Influence of the spacer on the inhibitory effect of different polycarbophil-protease inhibitor conjugates

Within the present study various polycarbophil (PCP)-serine protease inhibitor conjugates were synthesized and the influence of different spacers on their inhibitory efficacy was evaluated in vitro. Results demonstrated that 4.2+/-0.15 units (n=3; +/-SD) of alpha-chymotrypsin were inhibited by 50% u...

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Veröffentlicht in:	European journal of pharmaceutics and biopharmaceutics 2001-09, Vol.52 (2), p.137-144
Hauptverfasser:	MARSCHÜTZ, Michaela K, VERONESE, Francesco M, BERNKOP-SCHNÜRCH, Andreas
Format:	Artikel
Sprache:	eng
Schlagworte:	Acrylic Resins - chemistry Adhesives - chemistry Biological and medical sciences Cathartics - chemistry Chemistry, Pharmaceutical Drug Delivery Systems General pharmacology Medical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Protease Inhibitors - chemistry
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Zusammenfassung:	Within the present study various polycarbophil (PCP)-serine protease inhibitor conjugates were synthesized and the influence of different spacers on their inhibitory efficacy was evaluated in vitro. Results demonstrated that 4.2+/-0.15 units (n=3; +/-SD) of alpha-chymotrypsin were inhibited by 50% utilizing 0.86% (w/v) of a PCP-tetramethylenediamine (TMDA)-chymostatin 20:1 conjugate. In contrast, only 0.6+/-0.05 units (n=3; +/-SD) of alpha-chymotrypsin were inhibited by a corresponding PCP-poly(ethylene glycol) (PEG)-chymostatin conjugate. Inhibitory effects of PCP-TMDA-antipain and -elastatinal conjugates towards trypsin and elastase, respectively, were also significantly higher (P
ISSN:	0939-6411 1873-3441
DOI:	10.1016/S0939-6411(01)00175-8