Use of celery derivatives for the preparation of anticancer drugs
A technology of anti-cancer drugs and derivatives, which is applied in the direction of anti-cancer drugs, drug combinations, active ingredients of heterocyclic compounds, etc., and can solve the problems of unclear anti-cancer efficacy of derivatives
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Embodiment 1
[0041] Evaluation of the In Vitro (Cell Experiment) Tumor Suppressive Effect of Anticancer Drugs in Embodiments 1 and 3
[0042] Apiole and its derivatives AP-02, AP-04, and AP-05 used, a total of four anticancer drugs are:
[0043]
[0044] The experimental cell lines were two cancer cell lines and one normal cell line from Colon, Breast, Lung and Liver, respectively: two human colorectal cancer cell lines (HT- 29 and colon205) and a normal human colon epithelial cell line (FHC). Two human breast cancer cell lines (MDA-MB231 and ZR75) and one normal human breast epithelial cell line (MCF-10A). Two lung cancer cell lines (A549 and PE089), one normal human lung cell line (HEL-229), two liver cancer cell lines (Hep3B and HepG2) and one normal human liver cell line (BNL cl.2). And do the following analysis:
[0045] 1. Cell viability analysis (MTT) test:
[0046]The MTT test was used to test whether the four drugs have the ability to inhibit the growth of cancer cells. Af...
Embodiment 2
[0067] Evaluation of the in vivo (animal test) tumor suppressive effect of embodiment 2 medicine:
[0068] Based on the results of the above cell experiments, the cancer cell lines most sensitive to drugs and the drugs with the strongest tumor suppressing effect and ability to kill cancer cells were screened out for the following animal experiments. 4-week-old nude mice (Nude mice) were used for animal experiments, and each mouse was implanted with freshly cultured 2X 10 6 A suspension of cancer cells was collected and measured after the tumors had grown to group the mice. The groups are divided into no-drug control group (vehicle), high-dose drug 1 experimental group, medium-dose drug 1 experimental group, and low-dose drug 1 experimental group. There are 4 groups in total, with 7 mice in each group, and a total of 28 mice are required. mouse. The drug administration method is intraperitoneal injection once a week, continuous observation and stopping the drug administration...
Embodiment 3
[0070] The discussion of the animal experiment tumor suppression mechanism of embodiment 3 medicine:
[0071] The tumors of two mice were randomly selected from the low-, medium-, and high-dose AP-02 and PBS groups in the animal experiment, and they were ground with a homogenizer and their proteins were extracted for Western blot experiments. Antibodies explore the tumor suppressor mechanism of drugs.
[0072] The experimental data show as Figure 8 , Apoptosis-related proteins p53, Bad, Bcl2 and Apaf 1 were significantly expressed in AP02 (5mg / kg) group, while caspase 9, caspase 3 and caspase 8 could be observed in AP02 (1mg / kg) The expression of activated state, GAPDH was used as an internal control among the tumors of each group. According to the experimental results, AP02 can achieve the purpose of inhibiting tumor growth by expressing a large amount of tumor suppressor protein p53.
[0073] It can be known from the above examples that AP-02 has a higher effect on inhib...
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