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首页> 外文期刊>European Journal of Pharmacology: An International Journal >Anti-angiogenic effects of Shiraiachrome A, a compound isolated from a Chinese folk medicine used to treat rheumatoid arthritis.
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Anti-angiogenic effects of Shiraiachrome A, a compound isolated from a Chinese folk medicine used to treat rheumatoid arthritis.

机译：Shiraiachrome A（一种从中药中分离出来的化合物，用于治疗类风湿关节炎）的抗血管生成作用。

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摘要

The Chinese folk medicine Shiraia bambusicola has long been utilized in the treatment of rheumatoid arthritis, a disease in which angiogenesis plays an important role. We report here the isolation of the compound Shiraiachrome A from S. bambusicola and the demonstration of its anti-angiogenic properties. We found that Shiraiachrome A significantly inhibited the proliferation, migration, and tube formation of human microvascular endothelial cells (HMEC) in a dose-dependent manner, with average IC(50) values of 2.1+/-0.36, 1.97+/-0.44, and 1.65+/-0.59 microM, respectively. In addition, Shiraiachrome A inhibited the formation of new microvessels in a rat aorta culture model as well as in the chick embryo chorioallantoic membrane (CAM) assay. Investigation of the mechanism of action of Shiraiachrome A demonstrated that this compound suppressed the autophosphorylation of four receptor tyrosine kinases (RTKs), with IC(50) values ranging from 2.2 to 4.3 microM. These results suggest that Shiraiachrome A inhibits angiogenesis by blocking growth factor-stimulated autophosphorylation of RTKs. These findings also indicate that Shiraiachrome A may be a potent therapeutic agent for angiogenesis-related diseases such as cancer, rheumatoid arthritis, and diabetic retinopathy.
机译：长期以来，中药白粉菌在风湿性关节炎的治疗中得到了应用，该疾病在血管生成中起着重要的作用。我们在这里报告了从S. bambusicola中分离出化合物Shiraiachrome A的方法及其抗血管生成特性的证明。我们发现Shiraiachrome A以剂量依赖性方式显着抑制人微血管内皮细胞（HMEC）的增殖，迁移和管形成，其平均IC（50）值为2.1 +/- 0.36、1.97 +/- 0.44，和1.65 +/- 0.59 microM。此外，在大鼠主动脉培养模型以及鸡胚绒膜尿囊膜（CAM）分析中，Shiraiachrome A抑制了新的微血管的形成。 Shiraiachrome A的作用机理研究表明，该化合物抑制了四个受体酪氨酸激酶（RTK）的自磷酸化，IC（50）值范围为2.2至4.3 microM。这些结果表明，Shiraiachrome A通过阻断生长因子刺激的RTKs自磷酸化来抑制血管生成。这些发现还表明，Shiraiachrome A可能是血管生成相关疾病（如癌症，类风湿性关节炎和糖尿病性视网膜病）的有效治疗剂。

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