Bailey, M.A., Ingram, Matthew and Naughton, D.P. (2004) A novel anti-oxidant and anti-cancer strategy: a peptoid anti-inflammatory drug conjugate with SOD mimic activity Biochemical and Biophysical Research Communications, 317 (4). pp. 1155-1158. ISSN 0006-291XFull text not available from this repository.
Activation of reactive oxygen and nitrogen species (RONS) by redox-active metal ions has been proposed to contribute to oxidative damage in inflamed tissues. Here, we report a dual-function anti-oxidant conjugate comprising an anti-inflammatory agent (5-aminosalicylic acid) and a chelator with potential as a superoxide dismutase mimic. The conjugate ethylenediaminetetraacetic acid bis-(5-aminosalicylic acid methyl ester) [EBAME] chelates Cu(II) ions in a 1:1 ratio, as assessed spectrophotometrically using Job’s method. Superoxide dismutase (SOD) activity was determined for the Mn(II)-conjugate as 0.758 ± 0.130 U at a concentration of 0.99 μM. In inflamed tissues, peptidase mediated release of active 5-ASA would also release the EDTA chelator which has significant SOD mimic activity when complexed to Cu(II) ions. Thus, EBAME has potential as a dual-function anti-inflammatory agent with reduced gastric irritability.
|Item Type:||Journal article|
|Uncontrolled Keywords:||Superoxide dismutase mimic; 5-Aminosalicylic acid; Ethylenediaminetetraacetic acid; Metal ions; Inflammation|
|Subjects:||C000 Biological and Biomedical Sciences > C700 Molecular Biology, Biophysics and Biochemistry|
|DOI (a stable link to the resource):||10.1016/j.bbrc.2004.03.162|
|Faculties:||Faculty of Science and Engineering > School of Pharmacy and Biomolecular Sciences > Biomedical Materials|
|Depositing User:||editor spbs|
|Date Deposited:||08 Nov 2007|
|Last Modified:||24 Mar 2015 15:09|
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