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Application of sodium ion channel blocker in preparation of drugs to treat melanoma

A sodium ion channel and melanoma technology, applied in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., can solve problems such as the application of sodium ion channel blockers that have not yet been discovered, and achieve shortened development time, target specificity, reduced side effects and The effect of drug resistance

Active Publication Date: 2019-06-21
THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The application of sodium ion channel blockers in the preparation of drugs for the treatment of melanoma has not yet been found

Method used

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  • Application of sodium ion channel blocker in preparation of drugs to treat melanoma
  • Application of sodium ion channel blocker in preparation of drugs to treat melanoma
  • Application of sodium ion channel blocker in preparation of drugs to treat melanoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Tetrodotoxin, dehydrated tetrodotoxin, and combinations of dehydrated tetrodotoxin and tetrodotoxin inhibit melanotic solid tumors in mice

[0036] (1) Experimental materials

[0037] (1) Melanoma cell line: melanoma cell B16F10 is cryopreserved in our laboratory;

[0038] (2) Test drugs: dehydrated tetrodotoxin, tetrodotoxin, crude tetrodotoxin (composition representing dehydrated tetrodotoxin and tetrodotoxin), cisplatin freeze-dried powder and normal saline;

[0039] (3) Experimental animals: clean grade ICR mice, half male and half male.

[0040] (2) Experimental method

[0041] B16F10 melanoma cells were resuscitated and cultured in vitro. After passage and expansion, the cells in the logarithmic growth phase were collected, suspended in DMEM liquid medium containing 10% fetal calf serum, and inoculated with the cell suspension in the right axilla of each mouse. Liquid 0.2ml (1×10 6 tumor cells). On the day after melanoma cell inoculation, the inoculated mice ...

Embodiment 2

[0052] Dehydrated tetrodotoxin, tetrodotoxin and crude tetrodotoxin inhibit human melanoma cell lines

[0053] (1) Experimental materials

[0054] (1) Melanoma cell line: melanoma cell G-361 was purchased from ATCC in the United States;

[0055] (2) Main test drugs: dehydrated tetrodotoxin, tetrodotoxin, acetic acid and cisplatin freeze-dried powder.

[0056] (2) Experimental method

[0057] The cytotoxic effect of test sample A (tetrodotoxin dehydrate) and test sample B (tetrodotoxin) on human melanoma cell line G-361 was investigated by MTS method.

[0058] Human melanoma cell G-361 was made into a single-cell suspension with McCoy's 5A (containing 2 mM glutamine) liquid medium containing 10% fetal calf serum by volume fraction, and the human melanoma cell G-361 was diluted 2×10 3 Each well was inoculated in a 96-well plate, 90 μl per well. After conventional culture for 24 hours, 10 μl of dehydrated tetrodotoxin solution of different concentrations were added to each we...

Embodiment 3

[0069] Combination of dehydrated tetrodotoxin and tetrodotoxin with trametinib or cabitinib inhibits the proliferation of human melanoma cells

[0070] (1) Experimental materials

[0071] (1) Melanoma cell line: melanoma cell A375 (CRL1619IG-3) was purchased from ATCC, USA;

[0072] (2) The main test drugs: dehydrated tetrodotoxin (A), tetrodotoxin (B), trametinib (D), cabetinib (E), acetic acid and normal saline.

[0073] (2) Experimental method

[0074] Using CCK8 method to investigate dehydrated tetrodotoxin, tetrodotoxin, trametinib, cabetinib, combination of dehydrated tetrodotoxin and trametinib, combination of tetrodotoxin and trametinib, combination of dehydrated tetrodotoxin and cabetinib, And the cytotoxic effect of tetrodotoxin combined with carbitinib on human melanoma cell line A375.

[0075] The melanoma cell line A375 was made into a single-cell suspension with DMEM liquid medium containing 10% fetal calf serum by volume fraction, and the melanoma cell line A...

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Abstract

The invention discloses application of a sodium ion channel blocker in the preparation of drugs to treat melanoma. The sodium ion channel blocker is made with any one or two of tetrodotoxin and dehydrated tetrodotoxin. The invention also provides a drug to treat melanoma; the drug comprises the sodium ion channel blocker, a second therapeutic agent and a pharmaceutically acceptable carrier; the second therapeutic agent includes one or more of a chemotherapeutic agent, an immunotherapeutic agent, a gene therapeutic agent and a radiotherapeutic agent. The sodium ion channel blocker can inhibit the proliferation and tumorigenesis of melanoma cells, and can cooperate with the second therapeutic agent, especially mitogen-activated extracellular signal regulation kinase inhibitor, to arrive at better treatment of melanoma.

Description

technical field [0001] The invention relates to the technical field of research and development of medical drugs, and relates to the application of a specific sodium ion channel blocker in the preparation of drugs for treating melanoma. Background technique [0002] Melanoma has a high degree of malignancy, early metastasis, and a high mortality rate, accounting for 80% of skin cancers. Currently, the treatment of melanoma mainly includes radiotherapy, chemotherapy and surgery. Very early melanoma can be cured by surgery, but because the early symptoms of melanoma are not obvious, most patients are already in the middle and late stages when they are discovered, and they mainly rely on radiotherapy or chemotherapy, which have poor sensitivity and drug resistance to radiotherapy or chemotherapy drugs. Current bottleneck in melanoma treatment. [0003] Finding new therapeutic targets has always been a research hotspot in the treatment of melanoma. Studies have shown that mel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/529A61P35/00
Inventor 何建林洪碧红谢全灵陈伟珠张怡评易瑞灶
Owner THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES
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