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Multi-mode targeted probe for early hepatic fibrosis diagnosis and preparation method thereof

A liver fibrosis, multi-mode technology, applied in the field of multi-mode targeted probes and its preparation, to achieve the effects of prolonging circulation time, reducing steric hindrance, and improving water solubility

Inactive Publication Date: 2013-01-23
ZHONGSHAN HOSPITAL FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In liver fibrosis, there are no related research reports

Method used

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  • Multi-mode targeted probe for early hepatic fibrosis diagnosis and preparation method thereof
  • Multi-mode targeted probe for early hepatic fibrosis diagnosis and preparation method thereof
  • Multi-mode targeted probe for early hepatic fibrosis diagnosis and preparation method thereof

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Embodiment 1

[0045] Such as figure 1 Shown is a synthetic route map of the multi-modal targeting probe of the present invention, and the synthetic steps of the synthetic route map of the multi-modal targeting probe (Den-RGD) are as follows:

[0046] 1. Synthesis of c(RGDyK):

[0047] The present invention uses Fmoc-protected solid-phase peptide synthesis method to synthesize c(RGDyK) (MW=619.68Da):

[0048] (1) Weigh 0.4g resin-Gly (Fmoc-Gly-2-Cl-Trt, degree of substitution 0.6mmol / g, about 0.25mmol), rinse with dichloromethane (DCM) and swell for 20 minutes, use DMF (N , N-dimethylformamide) wash several times.

[0049] (2) Deprotection with 20% piperidine (DMF: piperidine=2ml:0.5ml) consecutively for 2 times, each time for 10-15 minutes. DMF wash several times.

[0050] (3) Weigh 1.25mmol of the required amino acid, and add 0.18g of HOBt (1-hydroxybenzotriazole), use 2.45ml of HBTU (benzotriazole-N, N, N', N'-tetrazolium Methylurea hexafluorophosphate) and 0.44ml of DIEA (N,N-diisopropylethylam...

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Abstract

The invention relates to a multi-mode targeted probe for early hepatic fibrosis diagnosis and a preparation method thereof. The multi-mode targeted probe for the early hepatic fibrosis diagnosis is characterized by comprising a vector, and the vector is connected with a fluorescence group and a magnetic resonance imaging group and can be connected with a targeted compound group, which can be combined with a receptor on the surface of a hepatic stellate cell in hepatic fibrosis / cirrhosis, through a bridging group. The preparation method comprises the steps of: connecting the targeted compound group, which can be combined with the receptor on the surface of the hepatic stellate cell in the hepatic fibrosis / cirrhosis, with the bridging group, and sequentially connecting the targeted compoundgroup, the fluorescence group and the magnetic resonance imaging group on the vector. The targeted probe has higher sensitivity when being used for diagnosing and evaluating the fibrosis diagnosis.

Description

Technical field [0001] The invention relates to a multi-mode targeting probe for early diagnosis of liver fibrosis and a preparation method thereof, which are used for evaluating liver fibrosis by using multi-mode non-invasive imaging of integrin αvβ3 receptors such as magnetic resonance, optics, etc. Background technique [0002] So far, liver biopsy is still the only "gold standard" for evaluating liver fibrosis. However, liver biopsy is invasive and can cause fatal complications, so it cannot be generally accepted by patients. This has caused a large number of patients with chronic liver disease to delay diagnosis and treatment; at the same time, in patients with no obvious symptoms, It is difficult to repeat liver biopsy, which makes it impossible to accurately follow up the changes of patients with chronic liver disease; in addition, sample sampling errors and inconsistencies in pathological observations affect the accuracy of liver biopsy. Therefore, an accurate non-invasi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/12A61K49/06C07K7/06
Inventor 王吉耀李聪严蕙蕙
Owner ZHONGSHAN HOSPITAL FUDAN UNIV
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