Application of carbocyanine dye near infrared fluorescent compound

A carbocyanine dye and fluorescent compound technology, applied in the field of medicine, can solve the problems of enrichment, unclear photosensitive therapeutic effect of cyanine dyes, and lack of targeting properties.

Active Publication Date: 2014-02-26
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

[0085] Particularly preferred carbocyanine compounds provided by the present invention

[0086]

[0087]

[0088]

Embodiment 11

[0090] In vivo tumor cell uptake and fluorescence imaging test

[0091] Materials and Method

Embodiment 1

[0092] Preferred compounds 1, 2 and 3 provided in Examples 1, 2 and 3;

[0093] Human lung cancer H358 cells, purchased from ATCC, USA;

[0094] Kodak In-vivo Fx multifunctional live animal fluorescence imaging system, purchased from Kodak, USA.

[0095] 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 size of 0.5-1 cm in diameter, the preferred compounds 1, 2 and 3 provided in Examples 1, 2 and 3 were administered through the tail vein 3. The dose is 0.2mg / kg body weight, and the fluorescence imaging of the tumor site is detected by Kodak In-vivo Fx multifunctional live animal fluorescence imaging system at different times after administration.

[0096] See the result figure 1 (Indicated by arrows): After the preferred compounds provided in Examples 1, 2 and 3 are administered to tumor-bearing animals, they are rapidly distributed throughout the body with blood circulation, and the overall f...

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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 present 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 tissues. Background technique [0002] The further improvement of the treatment effect of malignant tumors depends on the development of more sensitive detection and diagnosis technologies. 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. It is currently the frontier field of research and development of tumor in vivo diagnostic technology. Optical imaging methods have the advantages of high sensitivity, safety and no radioactivity. The application of light in medical diagnosis has recently received attention and is the main content of molecular imaging research and development, especially in the sp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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