AIM:To investigate the effect of 3,5-hydroxy-6,7,3',4'-tetramethoxyflavone (HTMF) isolated from Laggera pterodonta on Hep-2 cell apoptosis and the underlying mechanism.METHODS:The MTT assay was used to observe the cytotoxicity of HTMF to the normal cells and the inhibitory effect of HTMF on the proliferation of tumor cells.The apoptosis was determined by flow cytometry.Western blotting was used to detect the expression of caspase-3 and caspase-9.RESULTS:HTMF significantly inhibited the growth of Hep-2 cells in dose and time dependent manners.HTMF exhibited weak cytotoxicity to the two normal cell lines Vero and EVC304,while showed low effect of anti proliferation on HepG2 cells and A549 cells.The increase in apoptosis of Hep-2 cells by HTMF was observed with dose and time dependent manners.Western blotting showed that HTMF time dependently increased the expression of caspase 3 and caspase-9 in Hep-2 cells.CONCLUSION:HTMF has high inhibitory effect on the proliferation of Hep-2 cells by induction of apoptosis in the tumor cells through caspase-9 and caspase-3 activation.However,the cytotoxicity of HTMF to the normal cells is low.

OBJECTIVETo research the cytotoxicity and in vitro antiproliferative effect of the six flavone compounds extracted from Laggera pterodonta.

METHODThe cytotoxicity on the normal cells and antiproliferative effect on tumor cells were tested by MTT assay, and then the preliminary structure-activity relationship was analysed. The phase distribution of the cell cycle and apoptosis rate were analyzed by flow cytometry.

RESULTThe results of MTT assay showed 5,7,3',4'-tetramethoxy-3-hydroxyflavone and chrysosplenetin B inhibited growth of A549 and Hela cells significantly with a dose dependent mode, while exhibited low cytotoxicity to the two normal cells, Vero and EVC304. Both compounds contain ortho-phenolic methoxyl moietys in their structures. Flow cytometry analysis revealed that Hela cells treated with increasing quantities of chrysosplenetin B increased the percentage of cells in the G2/M phase, and Hela and A549 cells treated with increasing quantites of the 5,7,3',4'-tetramethoxy-3-hydroxyflavone and chrysosplenetin B increased the apoptosis rates.

CONCLUSIONThe 5,7,3',4'-tetramethoxy-3-hydroxyflavone and chrysosplenetin B extracted from L. pterodonta showed high antiproliferative effect on cancer cells with low cytotoxicity on normal cells, and took the effects on A549 and Hela cells through the hold-up of the G2/M phase of the cell cycle and induction of the apoptosis.

Animals ; Asteraceae ; chemistry ; Cell Line ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Cercopithecus aethiops ; Flavones ; chemistry ; pharmacology ; Flavonoids ; pharmacology ; Flow Cytometry ; HeLa Cells ; Humans ; Vero Cells