Preparation method of folate-targeted 99mTc marked manganese-based chelate MR/SPECT dual-mode probe

A folic acid-targeted, 99mtc technology, applied in the direction of radioactive carriers, etc., to achieve the effects of good biocompatibility and blood compatibility, easy operation, mild and controllable reaction conditions

Inactive Publication Date: 2015-05-27
DONGHUA UNIV +1
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  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Searching the literature at home and abroad has not found any information about folic acid targeting radionuclides 99m Preparation of Tc-labeled dendrimer-based manganese chelate MR / SPECT dual-modality molecular imaging probe and related reports on its application in in vivo tumor model-targeted MR / SPECT dual-modality imaging

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  • Preparation method of folate-targeted 99mTc marked manganese-based chelate MR/SPECT dual-mode probe
  • Preparation method of folate-targeted 99mTc marked manganese-based chelate MR/SPECT dual-mode probe
  • Preparation method of folate-targeted 99mTc marked manganese-based chelate MR/SPECT dual-mode probe

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Embodiment 1

[0070] First, weigh 13mg of G5 and 11.5mg of DOTA-NHS and dissolve them in 10mL and 3mL of dimethyl sulfoxide (DMSO) solvent respectively. After they are completely dissolved, add the DOTA-NHS solution dropwise while stirring. Into the G5 solution, continue to stir the reaction for 24 hours to obtain the intermediate product G5.NH 2 -DOTA. Then, 2.5 mg of FA and 5 mg of EDC were weighed and dissolved in 1.5 mL of DMSO solvent. After complete dissolution, the EDC solution was added dropwise to the FA solution in the dark and kept stirring for 30 minutes, and then weighed 3.2 mg of NHS Dissolve in 1.5mL DMSO solvent, add dropwise to FA and EDC solution after completely dissolved, keep stirring in the dark for 3 hours, add the activated FA solution dropwise to G5.NH while stirring 2 -In the DOTA reaction system, the reaction was continued in the dark for 72 hours to obtain the crude product G5.NH 2 -FA-DOTA. Next, dissolve 1.5 mg of fluorescein isothiocyanate (FI) in 2 mL of D...

Embodiment 2

[0073] Take 2 mg of the G5.NHAc-FI-FA-DOTA-Mn material prepared in Example 1 and dissolve it in ultrapure water, ultrasonically dissolve to obtain a solution, and measure the ultraviolet absorption picture spectrum (see figure 1 ). The results of UV-Vis spectrum test showed that G5.NHAc-FI-FA-DOTA-Mn had an obvious UV absorption peak at 500nm, which indicated that FI was successfully modified on the surface of G5.

[0074] Weigh about 2-4 mg of the material G5.NHAc-FI-FA-DOTA-Mn prepared in Example 1 and the control group material G5.NHAc-FI-DOTA-Mn obtained in Comparative Example 1 and dissolve them in ultrapure water for surface Potential and hydrated particle size test ( as table 1 shown). The surface potential and hydrated particle size of the synthesized G5.NHAc-FI-FA-DOTA-Mn were -0.463mV and 863.6nm, respectively, while the surface potential and hydrated particle size of the control material G5.NHAc-FI-DOTA-Mn were respectively is +0.693mV and 549.5nm. From the...

Embodiment 3

[0077] In order to ensure that the molecular imaging probe prepared by the present invention can be safely used for in vivo bioimaging diagnosis, we evaluated the prepared G5.NHAc-FI-FA-DOTA-Mn (Example 1) and the reference material G5.NHAc-FI - Hemocompatibility of DOTA-Mn (comparative example 1). Calculate and weigh G5.NHAc-FI-FA-DOTA-Mn (embodiment 1) and reference material G5.NHAc-FI-DOTA-Mn (comparative example 1) according to the manganese concentration of two kinds of materials measured in embodiment 2 Two kinds of dry powders with 1 mg of total manganese content were respectively dispersed in PBS buffer solution to make a concentration of 1 mg / mL and used as the mother solution, and then prepared in PBS buffer solution in sequence with concentrations of 10 μg / mL, 25 μg / mL, and 50 μg / mL , 75 μg / mL and 100 μg / mL solutions. Take an appropriate amount of human fresh blood, first centrifuge (2000rpm, 5 minutes) to remove the supernatant, then wash the red blood cells 5 tim...

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Abstract

The invention relates to a preparation method of a folate-targeted 99mTc marked manganese-based chelate MR / SPECT dual-mode probe. The method comprises the following steps of: modifying G5 surface with a chelating reagent DOTA-NHS; connecting a targeting molecule to the G5 surface; marking the G5 with FI; chelating manganese ions in coordination with DOTA; converting G5 surface amino into acetyl through acetylation reaction; finally, marking the residual DOTA with radioactive nucleus 99mTc, thus obtaining the probe. The molecular imaging probe prepared by the invention realizes MR / SPECT dual-mode imaging at the cell level and the animal level; moreover, by mediation of FA, the probe prepared by the invention has remarkable targeting effect on a Hela cell tumor model of high-expression cancer cell strain of an FA receptor, and is expected to be used for realizing dual-mode targeting diagnosis on cancer.

Description

technical field [0001] The invention belongs to the field of preparation of dual-mode molecular imaging probes, in particular to a folic acid targeting 99m A preparation method of a Tc-labeled manganese-based chelate MR / SPECT dual mode probe. Background technique [0002] Cancer, also known as malignant tumor in medical terms, has directly or indirectly affected the lives of many people and has become the number one killer threatening human health. Therefore, early diagnosis and treatment become the key to cure cancer. In the early diagnosis of tumors, traditional imaging techniques can only understand tumor volume and anatomical location, while molecular imaging techniques can obtain more detection parameters, such as the evaluation of tumor growth kinetics, the detection of molecular abnormalities before malignant transformation, tumor cell Markers, etc., and in vivo molecular imaging can realize the study of pathogenesis without damaging the microenvironment of organism...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/06A61K51/04A61K103/10
Inventor 史向阳罗宇赵晋华赵凌舟
Owner DONGHUA UNIV
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