73
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: not found

      Cytotoxicity, cytoprotection and neurotoxicity of novel deprenyl-related propargylamines, stable nitroxide free radicals, in vitro and in vivo.

      Read this article at

      ScienceOpenPubMed
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          Since novel synthesized deprenyl-related derivatives of nitroxides, named "JSAKs", have been shown to possess antioxidative properties, their cytotoxicity on neuronal-like PC-12 cells line was examined. The antiproliferative effect of two selected JSAKs was examined and expressed as IC10, IC50 and IC90, and compared with those of the parent nitroxide (Nx-640), model nitroxide TEMPO and deprenyl. There were substantial differences in the dose-dependence of all the observed antiproliferative and cytotoxic effects. Compared to anticancer drugs and apoptosis inducers with topoisomerase inhibitor properties (etoposide and camptothecin), novel compounds displayed cytotoxicity at considerably higher concentrations. The dose-dependent anti-apoptotic potency of JSAKs and Nx-640 was also investigated and compared to TEMPO and deprenyl effects. The observed structure-dependent correlation was very encouraging and prompted us to screen and to compare the in vivo time-dependent effects of JSAKs, Nx-640 and deprenyl administration on the rat intact nigrostriatal neurocytes. TH-immunochemistry was applied as the test method and marker for the changes in the state of the rat catecholaminergic system, also giving evidence that low-toxic and cell-permeable JSAKs can cross the blood-brain barrier, which is the mandatory prerequisite for the therapeutic application of antioxidants and drugs to the brain. Taken together, it can be concluded with great certainty that novel deprenyl-related JSAKs might be especially good candidates for further anticancer investigations in vitro and in vivo and future pharmacological applications.

          Related collections

          Author and article information

          Journal
          In Vivo
          In vivo (Athens, Greece)
          0258-851X
          0258-851X
          April 29 2004
          : 18
          : 2
          Affiliations
          [1 ] Department of Molecular Biophysics, University of Lodz, Poland.
          Article
          15113044
          e554ae64-da8b-49fa-bda0-9aef232e40db
          History

          Comments

          Comment on this article