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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 cationic modification, and the biological activity of lentinan is retained. Public reports that play an immunomodulatory role

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] In the specific implementation of the present invention, the cationized lentinan can be as follows: 1) Dissolve 100 mg lentinan in 10 mL deionized water, add 150 mg potassium periodate while stirring, and react at 25°C under nitrogen protection to avoid light After 48 hours, add 5 mL of phosphate buffer solution containing 200 μL ethylenediamine dropwise, and complete the dropwise addition within 1 hour. Stir in the dark for 36 hours under nitrogen protection, and dialyze the reaction solution in ultrapure water for 3 days to obtain activated lentinan. liquid;

[0014] 2) Add 2 mL of 3.7% hydrochloric acid containing 250 mg of polyethyleneimine dropwise to the activated lentinan reaction liquid, stir at 25 °C for 72 h in the dark under the protection of nitrogen, and dialyze in ultrapure water 2d, freeze-drying to obtain polyethylenimine-modified lentinan, that is, cationized lentinan.

Embodiment 2

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

[0017] 2) Then add 6 mL of dimethyl sulfoxide (DMSO) solution containing 100 mg of polyethyleneimine dropwise to the activated lentinan reaction liquid, stir at 23 °C for 24 hours in the dark under the protection of nitrogen, and dissolve in ultrapure water Dialyzed for 2 days and freeze-dried to obtain polyethylenimine-modified lentinan, that is, cationized lentinan.

Embodiment 3

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

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

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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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