甲氧醉椒素是從卡瓦植物(Piper methysticum)中分離的內(nèi)酯?？ㄍ叩幕钚猿煞质且唤M約。18種化合物統(tǒng)稱為卡瓦內(nèi)酯或卡瓦吡酮?？ㄍ邇?nèi)酯、二氫卡瓦內(nèi)酯、甲基卡瓦內(nèi)酯、二氫甲基卡瓦內(nèi)酯、甲氧醉椒素和去甲氧基醉椒素是6種主要的卡瓦內(nèi)酯。卡瓦飲料和其他制劑被認(rèn)為是抗焦慮的，用于治療焦慮癥。含有卡瓦灌木根的膳食補(bǔ)充劑已經(jīng)涉及到幾個人的肝臟毒性案例，包括幾個在使用卡瓦補(bǔ)充劑后需要肝臟移植的人。
CB1
1.79 μM (IC 50 )
0.72 μM (Ki)
RelA
Yangonin is one of the six major kavalactones found in Piper methysticum .Yangonin potently inhibits NF-κB activation through suppression of the transcriptional activity of the RelA/p65 subunit of NF-κB. Yangonin significantly inhibits the induced expression of the NF-κB-reporter gene. However, Yangonin does not interfere with TNF-α-induced inhibitor of κBα (IκBα) degradation, p65 nuclear translocation, and DNA-binding activity of NF-κB. Yangonin inhibits not only the induced NF-κB activation by overexpression of RelA/p65, but also transactivation activity of RelA/p65. Yangonin does not inhibit TNF-α-induced activation of p38, but it significantly impairs activation of ERK 1/2 and stress-activated protein kinase/JNK.