A lactosylated steroid contributes in vivo therapeutic benefits in experimental models of mouse lymphoma and human glioblastoma

Journal of Medicinal Chemistry
Laurent IngrassiaRobert Kiss

Abstract

Various mono- and disaccharides were grafted onto a steroid backbone. Whereas in vitro these glycosylated steroids had no cytotoxic effects on six different human cancer cell lines, several of the glycosylated steroids under study did significantly modify the levels of in vitro migration of the human U373 glioblastoma, the A549 non-small-cell-lung cancer (NSCLC), and the PC-3 prostate cancer cells, with more pronounced effects in the case of a monosubstituted beta-L-fucopyranosyl-steroid (19), a monosubstituted beta-D-isomaltosyl-steroid (22), and a monosubstituted beta-D-lactosyl-steroid (24). These three compounds significantly increased the survival of conventional mice grafted subcutaneously with the P388 lymphoma, a lymphoma that metastasizes toward the liver. In vivo, the monosubstituted beta-D-lactosyl-steroid (24) also increased the antitumor effectiveness of cisplatin, a cytotoxic pro-apoptotic drug, in the case of the P388 lymphoma model. This compound also increased the survival of immunodeficient mice into whose brains human U373 glioblastoma cells had been orthotopically grafted.

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Citations

Mar 25, 2011·Journal of Biomolecular NMR·Víctor P García
May 12, 2012·Journal of Medicinal Chemistry·Ruud P M DingsKevin H Mayo
Nov 23, 2007·Natural Product Reports·James R Hanson
Dec 13, 2012·The Journal of Pharmacology and Experimental Therapeutics·Ruud P M DingsKevin H Mayo
Apr 18, 2009·Brain Pathology·Marie Le MercierFlorence Lefranc
Jan 1, 2014·Cell Biology International·Muhammad Fawwaz AbdullahKhairani Idah Mokhtar
Mar 8, 2016·Expert Opinion on Therapeutic Patents·Helen BlanchardXing Yu
Nov 26, 2009·European Journal of Medicinal Chemistry·Sébastien MadonnaJean-Louis Kraus
Feb 23, 2008·Chemistry : a European Journal·Seniz Ozalp-YamanJan Reedijk
Jul 15, 2006·Glycobiology·Isabelle CambyRobert Kiss

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