The Screening Of Antitumor Compounds And Research On Their Mechanisms Of Antitumor

Objective Establish a antitumor substances screening method, to screen compou nds extraction from traditional Chinese medicine, in order to obtain compounds with antitumor activity; And further research to find antitumor activity of compounds of tu mor suppression mechanism, lay a foundation for the development of new antitumor drugs.Methods Determined by MTT colorimetry to detect different concentrations (10 0/ml and 50μg/mL,10μg/mL,2μg/mL, 0.4 μg/mL,0.08 μg/mL,0.16 μg/mL) ci splatin role within 24 h of human liver cancer cells SNU-387, the influence of the bone sarcoma cells-63 MG, calculate the corresponding to different concentrations of inhibition rate, and the half inhibitory concentration IC50; Cisplatin, for reference, select high concentration 50 μg/mL as initial concentration of screening, respectively for Atractyloside, BTW series compounds, ZC series compounds, MD series compou nds and LZ series of 2 kinds of cells. By comparing with cisplatin, choose the inhib itory effect is relatively obvious drug for further screening, calculate the IC50; Finall y chose four drugs (ZC-17, MD-4, BTW 10, BTW11) the Annexin V-FITC/PI double staining flow cytometry instrument is used to detect the apoptosis, drug conce ntration of 50μg/mL, respectively 10μg/mL,2μg/mL, duration of 24 h; By Elisa method to detect 4 kinds of different drug concentrations (50μg/mL,10μg/mL,2 u g/mL) of bax and the influence of the BCL-2 protein expression.Results Cisplatin can effectively restrain human liver cancer cells SNU-387、 MG-63, bone sarcoma cells growth,24 h half inhibitory concentration IC50 were 6. 391 μg/mL,16.592 μg/mL, the concentration of up to 50 μg/mL inhibition rate arou nd 90%;Except LZ series compounds and Atractyloside, the other three kinds of sa mples (BTW)series compounds, ZC series compounds, MD series compounds) are f ound to have highly active substances. ZC-17, MD-4, BTW 10, BTW 11 for hum an liver cancer cells SNU-387 half inhibitory concentration were 10.86 μg/mL、3.0 97 μg/mL、1.633 μg/mL、3.104 μg/mL; ZC-17, MD-4 half inhibitory concentrat ion on the bone sarcoma cells IC50 were 5.465 μg/mL,2.639 μg/mL; By flow cyto metry test results, comparative and positive group (cisplatin) and negative (DMSO) f ound that four drugs (ZC-17, MD-4, BTW10, BTW11) can promote the SNU-387 human liver cells apoptosis, apoptosis rate, associated with the drug concentrati on in the induction of apoptosis, BTW11 high concentration group was obviously.2 drugs (ZC-17, MD-4) all can promote bone sarcoma cells apoptosis, MD-4 i n high doses of necrosis.; Compared with the control group, found that positive gro up and the three drugs (ZC-17, BTW10, BTW11) can raise people SNU-387 ba x protein expression in liver cells, cut the BCL-2 protein expression. At the same time ZC-17 can increase bone sarcoma cells in bax protein expression capacity, cut the BCL-2 protein expression.Conclusions Four drugs (ZC-17, MD-4, BTW10, BTW11) can inhibit tumor growth, and concentration into a certain relationship; Four drugs (ZC-17, MD-4, BTW10, BTW11) can induce liver cancer cell apoptosis SNU-387,2 drugs (Z C-17, MD-4) are bone sarcoma cells can be induced apoptosis of MG-63; B y means of apoptosis proteins bax and BCL-2 test, prove that ZC-17, BTW10, BTW11 induced apoptosis may be through the Bax, cut the Bcl-2, MD-4 induce d apoptosis may be the other way.