Objective: To research the cytotoxicity and in vitro antiproliferative effect of the six flavone compounds extracted from Laggera pterodonta.
Method: The 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.
Result: The 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.
Conclusion: The 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.