Antitumor activities of the four sesquiterpene lactones from Elephantopus scaber L.
OBJECTIVE
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.


CONCLUSIONS
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.
Xu
G
G
Center for New Drug Research & Development, College of Life Science, Nanjing Normal University, Nanjing, China. biopharmacology@126.com
Liang
Q
Q
Gong
Z
Z
Yu
W
W
He
S
S
Xi
L
L
D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival; D053938:DNA Fragmentation; D004273:DNA, Neoplasm / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology*; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D004273:DNA, Neoplasm; D007783:Lactones; D012717:Sesquiterpenes