SOUTH AFRICAN JOURNAL OF BOTANY, vol.111, pp.37-43, 2017 (SCI-Expanded)
Malignancies constitute a global health concern and chemotherapy remains the main mode of treatment. The present study was designed to evaluate the cytotoxicity of 8 compounds from Desbordesia glaucescens namely lanosta-7,24-dien-3-one (1), friedelanone (2), friedelanol (3), 3,3'-di-O-methylellagic acid (4), 3,3',4'-tri-0-methylellagic acid (5), ellagic acid (6), 3',4'-di-0-methylellagic acid 4-0-beta-o-glucopyranoside (7) and 3,3'-di-0-methylellagic acid 4'-0-beta-c-xylopyranoside (8) against 4 human carcinoma cell lines and normal CRL2120 fibroblasts. The neutral red uptake (NRU) assay was used for cytotoxicity testing. Caspase-Glo assay, cell cycle analysis, measurements of mitochondrial membrane potential (MMP) and levels of reactive oxygen species (ROS) were used to evaluate apoptosis induction. Compounds 4 and 6 as well as doxorubicin had IC50 values below 45 pM in the four tested cancer cell lines meanwhile other compounds displayed selective activity. The IC50 values ranged from 11.23 mu M (towards breast adenocarcinoma MCF-7 cells) to 44.65 mu M (colon carcinoma Caco-2 cells) for 4, from 14.07 mu M (towards MCF-7 cells) to 77.73 mu M (Caco-2 cells) for 6 and from 0.07 mu M (towards SPC212 cells) to 1.01 mu M (A549 cells) for doxorubicin. Compound 4 induced apoptosis in MCF-7 cells mediated by MMP loss. The constituents of Desbordesia glaucescens and especially ellagic acid (6) and its derivative 4 are potential cytotoxic compounds that deserve more investigations towards developing novel antiproliferative drugs against human carcinoma. (C) 2017 SAAB. Published by Elsevier B.V. All rights reserved.