A radioactive iodine-labeled two-dimensional palladium-based probe and its preparation method and application
A radioactive iodine and palladium-based technology, applied in the field of medical imaging probes, can solve problems such as insufficient combination of drugs and targets, unsatisfactory target/non-target ratio, increased dosage, etc., to facilitate large-scale production, enrich anatomy and Functional information, effect of increasing distance
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Embodiment 1
[0044] The synthetic route of the present embodiment is as follows:
[0045]
[0046] Specifically include the following steps:
[0047] 1) Synthesis of FA-PEG-SH
[0048] I) Synthesis of FA-NHS: After dissolving 1-2g folic acid in dimethyl sulfoxide, add 1-1.5 equivalents of N-hydroxysuccinimide (NHS) and 1-1.5 equivalents of dicyclohexylcarbodiethylene Amine (DCC), activated overnight in the dark and filtered.
[0049] II) Synthesis of FA-PEG-SH: the equivalent amount of NH 2 -PEG-SH (molecular weight 3400Da) was dissolved in DMSO and added dropwise to the above FA-NHS filtrate, adding 0.5-1 equivalent of N,N-diisopropylethylamine (DIPEA), and reacted at 20-50°C 1-2 days. After the reaction is complete, transfer the reaction solution to a dialysis belt with a molecular weight cut-off of 1000, first dialyze with PBS7.4 buffer solution for 1-2 days, and then dialyze with pure water for 1-2 days. After the dialysis, the liquid in the dialysis zone was collected and free...
Embodiment 2
[0061] 1) 131 In vitro stability determination of I-Pd@Au-PEG-FA
[0062] The above-mentioned embodiment 1 is made 131 I-Pd@Au-PEG-FA probe was incubated with normal saline, PBS 7.4 buffer and mouse serum for 24 hours. Stability was determined by TLC (polyamide film / physiological saline system) method. Such as Figure 4 Shown: the present invention 131 The I-Pd@Au-PEG-FA probe can exist stably in the above systems, and its radiochemical purity does not change significantly.
[0063] 2) 125 I-Pd@Au-PEG-FA in ApoE - / - SPECT imaging and vascular autoradiography in model mice
[0064] ApoE - / - Gene knockout mice were fed a special high-fat diet for 2-6 months to form plaques. Before injecting the radiolabeled probe, inject 0.1mL NaI solution (2mg) in advance to seal the mouse thyroid. Prepared according to the example 125 I-Pd@Au-PEG-FA dispersion, take 0.1mL (about 37MBq) and inject it into ApoE - / - Tail veins of knockout mice (about 20 g body weight) were subjected t...
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