Immobilization of Thrombin Inhibitors on Polyesters Surface: An Original Approach towards Materials Blood Compatibilization


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Piperazinyl-amide derivatives of N--(3-trifluoromethyl-benzenesulfonyl)-L-arginine were synthesized as graftable thrombin inhibitors. Their biological activity was evaluated in vitro, against human -thrombin, and in blood coagulation assay. The piperazinyl-amide derivatives were found to inhibit the activity of -thrombin in the micromolar range. The designed molecules were fixed on poly(ethylene terephthalate) (PET), and poly(butylene terephthalate) (PBT) by wet chemistry treatment (activation of hydroxyl chain-ends) and photochemistry (nitrene insertion by photoactivation of aromatic azide). The protocols were validated by X-ray photoelectron spectroscopy (XPS) and by radiochemical assay (liquid scintillation counting, LSC).



Materials Science Forum (Volumes 514-516)

Edited by:

Paula Maria Vilarinho




C. Salvagnini and J. Marchand-Brynaert, "Immobilization of Thrombin Inhibitors on Polyesters Surface: An Original Approach towards Materials Blood Compatibilization", Materials Science Forum, Vols. 514-516, pp. 961-965, 2006

Online since:

May 2006




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[13] Membranes activation by wet chemistry: PET (Whatman, track-etched, membrane, thickness 12 µm, density 1. 39 g/cm3, pores diameter 0. 49 µm, pore distribution 1. 45x10 6 pores/cm2) and PBT (John Manville, meltblown membrane, 0. 133 mm thickness, mean flow pore of 5 µm) membranes were cut in disks (13 mm of diameter) and immersed, by groups of 10 samples, into a solution of TsCl (5 g), pyridine (0. 8 g), acetone (50 mL) for 1 h at 20°C (PBT) or 60°C (PET). The samples were washed with acetone (50 mL, 5min), water (50 mL, 5 min) and dried over filter paper.


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[17] Grafting target molecules on polyesters membranes: activated and blank samples were individually incubated for 2 h at 20°C with 1 mL of a 10 -3 M solution of target compound in a phosphate buffer (PBS)-CH3CN mixture (1: 1); the samples were washed successively with PBSCH3CN (1: 1) (1 mL, 2 x 10 min), water (1 mL, 2 x 5 min), 5. 10 -3 M HCl (1 mL, 2 x 5 min) and water (1 mL, 2 x 10 min). Finally the samples were drained over filter paper and directly analysed by LSC or XPS.


[18] Salvagnini, C ; Marchand-Brynaert, J unpublished results.

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