Preparation method and application of cationization lentinan

A technology of lentinan and cationization, which is applied in the field of medicine, can solve the problems such as no immune regulation effect, and achieve the effect of uniform shape, stable structure and high-efficiency loading

Inactive Publication Date: 2017-05-24
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The molecular structure of lentinan contains a large number of active groups. The function of gene delivery can be realized by

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0012] Example 1

[0013] In the specific implementation of the present invention, the cationized lentinan can be: 1) Dissolve 100 mg of lentinan in 10 mL of deionized water, add 150 mg of potassium periodate while stirring, and react at 25°C and protected from light under nitrogen After 48h, add 5mL phosphate buffer solution containing 200μL of ethylenediamine. After the addition is completed within 1h, stir for 36h under nitrogen protection and avoid light. The reaction solution is dialyzed in ultrapure water for 3d to obtain activated lentinan reaction liquid;

[0014] 2) Add 2 mL of hydrochloric acid with a volume concentration of 3.7% containing 250 mg of polyethyleneimine to the activated lentinan reaction solution drop by drop, stir for 72 h in the dark under the protection of nitrogen at 25℃, and dialyze in ultrapure water 2d, freeze-drying, obtain polyethyleneimine modified lentinan, that is, cationized lentinan.

Example Embodiment

[0015] Example 2

[0016] In the specific implementation of the present invention, the cationic lentinan can also be: 1) Dissolve 100 mg of lentinan in 8 mL of dimethyl sulfoxide, then add 30 mg of carbonyl diimidazole and 100 μL of triethylamine, at 26°C under nitrogen protection Stir in the dark for 4 hours to obtain an activated lentinan reaction solution;

[0017] 2) Add 6 mL of dimethyl sulfoxide (DMSO) solution containing 100 mg of polyethyleneimine dropwise to the activated lentinan reaction solution, and stir for 24 hours at 23°C, protected from light, in ultrapure water under nitrogen protection After 2 days of dialysis, freeze-drying, polyethyleneimine-modified lentinan, that is, cationized lentinan, was obtained.

Example Embodiment

[0018] Example 3

[0019] In the specific implementation of the present invention, the cationic lentinan can also be: 1) Dissolve 100 mg of lentinan in 10 mL of dimethyl sulfoxide, add 10 mg of 4-dimethylaminopyridine and 400 mg of maleic anhydride, 50 Stir at ℃ for 24h, then add 10mg 1-ethyl(3-dimethylaminopropyl)carbodiimide hydrochloride and 5mg N-hydroxysuccinimide in sequence, stir and react for 4h, get activated lentinan reaction liquid;

[0020] 2) Add 300mg polyethyleneimine to the activated lentinan reaction solution, stir for 48h in the dark under the protection of nitrogen, dialyze it in ultrapure water for 2d, freeze-dry, and obtain polyethyleneimine-modified lentinan, that is, cation Mushroom polysaccharide.

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Abstract

The invention relates to a preparation method and application of cationization lentinan. The cationization lentinan can be used as a gene vector delivery system, plays an immunoregulation effect, and effectively solves the application problem in tumor treatment. The invention adopts a technical scheme: the lentinan is connected with low-molecular-weight polyethyleneimine by virtue of a pH sensitive chemical bond, the molecular weight of the lentinan is 20 to 800 kD, the molecular weight of the polyethyleneimine is 600 to 1200 D, and a molar ratio of the polyethyleneimine to the lentinan is 1 : (3 to 10). The preparation process is simple, the sources of raw materials are wide, the cost is low, and the development and application prospect is promising; the prepared cationization lentinan is uniform in shape, the particle size is about 200 nm and is uniform in distribution, the structure is stable, the biological compatibility is good, nucleic acid can be effectively loaded and delivered to tumor cells, and an antitumor effect combining gene therapy and immunotherapy is realized.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method of cationized lentinan with anti-tumor activity and nucleic acid delivery function and its application as a gene carrier while exerting immunological activity. Background technique [0002] Tumor is one of the common diseases that threaten human health and life. Its morbidity and mortality are on the rise. The International Cancer Research Center predicts that in the next 20 years, the number of new cancer cases in the world will rise to 22 million per year, and the death cases of cancer patients will rise to 13 million per year (IARC Science Public Lyon, 2014, 1: 1365). Tumor has become an extremely important public health disease of worldwide concern. At present, most of the chemotherapeutic drugs clinically used for tumor treatment mainly play their role by inhibiting cell proliferation and tumor growth, killing tumor cells as well as normal cells, and their expen...

Claims

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Application Information

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IPC IPC(8): A61K47/58A61K47/61A61K48/00A61K31/715A61P35/00C08G81/00
CPCA61K48/005A61K31/715C08G81/00
Inventor 任雪玲张振中武园园张红岭林静刘晓孟二娟张瑞桑延晓韩淼
Owner ZHENGZHOU UNIV
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