The invention provides an isoalantolactone derivative TYJ2517, namely 3, 4, 5-trimethoxybenzyl aminomethyl 3-demethyleneisoalantolactone as well as preparation and application thereof, and relates to the field of medicinal compounds, the structure of the isoalantolactone derivative is shown as follows: although many anti-
cancer drugs have anti-
cancer ability, the drugs generate
toxicity to normal cells, and the drugs cannot generate
toxicity to the normal cells. Therefore, the development of selective anti-
cancer active drugs safe to normal cells is particularly important. According to the invention, TYJ2517 is synthesized, the IC50 value of the TYJ2517 to MCF-7 cells is 3.6 + / -0.8 [mu] M, and the IC50 value of the TYJ2517 to L-02 normal cells exceeds 100 [mu] M. A
cell drug uptake capability test result shows that the TYJ2517 uptake capability of L-02 normal cells is low, and the TYJ2517 uptake capability of MCF-7 cancer cells is high. When the
administration time is 1 hour, the selective anti-cancer index (SI) of the TYJ2517 to MCF-7
breast cancer cells and L-02 normal cells exceeds 40. Mechanism research shows that the activity of the TYJ2517 for resisting MCF-7 cancer cells is a result of inhibiting the expression quantity of PARP1
protein kinase and ROS, inducing early and late
apoptosis of the MCF-7 cells and hindering migration and colony of the MCF-7 cells.