6602-90-0Relevant academic research and scientific papers
Synthesis and in vitro evaluation of targeted tetracycline derivatives: Effects on inhibition of matrix metalloproteinases
Vidal, Aurelien,Sabatini, Massimo,Rolland-Valognes, Gaelle,Renard, Pierre,Madelmont, Jean-Claude,Mounetou, Emmanuelle
, p. 2368 - 2374 (2007)
Among other non-antibiotic properties, tetracyclines inhibit matrix metalloproteinases and are currently under study for the treatment of osteoarthritis. Quaternary ammonium conjugates of tetracyclines were synthesized by direct alkylation of the amine function at the 4-position with methyl iodide. When tested in vitro, they inhibited cytokine-induced MMP expression to a lesser extent than parent tetracyclines. This was compensated by an improved inhibition of MMP catalytic activity. Since inhibition of collagen degradation was maintained these derivatives could be potent drug candidates for cartilage-targeted chondroprotective treatment.
TETRACYCLINES AND THEIR USE AS CALPAIN INHIBITORS
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Page/Page column 52, (2010/02/13)
Tetracyclines are useful as calpain inhibitors, particularly inhibitors of calpain I and II, as demonstrated in enzymatic assays as well as at the cellular and animal levels. Tetracyclines may be used in the treatment of a wide range of conditions implicated by or associated with calpain activity or activation, including cellular protection from apoptosis and necrosis, particularly n eu ro protection, prevention of cell motility (e.g. anti-metastasis of cancer) and treatment of certain infectious diseases (e.g. malaria and AIDS). Some tetracyclines are particularly useful as calpain inhibitors since they are also antioxidants, oxidative stress often being associated with conditions where calpain is activated.
