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Amphipathy micromolecule IR820-1MT, preparation of IR820-1MT and preparation method and application of preparation

A technology of IR820-COOH and IR820, applied in the field of medicine, can solve the problems of multi-drug resistance in chemotherapy and achieve excellent anti-tumor effect

Active Publication Date: 2019-07-12
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inventors found that photodynamic therapy depends on the oxygen microenvironment of cancer tissue, and chemotherapy may have multidrug resistance

Method used

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  • Amphipathy micromolecule IR820-1MT, preparation of IR820-1MT and preparation method and application of preparation
  • Amphipathy micromolecule IR820-1MT, preparation of IR820-1MT and preparation method and application of preparation
  • Amphipathy micromolecule IR820-1MT, preparation of IR820-1MT and preparation method and application of preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1 Synthesis of Amphiphilic Small Molecule IR820-1MT

[0055] Precisely weigh a certain amount of IR820 with an analytical balance in a round-bottomed flask, add anhydrous DMF to dissolve it, accurately weigh 6-aminocaproic acid in anhydrous DMF and ultrasonically mix it into a round-bottomed flask, add three Ethylamine was reacted in an oil bath at 85°C for 4 h under the protection of nitrogen. After the reaction was complete, the anhydrous DMF in the filtrate was removed by suction filtration under reduced pressure, and the crude product was dried overnight in a vacuum oven. The dried product was redissolved in methanol, mixed with silica gel, evaporated to dryness, and the solid was separated through a silica gel column, eluted with a gradient of ethyl acetate and methanol, and the product was collected and dried to obtain IR820-COOH. Precisely weigh a certain amount of 1MT with an analytical balance into a round-bottomed flask, add tetrahydrofuran for ultr...

Embodiment 2

[0056] Example 2 H NMR spectrum ( 1 H-NMR) to identify the chemical structure of IR820-1MT

[0057] Weigh about 3 mg of IR820-1MT (prepared according to the method of Example 1), dissolve it in deuterated dimethyl sulfoxide (DMSO-d6) and place it in a nuclear magnetic tube, and measure its hydrogen nuclear magnetic resonance spectrum by using 400 MHz hydrogen nuclear magnetic resonance spectrum. Methylsilane was used as an internal standard, and the chemical shift values ​​(ppm) of the compounds were recorded. The result is as figure 1 As shown, the NMR results can confirm that the peaks of IR820 and 1MT in the newly synthesized purified molecule can be assigned. pass 1 H-NMR spectrum can confirm the successful synthesis of IR820-1MT.

Embodiment 3

[0058] Example 3 IR820-1MT Chemical Structure Identified by Mass Spectrometry (MS)

[0059] About 1 mg of IR820-1MT (prepared according to the method in Example 1) was weighed, dissolved in methanol, and analyzed by mass spectrometry. The result is as figure 2 As shown, the mass spectrometry results can be seen, the molecular ion peak [M-Na+H] + (1180.6) and [M+NH 4 ] + The appearance of (1220.7) proves that the IR820-1MT small molecule was synthesized successfully.

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Abstract

The invention provides an amphipathy micromolecule IR820-1MT, a preparation of the IR820-1MT and a preparation method and application of the preparation. The structure of the amphipathy micromoleculeIR820-1MT is shown in a formula (I). The amphipathy micromolecule IR820-1MT and a composition or preparation, such as a nano particle preparation, of the amphipathy micromolecule IR820-1MT can be applied to anti-cancer and anti--tumor treatment through photo-thermal treatment and IDO-inhibitor-mediated immunotherapy, and the inhibition ratio of the amphipathy micromolecule IR820-1MT to tumors reaches 70%. Particularly, the amphipathy micromolecule IR820-1MT and the composition or preparation, such as the nano particle preparation, of the amphipathy micromolecule IR820-1MT and aPD-L1 are used as a medicine combination or applied to medicine cooperation, and the inhibition ratio of the IR820-1MT and aPD-L1 to tumors can reach 87%. The amphipathy micromolecule IR820-1MT has a particularly excellent anti-tumor effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an amphiphilic small molecule IR820-1MT, its preparation, its preparation method and application. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Cancer is one of the major diseases causing human death worldwide. At present, traditional tumor treatment methods mainly include surgery, chemotherapy and radiotherapy. With the deepening of tumor research, it is found that the immune system is closely related to the anti-tumor effect. Immunotherapy works by stimulating the immune system to recognize and kill tumor cells. Systemic anti-tumor immune activation and immune memory f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/60A61K31/404A61K39/395A61K41/00A61K9/14A61P35/00
CPCA61K9/0019A61K9/14A61K31/404A61K39/39566A61K41/0052A61P35/00C07D209/60A61K2300/00
Inventor 栾玉霞张荻
Owner SHANDONG UNIV
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