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Polyamine cationic lipid, transgenic vector and preparation methods of polyamine cationic lipid and transgenic vector

A technology of cationic lipids and transgenic carriers, applied in other methods of inserting foreign genetic materials, using microcapsules, recombinant DNA technology, etc., can solve the problems of limited application, small immune response load, etc., and achieve easy control and preparation methods simple effect

Inactive Publication Date: 2018-08-24
NORTHWESTERN POLYTECHNICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the disadvantages of potential immune response and small load greatly limit its clinical application.

Method used

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  • Polyamine cationic lipid, transgenic vector and preparation methods of polyamine cationic lipid and transgenic vector
  • Polyamine cationic lipid, transgenic vector and preparation methods of polyamine cationic lipid and transgenic vector
  • Polyamine cationic lipid, transgenic vector and preparation methods of polyamine cationic lipid and transgenic vector

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0038]

[0039] Step 1, weigh formula 2 compound (0.86mmol), n-butylamine compound (0.86mmol), 1-hydroxybenzotriazole catalyst (1.72mmol), 1-ethyl-(3-dimethylaminopropyl Base) carbodiimide hydrochloric acid condensing agent (1.72mmol) and triethylamine (2.58mmol), add dichloromethane solvent 40mL to dissolve, react under nitrogen atmosphere for 8-10 hours, after the reaction is over, evaporate the solvent under reduced pressure , add 35mL of water, extract with dichloromethane (40mL x 2), combine the organic phases, wash with saturated brine, dry over anhydrous sodium sulfate, remove the solvent, and separate by silica gel column chromatography (petroleum ether / ethyl acetate volume ratio=4 / 1) Obtain a white solid to obtain the compound of formula 3a, yield: 89%;

[0040]

[0041] NMR 1 H NMR (400MHz, CDCl 3)δ7.67(s,2H),7.40(s,1H),6.18(brs,1H),4.43(s,4H),3.47(dd,J=3.0,7.1Hz,2H),1.65-1.60(m ,2H),1.47-1.38(m,2H),0.97(t,J=7.3Hz,3H);

[0042] NMR 13 C NMR (101MHz, CDCl ...

example 2

[0050]

[0051] Step 1, weigh formula 2 compound (0.86mmol), n-octylamine compound (0.86mmol), 1-hydroxybenzotriazole catalyst (1.72mmol), 1-ethyl-(3-dimethylaminopropyl Base) carbodiimide hydrochloric acid condensing agent (1.72mmol) and triethylamine (2.58mmol), add dichloromethane solvent 40mL to dissolve, react under nitrogen atmosphere for 8-10 hours, after the reaction is over, evaporate the solvent under reduced pressure , add 35mL of water, extract with dichloromethane (40mL x 2), combine the organic phases, wash with saturated brine, dry over anhydrous sodium sulfate, remove the solvent, and separate by silica gel column chromatography (petroleum ether / ethyl acetate volume ratio=4 / 1) Obtain a white solid to obtain the compound of formula 3b, yield: 91%;

[0052]

[0053] NMR 1 H NMR (400MHz, CDCl 3 )δ7.67(s,2H),7.39(s,1H),6.24(brs,1H),4.42(s,4H),3.44(dd,J=13.2,7.1Hz,2H),1.64-1.60(m ,2H),1.37-1.29(m,10H),0.87(t,J=6.8Hz,3H);

[0054] NMR 13 C NMR (101MHz, CD...

example 3

[0061]

[0062] Step 1, weigh formula 2 compound (0.86mmol), 1-dodecylamine compound (0.86mmol), 1-hydroxybenzotriazole catalyst (1.72mmol), 1-ethyl-(3-dimethyl Aminopropyl) carbodiimide hydrochloric acid condensing agent (1.72mmol) and triethylamine (2.58mmol), add 40mL of dichloromethane solvent to dissolve, react under nitrogen atmosphere for 8-10 hours, after the reaction is completed, evaporate under reduced pressure Remove the solvent, add 35mL of water, extract with dichloromethane (40mL x 2), combine the organic phases, wash with saturated brine, dry over anhydrous sodium sulfate, remove the solvent, and separate by silica gel column chromatography (petroleum ether / ethyl acetate volume ratio= 4 / 1) A white solid was obtained to obtain the compound of formula 3c, yield: 89%;

[0063]

[0064] NMR 1 H NMR (400MHz, CDCl 3 )δ7.67(s,2H),7.41(s,1H),6.13(brs,1H),4.44(s,4H),3.46(dd,J=13.2,7.1Hz,2H),1.64-1.61(m ,2H),1.38-1.24(m,18H),0.88(t,J=6.8Hz,3H);

[0065] NMR 13...

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PUM

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Abstract

The invention provides a polyamine cationic lipid and a transgenic vector comprising the polyamine cationic lipid. The invention further discloses preparation methods of the polyamine cationic lipid and the transgenic vector. The provided polyamine cationic lipid comprises hydrocarbyl chains at different lengths, benzene ring, triazole and a polyamine molecule, the provided polyamine cationic lipid acts with an auxiliary lipid dioleyl dimyristoyl phosphoethanolamine to form a cationic liposome, the cationic liposome has an excellent property of retarding DNA, the cytotoxicity is relatively low, moreover, the transfection efficiency is relatively high, and the preparation methods of the polyamine cationic lipid and the transgenic vector are simple and mature, and are easy to control.

Description

technical field [0001] The invention relates to a cationic lipid and a transgene carrier, in particular to a class of cationic lipid containing hydrocarbon chains, benzene rings, triazoles and polyamine compounds, a transgenic carrier containing the cationic lipid and a preparation method thereof. Background technique [0002] As one of the most cutting-edge medical methods, gene therapy has shown great power in the treatment of various major diseases such as cancer and AIDS. In the process of gene therapy, gene carrier plays a very important role. [0003] The naked DNA is relatively loose and bulky, and generally exists in the form of a stretched linear helix, and is negatively charged, so it is difficult for itself to enter the cell across the membrane. Even if a small amount of DNA enters the cell, it is easy before it reaches the nucleus for expression Degraded by intracellular nucleases. These unfavorable factors make it difficult for DNA molecules to perform effecti...

Claims

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Application Information

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IPC IPC(8): C07D249/04C12N15/88
CPCC07D249/04C12N15/88
Inventor 高永光骞爱荣党凯田野张文娟姜山峰赵欣罗晓庆
Owner NORTHWESTERN POLYTECHNICAL UNIV