Emodin,　a　natural　anthraquinone　derivative　isolated　from　Rheum　palmatum　L,　has　been　demonstrated　to　exhibit　good　anti-cancer　effect.　In　this　study,　a　series　of　novel　quaternary　ammonium　salts　of　emodin,　anthraquinone　and　anthrone　were　synthesized　and　their　anticancer　activities　were　tested　in　vitro.　The　effects　of　emodin　quaternary　ammonium　salts　on　cell　viability,　apoptosis,　intracellular　ROS,　and　mitochondrial　membrane　potential　were　investigated　in　A375,　BGC-823,　HepG2　and　HELF　cells.　The　results　demonstrated　that　compound　4a　induced　morphological　changes　and　decreased　cell　viability.　Apoptosis　triggered　by　compound　4a　was　visualized　using　DAPI　staining　and　Annexin　V-FITC/PI　staining.　Compound　4a-induced　apoptosis　of　A375　cells　were　showed　to　be　associated　with　the　dissipation　of　mitochondrial　membrane　potential　(Delta　Psi　m)　as　a　result　of　the　up-regulation　of　P53　and　Caspase-3.　When　cancer　cells　were　treated　with　emodin　derivative,　their　ability　to　generate　reactive　oxygen　species　(ROS)　rose　significantly　and　the　mitochondrial　membrane　potential　decreased.　Additionally,　confocal　microscopy　assay　confirmed　that　compound　4a　was　primarily　located　in　the　mitochondria　of　A375　cells.　These　results　suggested　that　compound　4a　has　the　potential　for　use　in　cancer　therapy.　(C)　2016　Elsevier　Masson　SAS.　All　rights　reserved.