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Application of galangin an active component of Alpinia officinarum Hance (Zingiberaceae) for use in drug-eluting stents

机译:高良姜素(高良姜(姜科)的活性成分)在药物洗脱支架中的应用

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摘要

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 G0/G1 to the S phase via the up-regulation of p27KIP1 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 p27KIP1 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 p27KIP1, 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.
机译:在临床病理中,支架置入术可用于治疗血管疾病,但可导致再狭窄。药物洗脱支架(DES)最常用于抑制再狭窄,但也可能有副作用。因此,我们在体外和体内研究了抗增殖作用及其可能的靶标。我们发现高良姜提取物通过上调p27 KIP1 的表达阻止了从G0 / G1到S期的过渡,从而有效抑制了VSMC的增殖。高良姜精(GA)被确定为该提取物中的重要成分,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表明,AO提取物和GA均靶向上调p27 KIP1 的表达。因此,我们接下来在体内研究了这些化合物在袖套损伤的新内膜增生模型中的作用。在该动物模型中,AO提取物和GA都完全抑制了新内膜的形成,并且这种抑制作用还被证明针对p27 KIP1 的上调,包括抑制增殖细胞核抗原的表达。 。我们的发现表明,AO提取物和GA具有有效的抗增殖活性,靶向上调p27表达。因此,GA可能代表DES中使用的替代药物。

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