Targeting molecular imaging probe and living molecular imaging method

Abstract

The invention, relating to the technical field of medical use, particularly relates to a living molecular imaging method and a targeting molecular imaging probe. The living molecular imaging method is characterized by introducing the targeting molecular imaging probe capable of being detected by an imaging device to reflect biochemical change characteristics of connexin protein 43 (Cx43) of cardiovascular diseases (especially arrhythmia), tumor and the like in the form of images, and has accurate detection results. According to the invention, the distribution and amount of the Cx43 can be displayed visually, and the method can be directly applied to human body. The Cx43 targeting molecular imaging probe disclosed herein comprises a signal component, a Cx43 targeting compatible component and a connector, and has good pharmacokinetic characteristics and biological distribution characteristics.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a Cx43-targeted molecular imaging probe and a molecular imaging method in vivo. Background technique [0002] Gap junction remodeling is one of the common pathological foundations involved in the occurrence and development of arrhythmia, tumors, atherosclerosis and other diseases, and connexin43 (Cx43) is the basic structure of gap junctions The unit is the main structural basis of the gap junctions between cardiomyocytes. Cx43 is a connection protein with a molecular weight of 43Kd, and its main function is to mediate direct communication between adjacent cells. In the heart, its main function is to form rapid electrical impulses between cells, ensure the synchronization and coordination of the overall electrical activity of the heart, and maintain the electrical activity of cardiomyocytes as well as the synchronization of mechanical contraction and relaxation functions. Ther...

AI Technical Summary

Problems solved by technology

[0005] Although in vitro detection methods can judge and analyze the expression level and functional state of Cx43 in cells or tissues, there are certain limitations in technical analysis:

[0006] ① Specimens need to be obtained through cell culture, biopsy or autopsy, and cannot be directly applied to the human body;

[0007] ②The results of in vitro experiments may not be consistent with the real situation in the living body: in vitro experiments are greatly affected by experimental conditions, experimental equipment, and experimental methods. During the processing of samples, some important components may be lost, resulting in large errors. Make the experimental results inconsistent with the real situation in the living state;

[0008] ③In vitro experiments are not conducive to dynamic research: in vitro experiments need to kill experimental animals at different time points to obtain tissues or repeated biopsy materials, and can only observe a certain stage of the disease, and cannot achieve real dynamic research in the same animal body. Get accurate conclusions about the whole process of complex and progressive diseases;

[0009] ④The operation is complicated, time-consuming and expensive, and the randomness is very large

[0011] The Cx43 visualization scheme carried out by V Baklaushev et al. synthesized a specific antibody for the extracellular E2 segment of the Cx43 protein as a targeting affinity component, and a radioactive isotope 125 I and the fluorescent dye Alexa660 are used as probes for signaling components, and the abnormal expression of Cx43 in gliomas is detected by using a γ-ray counter and a fluorescence microscope, but they still do not get rid of the limitations of in vitro inspection methods:

[0012] ① 125 I is not a nuclide suitable for in vivo imaging, it can only be detected with a gamma ray counter, and the inspection results are not intuitive enough

[0014] ③Using MAbE2Cx43 antibody as the affinity component, the antibody is expensive and may cause immunogenic reactions and cause side effects

More importantly, due to the large molecular weight of the antibody, the non-specific absorption will be high, and it is difficult to obtain ideal pharmacokinetic characteristics and biological distribution characteristics after injection into the body, resulting in inaccurate test results and inconvenient application

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