Spherical rare earth cluster, preparation method thereof and application of spherical rare earth cluster in preparation of nuclear magnetic resonance imaging contrast agent
A contrast agent and rare earth technology, applied in organic chemistry methods, chemical instruments and methods, pharmaceutical formulations, etc., can solve the problems of low proton relaxation efficiency and poor stability of contrast agents, and achieve rapid and effective metabolism, low toxicity and side effects, The effect of high resolution and clear imaging effect
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Embodiment 1
[0050] A spherical rare earth cluster (Ho 32 ), whose molecular formula is:
[0051] [Ho 32 (L) 24 (μ 3 -OH) 48 (μ 4 -O) 6 Cl 8 ]Cl 4 45H 2 O·5CH 3 OH·2CH 3 CN.
[0052] Its specific preparation method is as follows:
[0053] Add 1mmol of benzimidazole-2-methanol (HL, 147mg) and 0.5mmol of holmium chloride hexahydrate (189.69mg) into a 25mL polytetrafluoroethylene reactor, then add 5mL of methanol and 5mL of of acetonitrile, and finally add 250 μL of triethylamine. After stirring and dissolving, seal it, put it in an oven at 100°C for 48 hours, then slowly cool down to room temperature, and volatilize the solution at room temperature to obtain yellow transparent block crystals (about 10 hours down to room temperature), that is:
[0054] [Ho 32 (L) 24 (μ 3 -OH) 48 (μ 4 -O) 6 Cl 8 ]Cl 4 45H 2 O·5CH 3 OH·2CH 3 CN.
[0055] Wherein, the yield calculated based on the amount of ligand L is about 27.2% (calculated based on the amount of ligand L).
[0056] ...
Embodiment 2
[0076] A spherical rare earth cluster (Gd 32 ), its molecular formula is: [Gd 32 (L) 24 (μ 3 -OH) 48 (μ 4 -O) 6 Cl 8 ]Cl 4 ·35H 2 O·6CH 3 OH·2CH 3 CN.
[0077] Its specific preparation method is as follows:
[0078] Add 1mmol of (benzimidazole-2-)methanol (HL, 147mg) and 0.5mmol of gadolinium chloride hexahydrate (185.80mg) into a 25mL polytetrafluoroethylene reactor, and then add 5mL of methanol and 5 mL of acetonitrile, and finally 250 μL of triethylamine. After stirring and dissolving, seal it, put it in an oven at 100°C for 48 hours, then slowly cool down and volatilize the solution at room temperature to obtain yellow transparent block crystals (about 10 hours down to room temperature), that is, spherical rare earth clusters (Gd 32 ).
[0079] Wherein, the yield is about 17% based on the amount of ligand L.
[0080] For the above yellow transparent bulk crystals (Gd 32 ) for single crystal X-ray structure diffraction test, the results show that it is compa...
Embodiment 3
[0084] Spherical rare earth clusters [Gd 32 (L) 24 (μ 3 -OH) 48 (μ 4 -O) 6 Cl 8 ]Cl 4 ·35H 2 O·6CH 3 OH·2CH 3 CN(Gd 32 ) Toxicological analysis
[0085] MTT, the Chinese name is thiazole blue, which is a tetrazolium salt. In living cells, succinate dehydrogenase in the mitochondria can reduce MTT to produce a blue-purple product-formazan (soluble in DMSO), and The product has an absorption peak at 490nm, so A490nm can be used to analyze cell proliferation. Analysis of Gd by MTT colorimetry 32 Antiproliferative effects of cisplatin on human umbilical vein endothelial cells (HUVEC) and mouse breast cancer cells (4T1). Gd at a dose of 10 mg / Kg was injected via the tail vein 32 After entering the normal mice, the mice were euthanized one week later and their vital organs were analyzed by H&E staining for toxicology.
[0086] Such as Figure 8 As shown, it is a spherical rare earth cluster Gd 32 Compared with the toxicity of cisplatin on HUVEC. Place the cells at ...
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