Morounke Saibu1, Sunil Sagar2, Ivan Green2, Farouk Ameer2, Mervin Meyer3. 1. Department of Biotechnology, University of the Western Cape, Bellville, South Africa. 2. Department of Chemistry, University of the Western Cape, Bellville, South Africa. 3. Department of Biotechnology, University of the Western Cape, Bellville, South Africa memeyer@uwc.ac.za.
Abstract
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. Copyright
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 humancancer 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 humancancer cells and are therefore promising lead compounds for the development of novel anticancer drugs. Copyright
Authors: Hung N Mai; Luis Fernando Aranguren Caro; Roberto Cruz-Flores; Brenda Noble White; Arun K Dhar Journal: Front Immunol Date: 2021-05-13 Impact factor: 7.561