Active targeting folate receptor near-infrared fluorescent molecule as well as preparation method and application thereof

Abstract

The invention discloses an active targeting folate receptor near-infrared fluorescent molecule as well as a preparation method and application thereof, the structural formula of the active targeting folate receptor near-infrared fluorescent molecule is shown in the specification, and M is independently selected from H, Na and K. The active targeting near-infrared fluorescent micromolecule taking folic acid and a derivative thereof as an active targeting group is prepared by utilizing an organic total synthesis method. The active targeting near-infrared fluorescent molecule has the advantages of high active targeting property, strong specificity, good water solubility, high fluorescence quantum yield and the like.

Description

technical field [0001] The invention relates to the fields of near-infrared surgical navigation fluorescent molecules and cell labeling imaging, in particular to an active targeting near-infrared fluorescent small molecule and a preparation method and application thereof. Background technique [0002] Indocyanine green (ICG) is a hydrophilic fluorescent tracer with a molecular weight of about 776Da. It is also widely used in the assessment of liver function, the assessment of cardiac output, and fundus angiography before being used for fluorescence tracing. Under the irradiation of near-infrared fluorescence with a wavelength of 780 nm, it can emit fluorescence with a wavelength of 820 nm, and has good penetrability. Some deep tissues can be detected by ICG. When ICG enters the blood, it can quickly combine with plasma proteins to form protein-coated ICG nano-molecules, which can be enriched in tumor tissue through the EPR effect and phagocytosed by the reticuloendothelial ...

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Problems solved by technology

According to my country's drug regulatory regulations, the maximum injection dose of human ICG should be less than 2mg / kg. At this dose, literature reports and our own test data found that the concentration of ICG in human tumors is 10-1000nM, and most current equipment is effective in the detection range. At 10-1000μM, the difference is 1000 times

[0004] 2) In clinical practice, it is found that the metabolic rate of ICG in tumors and normal tissues is not much different, and it takes at least 12 hours to produce sufficient fluorescence contrast (tumor: normal tissues), which increases the burden on hospitals and patients

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