| Oridonin is a diterpenoid isolated from Rabdosia rubescens (Hemsl.) Hara. Experiments in vitro and in vivo proved that oridonin have strong anti-tumor activity,and it had been used to treat esophageal cancer and liver cancer with specific curative effect.Many research showed that oridonin can inhibit cell growth by down-regulation of Bcl-2 and up-regulation of Bax expression. Therefore, Oridonin is a new promising anticancer drug. As a lead compound, its solubility is poor both in the water and oil. Oridonin was modified and esterified to improve the solubility in the water or oil on hydroxy group.In this paper, Oridonin was used as the lead compound. Eleven derivatives of Oridonin were synthesized (Fig.1) and six derivatives were first synthesized (compound 4,5,8,9,10,11). Their structures were identified by spectrum analysis. In order to investigate the function of 1-hydroxyl in its ant-tumor activity, compounds 1 to 9 were synthesized. Their cytotoxicity was evaluated by measurement of MTT on three tumor cells (Hela,HT-1080,MCF-7). The result showed that Oridonin and lots of derivatives showed stronger cytotoxicity on MCF-7 cell than Cisplatin .To improve the solubility in the water of Oridonin, compounds 10 and 11 were synthesized. Experiments show that Compound 11 had well water solubility than Oridonin, so it probably can be used as potential water solubility prodrugs and the farther research was in progress.
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