Brevilin A

具有抗癌活性的倍半萜内酯；STAT3信号抑制剂（A549R细胞中的IC50=10.6µM）；抑制JAK1、JAK2、JAK3和JAK4JH1亚基的酪氨酸激酶活性（IC50s分别为11.2、8.4、10.2和11.9µM）；以浓度依赖性方式抑制多种癌细胞的增殖；降低线粒体膜电位、诱导细胞凋亡并增加CT26细胞中的ROS水平；以PI3K依赖性方式诱导自噬体形成；以每天5mg/kg的剂量增加LC3-II的肿瘤内表达并减少小鼠CT26结肠癌模型中的肿瘤生长。A sesquiterpene lactone with anticancer activity; an inhibitor of STAT3 signaling (IC50 = 10.6 µM in A549R cells); inhibits the tyrosine kinase activity of the JAK1, JAK2, JAK3, and JAK4 JH1 subunit (IC50s = 11.2, 8.4, 10.2, and 11.9 µM, respectively); inhibits proliferation of a variety of cancer cells in a concentration-dependent manner; decreases the mitochondrial membrane potential, induces apoptosis, and increases ROS levels in CT26 cells; induces autophagosome formation in a PI3K-dependent manner; increases intratumor expression of LC3-II and reduces tumor growth in a murine CT26 colon cancer model at 5 mg/kg per day.分子式C20H26O5分子量346.4C/C=C(C)\C(O[C@H]1[C@@]2([H])[C@@](OC([C@H]2C)=O)([H])C[C@H]([C@@]3([H])[C@]1(C(C=C3)=O)C)C)=O