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Radioactive molecular probe and application thereof in detection of living pancreas islets

A molecular probe and radioactive technology, which is applied in the field of radioactive molecular probe and its application in the detection of living pancreatic islets, can solve the problem that the influence of islet activity is difficult to evaluate

Active Publication Date: 2018-07-17
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(Evgenov NV, etal.Nature Medicine.2006.DOI:10.1038 / nm1316.) However, the effect of exogenous modification on the viability of islets after transplantation is difficult to evaluate

Method used

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  • Radioactive molecular probe and application thereof in detection of living pancreas islets
  • Radioactive molecular probe and application thereof in detection of living pancreas islets
  • Radioactive molecular probe and application thereof in detection of living pancreas islets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of embodiment 1 glycine boron trifluoride precursor

[0040]

[0041] Specifically: the temperature is controlled at 10°C, in a 100mL round-bottomed flask, dissolve 1g of iodomethylboronic acid pinacol ester in 35mL of THF, stir for 10min, after the solution is cooled, add 10 times the equivalent of the newly prepared methylamine solution , continue to react for 30 min, after the reaction is completed, spin dry, and pass through a silica gel column to obtain 300 mg of glycine boron trifluoride precursor (white solid), with a yield of 27.8%.

Embodiment 2

[0042] Example 2 Preparation of Radioactive Molecular Probe X1

[0043]

[0044] In this scheme, free fluoride ions in the reaction system are removed through a neutral aluminum column, and the elution system is physiological saline.

Embodiment 3

[0045] Example 3 STZ-induced diabetes modeling in mice

[0046] Experimental principle: STZ (a broad-spectrum anticancer drug) was once used to treat giant insulinoma, which can destroy pancreatic islet β cells, and repeated small-dose injections can cause diabetes.

[0047] Experimental steps:

[0048] 1. Select 30 mice, weighing 170-220 g, aged 4-6 weeks. The mice were fed with conventional pellet diet and had free access to drinking water. The room temperature in the laboratory is kept at 18-22°C, and the animals are fed normally for one week.

[0049] 2. Tail vein blood glucose measurement and body weight.

[0050]3. Divide the mice into three groups, ten in each group, and use STZ to create a model. Among them, the first group was used as a control group and fed normally. The second group used STZ solution (STZ was dissolved in 0.1 mol / L citrate buffer, prepared before use), and was injected continuously for three days according to each dose of 40 mg / kg, once a day. ...

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Abstract

The invention relates to a radioactive molecular probe and application thereof in detection of living pancreas islets, and the structure of the radioactive molecular probe is as shown in the specification, wherein R1 is a halogen, a saturated aliphatic hydrocarbon group, an unsaturated aliphatic hydrocarbon group and an aromatic hydrocarbon group, R2 is a halogen, a saturated aliphatic hydrocarbongroup, an unsaturated aliphatic hydrocarbon group and an aromatic hydrocarbon group, R3 is hydrogen, a saturated aliphatic hydrocarbon group, an unsaturated aliphatic hydrocarbon group and an aromatic hydrocarbon group, and R4 is hydrogen, an saturated aliphatic hydrocarbon group, an unsaturated aliphatic hydrocarbon group and an aromatic hydrocarbon group, R5 is hydrogen, a saturated aliphatic hydrocarbon group, an unsaturated aliphatic hydrocarbon group and an aromatic hydrocarbon group, R6 is hydrogen and deuterium, R7 is hydrogen and deuterium, and the radioactive molecular probe can perform imaging and assessment of the number of the living pancreas islets.

Description

technical field [0001] The invention relates to the field of molecular probes, in particular to a radioactive molecular probe and its application in living pancreas islet detection. Background technique [0002] Diabetes mellitus is a disease in which the function of pancreatic β cells is reduced or exhausted due to various reasons, resulting in absolute or relative insufficiency of insulin, and glucose metabolism disorder in the matrix, which in turn causes damage to multiple organs throughout the body. Among them, patients with type 1 diabetes depend on insulin therapy for life, which brings great inconvenience to the lives of patients. [0003] Most patients with type 1 diabetes, type 2 diabetes without insulin antibodies and low levels of C-peptide, diabetic nephropathy, diabetes after organ transplantation, pancreatic disease or diabetes caused by pancreatectomy are suitable for adult islet cell transplantation. [0004] According to the statistics of the International...

Claims

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Application Information

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IPC IPC(8): C07F5/02A61K51/04A61K101/02
CPCA61K51/0406C07F5/02C07B59/004
Inventor 刘志博韩宇翔
Owner PEKING UNIV
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