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Glycobiology Advance Access originally published online on November 10, 2005
Glycobiology 2006 16(3):210-220; 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

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

Gabriel A. Rabinovich1,2, Albana Cumashi3, Germán A. Bianco2, Domenico Ciavardelli3, Ida Iurisci3, Maurizia D’Egidio3, Enza Piccolo3, Nicola Tinari3, Nikolay Nifantiev4 and Stefano Iacobelli3

2 Division of Immunogenetics, Hospital de Clínicas "José de San Martín," University of Buenos Aires, Buenos Aires, Argentina; 3 Department of Oncology & Neurosciences, University G. D’Annunzio, Medical School & Foundation, 66013 Chieti, Italy; and 4 Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow 119991, Russia

1 To whom correspondence should be addressed; e-mail:gabyrabi{at}ciudad.com.ar

Received on August 25, 2005; revised on October 30, 2005; accepted on November 6, 2005

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 synthetic lactulose amines (SLA): (1) N-lactulose-octamethylenediamine (LDO), (2) N,N'-dilactulose-octamethylenediamine (D-LDO), and (3) 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.

Key words: apoptosis / galectin inhibitors / tumor escape / tumor progression


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