阅读说明：本技术 12α-甲氧基-吉玛烷-三烯-12,6α-缩醛的抗人胶质瘤用途 (Use of 12 α -methoxy-germacrane-triene-12, 6 α -acetal for anti-human glioma ) 是由 于海涛 杨晓旭 李涛 于 2020-05-07 设计创作，主要内容包括：本发明公开了12α-甲氧基-吉玛烷-三烯-12,6α-缩醛的抗人胶质瘤用途。本发明发现,12α-甲氧基-吉玛烷-1(10),4,11(13)-三烯-12,6α-缩醛对人乳腺癌MCF-7细胞株、人胶质瘤U87细胞株和人横纹肌肉瘤RD细胞株的增殖均具有显著的抑制作用,具有开发成抗人乳腺癌、人胶质瘤或人横纹肌肉瘤药物的前景。(The invention discloses an application of 12 α -methoxy-germacrane-triene-12, 6 α -acetal in resisting human glioma, and finds that the 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal has a remarkable inhibiting effect on the proliferation of human breast cancer MCF-7 cell strains, human glioma U87 cell strains and human rhabdomyosarcoma RD cell strains, and has a prospect in developing medicaments for resisting human breast cancer, human glioma or human rhabdomyosarcoma.)

The medical application of 12 1.12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal in preparing anti-human glioma medicine is as follows:

2. a medicine for resisting human glioma is characterized in that 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal is used as an active ingredient, and pharmaceutically acceptable auxiliary materials are used for preparing pharmaceutically acceptable dosage forms.

3. The medicament of claim 2, wherein: the auxiliary material can be solid auxiliary material or liquid auxiliary material.

4. The medicament of claim 2, wherein: the preparation can be tablet, capsule, granule, and injection.

Technical Field

The invention relates to the field of medicines, in particular to an application of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal in resisting human glioma.

Background

Cancer is one of the major diseases and serious public health problems seriously threatening human survival and social development, and cancer control has become the key point of the health strategy of governments around the world. In recent years, with global economic development, population aging, lifestyle changes and ecological environment changes, the morbidity and mortality of cancer are on the rise as a whole, and the burden of cancer is increasing.

Human glioblastoma is one of the most common, most aggressive brain tumors, and the most mortality tumor of brain tumors. Although there are many treatment methods such as surgery, radiotherapy, chemotherapy, gene therapy, etc., human glioma has a high fatality rate and disability rate due to its strong invasiveness, high recurrence rate, special location and poor prognosis, and seriously threatens human health. At present, the treatment of human glioma remains one of the major challenges in the tumour field, and therefore, the search for effective therapeutic drugs is particularly urgent.

Disclosure of Invention

The invention aims to provide an application of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal in resisting human glioma.

The technical scheme for realizing the purpose is as follows:

the medical application of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal in preparing anti-human glioma drugs is as follows:

a medicine for resisting human glioma is prepared from 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal as active component, and pharmaceutically acceptable adjuvants.

Preferably, the adjuvant may be a solid adjuvant or a liquid adjuvant.

Preferably, the dosage form can be tablets, capsules, granules and injections.

Has the advantages that:

the invention discovers that 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal has obvious inhibition effect on the proliferation of human breast cancer MCF-7 cell strain, human glioma U87 cell strain and human rhabdomyosarcoma RD cell strain, and has a prospect of developing drugs for resisting human breast cancer, human glioma or human rhabdomyosarcoma.

Drawings

FIG. 1 is a chemical structural formula of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal;

FIG. 2 is the anti-tumor profile of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal against 4 tumor cells.

Detailed Description

First, test materials

Human breast cancer MCF-7 cell line, human acute myelogenous leukemia MV4-11 cell line, human glioma U87 cell line and human rhabdomyosarcoma RD cell line were purchased from American ATCC company and frozen in liquid nitrogen.

The purity of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal is not less than 98%, the structural formula is shown in figure 1, and the medicine solution is prepared for standby.

RPMI 1640 medium, DMEM medium, fetal bovine serum were purchased from Gibco.

Penicillin, streptomycin was purchased from Sigma.

