Water-soluble fullerene and application thereof

A fullerene, water-soluble technology, applied in fullerenes, organic active ingredients, medical preparations of non-active ingredients, etc., can solve the problems of large side effects, can not well inhibit tumor cell proliferation, etc., and achieve small side effects. , good physical and chemical stability, rich source of raw materials

Inactive Publication Date: 2013-01-30
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of the above situation, in order to solve the defects of the prior art, the purpose of the present invention is to provide a kind of water-soluble fullerene and its application, which can effectively solve the problems that the existing tumor treatment drugs have large side effects and cannot well inhibit the proliferation of tumor cells

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1) Add 20ml of ethylenediamine and 1g of sodium hydroxide to 60ml of a mixed solution of water and absolute ethanol with a weight ratio of 1:5. After stirring evenly, add 50ml of a toluene solution of 1mg / ml fullerene dropwise. ℃, 200r / min, stirred and reacted for 7 days, removed the toluene in the upper layer, distilled off the mixed solution of water and absolute ethanol, then filtered and washed 15 times with 500ml of absolute ethanol, and dried in vacuum at 40°C for 48h to obtain amino Fullerene;

[0033] 2) Weigh 50 mg of the above-mentioned aminofullerene, 80 mg of hyaluronic acid, 160 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride, and 120 mg of N-hydroxysuccinimide in Mix well in 20ml of formamide, stir and react at 40°C and 200r / min for 24h, then filter and wash with 500ml of absolute ethanol for 20 times to remove unreacted 1-ethyl-(3-dimethylaminopropyl) Carbodiimide hydrochloride, N-hydroxysuccinimide and hyaluronic acid were dried in vacu...

Embodiment 2

[0035] 1) Add 20ml of 1,3-propylenediamine and 1g of sodium hydroxide to 60ml of a mixed solution of water and absolute ethanol with a weight ratio of 1:5, stir evenly, and then add 1mg / ml of fullerene in benzene solution dropwise 50ml, stirred and reacted at 30°C and 200r / min for 7 days, removed the benzene in the upper layer, distilled off the mixed solution of water and absolute ethanol, then washed with 500ml methanol for 15 times, and dried in vacuum at 20°C for 72h. Get aminofullerene;

[0036] 2) Weigh 50 mg of the above-mentioned aminofullerene, 80 mg of hyaluronic acid, 160 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride, and 120 mg of N-hydroxysuccinimide in 20ml of N,N-dimethylformamide was mixed evenly, stirred and reacted at 40°C and 200r / min for 24h, and then washed with 500ml of acetone for 20 times by suction filtration to remove unreacted 1-ethyl-(3-dimethylformamide Aminopropyl) carbodiimide hydrochloride, N-hydroxysuccinimide and hyaluronic...

Embodiment 3

[0038] 1) Add 20ml of 1,6-hexamethylenediamine and 1g of sodium hydroxide into 60ml of a mixed solution of water and absolute ethanol with a weight ratio of 1:5. After stirring evenly, add 1mg / ml fullerene tetrahydrofuran dropwise 50ml of the solution, stirred and reacted at 30°C and 200r / min for 7 days, removed the tetrahydrofuran in the upper layer, distilled off the mixed solution of water and absolute ethanol, then filtered and washed 15 times with 500ml of methanol, and dried in vacuum at 60°C for 24h , to get aminofullerene;

[0039] 2) Weigh 50 mg of the above-mentioned aminofullerene, 80 mg of hyaluronic acid, 160 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride, and 120 mg of N-hydroxysuccinimide in 20ml of N,N-dimethylformamide was mixed evenly, stirred and reacted at 40°C and 200r / min for 24h, and then washed with 500ml of acetone for 20 times by suction filtration to remove unreacted 1-ethyl-(3-dimethylformamide Aminopropyl) carbodiimide hydroc...

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Abstract

The invention relates to a water-soluble fullerene and an application thereof; and problems that the traditional tumor therapeutic drug has a large side effect and cannot very well suppress tumor cell proliferation can be effectively solved; and a technical scheme for solving the problems is as follows: on the basis that the original fullerene is purified, the purified fullerene reacts with an ammoniation reagent; and after an amino with stronger reaction activity is connected to the surface of the fullerene, the fullerene reacts with a hyaluronic acid, so as to generate fullerene-hyaluronic acid polymer, wherein the mass ratio of the hyaluronic acid and the fullerene is 0.18-0.25:1; and the water-soluble fullerene provided by the invention has the advantages of good physical and chemical stability, easiness for satisfying preparation conditions, rich raw material sources, low cost and small side effect and is an innovation on a tumor therapeutic drug carrier.

Description

technical field [0001] The invention relates to the field of chemical industry, in particular to a water-soluble fullerene and its application. Background technique [0002] The discovery of the fullerene family, the third allotrope of carbon, is one of the most important breakthroughs in the history of natural science in the last century. Kroto and others also won the 1996 Nobel Prize in Chemistry for their pioneering work in the study of fullerenes. Fullerene has attracted much attention due to its unique structure and properties. In the past ten years, scientists from almost all famous universities and research institutes in the world have carried out research related to fullerene. It has become a common concern of researchers in physics, chemistry, materials and life sciences. The important scientific significance of fullerene molecules was named "Star Molecule" in 1991 by the American "Science" magazine. Among nanomaterials, carbon nanomaterials including fullerenes ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/08C01B31/00A61K31/728A61K41/00A61K47/02A61K47/36A61P35/00C01B32/154
Inventor 张红岭史进进张振中刘艳叶凡高君刘瑞瑗马柔柔余晓媛张静王蕾侯琳
Owner ZHENGZHOU UNIV
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