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Application of polyesteramide compound in preparation of medicine for preventing and/or treating blood system diseases

A polyester amide and blood system technology, applied in the field of biomedicine, can solve the problems of single polymer function and inability to regulate the immune microenvironment of the blood system, and achieve safety assurance, low toxicity, and regulation of the immune microenvironment of the blood system Effect

Pending Publication Date: 2022-04-12
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the defects and deficiencies in the existing nano-drug delivery system for blood system diseases that the polymer has a single function and cannot regulate the role of the immune microenvironment of the blood system, and to provide a polyester amide compound in the preparation of preventive and / or the application of drugs for the treatment of blood system diseases

Method used

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  • Application of polyesteramide compound in preparation of medicine for preventing and/or treating blood system diseases
  • Application of polyesteramide compound in preparation of medicine for preventing and/or treating blood system diseases
  • Application of polyesteramide compound in preparation of medicine for preventing and/or treating blood system diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] The synthesis of embodiment 1 polyester amides compound (8P4)

[0083] (1) Synthetic monomer p-nitrophenol sebacate (N8)

[0084] Dissolve p-nitrophenol (0.31 mol) and triethylamine (0.32 mol) in 500 mL of pyruvic acid together and cool in ice water at 0°C to obtain solution a. Dissolve sebacoyl chloride (0.15mol) in 100mL of pyruvic acid to obtain solution b, then add solution b dropwise to solution a, stir in an ice-water bath at 0°C for 2 hours, and gradually heat the reaction to room temperature under stirring for 12 hours before pouring Pour it into 2000mL distilled water to precipitate the product, filter it with suction, wash the precipitate, recrystallize it three times with ethyl acetate, dry it in vacuum at 40°C to constant weight, and obtain monomer N8, which is sealed and stored. Dissolve the purified monomer N8 in deuterated DMSO by 1 H NMR identified its chemical structure. Its chemical structural formula is as follows:

[0085]

[0086] (2) Synthes...

Embodiment 2

[0093]The synthesis of embodiment 2 polyester amides compound (8P6)

[0094] (1) Synthetic monomer N8

[0095] Consistent with the method of Example 1.

[0096] (2) Synthesis of monomer phenylalanine-6 ​​(Phe-6)

[0097] Mix L-phenylalanine (0.04mol) and 1,6-hexanediol (0.02mol) directly, then add toluene (400mL) and p-toluenesulfonic acid monohydrate (0.082mol) and heat to 130°C, stir Reflux for 24 hours, produce 2.16mL (0.12mol) of water, cool to room temperature, pour into toluene to precipitate, filter, dissolve the filter residue in isopropanol at 75°C under stirring, then cool to 4°C to precipitate, repeat 3 times , to obtain monomeric Phe-6, sealed and preserved. Dissolve the purified monomeric Phe-6 in deuterated DMSO by 1 H NMR identified its chemical structure. Its chemical structural formula is as follows:

[0098]

[0099] (3) Synthesis of polyester amide compounds (8P6)

[0100] Dissolve monomer N8 (5 mmol) and monomer Phe-6 (5 mmol) in anhydrous DMSO (8...

Embodiment 3

[0104] Embodiment 3: the preparation of the polyester amide compound nanoparticle of loading doxorubicin

[0105] Dissolve 3.6 mg of 8P6 prepared in Example 2, 2 mg of DSPE PEG 2000 and 0.4 mg of doxorubicin (DOX) in 0.6 mL of dimethyl sulfoxide, and add dropwise to 6 mL of deionized water under magnetic stirring (1000 rpm) to form Doxorubicin-loaded polyester amide nanoparticles (DOX@8P6 NPs), and then the organic solvent DMSO in the medium was removed by multiple ultrafiltration. The prepared nanoparticles were stored in a refrigerator at 4°C until use.

[0106] Characterization tests:

[0107] The DOX@8P6 NPs were subjected to DLS and TEM tests. like image 3 Shown in A: The average particle size of DOX@8P6 NPs is about 73nm, and the particle size is small, which is conducive to the uptake of the carrier by tumor cells and exerts its anticancer effect. like image 3 Shown in B: The TEM image of DOX@8P6NPs shows that the nanoparticles are spherical.

[0108] The stabil...

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Abstract

The invention belongs to the technical field of biological medicine, and particularly relates to application of a polyesteramide compound in preparation of a medicine for preventing and / or treating blood system diseases. The polyesteramide compound synthesized by taking L-phenylalanine as a main raw material has the effects of remarkably inhibiting MDSCs pyruvate kinase and regulating the immune microenvironment of a blood system, and can be used for treating diseases of the blood system; when the traditional Chinese medicine composition is used together with small molecular medicines, the effect of remarkably treating blood system diseases can be achieved through a synergistic effect. In addition, the polyesteramide compound provided by the invention is low in toxicity, and the safety is guaranteed.

Description

technical field [0001] The invention belongs to the technical field of biomedicine. More specifically, it relates to the application of a polyester amide compound in the preparation of drugs for the prevention and / or treatment of blood system diseases. Background technique [0002] Blood system diseases are mostly related to the abnormal decline of immune system function. Studies have found that myeloid-derived suppressor cells (MDSCs) do not exist in the steady state of healthy individuals. Conditions; by inhibiting the production of ROS in MDSCs can reduce its inhibitory effect on the immune system. Therefore, reducing the content of MDSCs plays a key role in the treatment of anti-blood system diseases and regulation of the immune microenvironment of the blood system. [0003] In addition, drug resistance induced by the immune microenvironment of the blood system and off-target drugs lead to damage to normal organs or tissues of the human body, making the clinical effect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/51A61K31/787A61K45/06A61P7/00A61P7/02A61P7/04A61P35/02A61P35/00C08G69/44
Inventor 吴钧赵萌游欣如李昌正代春雷
Owner SUN YAT SEN UNIV
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