A7R glycopeptide and application thereof in preparation of tumor diagnosis and treatment drug
A glycopeptide and drug technology, applied in the field of A7R glycopeptide and its use in the preparation of tumor diagnosis and treatment drugs, can solve the problems of inability to achieve efficient targeting of brain tumors, reduced targeting ability, poor stability, etc., and achieve good tumor The effect of targeting performance, high stability, and strong anti-tumor effect
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Embodiment 1
[0083] A7R glycopeptide, A7R glycopeptide-Fluorescein, A7R glycopeptide-Cy7, A7R glycopeptide-DTPA-Gd, A7R glycopeptide-DTPA- 99m Synthesis and Characterization of Tc, A7R Glycopeptide-drug, A7R Glycopeptide-PEG-DSPE
[0084] 1. Glucosylated threonine Fmoc-Thr(O-β-Glu(OAc) 4 ) synthesis and characterization
[0085] Fmoc-Thr(O-β-Glu(OAc) 4 ) synthesis steps as attached figure 1 As shown, Fmoc-protected threonine (Fmoc-Thr-OH) and peracetylated glucose (2,3,4,6-tetra-O-acetyl-β-D-glucopyranose) were dissolved in CH 2 Cl 2 In ice bath, slowly add BF dropwise 3 ·Et 2 0, until the solution becomes clear, continue to stir under room temperature conditions, and the thin-layer chromatographic plate monitors the degree of reaction (developing agent is CH 2 Cl 2 :CH 3 OH=15:1). Under ice-cooling conditions, an equal volume of 1M hydrochloric acid solution was added dropwise to terminate the reaction. Extract three times, collect the lower organic phase, anhydrous Na 2 SO 4...
Embodiment 2
[0099] Example 2 Investigation of the Serum Stability of A7R Glycopeptides
[0100] Will 9 G-A7R, 9,10 G-A7R and 12 G-A7R was respectively configured into 1 mg / mL PBS solution, 0.1 mL was added to 0.9 mL of 25% rat serum, and then 10 μL of 1% TCEP in EDTA solution was added, placed in a shaker at 37°C and shaken at 100 rpm. Take 0.1mL reaction solution at 0, 0.25, 0.5, 1, 2, 4, 8, 12, and 24h, add 20μL of 15% TCA to precipitate protein, vortex, let stand at 4°C for 20min, centrifuge at 12000rpm for 10min, and take the supernatant 20μL for HPLC qualitative and quantitative analysis, serum stability results (such as Figure 7 shown) shows that, 9 G-A7R, 9,10 G-A7R and 12 G-A7R has better serum stability than A7R.
Embodiment 3
[0101] Example 3 In vitro cell targeting verification of A7R glycopeptide
[0102] In vitro targeting of A7R glycopeptides to brain capillary endothelial cells: Take brain capillary endothelial cells in logarithmic growth phase (bEND.3), digest the monolayer culture cells with 0.25% trypsin, and use 10% fetal bovine serum DMEM culture medium to make a single cell suspension, with 1×10 per well 5 Cells were inoculated in a 12-well culture plate with a volume of 1 mL per well, and the culture plate was moved into a carbon dioxide incubator at 37°C and 5% CO 2 After culturing for 24 hours under the condition of saturated humidity, the concentration of 5μM 9 G-A7R-Fluorescein, 9,10 G-A7R-Fluorescein, 12 For G-A7R-Fluorescein, suck out the culture medium in the culture plate, add the above solution respectively, and incubate at 37°C for 4h. Wash three times with PBS solution, fix the cells with formaldehyde fixative, stain the cell nucleus with DAPI, observe the cell uptake by ...
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