Anti-cancer drug, anti-cancer drug composition, and preparation method and application thereof

A technology of anticancer drugs and compositions, applied in the field of biomedicine, can solve the problems of poor selectivity, large toxic and side effects, etc.

Inactive Publication Date: 2021-05-07
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In view of the above problems, the present invention provides an anticancer drug, an anticancer drug composition and its application, which are used to at least partially solve the technical problems of traditional chemotherapy drugs such as poor selectivity and large toxic and side effects

Method used

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  • Anti-cancer drug, anti-cancer drug composition, and preparation method and application thereof
  • Anti-cancer drug, anti-cancer drug composition, and preparation method and application thereof
  • Anti-cancer drug, anti-cancer drug composition, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] In vitro anticancer evaluation of 2-amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole and its combination with phenylboronic acid polymer

[0045] MTT method was used to test the anti-cancer effect in vitro: take cancer cells (HeLa) and add them to 96-well plates, incubate in the incubator for 24 hours, add 100 μL of cell solution to each well, and inoculate 6×10 cells per well. 3 up to 8×10 3 , and the number of inoculations per well was approximately the same. 2-Amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole (Formula I) and the composition are configured to a concentration of 0.5 mg / mL, where The solvent used for the structure of the coordination interaction is DMF, wherein in the anticancer drug composition 2-amino-5-[(5-nitro-2-thiazolyl) thio]-1,3,4-thiadiazole and The ratio of the amount of phenylboronic acid in the phenylboronic acid polymer is 1:1, the degree of polymerization of the segment where the phenylboronic acid is located in the phenylboron...

Embodiment 2

[0047] Correlation Evaluation of Proton Motive Potential of 2-amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole

[0048] The proton kinetic potential related experiments were evaluated by the MTT method. Take 5 centrifuge tubes, add 10mL medium with serum in it, adjust the pH value with 1M hydrochloric acid and 1M sodium hydroxide, adjust to 5.4, 6.4, 7.4, 8.4, 9.4 respectively for use. Take cancer cells (HeLa) and add them to 96-well plates, incubate in the incubator for 24 hours, add 100 μL of cell solution to each well, and inoculate 6×10 cells per well. 3 up to 8×10 3 , and the number of inoculations per well was approximately the same. 2-Amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole (Formula I) was formulated at a concentration of 0.5 mg / mL. Take culture media with different pH values, and prepare media containing different concentrations of anticancer drugs. The concentration of anticancer drugs is 0.25 μg / mL to 10 μg / mL. Cancer drug medium, incubated in ...

Embodiment 3

[0050] Evaluation of membrane potential change of 2-amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole and its composition

[0051] The mitochondrial membrane potential detection kit JC-1 was used to stain the cells and observe the color change with a fluorescence microscope to evaluate the membrane potential. The kit JC-1 was purchased from Shanghai Beyond Biotechnology Co., Ltd., model C2006. Take cancer cells (HeLa) and add them to 24-well plates, incubate in the incubator for 24 hours, add 400 μL of cell solution to each well, and inoculate 2×10 cells per well. 4 to 4×10 4 , and the number of inoculations per well was approximately the same. Aspirate the original medium, add the prepared 2-amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole (Formula I) at a concentration of 10 μg / mL for culture medium and incubated for 4 h in the incubator. Take an appropriate amount of JC-1 (200X), and dilute JC-1 by adding 8 mL of ultrapure water to every 50 μL of JC-1 (200X). V...

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Abstract

The invention provides an anti-cancer drug, an anti-cancer drug composition, and a preparation method and application thereof. The anti-cancer drug comprises 2-amino-5-[(5-nitro-2-thiazolyl) thio]-1, 3, 4-thiadiazole. The anti-cancer drug composition comprises 2-amino-5-[(5-nitro-2-thiazolyl) thio]-1, 3, 4-thiadiazole and phenylboronic acid polymer. The 2-amino-5-[(5-nitro-2-thiazolyl) thio] -1, 3, 4-thiadiazole has broad-spectrum anticancer property, has obvious inhibiting effect on various cancers, and has lower toxicity to normal cells than cancer cells. The small molecule has simple structure and low hemolysis rate. The phenylboronic acid polymer in the anti-cancer drug composition is used as an auxiliary material, and is combined with the anti-cancer drug through donor-receptor interaction to help deliver the drug into cells; and the phenylboronic acid is sensitive to excessive active oxygen generated in cancer cells, and the excessive active oxygen can selectively release the drug, thereby enhancing the anticancer effect.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to an anticancer drug, an anticancer drug composition, a preparation method and application thereof. Background technique [0002] Cancer is a major disease that seriously endangers human life in today's society. In recent years, people have adopted a variety of methods to treat cancer, including surgery, radiation therapy, chemotherapy, hormone therapy and so on. Although various treatments have certain effects on cancer treatment, chemotherapy, as a systemic treatment, plays an important role in the treatment of cancer. However, there are still many problems with the chemotherapy drugs currently used in clinical practice. For example, the rapid clearance and poor selectivity of the drugs will reduce the efficacy of the drugs, and at the same time cause systemic toxicity, large toxic and side effects, and drug resistance will occur when the drug is used for a long time. There...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/433A61P35/00A61K47/59
CPCA61K31/433A61P35/00A61K47/59
Inventor 尤业字古晗聂旋张泽夏磊高凡黄伟强
Owner UNIV OF SCI & TECH OF CHINA
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