The CCK8 test kit was purchased from Nanjing Binyan Yuntan.

Second, test method

1. Cell culture

Recovering human breast cancer MCF-7 cell line frozen by liquid nitrogen according to conventional method, suspension culturing in DMEM culture solution containing 10% fetal calf serum, 100U/ml penicillin and 100 μ g/ml streptomycin, and culturing at 37 deg.C with 5% CO₂And culturing in a constant-temperature incubator with saturated humidity, changing liquid for passage every 2-3 d, and taking cells in logarithmic growth phase for experiment.

Recovering human acute myelogenous leukemia MV4-11 cell line frozen in liquid nitrogen according to conventional method, suspension culturing in RPMI 1640 culture solution containing 10% fetal calf serum, 100U/ml penicillin and 100 μ g/ml streptomycin, and culturing at 37 deg.C with 5% CO₂And culturing in a constant-temperature incubator with saturated humidity, changing liquid for passage every 2-3 d, and taking cells in logarithmic growth phase for experiment.

Recovering human glioma U87 cell line frozen by liquid nitrogen according to conventional method, suspension culturing in DMEM culture solution containing 10% fetal calf serum, 100U/ml penicillin, and 100 μ g/ml streptomycin, and culturing at 37 deg.C with 5% CO₂And culturing in a constant-temperature incubator with saturated humidity, changing liquid for passage every 2-3 d, and taking cells in logarithmic growth phase for experiment.

Recovering human rhabdomyosarcoma RD cell strain frozen by liquid nitrogen according to conventional method, suspension culturing in DMEM culture solution containing 10% fetal calf serum, 100U/ml penicillin, and 100 μ g/ml streptomycin, at 37 deg.C and 5% CO₂Culturing in a constant-temperature incubator with saturated humidity, changing liquid for passage every 2-3 days, and takingExperiments were performed on cells in logarithmic growth phase.

2. CCK8 method for determining proliferation inhibition effect of drug on MV4-11 cells

Respectively taking each tumor cell in logarithmic growth phase, digesting and re-suspending to prepare the tumor cells with the density of 1.5 × 10⁵The cell suspension of/m L was inoculated into 96-well plate at an inoculum size of 90 μ L per well, and drug solutions of 10 μ L different concentrations were added, 3 multiple wells were provided for each concentration, non-drug-added cells were used as control, and non-cell-added culture medium was used as blank, and the blank was placed at 37 ℃ with 5% CO₂Culturing in a constant temperature incubator with saturated humidity for 48h, adding 10 mu L of CCK8 reagent into each hole, incubating for 4h, measuring the OD450 value of each hole at the wavelength of 450nm of an enzyme linked immunosorbent assay (ELISA) detector, taking the average value of 3 holes, calculating the proliferation inhibition rate according to the following formula, and calculating the IC50 value.

The proliferation inhibition ratio (%) was × 100% (1- (OD drug group-OD blank)/(OD control group-OD blank)).

3. Statistical analysis

The software SPSS 17.0 is adopted to carry out statistical analysis processing, the metering data is expressed by mean plus or minus standard deviation, the comparison among groups adopts t test, the comparison among groups adopts variance analysis, and the difference P less than 0.05 has statistical significance.

Third, test results

The IC50 values of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal on the proliferation inhibition of different tumor cells are shown in Table 1, and as can be seen from Table 1, 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal all have excellent proliferation inhibition on human breast cancer MCF-7 cell strain, human glioma U87 cell strain and human rhabdomyosarcoma RD cell strain, and the proliferation inhibition on human acute myelogenous leukemia MV4-11 cell strain is not obvious.

TABLE 112 IC50 values of 112 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal on 4 tumor cells

FIG. 2 shows the anti-tumor spectrum of 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal on 4 tested tumor cells, which shows that 12 α -methoxy-germacrane-1 (10),4,11(13) -triene-12, 6 α -acetal all have significant inhibition effect on the proliferation of human breast cancer MCF-7 cell strain, human glioma U87 cell strain and human rhabdomyosarcoma RD cell strain, and have the prospect of developing drugs for resisting human breast cancer, human glioma or human rhabdomyosarcoma.