Cytotoxic sesquiterpenoids from the ethanol extract of fruits of Celastrus orbiculatus.
OBJECTIVE
To investigate the cytotoxic compounds against human melanoma A375-S2 and human cervical carcinoma Hela cell lines from the fruits of Celastrus orbiculatus.


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.
Xu
Jing
J
Department of Pharmaceutical Sciences, Nankai University, Tianjin 300071, PR China.
Guo
Yuan-Qiang
YQ
Li
Xian
X
Wei
Kun
K
Zhao
Xiao-Jun
XJ
D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D031247:Celastrus / Q000737:chemistry*; D005638:Fruit; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008545:Melanoma / Q000188:drug therapy / Q000473:pathology; D010936:Plant Extracts / Q000737:chemistry*; D012717:Sesquiterpenes / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts; D012717:Sesquiterpenes