Preparation method and applications of polyasparagine-RGDF-antitumor drug compound
An anti-tumor drug, polyaspartic acid technology, which is applied in the field of preparation and application of polyaspartic acid-RGDF-anti-tumor drug complexes, and can solve problems such as unsolved main problems
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Embodiment 1
[0019] Example 1 Mesoscopic simulation of the three-dimensional morphology of polyaspartyl-RGDF at neutral and pH5.4
[0020] Construction of dimers of α,β-dl-asparagine-Arg-Gly-Asp-Phe was energy optimized with Discovery Studio 4.0. Input the energy-optimized dimer into Materials Studio 7.0 to construct polyaspartate-RGDF with a chain length of 119 aspartic acid residues and 118 RGDF tetrapeptides with a molecular weight of 69753. N-terminal NH 2 The H atoms (also known as head H atoms) are labeled H1 and H2, and the C-terminal CO 2 The oxygen atoms (also known as tail oxygen atoms) of H are labeled O1 and O2.
[0021] Correspondingly, when the dimer of α, β-dl-asparagine-Arg-Gly-Asp-Phe forms a tetramer, there are H1 / O1, H2 / O1, H2 / O1 when the head H atom and the tail oxygen atom form a peptide bond, Approximate pathways of four collocations of H1 / O2 and H2 / O2. Their energies were minimized using Material Studio 7.0's COMPASS force field until the energies stabilized. Th...
Embodiment 2
[0023] Embodiment 2 prepares polyasparagine-RGDF
[0024] The chain length is 119 aspartic acid residues, 118 RGDF tetrapeptides are linked, and the preparation of polyasparagine-RGDF with a molecular weight of 69753 is carried out completely according to the disclosed method.
[0025] 1) Preparation of Boc-Arg(Tos)-Gly-OBzl
[0026]Dissolve 4.986g (11.64mmol) of Boc-Arg (Tos), 1.310g (9.7mmol) of HOBt in 30mL of anhydrous THF, add 2.398g (11.64mmol) of DCC in anhydrous THF to the resulting solution, and stir in an ice bath 20min, the reaction solution I was obtained. A solution of 3.273 g (9.7 mmol) Tos·Gly-OBzl and 30 mL of anhydrous THF was adjusted to pH 9 with NMM to obtain reaction solution II. The reaction solution II was added to the reaction solution I, and reacted at room temperature for 12 hours. TLC (acetone:petroleum ether=2:1) showed that the reaction was complete. The DCU precipitate was removed by filtration, the filtrate was concentrated under reduced pr...
Embodiment 3
[0044] Example 3 Determination of the nanostructure of polyaspartic acid-RGDF by transmission electron microscopy
[0045] Polyaspartyl-RGDF was formulated in ultrapure water to a concentration of 10 -6 nM solution, and then drop this solution on the copper grid, and observe the nano-morphology under the JEM-1230 transmission electron microscope after the solvent is evaporated. The measurement shows that the polyaspartyl-RGDF forms a diameter of 38-200nm, and most of the nanospheres have a diameter of 38-180nm. The surface of the nanospheres is covered with pores with a diameter of 4-11 nm (see image 3 , A-D). It is easy to imagine that when hyacinth-like nanorod-like polyaspartyl-RGDF molecules distributed with pores and circular channels are assembled into nanospheres, the surface of the nanospheres will of course be covered with pores.
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