erythro-Austrobailignan-6

erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

erythro-Austrobailignan-6 (100 μM) 抑制 DNA 拓扑异构酶 I 活性超过 50%[1]。 erythro-Austrobailignan-6 (0-30 μM, 24 或 48 h) 抑制 4T-1 细胞和 MCF-7 细胞的增殖[1]. erythro-Austrobailignan-6 (2-30 μM，24 或 48 小时) 诱导 4T-1 和 MCF-7 细胞凋亡[1]。 erythro-Austrobailignan-6 (10 μM，30-120 分钟) 增加4T-1 和 MCF-7 细胞 p38 和 JNK 的磷酸化水平[1]。 erythro-Austrobailignan-6 (5 和 10 μM，24 小时) 降低 4T-1 和 MCF-7 细胞中的 EGFR/HER2 和拓扑异构酶水平[1]。 Cell Viability Assay[1] Cell Line: 4T-1 and MCF-7 cells Concentration: 0-30 μM Incubation Time: 24 or 48 h Result: Dose dependently inhibited cell proliferation. Western Blot Analysis[1] Cell Line: 4T-1 and MCF-7 cells Concentration: 100 μM Incubation Time: 30, 60 or 120 min Result: Increased phosphorylation of p38 and JNK. Activated caspase-3 and inhibited CDK-4 and cyclin D1.

erythro-Austrobailignan-6 (食物摄取，持续 20 天) 抑制 4T-1 荷瘤小鼠的肿瘤生长[1]。 Animal Model: 4T-1 tumor bearing mice[1] Dosage: 20 mg/kg/day Administration: Food intake Result: Inhibited tumor growth by 40.8%; Down-regulated CDK-4, cyclin D1, HER2 and integrin β3; Up-regulated cleaved caspase-3 in tumor.

[1]. Han JH, et al. Erythro-austrobailignan-6 down-regulates HER2/EGFR/integrinβ3 expression via p38 activation in breast cancer. Phytomedicine. 2017 Jan 15;24:24-30.  

[2]. Lee YK, et al. Inhibition of DNA topoisomerases I and II and cytotoxicity by lignans from Saururus chinensis. Arch Pharm Res. 2009 Oct;32(10):1409-15.