Screening And Evaluating Of Composition Which Have Es Trogen-like Activities In Xiaoyao Powder

Objective:By studying the effects of ten active ingredients in Xiaoyao pow der on the proliferation of mammary cancer cell MCF-7,in vitro to dis cuss its potential mechanism and preliminary clarify the mechanism of active ingredients in Xiaoyao powder for estrogen-like activities,and to provide theoretical basis for rational use of Xiaoyao powder in treating Perimenopausal syndrome.Methods:The ER-positive cell MCF-7 was treated with ten active ingreden ts in Xiaoyao powder which include Umbelliferone、Ferulic acid、L icoflavone、Liquiritigenin、Glycyrrhizin、Saikogenin-d、Quercetin、Kaempferol、Isorhmnetin、Glycyrrhetinic and estrogen as well as ICI 1 82780.MTT test was used to detect the cell proliferation,Western Blot and RT-PCR were respectively adopted to test Eα、ERβ protein and mRNA expression level.Results:Umbelliferone(100μmol/L)、Ferulic acid(100μmol/L)、Saikogeni n-d(100μmol/L)、Licoflavone(100μmol/L、10μmol/L、1μmol/L、10-1μmol/L)、Liquiritigenin(10μmol/L、1μgmol/L、10-1μmol/L)、Glycyrrhiz in(100μmol/L、10μmol/L)、Quercetin(100μmol/L、10μmol/L)can signi ficantly inhibit the MCF-7 cell proliferation(P<0.05),which showed significant cytotoxity on human melanoma and didn’t fit for the next research.Quercetin(1 0-2μmol/L、10-3μmol/L)、Kaempferol(0-2μmol/L、10-3μmol/L)、Isorhmnetin(10-3μmol/L)、Glycyrrhetinic(100μmol/L、μmol/L、10-2μmol/L)can significantly promote the MCF-7 cells pr oliferation(P<0.05);The Western Blot result showed that 1μmol/L Qu ercetin,10μmol/LKaempferol、Glycyrrhetinic,100μmol/L Isorhmnetin can raise ERα、ERβ protein level(P<0.05);The RT-PCR result showed that 1μmol/LQuercetin,10μmol/LKaempferol、Glycyrrhetinic,100μmo 1/L Isorhmnetinl can raise ERα、ERβ mRNA level(P<0.05);The above effects can be blocked by adding estrogen receptor antagonisrn ICI182780.Conclusion:Quercetin、Kaempferol、Isorhmnetin、Glycyrrhetinic are the ac tive ingredients in Xiaoyao powder for estrogen-like activities.they c an promote ER-positive MCF-7 proliferation,raise ERα、ERβ protein and mRNA level.It is speculated that they have the estrogen-like acti vities through the estrogen response pathway.In addition,Umbellifero ne、Ferulicacid、Saikogenin-d、Licoflavone、Liquiritigenin、Glycyrrhi zin can significantly inhibit the MCF-7 cell proliferation for anti-est rogen activity.But it has yet to the further study of its potential mech anism.