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Cation lipid containing imidazolium salt and macrocyclic polyamines, transgenetic vector and method for preparing same

A technology of cationic lipids and transgenic carriers, applied in gene therapy, using carriers to introduce foreign genetic material, pharmaceutical formulations, etc., can solve the problems of high cytotoxicity and achieve the effect of strong encapsulation ability and low cytotoxicity

Inactive Publication Date: 2010-06-16
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The previous research of the inventor of this patent application (A novel macrocyclic polyamine cationic lipid containing animidazolium salt group: Synthesis, characterization and its transfection activity as a genedelivery vector. Chem. Bio1. Drug Des., 2008, 71 (3): 224-229 .) It was found that compounds containing imidazolium salts and macrocyclic polyamines have a strong ability to wrap and concentrate genes at a certain nitrogen-phosphorus ratio (N / P), and have a certain transfection ability, but the cytotoxicity is relatively large

Method used

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  • Cation lipid containing imidazolium salt and macrocyclic polyamines, transgenetic vector and method for preparing same
  • Cation lipid containing imidazolium salt and macrocyclic polyamines, transgenetic vector and method for preparing same
  • Cation lipid containing imidazolium salt and macrocyclic polyamines, transgenetic vector and method for preparing same

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: the synthesis of compound 3a

[0041] Compound 3a is synthesized from compound 2a—cholesteryl chloroacetate, imidazole, and potassium iodide. The structural formula of compound 3a is as follows:

[0042]

[0043] Raw materials include cholesterol chloroacetate, imidazole, potassium iodide and solvent, cholesterol chloroacetate 0.01mol (4.74g), imidazole 0.2mol (13.62g), potassium iodide 0.0005mol (0.08g), solvent from dimethyl sulfoxide and no Composition of water chloroform, dimethyl sulfoxide 10ml, anhydrous chloroform 60ml. Add the above-mentioned solvent, cholesterol chloroacetate, imidazole and potassium iodide into the reaction vessel at room temperature (25°C) and normal pressure, and stir and mix. After the solid matter is completely dissolved, heat to the reflux temperature, and maintain this temperature for reflux reaction. The reaction time is 4 hours. After the reaction is completed, cool to room temperature, then add 2.80 g of anhydrous po...

Embodiment 2

[0044] Embodiment 2: the synthesis of compound 3b

[0045] Compound 3b is synthesized from compound 2b—saponin chloroacetate, imidazole, and potassium iodide. The structural formula of compound 3b is as follows:

[0046]

[0047] Raw material comprises saponin chloroacetate, imidazole, potassium iodide and solvent, saponin chloroacetate 0.013mol (6.30g), imidazole 0.13mol (9.10g), potassium iodide 0.00065mol (0.10g), solvent dimethyl sulfoxide and Composed of anhydrous chloroform, dimethyl sulfoxide 10ml, anhydrous chloroform 40ml. Add the above solvent, saponin chloroacetate, imidazole and potassium iodide into the reaction vessel at room temperature (25°C) and normal pressure and stir and mix. After the solid matter is completely dissolved, heat to reflux temperature and maintain this temperature for reflux Reaction, the reaction time is 6 hours, after the reaction is completed, cool to room temperature, then add 3.00 g of anhydrous potassium carbonate to neutralize the ...

Embodiment 3

[0048] Embodiment 3: the synthesis of compound 5a

[0049] Compound 5a is synthesized from compound 3a and 1-p-bromomethylbenzyl-4,7,10-three (tert-butoxycarbonyl)-1,4,7,10-tetraazacyclododecane, compound 5a The structural formula is as follows:

[0050]

[0051] Raw materials include compound 3a prepared in Example 1, 1-p-bromomethylbenzyl-4,7,10-tri(tert-butoxycarbonyl)-1,4,7,10-tetraazacyclododecane and Solvent anhydrous acetonitrile, compound 3a 2.00mmol (1.04g), 1-p-bromomethylbenzyl-4,7,10-tris(tert-butoxycarbonyl)-1,4,7,10-tetraazacyclo Dodecane 3.30mmol (2.16g), anhydrous acetonitrile 40mL. At room temperature (25°C) and normal pressure, the above-mentioned anhydrous acetonitrile, compound 3a and 1-p-bromomethylbenzyl-4,7,10-tri(tert-butoxycarbonyl)-1,4,7,10 - Tetraazacyclododecane is added to the reaction vessel and stirred and mixed. After the solid matter is completely dissolved, it is heated to reflux temperature, and the temperature is maintained for reflux ...

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Abstract

The invention provides the cation lipid containing imidazolium salt and macrocyclic polyamines. The cation lipid has a structural formula below. In the formula, R is cholesteryl or saponin group. The transgenetic vector is prepared from the cation lipid containing imidazolium salt and macrocyclic polyamines, the cholesterol and deionized water; and in the transgenetic vector, the molar concentration of the cation lipid containing imidazolium salt and macrocyclic polyamines is 1 to 4mmol / L / , and the molar ratio of the cation lipid containing imidazolium salt and macrocyclic polyamines to the cholesterol is 1-2:1.

Description

technical field [0001] The invention relates to a cationic lipid, a transgene carrier containing the cationic lipid and a preparation method thereof. Background technique [0002] With the continuous development of biochemistry and molecular biology, people's understanding of the functions of nucleic acids (DNA, RNA) is deepening, and at the same time, they have further understanding of the molecular mechanisms of various diseases. Thousands of known human diseases are related to genes, including congenital genetic diseases related to single genes and acquired diseases related to polygenes. Most acquired diseases are caused by various internal and external factors acting on the genetic material of the human body to make its function disorder. The main cause of disease is gene defect and gene deletion. The appropriate foreign gene is introduced into human cells to make up for the defect or missing gene, express the corresponding protein, and fundamentally eliminate the inter...

Claims

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Application Information

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IPC IPC(8): A61K48/00C12N15/63C07J43/00C07J71/00
Inventor 余孝其黄清东朱文
Owner SICHUAN UNIV
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