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 targeting probes and its preparation, to achieve the effects of improving water solubility, reducing steric hindrance, and prolonging circulation time

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

CN101991867AInactive Publication Date: 2011-03-30ZHONGSHAN HOSPITAL FUDAN UNIV +1
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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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Experimental program
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Effect test

Embodiment 1

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

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

[0047] The present invention synthesizes c(RGDyK) (MW=619.68Da) with Fmoc-protected solid-phase polypeptide synthesis method:

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

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

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

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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 is used for evaluating liver fibrosis by multi-mode non-invasive imaging of integrin Ξ±vΞ²3 receptors such as magnetic resonance and optics. Background technique [0002] To date, liver biopsy remains the only "gold standard" for assessing liver fibrosis. However, liver biopsy is invasive and can cause fatal complications, so it is not universally accepted by patients, which causes a large proportion of patients with chronic liver disease to delay diagnosis and treatment; meanwhile, in asymptomatic patients, It is difficult to repeat liver biopsy, which prevents accurate follow-up of changes in patients with chronic liver disease; in addition, sample sampling errors and inconsistencies in pathological observations all affect the accuracy of liver biopsy. Therefore, there is a need for an accurate and non-invasive method to ...

Claims

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Application Information

Patent Timeline
30 Mar 2011
Publication
CN101991867A
IPC
A61K49/12; A61K49/06; C07K7/06
Inventors
ηŽ‹ε‰θ€€; 李θͺ