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Application of carbocyanine dye near infrared fluorescent compound

A technology of carbocyanine dyes and fluorescent compounds, which is applied in the field of medicine and can solve the problems of enrichment, lack of targeting properties, and affecting the optical properties of cyanine dyes, biomolecular targeting properties, etc.

Active Publication Date: 2009-09-02
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the compounds in such dyes currently used do not have targeting properties for tumor tissues and other tissues. Once they enter the blood circulation, they can be quickly eliminated by the body's metabolism and cannot be effectively enriched in specific target tissues such as tumors. , it needs to be chemically coupled with specific targeting molecules, such as specific antibodies that can recognize tumor cell surface antigens, so that targeted imaging can be performed, and this chemical coupling reaction can affect the optical properties of cyanine dyes and the targeting properties of biomolecules; on the other hand, it is not clear whether cyanine dyes can have photosensitive therapeutic effects on diseases in vivo such as malignant tumors

Method used

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  • Application of carbocyanine dye near infrared fluorescent compound
  • Application of carbocyanine dye near infrared fluorescent compound
  • Application of carbocyanine dye near infrared fluorescent compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1—10

[0087] Particularly preferred carbocyanine compounds provided by the present invention

[0088]

[0089]

[0090]

Embodiment 11

[0092] In vivo tumor cell uptake and fluorescence imaging assays

[0093] Materials and methods

Embodiment 1

[0094] Preferred compounds 1, 2 and 3 provided by Examples 1, 2 and 3;

[0095] Human lung cancer H358 cells were purchased from ATCC, USA;

[0096] Kodak In-vivo Fx multifunctional live animal fluorescence imaging system was purchased from Kodak Company of the United States.

[0097] Human lung cancer H358 cells were inoculated subcutaneously in nude mice to prepare a nude mouse tumor-bearing model. When the tumor grew to a diameter of 0.5-1 cm, the preferred compounds 1, 2 and 3. The dose is 0.2mg / kg body weight, and the fluorescence imaging of the tumor site is detected by the Kodak In-vivo Fx multifunctional living animal fluorescence imaging system at different times after administration.

[0098] see results figure 1 (Indicated by the arrow): After the preferred compounds provided by Examples 1, 2 and 3 are administered to tumor-bearing animals, they are rapidly distributed throughout the body along with the blood circulation, and the overall fluorescence signal of the...

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Abstract

The invention discloses an application of a carbocyanine dye near infrared fluorescent compound in the preparation of a photosencitizer used for treating tumors or abnormal hyperplasia tissues, shown in formula I or II, wherein X is selected from iodine, chlorine, bromine, alkyl sulfide (OSO2-alkyl), BF4 or ClO4; R1 is selected from chlorine or bromine; R2 is selected from hydrogen, alkyl, hydroxyl group (-OH), carboxyl (-COOH), aryl, aromatic alkyl, alkyl sulfonate, alkyl carbonate and alkyl amine; and n is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, l1 or 12.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the use of a group of near-infrared fluorescent compounds from carbocyanine dyes in the preparation of photodynamic therapy drugs for tumors and abnormal hyperplasia. Background technique [0002] The further improvement of the treatment effect of malignant tumor depends on the development of more sensitive detection and diagnosis techniques. Molecular imaging technology can conduct qualitative, quantitative and visual research on tumor tissue cells at the cellular and molecular levels in living tissues and organs. The optical imaging method has the advantages of high sensitivity, safety and no radioactivity. The application of light in medical diagnosis has recently been paid attention to, and it is the main content of the research and development of molecular imaging, especially in the spectral range of near-infrared wavelengths (700-1200nm). , the photons are rarely absorbed by the bi...

Claims

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Application Information

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IPC IPC(8): A61K31/404A61K49/00A61P35/00
Inventor 史春梦朱颖粟永萍程天民
Owner ARMY MEDICAL UNIV
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