Abstract
Amiloride is a potent inhibitor of a urokinase type plasminogen activator which is involved in the invasive process of cancer cells leading to the initiation of metastasis. Synthesis, characterization and in vitro tests of four macromolecular conjugates of Amiloride are presented. One of them is a degradable derivative, HPMA-Gly-D,l-Phe-Leu-Gly-amiloride. In this case the in vitro release of Amiloride was monitored. Other conjugates are stable containing a new amiloride derivative, 6-aminohexyl amiloride [AHA], coupled to different polymeric carriers: a branched polypeptide, poly-[Lys(AcGlu1.0-D,l-Ala4.5)] [AcEAK], poly-[N-(2-hydroxy propyl) metacrylamide] [HPMA] and poly-[1-vinyl-2-pyrrolidone- co-maleic acid] [NVP MA]. Inhibition of uPA, plasminogen activation and proteinases secreted by cancer cells was measured as well as basement membrane degradation in vitro. Each amiloride AHA and the corresponding conjugates retained their activity in these experiments.
Published Version
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
