhibitory effect of ERK1/2 and AP-1 by hyperoside isolated from Acanthopanax sessiliflorus

• Published in: Food chemistry Vol. 130; no. 4; pp. 915 - 920
• Main Authors: Jung, Sung Keun, Lim, Tae Gyu, Kim, Jong Eun, Byun, Sanguine, Kim, Gye-Won, Choi, Jung Nam, Lee, Choong Hwan, Kim, Bo Yeon, Lee, Ki Won, Lee, Hyong Joo
• Format: Journal Article
• Language: English
• Published: Kidlington Elsevier Ltd 15.02.2012; Elsevier
• Subjects: Acanthopanax sessiliflorus; AP-1; Biological and medical sciences; ERK1/2; Food industries; Fundamental and applied biological sciences. Psychology; Hyperoside; Hyperoside; Acanthopanax sessiliflorus; ERK1/2; AP-1
• ISSN: 0308-8146; 1873-7072
• DOI: 10.1016/j.foodchem.2011.08.010

► We identified hyperoside as a major compound of Acanthopanax sessiliflorus. ► We used JB6 P+cells and UVB model. ► Hyperoside inhibits ERK1/2 activity by direct binding with ERK1/2. ► Hyperoside inhibits UVB-induced AP-1 transcritpion factor activity. ► Hyperoside inhibits UVB-induced ERK1/2 down-stream signalling. Consumption of fruits and vegetables is correlated with a lower incidence of cancer. Here, we identified hyperoside as an active compound from Acanthopanax sessiliflorus, and investigated the effect of hyperoside on UVB-induced transactivation of activator protein 1 (AP-1) and on the mitogen-activated protein kinase signalling pathway in JB6 P+cells. Hyperoside inhibited UVB-induced AP-1 transactivation. It inhibited the UVB-induced phosphorylation of p90RSK. Kinase assays revealed that hyperoside significantly inhibited ERK1/2 activity. Furthermore, hyperoside bound to ERK1/2 to suppress its activity. In addition, phosphorylation of cAMP response element binding protein (CREB) and signal transducers and activators of transcription (STAT) 3 were suppressed by hyperoside. Overall, these results indicate that hyperoside may be a promising chemopreventive agent that acts by suppressing the transactivation of AP-1 and the phosphorylation of p90RSK, CREB, and STAT3 through the binding and inhibition of ERK1/2.