Arctigenin,a natural lignan compound,has demonstrated anticancer activities in cancer. Arctigenin exhibits potent antioxidant, anti-inflammatory and antiviral (influenza A virus) activities [3,4].
Arctigenin (40 µM;48h) inhibited the growth of U87MG and T98G cells, induced G0/G1 cell-cycle arrest and triggered cell apoptosis in glioma cells[1]. Arctigenin (10,20,40,80 and 100μmol/L;48h) possesses anti-tumor activity in bladder cancer T24 cells. At the molecular level, arctigenin was able to reduce cyclin D1 and phospho-ERK1/2 expression, but induce phospho-p38 levels[4]. Arctigenin (0,1.56,12.5,100 μM; 24h) induce apoptosis in HCC cells via mitochondria and Fas/FasL-dependent apoptotic pathways[5].
Arctigenin (25 mg/kg;ip; twice daily ) for 23 day increased insulin-stimulated AKT phosphorylation in gastrocnemius muscle and liver, but not in perirenal fat[2]. Arctigenin (50mg/kg/day;ip) for 4 day confers protection against LPS-induced lung inflammatory and oxidative damage [6].
References:
[1]. Maimaitili A, Shu Z, Cheng X, Kaheerman K, Sikandeer A, Li W. Arctigenin, a natural lignan compound, induces G0/G1 cell cycle arrest and apoptosis in human glioma cells. Oncol Lett. 2017 Feb;13(2):1007-1013
[2]. Huang SL, Yu RT, Gong J, Feng Y, Dai YL, Hu F, Hu YH, Tao YD, Leng Y. Arctigenin, a natural compound, activates AMP-activated protein kinase via inhibition of mitochondria complex I and ameliorates metabolic disorders in ob/ob mice. Diabetologia. 2012 May;55(5):1469-81.
[3]. Hayashi K, Narutaki K, Nagaoka Y, Hayashi T, Uesato S. Therapeutic effect of arctiin and arctigenin in immunocompetent and immunocompromised mice infected with influenza A virus. Biol Pharm Bull. 2010;33(7):1199-205.
[4]. Yang S, Ma J, Xiao J, Lv X, Li X, Yang H, Liu Y, Feng S, Zhang Y. Arctigenin anti-tumor activity in bladder cancer T24 cell line through induction of cell-cycle arrest and apoptosis. Anat Rec (Hoboken). 2012 Aug;295(8):1260-6.
[5]. Lu Z, Cao S, Zhou H, Hua L, Zhang S, Cao J. Mechanism of Arctigenin-Induced Specific Cytotoxicity against Human Hepatocellular Carcinoma Cell Lines: Hep G2 and SMMC7721. PLoS One. 2015 May 1;10(5):e0125727.
[6]. Zhang WZ, Jiang ZK, He BX, Liu XB. Arctigenin Protects against Lipopolysaccharide-Induced Pulmonary Oxidative Stress and Inflammation in a Mouse Model via Suppression of MAPK, HO-1, and iNOS Signaling. Inflammation. 2015 Aug;38(4):1406-14.
Arctigenin是一种天然木脂素化合物，已证实具有抗癌活性。Arctigenin具有强效的抗氧化、抗炎和抗病毒（甲型流感病毒）活性[3,4]。
Arctigenin（40 μM；48h）抑制U87MG和T98G细胞生长，诱导G0/G1细胞周期阻滞并引发胶质瘤细胞凋亡[1]。Arctigenin（10、20、40、80和100μmol/L；48h）在膀胱癌T24细胞中具有有用的抗肿瘤活性。在分子水平上，Arctigenin能够降低细胞周期蛋白D1和磷酸化ERK1/2的表达，但诱导磷酸化p38的水平[4]。Arctigenin（0、1.56、12.5、100 μM；24h）通过线粒体和Fas/FasL依赖的凋亡途径诱导HCC细胞凋亡[5]。
Arctigenin（25 mg/kg；腹腔注射；每日两次）连续 23 天可增加腓肠肌和肝脏中胰岛素刺激的 AKT 磷酸化，但不会增加肾周脂肪中的 AKT 磷酸化[2]。Arctigenin（50 mg/kg/day；腹腔注射）连续 4 天可防止 LPS 引起的肺部炎症和氧化损伤[6]。