In vitro cytotoxicity of compounds isolated from Desbordesia glaucescens against human carcinoma cell lines

Abstract 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- O -methylellagic acid ( 5 ), ellagic acid ( 6 ), 3′,4′-di- O -methylellagic acid 4- O - β - d -glucopyranoside ( 7 ) and 3,3′-di- O -methylellagic acid 4′- O - β - d -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 IC 50 values below 45 μM in the four tested cancer cell lines meanwhile other compounds displayed selective activity. The IC 50 values ranged from 11.23 μM (towards breast adenocarcinoma MCF-7 cells) to 44.65 μM (colon carcinoma Caco-2 cells) for 4 , from 14.07 μM (towards MCF-7 cells) to 77.73 μM (Caco-2 cells) for 6 and from 0.07 μM (towards SPC212 cells) to 1.01 μM (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.