益智仁中二苯基庚烷类化合物的血管生成抑制活性

Inhibition of diarylheptanoids from Alpinia oxyphylla on angiogenesis

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。

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.