The invention discloses a silybin C-5 site
chemical modifier with anti-tumor activity and a preparation method thereof, and relates to an anti-tumor activity modifier prepared by modifying the structure of a
natural product and a preparation method of the anti-tumor activity modifier. Silybin is used as a
lead compound, firstly, silybin is dehydrogenated and oxidized into 2, 3-dehydrogenated silybin, and then the 2, 3-dehydrogenated silybin is added into the 2, 3-dehydrogenated silybin to prepare the silybin C-5 site
chemical modifier with the anti-tumor activity. The method comprises the following steps: carrying out
alkylation on silybin by using iodomethane on the basis of silybin to obtain 3, 5, 7, 20, 23-pentamethoxy-2, 3-dehydrosilybin, and further selectively demethylating a methoxy group at a C-5 site by using AlCl3 to obtain 5-hydroxy-3, 7, 20, 23-tetramethoxy-2, 3-dehydrosilybin, and further selectively demethylating a methoxy group at the C-5 site by using AlCl3 to obtain 5-hydroxy-3, 7, 20, 23-tetramethoxy-2, 3-dehydrosilybin. And finally, introducing different acyl groups on 5-OH to obtain the novel silybin derivatives I1-I19. Pharmacological experiment research shows that the compound has an obvious anti-proliferation effect on gastric
cancer cells SGC-7901 and
breast cancer cells MCF-7, and the anti-proliferation effect is better than that of
silibinin. The structure of the silybin derivative is shown in the figure.