A lipophilic heparin derivative protects elastin against degradation by leucocyte elastase.
An oleolylated derivative (I) of partially N-desulphated heparin was prepared containing an average number of three oleoyl residues for one molecule of heparin. The inhibitory capacity of I (IC50 = 0.55 microM) for leucocyte elastase resembles that of heparin (IC50 = 0.2 microM). In contrast to heparin, I is also an inhibitor of porcine pancreatic elastase (IC50 = 0.68 microM) and it also has the capacity to protect elastin fibres against the degradation by leucocyte elastase. When insoluble elastin is pretreated with I its degradation by leucocyte elastase is inhibited by almost 90% while pretreatment of elastin with heparin exhibited only a moderate effect on elastolysis (10% inhibition).
Moczar
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Laboratoire de Biologie du Tissue Conjonctif, CNRS, URA 1460, Université Paris XII, Créteil, France.
Hornebeck
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W
D000595:Amino Acid Sequence; D000818:Animals; D004549:Elastin / Q000378:metabolism*; D006493:Heparin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D019272:Leukocyte Elastase; D051379:Mice; D008969:Molecular Sequence Data; D009829:Oleic Acids / Q000494:pharmacology*; D009842:Oligopeptides / Q000494:pharmacology; D010179:Pancreas / Q000201:enzymology; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013552:Swine
D009829:Oleic Acids; D009842:Oligopeptides; C072705:oleoyl heparin; D006493:Heparin; D004549:Elastin; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase