The Research Of Antitumor Activity Of Baicalin Metal Complexes And Echinacoside,Verbascoside

Cancer is one of the larger global public health problem,which greatly endanger human health,and has become mankind's first killer,breaking tumor imminent.Studies have shown that ehinacoside(ECH),verbascoside(VER)and baicalin metal complexes(BMC)has a variety of pharmacological activities,but few studies of its anti-tumor effect,the corresponding action mechanism needs to be further improved.Therefore,this paper studied the antitumor activity of ECH,VER and BMC synthesized in the laboratory,and its possible mechanism of action,achieved the following results:(1)MTT assay and cell morphology found that ECH and VER has anti-tumor activity,as follows: A549 cells in a certain range of concentrations in a dose-dependent and time-dependent inhibition;of SMMC-7721 cells is low concentration promotes cell growth and inhibition at high concentration,which may be followed by protecting liver;fluorescence polarization parameter display ECH and VER acting on the A549 cells,and the degree of polarization p,anisotropy r increases,membrane fluidity becomes small,inhibit cancer cell mitosis,induce apoptosis;RT-PCR and Western blot showed that under the conditions set concentration and time,ECH and VER can make A549 cells Bcl-2 mRNA,protein expression decreased while mRNA,protein of Bax and p53 expression increased;description ECH and VER can significantly inhibit the growth of A549 cells,and its mechanism may be by blocking the cell membrane fluidity,down expression of Bcl-2 tumor suppressor gene,and regulated cancer-promoting gene Bax,p53,to inhibit the proliferation of cancer cells,thereby promoting apoptosis.(2)The effect of BMC in A549 cells by MTT assay,cell morphology microscopic,quantitative fluorescence polarization method to explore the universality of BMC antitumor activity.Results showed that BMC can significantly inhibit the proliferation of A549 cells,slowed membrane fluidity,prevent cell mitosis and the BMC action(except BC-Ni)was stronger than BC.Prima facie BMC have universal anti-tumor activity,but for different tumor may have different suppressor intensity.(3)Using whole cell patch clamp method studies BMC(Baicalin-copper(BC-Cu),Baicalin-cobalt(BC-Co),BC-Ni)on ion channel currents change.The results showed that BMC for ion channel inhibition rate size: BC-Cu>BC-Co>BC>BC-Ni,and with the increase of the concentration of BMC(0~30 ?mol·L-1),its for Kv1.4,Cav3.2 ion channel inhibition rate were enhanced;BC-Co on Kv1.4,Cav3.2 the IC50(?mol·L-1)were 1.69,0.81;BC-Cu for Kv1.4,Cav3.2 the IC50(?mol·L-1)were 1.66,0.58.Its ion channel inhibition rate and anti-tumor activity(A549 cells)are basically the same,to verify the ion channels associated with the tumor,indicating that BMC may through affect the ion channels open to inhibit cell proliferation and induce apoptosis,thereby exhibit anti-tumor activity.This paper clarifies the preliminary anti-tumor activity and its mechanism of ECH and VER;the establishment of anti-tumor activity of BMC and its effects on ion channel correlation,correlation results provides a new way of thinking for the design of new anticancer drugs,and plays a role in the promotion of research into and development of anticancer drugs.