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Cytolysosome-targeting anticancer cluster and preparation method thereof

A technology targeting cells and lysosomes, applied in the chemical industry, can solve the problems of uncontrollable dosage and poor targeting, and achieve the effect of rich structure types and good stability

Active Publication Date: 2021-11-19
ANHUI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Chemotherapy drugs currently used in cancer treatment suffer from poor targeting and uncontrollable dosing
Poor targeting can simultaneously kill tissue cells that normally undergo cell division, such as intestinal mucosal cells, and excessive doses of anticancer drugs can cause serious diseases such as skin cancer

Method used

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  • Cytolysosome-targeting anticancer cluster and preparation method thereof
  • Cytolysosome-targeting anticancer cluster and preparation method thereof
  • Cytolysosome-targeting anticancer cluster and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The synthesis of anticancer nanoclusters, the steps are as follows: chloroauric acid and 6-thioguanine are mixed uniformly at room temperature, wherein the molar ratio of chloroauric acid to 6-thioguanine is 1:40, and 1.5 gamma rays are irradiated. Anticancer nanoclusters were obtained after h, in which the radioactive source of gamma ray radiation 60 Co, dose rate 6kGy / h (provided by Beijing Hongyi Sifang Radiation Technology Co., Ltd.). Ultrafiltration was performed with a 3KDa ultrafiltration tube to finally obtain purified anticancer nanoclusters.

Embodiment 2

[0026] The synthesis of anticancer nanoclusters, the steps are as follows: chloroauric acid and 6-thioguanine are mixed uniformly at room temperature, wherein the molar ratio of chloroauric acid to 6-thioguanine is 10:1, and 2.5 gamma rays are irradiated Anticancer nanoclusters were obtained after h, in which the radioactive source of gamma ray radiation 60 Co, dose rate 6kGy / h (provided by Beijing Hongyi Sifang Radiation Technology Co., Ltd.). Ultrafiltration was performed with a 3KDa ultrafiltration tube to finally obtain purified anticancer nanoclusters.

Embodiment 3

[0028] Synthesis of anticancer nanoclusters, the steps are as follows: mix chloroauric acid and 6-thioguanine at room temperature, wherein the molar ratio of chloroauric acid to 6-thioguanine is 1:2, and irradiate with gamma rays for 2h After obtaining anticancer clusters, the radioactive source of γ-ray radiation 60 Co, dose rate 6kGy / h (provided by Beijing Hongyi Sifang Radiation Technology Co., Ltd.). Ultrafiltration was performed with a 3KDa ultrafiltration tube to finally obtain purified anticancer clusters.

[0029] Taking the anticancer cluster prepared in Example 3 as an example to perform related performance tests, wherein:

[0030] figure 1 For the mass spectrogram of anticancer clusters, 2mL of 1.5mmol / L anticancer nanoclusters were purified with a 3KDa ultrafiltration tube, and a high-resolution mass spectrometer (WatersQ-TOFpremier purchased from U.S. WatersQ-TOFpremier in negative ion mode was used) The world company conducts mass spectrometry test), and its m...

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Abstract

The invention discloses a cytolysosome-targeting anticancer cluster and a preparation method thereof. The anticancer cluster is prepared by mixing a small-molecular anticancer drug serving as a ligand with chloroauric acid and radiating a formed mixture with gamma rays. The prepared anticancer cluster is an 8e-structure anti-cancer nanocluster with precise atoms; the number of anti-cancer drugs in the nanocluster is precise, introduction of external lysosome targeting groups is not needed, the anti-cancer drugs can naturally penetrate through cell membranes to be enriched in lysosome, precise chemotherapy drug delivery is conducted, and cancer cells are effectively killed; and therefore, other diseases caused by excessive chemotherapeutic drugs in the body are avoided, and the nano-cluster directly synthesized by the anti-cancer drugs has an application value in realizing targeted quantitative administration and cancer treatment.

Description

technical field [0001] The invention relates to the technical field of chemical engineering, in particular to anticancer clusters targeting cell lysosomes and a preparation method thereof. Background technique [0002] The disadvantages of chemotherapy drugs currently used in cancer treatment are poor targeting and uncontrollable dosage. Poor targeting can also kill tissue cells that normally undergo cell division, such as intestinal mucosal cells, and excessive doses of anticancer drugs can cause serious diseases such as skin cancer. Therefore, the technical problem to be solved by the present invention is to develop an anticancer drug capable of quantitative administration and strong targeting. Contents of the invention [0003] Based on the technical problems in the background technology, the present invention proposes anticancer clusters targeting cell lysosomes and a preparation method thereof, which have the advantages of quantitative administration and stronger tar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/52A61P35/00C07D473/24C08G83/00B82Y5/00B82Y40/00
CPCA61K45/00A61K31/52A61P35/00C07D473/24C08G83/008B82Y5/00B82Y40/00
Inventor 张忠洁刘璐
Owner ANHUI UNIVERSITY
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