Liu Rongxia, Heiss Elke H, Schachner Daniel, Jiang Baohong, Liu Wanhui, Breuss Johannes M, Dirsch Verena M, Atanasov Atanas G
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University , Yantai, 264005, People's Republic of China.
Department of Pharmacognosy, University of Vienna , Vienna, 1090, Austria.
J Nat Prod. 2017 Jul 28;80(7):2146-2150. doi: 10.1021/acs.jnatprod.7b00268. Epub 2017 Jun 19.
Xanthohumol (1) is a principal prenylated chalcone found in hops. The aim of this study was to examine its influence on platelet-derived growth factor (PDGF)-BB-triggered vascular smooth muscle cell (VSMC) proliferation and migration in vitro and on experimentally induced neointima formation in vivo. Quantification of resazurin conversion indicated that 1 can inhibit PDGF-BB-induced VSMC proliferation concentration-dependently (IC = 3.49 μM). Furthermore, in a wound-healing assay 1 potently suppresses PDGF-BB-induced VSMC migration at 15 μM. Tested in a mouse femoral artery cuff model, 1 significantly reduces neointima formation. Taken together, we show that 1 represses PDGF-BB-induced VSMC proliferation and migration in vitro as well as neointima formation in vivo. This novel activity suggests 1 as an interesting candidate for further studies addressing a possible therapeutic application to counteract vascular proliferative disease.
黄腐酚（1）是啤酒花中发现的一种主要的异戊烯基化查耳酮。本研究的目的是检测其对血小板衍生生长因子（PDGF）-BB触发的血管平滑肌细胞（VSMC）体外增殖和迁移以及对体内实验性诱导的新生内膜形成的影响。刃天青转化定量分析表明，1能够浓度依赖性地抑制PDGF-BB诱导的VSMC增殖（IC = 3.49 μM）。此外，在伤口愈合试验中，1在15 μM时能有效抑制PDGF-BB诱导的VSMC迁移。在小鼠股动脉袖带模型中进行测试，1能显著减少新生内膜的形成。综上所述，我们表明1在体外可抑制PDGF-BB诱导的VSMC增殖和迁移，在体内也可抑制新生内膜的形成。这种新活性表明1是一个有趣的候选物，可用于进一步研究解决对抗血管增殖性疾病的可能治疗应用。
