title: Evaluating the cytotoxic effects of novel quinone compounds.
abstract: OBJECTIVE
  Quinone-containing compounds can induce cell death in cancer cells and are, therefore, promising lead compounds for the development of novel anti-cancer drugs.
  
  
  METHODS
  In the present study, we evaluated the cytotoxic effects of fifteen novel synthetic quinone-containing compounds in cell cultures in an attempt to establish structure/activity relationships for these compounds. The compounds were clustered into four groups (1, 2, 3, 4) based on common structural features. In vitro cell cultures were treated for 24 h with the compounds, after which cell viability was assessed by flow cytometry. The APOPercentage™ assay, the Terminal deoxynucleotidyl transferase mediated dUTP Nick End Labeling (TUNEL) assay and the caspase-3 assay was used to investigate the activation of apoptosis in the cells.
  
  
  RESULTS
  Compounds from groups 2 and 4 were highly toxic to the cells. The compounds induced apoptosis in some human cancer cell cultures and exhibited low toxicity towards the non-cancerous cell line, KMST-6. The induction of apoptosis in CHO cells was associated with the activation of caspase-3 cleavage, DNA fragmentation and the reactive oxygen species (ROS) generation.
  
  
  CONCLUSIONS
  The present study demonstrates that five of the quinone-containing compounds induced apoptosis in human cancer cells and are therefore promising lead compounds for the development of novel anticancer drugs.
authors: Department of Biotechnology, University of the Western Cape, Bellville, South Africa.
authors: Morounke
authors: M
authors: Saibu
authors: Department of Chemistry, University of the Western Cape, Bellville, South Africa.
authors: Sunil
authors: S
authors: Sagar
authors: Department of Chemistry, University of the Western Cape, Bellville, South Africa.
authors: Ivan
authors: I
authors: Green
authors: Department of Chemistry, University of the Western Cape, Bellville, South Africa.
authors: Farouk
authors: F
authors: Ameer
authors: Department of Biotechnology, University of the Western Cape, Bellville, South Africa memeyer@uwc.ac.za.
authors: Mervin
authors: M
authors: Meyer
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D016466:CHO Cells; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D003412:Cricetulus; D053938:DNA Fragmentation; D006801:Humans; D011809:Quinones / Q000494:pharmacology*; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D011809:Quinones; D017382:Reactive Oxygen Species; D053148:Caspase 3
keywords: Cancer; apoptosis; quinone; structure/activity relationships