Study On The Material Basis And Mechanism Of Antitumor Effect Of Abrus Cantoniensis

Objective:This study is based on the results of the preliminary screening and in vivo screening of the anti-tumor activity of petroleum ether,ethyl acetate,n-butanol and water extracts of Abrus cantoniensis.The purpose of this study is to explore the basis of the anti-tumor active substances of Abrus cantoniensis,to isolate and purify the extracts with anti-tumor activity,and to obtain the monomer compounds objective to study the antitumor activity and its mechanism.Methods:Silica gel column chromatography,thin-layer chromatography and high performance liquid chromatography were used to separate and purify the chemical constituents of the antitumor active parts.The structures of the isolated compounds were identified by IR,UV,MS,NMR and other modern spectral techniques.Then,the antitumor activity of monomer compounds was studied.MTT method was used to detect the proliferation inhibition of the monomers on human breast cancer MCF-7 cells,human gastric cancer SGC-7901 cells and human liver cancer BEL-7404 cells in vitro,and the IC₅₀value was calculated;Annexin V-FITC/PI labeling method was used to detect the apoptotic effects of the monomers on MCF-7,SGC-7901 and BEL-7404 cells.The effect of monomer compounds on the activity of DNA topoisomerase I and the direct cleavage of DNA were detected in cell-free system.Results:These compounds are:Chrysophanol,Luteolin,Abrine,Schaftoside,Protocatechuic acid.The results of pharmacological experiments showed that chrysophanol and luteolin had anti-tumor effect,and had proliferation inhibition effect on three kinds of tumor cells in a dose-dependent manner.Among them,luteolin had Pro apoptotic effect on three kinds of tumor cells and inhibition effect on DNA topoisomerase I;all the five monomers had no direct cutting effect on DNA.Conclusion:Five compounds were isolated and identified from the ethanol extract of Abrus cantoniensis.The results of antitumor activity experiment showed that chrysophanol and luteolin were the material basis of antitumor activity of Abrus cantoniensis.The structure-activity relationship and mechanism of action of the monomers were discussed,it was found that its mechanism of action might be to inhibit the proliferation of tumor cells by blocking the G2/M phase of cells;it may induce apoptosis and autophagy through mitochondrial pathway and affecting PI3K/Akt/m TOR/p38MAPK signal transduction pathway.