Sogo Takayuki, Kumamoto Takuma, Ishida Hisako, Hisanaga Ayami, Sakao Kozue, Terahara Norihiko, Wada Koji, Hou De-Xing
The United Graduate School of Agricultural Science, Kagoshima University, Kagoshima, Japan.
Faculty of Agriculture, Kagoshima University, Kagoshima, Japan.
Planta Med. 2015 Jan;81(1):26-31. doi: 10.1055/s-0034-1383311. Epub 2014 Dec 3.
Although anthocyanins are major forms distributed in many plant foods and promising as chemopreventive source, many molecular data are obtained from anthocyanidins, showing their low bioavailability. This study aims to clarify the inhibitory effects of delphinidin glycosides on cell transformation comparing them to those of delphinidin. Screening data revealed that delphinidin 3-sambubioside could directly bind to MAPK/ERK kinase 1. Affinity assay data confirmed that delphinidin 3-sambubioside had higher binding affinity to MAPK/ERK kinase 1 than ERK1/2 and B-Raf. Colony assay data further demonstrated that delphinidin 3-sambubioside inhibited 12-O- tetradecanoylphorbol-13-acetate-induced phosphorylation of MAPK/ERK kinase 1 and sequentially suppressed cell transformation. All of these effects caused by delphinidin 3-sambubioside were weaker than those by its aglycon, delphinidin. Our data suggested that the weaker anti- transformation activity of delphinidin glycosides compared to that of their aglycon is due to lower binding affinity to the target molecule MAPK/ERK kinase 1.
尽管花青素是分布于多种植物性食物中的主要形式，且有望成为化学预防的来源，但许多分子数据是从花色苷中获得的，显示出它们较低的生物利用度。本研究旨在比较飞燕草素糖苷和飞燕草素对细胞转化的抑制作用。筛选数据显示，飞燕草素3-接骨木二糖苷可直接与丝裂原活化蛋白激酶/细胞外信号调节激酶1（MAPK/ERK激酶1）结合。亲和分析数据证实，飞燕草素3-接骨木二糖苷对MAPK/ERK激酶1的结合亲和力高于对ERK1/2和B-Raf的亲和力。集落分析数据进一步表明，飞燕草素3-接骨木二糖苷可抑制12-O-十四烷酰佛波醇-13-乙酸酯诱导的MAPK/ERK激酶1磷酸化，并依次抑制细胞转化。飞燕草素3-接骨木二糖苷引起的所有这些效应均弱于其糖苷配基飞燕草素引起的效应。我们的数据表明，与糖苷配基相比，飞燕草素糖苷的抗转化活性较弱是由于其对靶分子MAPK/ERK激酶1的结合亲和力较低。
