Application of naphthalimide-polyamine derivatives combined with cyclosporin a in the preparation of antitumor drugs

An anti-tumor drug, naphthalimide technology, applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of obvious toxic and side effects, achieve no toxic and side effects, improve anti-tumor effect, and improve anti-tumor effect Effect

Active Publication Date: 2022-01-25
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the basis of the prior art, the inventor found through preliminary tests that under high concentration conditions, cyclosporine A and naphthalimide derivatives alone have certain antitumor effects, but the side effects are obvious

Method used

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  • Application of naphthalimide-polyamine derivatives combined with cyclosporin a in the preparation of antitumor drugs
  • Application of naphthalimide-polyamine derivatives combined with cyclosporin a in the preparation of antitumor drugs
  • Application of naphthalimide-polyamine derivatives combined with cyclosporin a in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1: In vitro biological activity evaluation of naphthalimide-polyamine derivative 6c and cyclosporine A (CsA) combined use

[0063] Test one:

[0064] Human liver cancer cells HepG2 and SMMC-7721 in the logarithmic growth phase were respectively taken, and the cancer cells were digested with trypsin, centrifuged at a speed of 1000r / min for 5 minutes, the supernatant was discarded, suspended in the complete medium, and the number of cells was counted by a hemocytometer. Density is 8×10 3 The inoculum amount of cells / well was inoculated in a 96-well plate, and after 24 hours of adherent growth, naphthalimide-polyamine derivative 6c, cyclosporine A (CsA) was added alone or in combination. The final concentration of single drug is CsA (5 μM), CsA (10 μM), CsA (20 μM), 6c (5 μM), 6c (10 μM), 6c (20 μM); the final concentration of combined drug is 6c (5 μM) + CsA (5 μM), 6c(5μM)+CsA(10μM), 6c(5μM)+CsA(20μM), 6c(10μM)+CsA(5μM), 6c(10μM)+CsA(10μM), 6c(10μM)+CsA(20μM), ...

Embodiment 2

[0089] Example 2: In vivo biological activity evaluation of naphthalimide-polyamine derivative 6c and cyclosporine A (CsA) combined use

[0090] Test nine:

[0091] H22 liver cancer cells from mice (Balb / c mice) were extracted from the abdominal cavity, centrifuged at 1000r / min for 5 minutes, the supernatant was discarded, and washed with pre-cooled saline until no blood remained, usually three times. Each mouse (the mouse is 6 weeks old and weighs about 20g) was inoculated with H22 cells in the tail vein, and the number of cells was 2×10 6. Tumor-bearing mice were divided into four groups, namely blank control group, naphthalimide-polyamine derivative 6c (2mg / kg / day) group, cyclosporine A (CsA, 25mg / kg / day) group and combined Medication group (6c2mg / kg / day+CsA 25mg / kg / day). Naphthalimide-polyamine derivative 6c was administered by tail vein injection, and cyclosporin A (CsA) was administered by intragastric administration for 12 consecutive days. After the experiment, acc...

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PUM

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Abstract

The invention belongs to the technical field of medicinal chemistry, and specifically relates to the application of naphthalimide-polyamine derivatives combined with cyclosporine A in the preparation of antitumor drugs. The present invention provides an application of naphthalimide-polyamine derivatives in combination with cyclosporin A in the preparation of antitumor drugs through the combined use of naphthalimide-polyamine derivatives and cyclosporine A. The test results prove that, compared with the single-drug group, the combined drug can significantly inhibit the in vivo metastasis of liver cancer cells and significantly improve the anti-tumor activity of the single-drug group. At the same time, compared with the single-drug group, combined administration can improve the survival rate of tumor-bearing mice. The doses of the two drugs can be significantly reduced after combined administration, and the anti-tumor effect is significantly improved, and the toxicity to normal liver cells is lower than that of liver cancer cells. Combination of cyclosporine A and naphthalimide-polyamine derivative 6c may become a new method for the treatment of patients with liver cancer.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to the application of naphthalimide-polyamine derivatives combined with cyclosporine A in the preparation of antitumor drugs. Background technique [0002] Liver cancer is a malignant tumor of the liver, which is divided into primary liver cancer and secondary liver cancer. Liver cancer is one of the most common malignant tumors and the leading cause of cancer death. Liver cancer can be caused by chronic infection with diseases such as hepatitis B (HBV), hepatitis C (HCV), nonalcoholic steatohepatitis (NASH), or alcoholic steatohepatitis (ASH). Most liver cancers are found in patients with long-term inflammatory liver damage and cirrhosis, and are usually diagnosed at advanced stages. At present, there are few targeted therapy drugs for liver cancer. Therefore, there is an urgent need to explore new and effective therapeutic strategies. [0003] Cyclospor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/13A61P35/00A61P35/04A61K31/473
CPCA61K38/13A61K31/473A61P35/00A61P35/04A61K2300/00
Inventor 代付军王超杰谢松强徐小娟王玉霞王森震戈超超冯永丽车得路范荣辉曹越高梦柯
Owner HENAN UNIVERSITY
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