High-activity anti-caner new medicament formalardeemin for inhibiting multi-drug resistance of tumor cells

A technology of formylademide and base formylademide, which is applied in the field of highly active anti-cancer drug formylademide, which can inhibit the multidrug resistance of tumor cells, can solve the problem of low yield and separation of acetylademide Mi 2 is difficult and restricts in-depth research and development and utilization

Inactive Publication Date: 2010-06-30
成都常春藤生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Due to the difficulty of extracting and isolating Acetamide 2 from fungal fermentation broth and mycelium, and the low yield, it greatly restricts its in-depth research, development and utilization.

Method used

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  • High-activity anti-caner new medicament formalardeemin for inhibiting multi-drug resistance of tumor cells
  • High-activity anti-caner new medicament formalardeemin for inhibiting multi-drug resistance of tumor cells
  • High-activity anti-caner new medicament formalardeemin for inhibiting multi-drug resistance of tumor cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Inhibitory effect of formylademide 4 on the proliferation of human breast cancer MCF-7 cells

[0026] experimental method:

[0027] Human breast cancer MCF-7 cells were cultured with PRMI1640 (Hyclone) medium containing 10% fetal bovine serum, and placed in a 37°C, 5% CO2 incubator. Tumor cells 0.7×10 4 Each well was inoculated on a 96-well plate, and after culturing for 24 hours, formylademide 4 with a final concentration of 10 μM, 20 μM, 40 μM, 80 μM, and 160 μM was added respectively. The control group was added with DMSO, and a zero-adjusted group (only culture medium was added) ), with three replicate wells for each group. The 96-well plate was placed in a 37°C, 5% CO2 incubator for another 72 hours, and the MTT colorimetric method was used to detect the survival rate of tumor cells, that is, 10 μl of 5 mg / ml MTT (Sigma, USA) reagent was added to each well, and the culture was continued for 4 hours. Remove the supernatant, wash with PBS, add 100 μl of ...

Embodiment 2

[0030] Example 2 Inhibitory effect of formylademide 4 on the proliferation of human cervical cancer Siha cells

[0031] experimental method:

[0032] Human cervical cancer Siha cells were cultured with PRMI1640 (Hyclone) medium containing 10% fetal bovine serum, and placed in a 37°C, 5% CO2 incubator. Tumor cells 0.7×10 4 Each well was inoculated on a 96-well plate, and after culturing for 24 hours, different concentrations of formylademide 4 were added according to Example 1. After continuing to cultivate for 72 hours, the survival rate of tumor cells was detected according to the method in Example 1.

[0033] result:

[0034] Such as Figure 4 As shown, formylademide 4 dose-dependently inhibited the growth of human cervical cancer Siha cells cultured in vitro.

Embodiment 3

[0035] Example 3 Formylademide 4 significantly increases the sensitivity of human cervical cancer Siha cells to doxorubicin

[0036] experimental method:

[0037] The culture conditions of human cervical cancer Siha cells are the same as those in Example 2. Tumor cells 0.7×10 4 Inoculate each well on a 96-well plate, and after culturing for 24 hours, add doxorubicin (0.4 μg / ml, Italian Pharmacia) or different concentrations of formylademide 4 (20 μM, 40 μM, 80 μM, 160 μM) , or add doxorubicin and different concentrations of formylademide 4 at the same time, add DMSO to the control group, and set up a zeroing group (only add culture medium), and set three replicate wells for each group. Place the 96-well plate in a 37°C, 5% CO2 incubator for another 72 hours, and then remove the lactic acid

[0038] Hydrogenase (LDH) release assay, using lactate dehydrogenase detection kit (Cyto Tox 96 Non-Radioactive Cytotoxicity Assay, Promega, Cat. No. G1780), to detect cell death. The...

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Abstract

The invention relates to indole alkaloid formalardeemin shown in a chemical structural formula ((-)-5-N-formalardeemin), pharmaceutically acceptable salts of the same, and application of the indole alkaloid formalardeemin serving as an anti-tumor medicament in curing malignant tumors of human beings. The indole alkaloid formalardeemin serving as an anti-tumor medicament can not only inhibit the growth of malignant tumors directly, but also can be used as a chemosensitizer when used together with other anti-tumor medicaments such as doxorubicine, vincristine and the like to achieve the effect of effectively killing tumor cells by reversing the multi-drug resistance of the tumor cells. More significantly, compared with the indole alkaloid formalardeemin serving as a tumor cell growth inhibitor directly, the indole alkaloid formalardeemin serving as the chemosensitizer has a better effect, so the indole alkaloid formalardeemin has important clinical application prospect.

Description

technical field [0001] The present invention relates to indole alkaloid formyl adeimide ((-)-5-N-formalardeemin), which can significantly inhibit the proliferation of tumor cells when used alone, and can significantly enhance the resistance of tumor cells to chemotherapy drugs when used in combination with various chemotherapeutic drugs. Sensitivity, and reversing the resistance of multidrug-resistant tumor cells to drugs can significantly improve the activity of anti-tumor drugs. Background technique [0002] In 1993, McAlpine et al. found that the extract of the fungus Aspergillus fischerii (var.brasiliensis) could reverse the drug resistance of tumor cells and restore the sensitivity of vincristine-resistant tumor cell lines to drugs, and isolated three species from the extract. The ingredients are named as ardeemin, 5-N-acetylardeemin and 15b-hydroxy-5-N-acetylardeemin. They all belong to indole alkaloid derivatives with trans-isoprenyl, and acetylademide 2 is the main ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P35/00
Inventor 秦勇林勇王霞何彬宋颢郑雪莲张林
Owner 成都常春藤生物科技有限公司
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