A photoresponsive degradable tumor koningine precursor compound and its preparation and application
A technology of precursor compound and tumorikinin, which is applied in the field of tumorikinin precursor compounds, can solve the problems of inability to release timed and fixed-point, incomplete and burst release of tumoricornin preparations, toxic and side effects, etc. The effect of large drug load and reduction of toxic and side effects
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Embodiment 1
[0035] Embodiment 1: the preparation of precursor compound molecule
[0036] Dissolve 180mg (0.6mmol) of Cyclonine in 10mL of anhydrous CH 2 Cl 2 After cooling in an ice bath, add 148mg (0.72mmol) of N,N'-dicyclohexylcarbodiimide, 13.8mg (0.072mmol) of 4-dimethylaminopyridine and 236mg (0.6mmol) of hexadecyl For nitrobenzyl derivatives, react at 0-5°C for 1 hour, then naturally rise to room temperature and keep reacting for 24 hours. After the reaction was finished, the white by-product (DCU) was filtered off, the filtrate was concentrated under reduced pressure, and the white solid product was obtained by silica gel column chromatography. The eluent was ethyl acetate:petroleum ether, and the yield was 75%.
[0037] The molecular structure of the precursor compound was characterized by H NMR and C NMR results. The results are as follows: figure 1 and figure 2 shown.
Embodiment 2
[0038] Example 2: Photodegradation Assay of Precursor Compound Molecules
[0039] Prepare 0.1mg / mL acetonitrile solution of precursor compound molecules, and irradiate with 365nm ultraviolet light (1mW / cm 2 ) irradiated for different times, using high-performance liquid chromatography to measure the behavior of precursor compound molecules transformed into Lianke Ning drug molecules by light, and the degradation efficiency was determined by comparing the integral areas of the two. The results are as follows image 3 shown. Experiments have shown that the precursor compound molecules are almost completely degraded after only 10 minutes of irradiation.
Embodiment 3
[0040] Embodiment 3: the preparation of nano drug
[0041] Precursor compound molecules (20 mg) and MSNs (18 mg) were dissolved in 3 mL of absolute ethanol, shaken at room temperature for 24 hours, centrifuged at 10,000 rpm for 10 minutes to collect nanoparticles, and washed twice with water to obtain nanomedicines. The morphology of the nanomedicine was characterized by transmission electron microscopy, and the results were as follows: Figure 4 shown.
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