P-oxycyclohexanone and l-phenylalanine mustard copolymer and its application
A technology of phenylalanine nitrogen mustard and copolymer, which is applied in the direction of drug combination, drug delivery, medical preparations of non-active ingredients, etc., can solve the problems of high drug toxicity and side effects, and achieve the effect of inhibiting proliferation
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Embodiment 1
[0031] Preparation and Characterization of PDCM Polymer
[0032] 1) Preparation of PDCM polymer
[0033] 4 g (13 mmol) of L-phenylalanine mustard and 3 g (10 mmol) of trimeric phosgene were placed in a round-bottomed flask, and after the air in the bottle was replaced with high-purity nitrogen, 50 mL of anhydrous tetrahydrofuran was added and refluxed for 3 hours. The solvent in the reaction solution was removed by rotary evaporation to obtain a yellow oil, which was the crude product of L-melphalan-N-carboxylic anhydride. The crude product was recrystallized three times from anhydrous tetrahydrofuran-n-hexane. Pure L-melphalan-N-carboxylic anhydride was obtained. 1 H NMR (400MHz, DMSO-d 6 , 9.13, s, 1H, NHCO; 7.01, d, J=8Hz, 2H, phenyl H; 6.68, d, J=8Hz, 2H, phenyl H; 4.71, t, J=4Hz, 1H, CONHCHCO; 3.71, br , 8H, NCH 2 CH 2 Cl; 2.90, d, J=4Hz, 2H, CH 2 -phenyl.), yield 57%.
[0034] L-phenylalanine mustard-N-carboxylic anhydride 2.47g (7.4mmol), p-oxycyclohexanone 5g (...
Embodiment 2
[0043] Covalently Bonded Chemotherapeutic Drug L-Phenylalanine Mustard Sustained Release Nanoparticles
[0044] PDCM-1, PDCM-2, and PDCM-3 were prepared into their corresponding nanoparticles by electrostatic spraying method. Take PDCM-3 as an example: Dissolve PDCM-3 in a mixed solvent of hexafluoroisopropanol / methanol (9:1, v / v) to prepare a solution with a concentration of 5% w / v, and add DTBA at 2mmol / Add the concentration of L into the solution, place the solution in a syringe whose needle tip is connected to an 8KV high-voltage DC power supply, place the syringe on a continuous micro-injection pump, the injection rate is 0.2mL / h, and place 75vol.% ethanol aqueous solution 10cm below the needle tip as the negative electrode The receiving device is connected to -2.5KV high voltage DC power supply. Under the action of electrostatic force, the polymer droplet cracks, dries, and shrinks to receive PDCM-3 nanoparticles in the receiving liquid. The size of the prepared PDCM ...
Embodiment 3
[0046] Inhibitory Effect of PDCM Nanoparticles on Cancer Cell Proliferation
[0047] Different concentrations of PDCM-2 nanoparticles were placed in the cell culture medium of U-87 (human glioma cell line), MCF-7 (human breast cancer cell line), and SKOV-3 (human ovarian cancer cell line) as Experimental groups 1, 2, and 3; normal culture medium was used in the control group, and the specific groups are shown in Table 2 below. The control group and the experimental group were incubated at room temperature for corresponding time.
[0048] Table 2. Test components of PDCM nanoparticles on cancer cell proliferation
[0049]
[0050] By comparing the OD value of the experimental group with the OD value of the control group, the inhibition rate of cell proliferation in the experimental group was obtained (such as figure 2 shown):
[0051] Proliferation inhibition rate={1-(OD value of experimental group / OD value of control group)}×100%
[0052] Depend on figure 2 It can be...
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