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Updated: Jul 14, 2026
Metabolic Glycoengineering of Sialic Acid Using N-acyl-modified Mannosamines
Published on: November 25, 2017
Inhibition of endothelial cell proliferation by per-O-acetylated mannose conjugates
Violeta Zaric1, Dearbhla Doyle, Paul V Murphy
1UCD School of Biomolecular and Biomedical Science, Conway Institute and University College Dublin, Belfield, Dublin 4, Ireland.
Background:
The inhibition of angiogenesis, defined as the process of new blood vessel formation, represents a promising strategy for treating cancer.
Materials And Methods:
The inhibitory properties of two N-(per-O-acetylated-beta-D- mannopyranosyl)thiophene-2-carboxamides derivatives (AMTCs, [1],[2]), N-(2,3,4,6-tetra-O-ethoxycarbonyl-beta-D-mannopyranosyl)- thiophene-2-carboxamide [3] and of 2,3,4,6-tetra-O-acetyl-beta-D-mannopyranosyl-acetamide [4] on the growth of bovine aortic endothelial cells (BAECs) induced by basic fibroblast growth factor (bFGF) were assessed using a [3H]thymidine incorporation assay. The cellular uptake of AMTCs and the non-acetylated homologue (MTC) into BAEC were compared using mass spectrometry analysis of cell lysates.
Results:
AMTCs [1],[2]), at 80 microM, reversed the increase of [3H]thymidine incorporation induced by bFGF, suggesting that these compounds inhibited bFGF-induced proliferative response in BAECs. The acetamide [4] was inactive showing the importance of the thiophene carboxamide for biological activity. The results of a study of AMTC uptake into BAEC suggest that AMTC is rapidly converted to its non-acetylated counterpart.
Conclusion:
The promising results obtained with AMTCs as inhibitors of BAEC growth could lead to the development of novel angiogenesis inhibitors.
