Inhibition of angiogenesis by chitooligosaccharides with specific degrees of acetylation and polymerization

Chitooligosaccharides (CHOS) inhibit angiogenesis and may be used in the treatment of cancer tumors. We have studied the effect of the fraction of acetylation (FA) and the degree of polymerization (DP) on CHOS anti-angiogenic activity. We tested enzymatically produced CHOS-mixtures with FA0.15, FA0.3 and FA0.6, and DP ≤ 12 in initial experiments with chorioallantoic membranes. All of the samples reduced the formation of new blood vessels, CHOS with FA0.3 giving the best effect. Single-DP fractions from the FA0.3 sample purified by size-exclusion chromatography (DP3-DP12) were then tested for inhibition of migration of human endothelial cells, which is an important element of the angiogenesis process. All of the fractions inhibited migration, meaning that, within the DP area tested in this study, FA is more important than DP for the effect. Generally, the results reveal that DP3–DP12 CHOS have considerable potential as anti-angiogenic compounds.