PMID- 25075032 OWN - NLM STAT- MEDLINE DCOM- 20141111 LR - 20140730 IS - 1791-7530 (Electronic) IS - 0250-7005 (Linking) VI - 34 IP - 8 DP - 2014 Aug TI - Evaluating the cytotoxic effects of novel quinone compounds. PG - 4077-86 AB - BACKGROUND/AIM: Quinone-containing compounds can induce cell death in cancer cells and are, therefore, promising lead compounds for the development of novel anti-cancer drugs. MATERIALS AND 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. CONCLUSION: 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. CI - Copyright(c) 2014 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved. FAU - Saibu, Morounke AU - Saibu M AD - Department of Biotechnology, University of the Western Cape, Bellville, South Africa. FAU - Sagar, Sunil AU - Sagar S AD - Department of Chemistry, University of the Western Cape, Bellville, South Africa. FAU - Green, Ivan AU - Green I AD - Department of Chemistry, University of the Western Cape, Bellville, South Africa. FAU - Ameer, Farouk AU - Ameer F AD - Department of Chemistry, University of the Western Cape, Bellville, South Africa. FAU - Meyer, Mervin AU - Meyer M AD - Department of Biotechnology, University of the Western Cape, Bellville, South Africa memeyer@uwc.ac.za. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Greece TA - Anticancer Res JT - Anticancer research JID - 8102988 RN - 0 (Antineoplastic Agents) RN - 0 (Quinones) RN - 0 (Reactive Oxygen Species) RN - EC 3.4.22.- (Caspase 3) SB - IM MH - Animals MH - Antineoplastic Agents/*pharmacology MH - Apoptosis/drug effects MH - CHO Cells MH - Caspase 3/metabolism MH - Cell Line, Tumor MH - Cricetulus MH - DNA Fragmentation MH - Humans MH - Quinones/*pharmacology MH - Reactive Oxygen Species/metabolism OTO - NOTNLM OT - Cancer OT - apoptosis OT - quinone OT - structure/activity relationships EDAT- 2014/07/31 06:00 MHDA- 2014/11/12 06:00 CRDT- 2014/07/31 06:00 PHST- 2014/07/31 06:00 [entrez] PHST- 2014/07/31 06:00 [pubmed] PHST- 2014/11/12 06:00 [medline] AID - 34/8/4077 [pii] PST - ppublish SO - Anticancer Res. 2014 Aug;34(8):4077-86.