Abstract
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.
Key words
delphinidin 3-sambubioside - delphinidin - MEK1 - cell transformation
