Study On Ferula Sinkiangensis K.M.Shen Chemical Constituents And Screening Antitumor Activities In Vitro

Objective:To Study on the anticancer constituents of Ferula sinkiangensis K.M.Shen by bioassay-guided fractionation.Methods:1.Solvent extraction,silica gel,Sephadex LH-20 and semi-preparing high performance liquid chromatography techniques were used to isolate and purify anticancer active constituents from Ferula sinkiangensis.2.Inhibiting effect of polar parts,fractions and compounds of F.sinkiangensis on SGC7901gastric cancer cells and SW620 colon cancer cells proliferation were detected by MTT and SRB methods.3.Influence of active components on SGC7901 cell cycle was determined by using the flow cytometry.Results:1.MTT assay showed that 95%ethanol extracts possessed significant antitumor activity among the three parts of petroleum ether,95%ethanol and water.2.95%ethanol extraxts were divided into nine fractions by silica gel column chromatography.In addition to Fr.1⁷2 and Fr.318³67,the seven fractions of Fr.73¹04,Fr.105¹98,Fr.199³17,Fr.368³97,Fr.398⁴33,Fr.434⁴86 and Fr.487⁵29 have been showed significant inhibiting effects on SGC7901 cells and inhibiting rates were more than 80%at the concentration of 400μg/mL.3.13 compounds were isolated from 7 active fractions,11 of which were identified as fekolone（1）,sinkianone（2）,lehmannolone（3）,fekrynol（4）,colladonin（5）,feselol（6）,compound 7,lehmannolol（8）,episamarcandin（9）,isosamarcandin（10）,sinkiangenorin E（11）,compound 12 and sinkiangenorin F（13）.4.Compounds 4,9,11,12 and 13 could inhibit proliferation of SGC7901 cells,of which effect of compound 9 was more than compound 4,11,12,13 and its IC₅₀0 value was 6.04μg/mL.For SW620 cells,the inhibitory effect of compounds 7,11and 12 was relatively strong on proliferation.5.Flow cytometric analysis of cell cycle showed that after treated with compounds（250μg/mL）,SGC7901 cells were arrested in G₀/G₁ phase by compounds 4,9,11;and were arrested in S phase by compound 12.Conclusion:Ferula sinkiangensis has active ingredients of significant antitumor activity.The results can provide basic data for the further development and utilization of this plant.