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Peptide dentritic macromolecular drug and preparation method and application thereof

A technology of dendritic macromolecules and peptides, applied in the field of biomedicine, can solve the problems of difficult synthesis and purification, low cell uptake, and high production costs, and achieve the effects of rich surface functional groups, high anti-tumor activity, and easy synthesis

Inactive Publication Date: 2015-05-27
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the major challenges facing peptide drugs are high production costs, difficult synthesis and purification, poor water solubility, and low cellular uptake; therefore, the development of a class of peptide drugs with easy synthesis and high efficiency is of great significance to the development of new drugs

Method used

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  • Peptide dentritic macromolecular drug and preparation method and application thereof
  • Peptide dentritic macromolecular drug and preparation method and application thereof
  • Peptide dentritic macromolecular drug and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: the preparation of peptide dendrimer

[0055] a) Protect the functional group of the amino acid: protect the amino acid according to the difference of the surface functional group of the core molecule of the peptide dendrimer to be prepared. If the surface functional group of the core molecule is an amino group or a hydroxyl group, protect the amino group of the amino acid, such as the core molecule If the surface functional group is a carboxyl group, the carboxyl group of the amino acid is protected;

[0056] b) Preparation of a first-generation dendrimer: Weigh branched cores (functionality n, n>1), amino acids (1.5n equivalents) containing protective groups, condensing agents (1.5n equivalents), catalysts (1.5 n equivalents) and an organic base (4n equivalents), at 0°C, under nitrogen protection conditions, add a solvent for dehydration condensation reaction; then react at room temperature, after the reaction, the resulting solution is washed and dried,...

Embodiment 2

[0062] Embodiment 2: the specific synthesis example of a kind of peptide dendrimer drug (synthetic route such as figure 2 )

[0063] Synthesis of a new generation of peptide dendrimers (G1-Poss-Lys)

[0064] Add 30 mL of concentrated hydrochloric acid dropwise to 350 mL of methanol at 50°C, continue to raise the temperature to 90°C, slowly add 15 mL of 3-aminopropyltriethoxysilane dropwise, and react in a closed state for 24 hours, tetrahydrofuran precipitates to obtain octamer (3 - Aminopropyl)silsesquioxane hydrochloride (Poss.HCl). 1 H NMR (600 MHz, DMSO-d 6 )δ8.14 (s, 2H), 3.61-3.59 (t, 2H), 1.69 (m, 2H), 0.75-0.72 (t, 2H).

[0065] Weigh 2.0g cage-type octamer (3-aminopropyl) silsesquioxane hydrochloride (Poss HCl), 8.0g O-benzotriazole-tetramethyluronium hexafluorophosphate (HBTU) and 2.5 Add 1-g 1-hydroxybenzotriazole (HOBT) into a 100mL single-neck flask, add 5.0g Boc-lys(Boc)-OH into a 50mL constant pressure dropping funnel, vacuumize and fill with nitrogen. Add...

Embodiment 3

[0073] Embodiment 3: to the peptide dendrimer drug prepared in embodiment 2, it is carried out the detection of following aspects:

[0074] (1) Use gel electrophoresis retardation experiments to observe the ability of different amounts of peptide dendrimer drugs to interact with DNA. - EGFPC1 plasmid DNA (including 200ng DNA) was compounded at room temperature for 30 minutes, and the W / P ratio refers to the molar ratio of tryptophan (W) in the peptide drug to the phosphate group (P) in the DNA. The complex was subjected to 1% agarose gel electrophoresis at 100mV for 45min, stained with ethidium bromide, and observed under a 254nm ultraviolet light. Figure 6 The results showed that when the molar ratio of the peptide dendrimer drug to the p-EGFPC1 plasmid was greater than 10:1, it could effectively interact with the p-EGFPC1 plasmid and block its movement.

[0075] (2) At the same time, the fluorescence spectrum further indicated that there was a supramolecular interaction be...

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Abstract

The invention discloses a peptide dentritic macromolecular drug and a preparation method and application thereof, and belongs to the field of biomedicine. The drug comprises a peptide dentritic macromolecular skeleton, and terminal-group functionalized groups. The biological activity of the drug is ensured through the terminal-group functionalized groups; and the periphery of the peptide dentritic macromolecular drug can be grafted with a lot of terminal-group functionalized groups, so that the biological effect of the terminal-group functionalized groups is effectively amplified by the amplification effect of dendritic macromolecules. The drug has an accurate molecular structure and abundant surface functional groups, is good in water solubility, and also has the biological characteristics of being similar to globulin, easy to be taken in by cells and the like; the biological effect of the peptide dentritic macromolecules is enriched; and the development of peptide drugs is promoted. The preparation method is simple in technology; and the structure of the peptide dentritic macromolecular drug is accurately controlled by controlling preparation of various raw materials.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a therapeutic peptide dendrimer anticancer drug. technical background [0002] With the increasingly serious problems of environmental pollution and food safety, the incidence of major diseases such as malignant tumors has increased significantly, and the treatment of diseases has attracted widespread attention. At present, chemotherapy based on chemical drugs is one of the most effective methods of disease treatment; drug molecules act on tumor cells to achieve the purpose of disease treatment. However, the development and application of new drugs has always been a major problem in cancer treatment research, but the development of new drugs is an important strategy to improve the efficacy of drugs, reduce side effects, and achieve the reversal of multidrug resistance. [0003] China is the largest drug production and export country in the world, but the production of gene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00A61K38/16A61P35/00
CPCA61K38/00C07K14/00
Inventor 顾忠伟徐翔晖张晓李亚超李芸焜张志军
Owner SICHUAN UNIV
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