Synthesis and Anti-Angiogenic Effect of Conjugates Between Serum Albumin and Non-Steroidal Anti-Inflammatory Drugs

Author(s): B. Kjær, C. Struve, T. Friis, A.-M. Engel, N. H. Beyer, P. Hojrup, G. Houen

Journal Name: Protein & Peptide Letters

Volume 17 , Issue 1 , 2010

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Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit tumor growth and angiogenesis. Covalent linkage of naproxen to human serum albumin (HSA) has been shown to target it efficiently to the liver and this may potentially be exploited for liver-selective inhibition of angiogenesis. With the aim of investigating the anti-angiogenic efficiency of NSAID-HSA conjugates in vitro, three NSAIDs, aspirin, ibuprofen, and naproxen were conjugated to HSA using different concentrations of their N-hydroxysuccinimide esters. Conjugation ratios from 10 to 50 were achieved and the conjugates retained a growth inhibitory effect on endothelial cells at or above the level of the non-conjugated NSAIDs in an in vitro angiogenesis assay.

Keywords: Angiogenesis, HUVEC, NSAID, HSA, conjugation

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Article Details

Year: 2010
Page: [121 - 130]
Pages: 10
DOI: 10.2174/092986610789909511

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