Anti-heparanase activity of ultra-low-molecular-weight heparin produced by physicochemical depolymerization

Non-Anticoagulant Heparins as Heparanase Inhibitors

“…The increase of heparanase inhibitory activity produced by glycol splitting of UFH, LMWH and ultra LMWH [76,87] was confirmed by assessing the effect of the heparin-related synthetic trisaccharide 4-OMeGlcNS6S-GlcA-α1,6 anhydro GlcNS. Strikingly, its gs derivative showed an increase of one order of magnitude in inhibiting the enzyme (IC 50 = 30 μg/ml versus IC 50 = 2 μg/ml for the gs derivative).…”

“…Preclinical in vivo evaluation in tumor xenografts models evidenced that tinzaparin was able to sensitize cis-platin resistant ovarian cancer [75]. A non-anticoagulant ultra LMWH (2.5 kDa), obtained by hydrogen peroxide catalyzed radical heparin hydrolysis assisted by ultrasonic waves, exhibited antiheparanase activity intermediate compared with those of tinzaparin (Mw 7 kDa), dalteparin (6.3 kDa) and enoxaparin (5.5 kDa) [76]. A glycopolymer constituted by a N-sulfated poly2-aminoethyl methacrylate carrying the heparin disaccharide ΔU2S-GlcNS,6S, was reported to inhibit heparanase, B16 melanoma cell migration, and adhesion to platelets and microvascular endothelial cells [77].…”

Assessment of Heparanase-Mediated Angiogenesis Using Microvascular Endothelial Cells: Identification of λ-Carrageenan Derivative as a Potent Anti Angiogenic Agent

“…The three polysaccharides studied here were submitted to depolymerization (RD) using a previously described method which associates radicals (from hydrogen peroxide) and ultrasonic waves [36]. After depolymerization, the compounds were submitted to glycol splitting (GS) [18] (Sodium periodate oxidation followed by sodium borohydride reduction) and then respectively called RD-GS-Heparin, RD-GS-DextranS and RD-GS-λ-Carrageenan.…”

Heparin length in the coating of extremely small iron oxide nanoparticles regulates in vivo theranostic applications

“…A calibration curve of heparin oligosaccharide standards (Iduron, Manchester, UK) ranging from 8 to 32 DP (degree of polymerisation) of the monomer unit (300 Da) was used. It allowed calculating the number average molecular weight (M n ), M w , polydispersity index (I) and DP according to a previously published method 48 and using the following equations:…”