Metallic fullerene compound as well as preparation method and applications thereof

A technology of metallofullerenes and complexes, applied in the field of medicine, can solve the problems of toxic side effects, lack of specificity, large dosage of chemotherapy drugs, etc., and achieve the effect of high curative effect and small dosage

Inactive Publication Date: 2017-01-04
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the research and development of anticancer drugs is facing serious challenges. The reason is that chemotherapy drugs are used in large amounts, most of which lack specificity, and cause serious side effects on both cancerous and normal tissues. In order to improve the curative effect of anticancer drugs and overcome the above deficiencies, drugs Targeted therapy has broad prospects in improving efficacy and reducing side effects

Method used

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  • Metallic fullerene compound as well as preparation method and applications thereof
  • Metallic fullerene compound as well as preparation method and applications thereof
  • Metallic fullerene compound as well as preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1, f-Gd@C 82 - Preparation of HSA complex:

[0055] Gadolinium metallofullerenes (f-Gd@C 82 ) and human serum albumin HSA as an example, f-Gd@C 82 Self-prepared by the laboratory, gadolinium metallofullerene is reacted with hydrogen peroxide and ammonia water to generate hydroxyl and amino derivatives. The specific preparation method is as follows: Gd@C 82 Nano powder (references Carbon, 2013,65,175) in hydrogen peroxide (mass concentration of 30% H 2 o 2 Aqueous solution) and ammonia water under the action of oxidation reaction to obtain the Gd@C modified amino group / hydroxyl group outside the cage 82 Water-soluble metallofullerene single-crystal nanoparticles, that is, gadolinium metallofullerene (f-Gd@C 82 ).

[0056] Dissolve 10mg of human serum albumin HSA in PBS buffer solution, add excess EDC / NHS to activate for 30min, add 10mg of f-Gd@C 82 After reacting for 4 hours, the small molecules were removed by dialysis, and the unreacted substances were s...

Embodiment 2

[0057] Example 2, f-Gd@C 82 -HSA complex in vivo magnetic resonance imaging and tumor treatment experiments:

[0058] 1) Establish an animal model of tumor-bearing mice:

[0059] Extract ascites from mice inoculated with H22 liver cancer cell line in the peritoneal cavity, centrifuge to remove the supernatant, and count the inoculated cells at a concentration of 10 7 50 μL of the cell suspension / mL was subcutaneously placed on the right thigh of each mouse. After 5-7 days of growth, the tumor size is about 5 mm for experiments.

[0060] 2) In vivo magnetic resonance imaging and tumor treatment experiments:

[0061] Inject f-Gd@C via tail vein 82 -100-150 μL of HSA complex (concentration: 1-10 mM) in tumor-bearing mice. Radiofrequency pulses were applied to the tumor site under a magnetic field for 10min-2h, the intensity of the radiofrequency pulses was 5-7mW, and the imaging conditions of tumor tissue, kidney and liver were collected at each time point.

[0062] Figur...

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Abstract

The invention relates to a metallic fullerene compound as well as a preparation method and applications of the metallic fullerene compound. The metallic fullerene compound is micro-nano particles obtained by compounding metallic fullerene or a derivative of metallic fullerene with a medical carrier through covalent bonds or non-covalent bonds. The preparation method of the metallic fullerene compound comprises the following step: bonding metallic fullerene to the medical carrier through the non-covalent effect or bonding the derivative of metallic fullerene with the medical carrier through the covalent effect. As the medicine for realizing the targeted diagnosis and / or treatment on tumor, the metallic fullerene compound is safe and non-toxic, has the aggregating size being 1-500 nm in an aqueous solution, can be effectively gathered to the tumor location through blood circulation by utilizing the EPP effect, has no toxic or side effect for the normal biological tissue, and has extremely high biosecurity, the targeted diagnosis and / or treatment on malignant tumor is realized, the use dosage of the antitumor drugs is reduced, and meanwhile, the metallic fullerene compound has high tumor targeting property, and has a broad prospect in the diagnosis and treatment integrated application of tumor.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a metal fullerene compound and its preparation method and application. Background technique [0002] In recent years, the morbidity and mortality of cancer are on the rise. At least 7 million people die of cancer every year in the world, of which about 1.3 million are in China. In the next 10 years, the incidence and mortality of cancer in China will continue to rise, seriously threatening human health. [0003] After more than half a century of continuous development and improvement, chemotherapy has become one of the important means of comprehensive treatment of malignant tumors. However, the research and development of anticancer drugs is facing serious challenges. The reason is that chemotherapy drugs are used in large amounts, most of which lack specificity, and cause serious side effects on both cancerous and normal tissues. In order to improve the curative effect of an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/00A61K49/04A61K49/08A61K33/44A61K47/04A61K47/42A61K47/36A61K47/40A61K47/48A61P35/00
Inventor 王春儒甄明明舒春英
Owner INST OF CHEM CHINESE ACAD OF SCI
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