Water-soluble fullerenes derivates, composition and application thereof in preparation of medicament for inhibiting tumor growth and metastasis

A technology of fullerene derivatives and tumor drugs, which is applied in the direction of drug combinations, anti-tumor drugs, carbon active ingredients, etc., can solve the problems of low solubility, violent reactions, toxic and side effects, etc., and achieve inhibition of tumor metastasis, small dosage, and high toxicity low effect

Inactive Publication Date: 2009-04-01
INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, surgical resection, chemotherapy and radiotherapy are the main methods for treating malignant tumors, but these methods all have their insurmountable defects: surgery can only remove the tumor mass visible to the naked eye but cannot remove the residual tumor cells; chemotherapy and radiotherapy have toxic and side effects Very strong, while inhibiting tumor growth, it also damages the normal tissues and organs of the body, thereby sharply reducing the quality of life of patients; for example, cyclophosp

Method used

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  • Water-soluble fullerenes derivates, composition and application thereof in preparation of medicament for inhibiting tumor growth and metastasis
  • Water-soluble fullerenes derivates, composition and application thereof in preparation of medicament for inhibiting tumor growth and metastasis
  • Water-soluble fullerenes derivates, composition and application thereof in preparation of medicament for inhibiting tumor growth and metastasis

Examples

Experimental program
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Effect test

Embodiment 1

[0063] Determination of the hydroxyl number of fullerenols

[0064] The XPS spectrum of Cls electrons of fullerenols, the relative strength between C-C and C-O bonds was used to analyze the number of hydroxyl groups in fullerenols. After Gaussian fitting analysis, it is shown that there are mainly three kinds of different carbon atoms in the molecule: the peak position at 284.8eV is the binding energy of the sp2 hybridized carbon atom (C-C) that is not connected to other groups; the peak at 286.6_eV is The hydroxylated carbon atom (C-OH), the peak around 288.19_eV belongs to the peak of ketone or epoxy structure C=O. Thus, the number of hydroxyl groups of the fullererol is obtained, and the fullererol prepared by the method of the present invention is mainly controlled at 10-50, wherein 15-25 is the optimum value, the carbon cage is stable, and the water solubility is good.

Embodiment 2

[0066] Determination of particle size of nanoparticles

[0067] Fullerene C 60 (OH) x The particle size of the molecule is about 1 nm. In different solvent environments, fullerenol molecules agglomerate into nanoparticles by interacting with themselves or other macromolecules, and the size of the particles can be controlled by means of ultrasonic waves to form particles with a diameter distribution in the range of 1-400nm.

[0068] Dissolve fullererol in double distilled water or normal saline at a concentration of 200 μmol / L, take 10 μl and drop it on a flat mica sheet, and air-dry it. High-resolution atomic force microscopy (SPM-9500J3, SHIMAZU) confirmed the presence of fullerenol in saline solution with an average particle size of 167nm, see Figure 4 . In a solvent environment containing serum, fullerenol can form particles of 200-400nm by interacting with macromolecules such as albumin.

Embodiment 3

[0070] Determination of particle size of nanoparticles

[0071] C 60 (C(COOH) 2 ) 2 The particle size of the molecule is about 1 nm. In different solvent environments, fullerenol molecules agglomerate into nanoparticles by interacting with themselves or other molecules, and the size of the particles can be controlled by means of ultrasonic waves to form particles with a diameter distribution range of 1-400nm.

[0072] Will C 60 (C(COOH) 2 ) 2 Dissolve in double distilled water or normal saline at a concentration of 200 μmol / L, take 10 μl and drop it on a flat mica sheet, and air-dry. Scanning with a 2.5 μm probe of a high-resolution atomic force microscope (SPM-9500J3) at a scanning speed of 1 Hz. Profile software analysis showed that the average particle size of C60(C(COOH)2)2 in the aqueous phase was 118.0nm. see Figure 5 . In a solvent environment containing serum, particles of 200-400nm can be formed by interacting with macromolecules such as albumin.

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Abstract

The invention provides a water-soluble fullerene derivative, composite and the applications in the preparation process of medicament used for inhibiting growth and transfer of tumor; the derivative is fullerols presented by a general formula: C60OxHy; wherein, y is more than 10 and less than or equal to x; x is less than 50 and more than or equal to y; alternatively, the derivative is fullerene carboxyl derivative presented by the general formula C60(C(COOH)2)n; wherein, n is equal to 1-3; the tumor inhibiting composite comprises the grains of the water-soluble fullerene derivative and pharmaceutically acceptable carrier. The invention has the advantages that: compared with cyclophosphamide, cisplatin, paclitaxel, and the like, which are generally applied to clinic at present; the fullerols and carboxylic fullerene nano grains have small dosage, low toxicity and can inhibite the growth and transfer of the tumor.

Description

technical field [0001] The invention relates to a novel nanometer material and its application in biomedicine. Specifically, involving fullerenol particles [C 60 o x h y ] n (10<Y≤X<50, n=15-50) and fullerene carboxylic acid derivative C60(C(COOH) 2 ) n (n=an integer of 1-4) and its application in inhibiting tumor growth and metastasis. Background technique [0002] Malignant tumor is an important disease that threatens human health and has become the main cause of human death. In China, lung cancer, gastric cancer, liver cancer and breast cancer are the tumors with the highest incidence rates. Statistics show that in China, the incidence rate of lung cancer is about 27 / 10,000, the incidence rate of gastric cancer is 26.8 / 10,000, and the incidence rate of breast cancer is about 16.39 / 10,000. At present, at least 7 million people in the world die of cancer, of which about 1.3 million are in my country. Tumor is a common and frequently-occurring disease that ser...

Claims

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Application Information

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IPC IPC(8): C01B31/02A61K33/44A61P35/00
Inventor 陈春英赵宇亮叶昶焦芳李炜
Owner INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI
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