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Near-infrared fluorescent heptamethine cyanine dye and application thereof in preparation of tumor diagnosis agent and/ or imaging agent

A heptamethine and tumor imaging technology, which is applied in the field of medicine and biology, can solve problems such as changing the affinity of target molecules, and achieve good potential effects

Active Publication Date: 2017-10-20
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since targeting fragments can only detect partially specific tumor cells, and chemical conjugation may alter the avidity of target molecules, it is necessary to develop novel NIRF dyes that are simple and can be directly used for non-invasive tumor imaging.

Method used

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  • Near-infrared fluorescent heptamethine cyanine dye and application thereof in preparation of tumor diagnosis agent and/ or imaging agent
  • Near-infrared fluorescent heptamethine cyanine dye and application thereof in preparation of tumor diagnosis agent and/ or imaging agent
  • Near-infrared fluorescent heptamethine cyanine dye and application thereof in preparation of tumor diagnosis agent and/ or imaging agent

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Embodiment Construction

[0040] The present invention will be further described in detail below in conjunction with specific embodiments, which are explanations of the present invention rather than limitations.

[0041] 1. Excitation spectrum and emission spectrum of DZ-1

[0042] The heptamethine dye DZ-1 is the (CH 2 ) 5 CO 2 - Replace with (CH 2 ) 4 SO 3 - , the water-solubility of the modified compound DZ-1 is improved, realizing the same intravenous injection route as the clinical near-infrared dye ICG.

[0043] The structural formula of the near-infrared fluorescent heptamethine dye (DZ-1) of the present invention is:

[0044]

[0045] The structural formula of the commercial near-red fluorescent dye MHI-148 is:

[0046]

[0047] Dissolve DZ-1 in PBS and detect the excitation spectrum and occurrence spectrum of the compound by F97Pro fluorescence spectrophotometer, the results are shown in Picture 1-1 with 1-2 , the optimal excitation wavelength of DZ1 is 767nm, and the optimal ...

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Abstract

The invention provides a near-infrared fluorescent heptamethine cyanine dye and application thereof in preparation of a tumor diagnosis agent and / or an imaging agent. The near-infrared fluorescent heptamethine cyanine dye is a compound DZ-1, wherein the side chain of the compound DZ-1 is (CH2)4SO3H, so that the compound DZ-1 can be directly dissolved in water; in addition, the near-infrared fluorescent heptamethine cyanine dye can be applied by intravenous injection during living imaging, thus achieving the same treatment and applying mode as clinic ICG (Indocyanine Green); the compound DZ-1 can be specifically absorbed by hepatoma carcinoma cell and is gathered at the tumor part to support no-intrusive NIRF imaging, so that the tumor growing part can be detected; the fluorescence intensity at the tumor part, the specificity and the targeting performance are prior to those of clinically-used ICG. Therefore, the tumor diagnosis agent and / or the imaging agent adopting the compound DZ-1 are high in tumor targeting performance and high in stability.

Description

technical field [0001] The invention belongs to the technical field of medicine and biology, and relates to a near-infrared fluorescent heptamethine dye and its application in the preparation of tumor diagnostic reagents and / or imaging reagents. Background technique [0002] The rapid development of molecular imaging technology has advanced the diagnosis of tumors from the traditional anatomical form to the molecular level of function, metabolism, and even receptors and genes. Among them, fluorescence imaging technology can detect tumors in a timely and accurate manner, continuously and non-invasively observe changes in tumors, has the advantages of fast detection time (up to 1 second), and does not need to inject substrates. It has become a hot spot in the field of tumor diagnosis and treatment research. Studies have found that the closer the fluorescence wavelength is to 900nm, the stronger the penetration ability. Therefore, near-infrared fluorescence (NIRF) with both abs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C09B23/10C09K11/06A61K49/00
CPCA61K49/0032C09B23/105C09K11/06C09K2211/1007C09K2211/1029
Inventor 师长宏吴开春钟维国赵海燕潘东风
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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