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Glycobiology Advance Access published online on November 10, 2005
Glycobiology, doi:10.1093/glycob/cwj056
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© The Author 2005. Published by Oxford University Press. All rights reserved. For permissions, please e-mail: journals.permissions@oxfordjournals.org.
Received August 25, 2005
Revised October 30, 2005
Accepted November 6, 2005

Article

Synthetic lactulose amines: Novel class of anticancer agents that induce tumorcell apoptosis and inhibit galectin-mediated homotypic cell aggregation and endothelial cell morphogenesis

Gabriel A. Rabinovich 1*, Albana Cumashi 2, Germán A. Bianco 1, Domenico Ciavardelli 2, Ida Iurisci 2, Maurizia D'Egidio 2, Enza Piccolo 2, Nicola Tinari 2, Nikolay Nifantiev 3, and Stefano Iacobelli 2

1 Division of Immunogenetics. Hospital de Clínicas "José de San Martín", Faculty of Medicine, University of Buenos Aires, Buenos Aires, Argentina
2 Department of Oncology & Neurosciences, University G. D'Annunzio, Medical School & Foundation, 66013 Chieti, Italy
3 Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow 119991, Russia

* To whom correspondence should be addressed.
Gabriel A. Rabinovich, E-mail: gabyrabi{at}ciudad.com.ar


  Abstract

Galectins, a family of structurally-related carbohydrate-binding proteins, contribute to different events associated with cancer biology, including apoptosis, homotypic cell aggregation, angiogenesis and tumor-immune escape. To interfere with galectin-carbohydrate interactions during tumor progression, a current challenge is the design of specific galectin inhibitors for therapeutic purposes. Here we report the synthesis of three novel low molecular weight lactulose amines (SLA): a) N-lactulose-octamethylenediamine (LDO), b) N,N'-dilactulose-octamethylenediamine (D-LDO) and c) N,N'-dilactulose-dodecamethylenediamine (D-LDD). These compounds showed a differential ability to inhibit binding of galectin-1 and/or galectin-3 to the highly glycosylated protein 90K in solid-phase assays. In addition, each compound demonstrated selective regulatory effects in different events linked to tumor progression including tumor cell apoptosis, homotypic cell aggregation and endothelial cell morphogenesis. Our results suggest that galectin inhibitors with subtle differences in their carbohydrate structures may be potentially used to specifically block different steps of tumor growth and metastasis.

Keywords: apoptosis/galectin inhibitors/tumor escape/tumor progression.
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