| Objective:To take rhein and aloe-emodin into ester, and observe its antitumor effect in vitro. Methods:DMF as dissolvent, DMAP as catalyst and DCC as dehydrant, and the ratio of rhein, aloe-emodin, DMAP and DCC was 1:1:0.5:2, Firstly,reacted for 0.5h in ice, then reacted for 2.5h at room temperature, the reaction process was tracked by TLC. The mixtures after reaction were filtered. The filterate were collected and solvent was recycled,the products were got and dried.The sample was isolated by silica gel column chromatography,which was eluted by petroleum ether(60～90℃) and ethyl acetate in grads.Eluents at the ratio of petroleum ether(60～90℃) and ethyl acetate (25:1) were collected. A compound was got by PTLC,whose purity was detected by TLC and HPLC. Its structure was elucidated by UV,IR,EI-MS,1H-NMR and 13C-NMR. HepG2 cells were thawed and passed on from generation to generation, and antitumor experiment of Rhein-aloe-emodin ester in vitro was studied on HepG2 cells in logarithmic phage.Several groups were assigned:negative control group,DMSO control group(the final concentration of DMSO was 1%),DDP group and rhein-aloe-emodin ester group.The concentrations of the rhein-aloe-emodin ester group(sample medicin group) were 6.25,12.5,25,50,100 and 200μg·mL-1.The absorbances were detected by CCK-8, the inhibitory rates and IC50 were analysised by SPSS software.Results: The purity of the compound by synthesis reaction was about 90%. Structure Characterization was rhein-aloe-emodin ester. The inhibitory rates of rhein-aloe-emodin ester in concentrations at 6.25,12.5,25,50,100 and 200μg·mL-1 to human liver cells HepG2 were separately 5.085%,15.90%,20.03%,32.40%,36.74% and 56.41%.The IC50 of the sample medicine was 146.1μg·mL-1.Conclusion:Rhein-aloe-emodin ester is synthesized by collage role of rhein and aloe-emodin,and it has some antitumor effect in vitro on human liver cells HepG2,which makes the foundation of exploiting it as an antitumor new drug.
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