Metal fullerol and its pharmaceutical use for inhibiting tumour growth

The technology of a tumor drug, fullerol, is applied in the direction of anti-tumor drugs, active ingredients of heavy metal compounds, drug combinations, etc. It can solve the problems of ineffectiveness, research and application limitations, etc., and achieve low toxicity, high tumor inhibition rate, and small dosage Effect

Active Publication Date: 2007-03-28
INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Because fullerenes and many of their derivatives are hydrophobic and cannot interact with "target molecules" in the human body, their research and application in the field of biochemistry are greatly limited

Method used

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  • Metal fullerol and its pharmaceutical use for inhibiting tumour growth
  • Metal fullerol and its pharmaceutical use for inhibiting tumour growth
  • Metal fullerol and its pharmaceutical use for inhibiting tumour growth

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Gd@C 2m (OH) x preparation of

[0052] First step Gd@C 2m Synthesis

[0053] High-purity (>99.999%) Gd 2 o 3 Mix it with high-purity graphite powder (>99.999%) according to the atomic ratio Gd:C=0.5~3:100, and press it into a mold to make a graphite-metal hybrid electrode; or drill a graphite rod with a diameter of 6~20mm and fill it with oxide Gadolinium yields graphite-metal hybrid electrodes. After high-temperature sintering at 1000-2000°C, use the inert gas arc discharge method to synthesize metallofullerene Gd@C 2m . The inert gas is He or Ar, the pressure is 50-600 Torr, and the current is 80-500A.

[0054] The second step Gd@C 82 and Gd@C 60 separation and purification of

[0055] a. Using high temperature reflux plus high temperature and high pressure two-step high-efficiency extraction method to extract and separate carbon nano-like substances. Firstly, the arc-shaped discharge soot is refluxed in toluene at 100-200°C for 12-24 hours, and then extra...

Embodiment 2

[0066] Determination of Gd@C 82 (OH) 22 and Gd@C 82 (OH) 12 hydroxyl number

[0067] Gd@C 82 (OH) 22 (a) and Gd@C 82 (OH) 12 The XPS spectrum of C1s electrons in (b) is shown in Fig. 3, and the relative intensities between C–C and C–O bonds are used to analyze the Gd@C 82 (OH) x The number of hydroxyl groups in . The Gaussian fitting analysis of the solid line in Figure 2 shows that there are two different carbon atoms in the molecule: the peak position at 284.4eV is the binding energy of the sp2 hybridized carbon atom (C-C) that is not connected to other groups; the peak position at 285.3 The eV peaks are hydroxylated carbon atoms (C-OH).

Embodiment 3

[0069] La@C 2m (OH) x preparation of

[0070] Using Gd@C prepared as above 82 A similar method was used to prepare La@C 82 and La@C 60 .

[0071] (1) Metal fullerenol La@C 82 (OH) 18 Synthesis

[0072] Using the NaOH method, the La@C 82 React with 28% NaOH solution, and after a series of separation and purification processes, after removing NaOH, La@C with a purity greater than 99.99% is obtained 82 (OH) 18 The product was stored freeze-dried.

[0073] (2) Metal fullerenol La@C 60 (OH) 22 Synthesis

[0074] Using the NaOH method, the La@C 60 React with 35% NaOH solution, and then go through a series of separation and purification processes to remove NaOH to obtain La@C with a purity greater than 99.99%. 60 (OH) 22 The product was stored freeze-dried.

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Abstract

The invention relates to metal fullerols and its application in preparing inhibition tumor medicine. Its general formula is M@C2m(OH)x, which M can be Gd, La, etc, m=41 or 30, x is not less than 10 and less than 50; it also can be M@C2mOxHy. Compared with clinic common using cyclophosphamide, cisplatin, paclitaxel etc, the metal fullerols M@C2m(OH)x or M@C2mOxHy has the advantages of little use level, low toxicity, high tumor inhibition ratio.

Description

technical field [0001] The invention relates to a novel nanometer material and its application in biomedicine. Specifically, it involves the general formula M@C 2m (OH) x The metal fullerenol nanoparticles and their application in the preparation of drugs for inhibiting tumor growth, wherein M is selected from rare earth metals such as Gd and La, and 10≤X<50. Background technique [0002] Malignant tumor is an important disease that threatens human health and has become the main cause of human death. In China, liver cancer, lung cancer, gastric cancer and breast cancer are the tumors with the highest incidence rates. At present, at least 7 million people die of cancer every year in the world, of which about 1.3 million are in my country. In addition to causing death, cancer also imposes a huge economic burden on families and society. The continuous discovery and in-depth research of new anti-tumor drugs have made tumor chemotherapy a subject and the birth of medical ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/00C07C35/44A61K31/28A61K31/045A61K33/04A61P35/00
Inventor 赵宇亮陈春英邢更妹
Owner INST OF HIGH ENERGY PHYSICS CHINESE ACADEMY OF SCI
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