G Xu1, Q Liang, Z Gong, W Yu, S He, L Xi. 1. Center for New Drug Research & Development, College of Life Science, Nanjing Normal University, Nanjing, China. biopharmacology@126.com
Abstract
AIM: To evaluate antitumor activity of sesquiterpene lactones (scabertopin (ES-2), isoscabertopin (ES-3), deoxyelephantopin (ES-4), isodeoxyelephantopin (ES-5)) isolated from Elephantopus scaber L. in vitro and in vivo. METHODS: SMMC-7721, Caco-2 and HeLa cell lines were treated with ES-2,3,4,5. Cell viability was determined by MTT assay. Agarose gel electrophoresis was used to detect DNA fragmentation. To evaluate in vivo antitumor activity of ES-4, experimental murine tumor model was used. RESULTS: It was shown that ES-2, ES-4, ES-5 exhibited significant antitumor effect in vitro in a concentration-dependent manner. However, the effect of ES-3 on the growth of tested cell lines was relatively weak. In HeLa cells exposed to ES-4 for 48 h, morphological changes and DNA ladder pattern evidencing on apoptosis were detected. ES-4 revealed in vivo antitumor activity. CONCLUSION: Antitumor activity of studied sesquiterpene lactones may be due, at least in part, to induction of apoptosis in vitro. ES-4 possesses also antitumor activity in vivo.
AIM: To evaluate antitumor activity of sesquiterpene lactones (scabertopin (ES-2), isoscabertopin (ES-3), deoxyelephantopin (ES-4), isodeoxyelephantopin (ES-5)) isolated from Elephantopus scaber L. in vitro and in vivo. METHODS:SMMC-7721, Caco-2 and HeLa cell lines were treated with ES-2,3,4,5. Cell viability was determined by MTT assay. Agarose gel electrophoresis was used to detect DNA fragmentation. To evaluate in vivo antitumor activity of ES-4, experimental murinetumor model was used. RESULTS: It was shown that ES-2, ES-4, ES-5 exhibited significant antitumor effect in vitro in a concentration-dependent manner. However, the effect of ES-3 on the growth of tested cell lines was relatively weak. In HeLa cells exposed to ES-4 for 48 h, morphological changes and DNA ladder pattern evidencing on apoptosis were detected. ES-4 revealed in vivo antitumor activity. CONCLUSION: Antitumor activity of studied sesquiterpene lactones may be due, at least in part, to induction of apoptosis in vitro. ES-4 possesses also antitumor activity in vivo.
Authors: Lisa A Stott; Cheryl A Brighton; Jason Brown; Richard Mould; Kirstie A Bennett; Robert Newman; Heather Currinn; Flavia Autore; Alicia P Higueruelo; Benjamin G Tehan; Cliona MacSweeney; Michael A O'Brien; Steve P Watson Journal: Heliyon Date: 2021-06-01