IR780 double-targeted near-infrared fluorescent probe preparation method and application on tumor diagnosis and treatment

A 1. IR780, fluorescent probe technology, applied in the field of biomedicine, can solve the problems of poor diagnosis and treatment effect, single imaging and treatment mode, tumor insensitivity, etc., to improve the effect of lack of targeting

Inactive Publication Date: 2019-05-21
ZUNYI MEDICAL UNIVERSITY
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  • Abstract
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Problems solved by technology

The main technical problem to be solved by the present invention is the multi-functional diagnosis and treatment combination drug of targeted delivery drug, original near-infrared fluorescence imaging diagnosis and photodynamic therapy drug with stronger tissue penetrability for clinical personalized treatment of tumors, to overcome At present, there are shortcomi

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  • IR780 double-targeted near-infrared fluorescent probe preparation method and application on tumor diagnosis and treatment
  • IR780 double-targeted near-infrared fluorescent probe preparation method and application on tumor diagnosis and treatment
  • IR780 double-targeted near-infrared fluorescent probe preparation method and application on tumor diagnosis and treatment

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Embodiment Construction

[0051] The content of the present invention will be described in detail below in conjunction with specific embodiments. It should be noted that what is described below is an explanation rather than a limitation of the present invention.

[0052] 1. The preparation of the near-infrared fluorescent probe based on IR780 tumor dual targeting of the present invention.

[0053] The preparation of the near-infrared fluorescent probe based on IR780 tumor dual-targeting for single-molecule multifunctional diagnosis and treatment of the present invention mainly includes the following steps:

[0054] Step 1: Dissolve IR780 and 4-(aminoethyl)-morpholine in a ratio of 1:2 in 50-100 mL of anhydrous acetonitrile, and 2 Under air atmosphere, react at 50-80 degrees Celsius for 6-10 hours, and evaporate the solvent under reduced pressure after the reaction is cooled;

[0055] Step 2: Pass the product after the above-mentioned evaporation of the solvent through a silica gel column, and carry o...

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Abstract

The invention relates to an IR780 double-targeted near-infrared fluorescent probe preparation method and application on tumor diagnosis and treatment, wherein the compound comprises two molecular units including an IR780 mother nucleus and morpholine. In the same molecular structure, mitochondria targeting, lysosome targeting, near-infrared fluorescence imaging diagnosis and photodynamic treatmenton tumors are integrated. The invention also discloses the application on tumor diagnosis and treatment. The fluorescent probe has the advantages of a simple structure, small molecular weight, a determined chemical structure, easy preparation and purification processes, low toxicity to mice and the like, so that the fluorescent probe can meet the basic requirements of clinical medication. In-vitro experiments prove that by means of the near-infrared fluorescence imaging, the electropositivity of tertiary amine and the negative electronegativity of the mitochondria in the near-infrared fluorescence probe structure based on IR780 tumor double targeting can obviously target tumor cells and tumor tissues, can generate photodynamic treatment action under near-infrared radiation, and can obviously inhibit tumor growth.

Description

technical field [0001] The invention relates to the preparation and application of an IR780 double-targeting near-infrared fluorescent probe and its application in tumor diagnosis and treatment, belonging to the field of biomedicine. Background technique [0002] In my country's planning, the research and development of innovative drugs for malignant tumors is clearly included in the strategic planning of major new drug creation with the content of major national science and technology projects: "Focus on malignant tumors, cardiovascular and cerebrovascular diseases and other 10 types (species) of major diseases, strengthen the development of major vaccines and antibodies , focusing on supporting the development of drugs with strong innovation, good curative effect, meeting important needs, and great industrialization prospects, as well as the construction of major common key technologies and basic research capabilities... Especially innovative drugs targeting new targets, new...

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Application Information

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IPC IPC(8): C07D209/14C09K11/06A61K31/5377A61K49/00A61K41/00A61P35/00
Inventor 袁泽利麦宇涵屈小芳丁尚丽高鹏源刘云
Owner ZUNYI MEDICAL UNIVERSITY
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