Cytotoxic sesquiterpenoids from the ethanol extract of fruits of Celastrus orbiculatus

Aim of the study: To investigate the cytotoxic compounds against human melanoma A375-S2 and human cervical carcinoma Hela cell lines from the fruits of Celastrus orbiculatus. Materials and methods: The ethanol extract of the fruits of C. orbiculatus was found to exhibit significant cytotoxic activity. After partition, the column chromatography and Semi-preparative HPLC were used for activity guided fractionation from the active petroleum ether-soluble part. NMR and ESI-MS spectra for structure analysis were recorded on spectrometers, respectively. The cytotoxic activities of the isolated compounds were determined using the MTT assay. Results: Four sesquiterpenoids (1-4) were isolated by activity guided fractionation from the ethanol extract of the fruits of C. orbiculatus. Compounds 1-3 exhibited promising cytotoxicities against the Hela cells and A375-S2 cells. The cytotoxic activities of compounds 1-3 seemed to be dose-dependent, which exhibited more potent inhibition for the proliferation of two cell lines when increased the concentrations of every compounds. Among these compounds, compound 2 showed most cytotoxicities against either Hela cells or the A375-S2 cells. Conclusions: The cytotoxic activity of the ethanol extract of fruits of C. orbiculatus against human melanoma A375-S2 and human cervical carcinoma Hela cells due to its content of sesquiterpenoids, supports its potential therapeutic value for the treatment of tumor. (C) 2008 Elsevier Ireland Ltd. All rights reserved.