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@ARTICLE{DellAlbani:120569,
      author       = {P. Dell'Albani and B. Di Marco$^*$ and S. Grasso and C.
                      Rocco and M. C. Foti},
      title        = {{Q}uercetin derivatives as potent inducers of selective
                      cytotoxicity in glioma cells.},
      journal      = {European journal of pharmaceutical sciences},
      volume       = {101},
      issn         = {0928-0987},
      address      = {New York, NY [u.a.]},
      publisher    = {Elsevier},
      reportid     = {DKFZ-2017-00998},
      pages        = {56 - 65},
      year         = {2017},
      abstract     = {Quercetin (Q) is a flavonoid widely distributed in the
                      plant kingdom and well-known for its ability to exert
                      antioxidant, prooxidant and anticarcinogenic activities in
                      several tumor cells. Furthermore, quercetin plays an
                      important role both in the regulation of key elements in
                      cellular signal transduction pathways related to apoptotic
                      cell death, and in cell cycle progression. Several studies
                      have reported of toxic effects of Q against glioma cell
                      lines. In this study, the effects of Q and of some
                      Q-derivatives (acyl esters and bromo-derivatives) on U373-MG
                      and 9L glioma cell lines survival are analyzed. The 24-hour
                      treatment of glioma cells with several concentrations of Q
                      (25, 50 and 100μM) did not cause any cytotoxic effects,
                      while the administration of Q-derivatives, such as acylated
                      and brominated quercetin, caused a sharp increase in cell
                      death. Among all tested derivatives, 3-O-decanoylquercetin
                      10 manifested the strongest cytotoxic effect at a
                      concentration as low as 25μM both in U373-MG (ca. $40\%$
                      viability after 24h) and in 9L cells (ca. $20\%$ viability
                      after 24h). The cytotoxic effects of the Q-derivatives 3 and
                      10-13 were proven to be satisfactorily selective for glioma
                      cells. When Q-derivatives were in fact administered to mouse
                      primary astroglial or human fibroblast cell cultures, a
                      higher cell survival rate $(~90-70\%$ and $55-45\%,$
                      respectively) was observed relative to that detected in
                      glioma cells. These results prove that selective
                      esterification and bromination of Q increase to a great
                      extent the toxicity of this polyphenol against glioma cells,
                      thereby providing a possible new tool for cyto-specific
                      glioma therapy.},
      cin          = {A231},
      ddc          = {610},
      cid          = {I:(DE-He78)A231-20160331},
      pnm          = {311 - Signalling pathways, cell and tumor biology
                      (POF3-311)},
      pid          = {G:(DE-HGF)POF3-311},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:28153636},
      doi          = {10.1016/j.ejps.2017.01.036},
      url          = {https://inrepo02.dkfz.de/record/120569},
}