Korean Medicine (KM) Application Center, Korea Institute of Oriental Medicine, Daegu, 701-300, Republic of Korea.
Department of Pharmacology, Chungnam National University College of Pharmacy, Daejeon, 305-764, Republic of Korea.
Sci Rep. 2017 Aug 15;7(1):8207. doi: 10.1038/s41598-017-08410-2.
In clinical pathology, stent interposition is used to treat vascular disease but can lead to restenosis. Drug-eluting stents (DES) are most commonly used to suppress restenosis but can also have side effects. Therefore, we investigated the anti-proliferative effect and its possible target in vitro and in vivo. We found that Alpinia officinarum Hance (AO) extract efficiently inhibited VSMC proliferation by arresting the transition from the G/G to the S phase via the up-regulation of p27 expression. Galangin (GA) was determined to be a significant component of this extract, with the same anti-proliferative activity as the raw extract. Immunoblotting and immunofluorescence staining showed that both the AO extract and GA targeted the up-regulation of p27 expression. Therefore, we next examined the effect of these compounds in a cuff-injured neointimal hyperplasia model in vivo. In this animal model, both the AO extract and GA completely suppressed the neointima formation, and this inhibitory effect was also demonstrated to target the up-regulation of p27, including the suppression of proliferating cell nuclear antigen expression. Our findings indicate that AO extract and GA have a potent anti-proliferative activity, targeting the up-regulation of p27 expression. Thus, GA may represent an alternative medicine for use in DES.
在临床病理学中,支架介入术被用于治疗血管疾病,但可能导致再狭窄。药物洗脱支架(DES)是最常用于抑制再狭窄的支架,但也可能有副作用。因此,我们在体外和体内研究了其抗增殖作用及其可能的靶点。我们发现高良姜(Alpinia officinarum Hance,AO)提取物通过上调 p27 表达将细胞从 G1/S 期阻滞有效地抑制 VSMC 增殖。山柰素(GA)被确定为该提取物的一个重要成分,具有与原始提取物相同的抗增殖活性。免疫印迹和免疫荧光染色显示,AO 提取物和 GA 均靶向 p27 表达的上调。因此,我们接下来在体内套管损伤性新生内膜增生模型中研究了这些化合物的作用。在该动物模型中,AO 提取物和 GA 完全抑制了新生内膜的形成,这种抑制作用也被证明靶向 p27 的上调,包括抑制增殖细胞核抗原的表达。我们的研究结果表明,AO 提取物和 GA 具有很强的抗增殖活性,靶向 p27 表达的上调。因此,GA 可能代表一种替代药物用于 DES。