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益智仁中二苯基庚烷类化合物的血管生成抑制活性

Inhibitory effect of diarylheptanoids from Alpinia oxyphylla on angiogenesis

  • 摘要: 探讨益智仁中两个已知二苯基庚烷类化合物Yakuchinone A和Yakuchinone B以及结构类似物姜黄素(curcumin)的血管生成抑制活性。采用了转基因荧光斑马鱼为体内实验动物模型,人脐静脉内皮细胞(HUVEC)为体外实验模型,评价了上述3个化合物的活性及毒性。以血管生成抑制指数(AI)代表化合物的活性与毒性之比。结果表明,无论是体外实验还是体内实验,姜黄素的血管生成抑制作用最强而毒性最低,Yakuchinone A次之,Yakuchinone B抑制活性最低而毒性最强。因此,姜黄素为三者中最佳的血管生成抑制剂。

     

    Abstract: This study investigated the anti-angiogenic activities of two diarylheptanoids, together with a structure analogue, curcumin. The activity and toxicity of these three compounds were compared using transgenic zebrafish as in vivo model and human umbilical vein endothelial cell(HUVEC)as in vitro model. Anti-angiogenic index(AI)was used as the ratio between LC50 and EC50. The results suggested that in both in vitro and in vivo assay, curcumin exerted the most potent anti-angiogenic effect but with lowest toxicity among these compounds; Yakuchinone A was the second potent; Yakuchinone B has the lowest activity but with the highest toxicity in all three compounds. Taken together, curcumin was the best angiogenic inhibitor in these three diarylheptanoids.

     

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