Anti-tumor Activities Of Effective Extracts And Active Compounds From Descurainia Sophia L.

Objectives:The effective fraction of anti-tumor activity was screened from the Descurainia sophia L,and the effects of its effective fractions on the proliferation and apoptosis of human non-small cell lung cancer H1975 cells were preliminarily investigated.The active fraction of the Descurainia sophia L.was studied by activity tracking separation method to find new drug-forming lead compounds.Methods:1.The characteristics and microscopy of the Descurainia sophia L.were identified by magnifying glass and optical microscope,and the expansion of the Descurainia sophia L.was measured by the method of dilatancy measurement.2.Using the mothod of solvent extraction and solvent extraction system,Descurainia sophia L.were divided,and obtain different polarity extract samples.3.MTT assay was used to detect the cytotoxicity of methanol extracts from Descurainia sophia L.and to screen out the effective fractions.4.Colony cloning method was used to detect the inhibitory activity of the methanol-ethyl acetate partitioned fraction from Descurainia sophia L.（MEDS）on the proliferation of human non-small cell lung cancer H1975 cells.5.To establish a nude mouse xenograft model of human non-small cell lung cancer H1975 cells,and to detect the antitumor activity and toxicity of the MEDS.6.Annexin V-FITC/PI method was used to detect the effect of the MEDS on apoptosis of human non-small cell lung cancer H1975 cells.7.Western blotting was used to detect the effects of the MEDS on protein kinase B（Akt）,B-cell lymphoma-2（Bcl-2）and Bax protein expression.8.Extraction and separation of the MEDS were carried out by preparative thin layer chromatography,column silica gel chromatography,semi-preparative high performance liquid chromatography and high performance liquid chromatography to obtain the active ingredients.9.The MTT assay was used to detect the inhibitory effect of the active ingredients on the proliferation of four human tumor cells（H1975,CNE-2Z,MDA-MB-231,SGC-7901）and the IC₅₀ value was calculated.Results:1.Microscopic identification and expansion measurement results showed that the sample used in this study is the Descurainia sophia L.2.The methanol extract 373.66 g,the hexane extract 108.28 g,the CH₂Cl₂extract 15.32 g,the ethyl acetate extract 6.23 g and the H₂O extract 197.42 g were obtained by the methanol extraction and fractional extraction of the Descurainia sophia L.3.MTT and colony cloning results showed that the MEDS inhibited the proliferation of human non-small cell lung cancer H1975 cells in a dose-and time-dependent manner.4.Human non-small cell lung cancer H1975 cell xenograft model showed that the MEDS showed good anti-tumor activity and low toxicity in nude mice.5.Annexin V-FITC/PI results showed that the MEDS could induce apoptosis of human non-small cell lung cancer H1975 cells.6.Western blotting results showed that the MEDS could down-regulate the expression of Akt and Bcl-2 proteins,and up-regulate the expression of Bax proteins.7.The active compounds sinapic acid,GJH2-51-1 and GJH2-52-1 were obtained through the separation of the MEDS.8.The IC₅₀ values of sinapic acid on H1975,CNE-2Z,MDA-MB-231 and SGC-7901 cells were 7.94,6.34,19.28,33.72μg/mL,and the IC₅₀ values of GJH2-51-1 on H1975,CNE-2Z,MDA-MB-231 and SGC-7901 cells were 6.23,7.26,22.06,12.09μg/mL,and the IC₅₀ values of GJH2-52-1 on H1975,CNE-2Z,MDA-MB-231 and SGC-7901 cells were 14.20,16.25,59.42,33.72μg/mL.Conclusions:1.The MEDS has the ability to inhibit the proliferation and induce apoptosis of human lung cancer H1975 cells,and has good anti-human lung cancer H1975 cell activity and low toxicity in vivo,which lays a foundation for the research and development of Chinese medicine the Descurainia sophia L.2.Sinapic acid,GJH2-51-1 and GJH2-52-1 have cytotoxic effect on human non-small cell lung cancer H1975,CNE-2Z,MDA-MB-231 and SGC-7901.