Cyclopeptide RAs,belonging to Rubiaceae-type cyclopeptides isolated from plants,are homodicyclohexapeptides formed with one-D-alanine,one N-methyl-L-alanine,three modified N-methyl-L-tyrosines and one other protein-L-amino acid [1].For RAs unique structure,potential anti-tumor in vitro and in vivo,unclear mechanism and cancer clinic use in Chinese herbs,more efforts have been done in the lab during past years.Herein we report RAs isolation from 8 Rubia medicinal plants,synthesis and QSAR,anti-tumor activity in vitro and in vivo,mechanisms involving into autophagy,apoptosis,anti-angiogenesis,NF-kB pathway,Hedgehog pathway,Hippo pathway,and gene chip.Now RAs have been listed and patented as one candidate for new drug R & D [2-3].