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
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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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