Application of chitosan-based norcantharidin derivatives in the preparation of antitumor compositions
A technology of chitosan derivatives and norcantharidin, which is applied in the field of medicine and biology, can solve the problems of increased toxicity, short absorption and elimination time, and reduced tumor treatment effect, so as to reduce toxic side effects, reduce drug dosage, and long retention time Effect
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Embodiment 1
[0022] Embodiment 1: Preparation of chitosan-based norcantharidin derivatives
[0023] Chitosan-based norcantharidin derivatives were prepared by reacting water-soluble carboxymethyl chitosan, hydroxyethyl chitosan, and hydroxypropyl chitosan as substrates with norcantharidin. The specific preparation process as follows:
[0024] (1) Preparation of chitosan-based norcantharidin derivative 1: Weigh 1.0 g carboxymethyl chitosan (95.5% carboxymethyl substitution degree, 83.2% deacetylation degree, 96.5 kD molecular weight, mol number of sugar units 0.0033 mol), placed in a 50ml three-necked flask, added 25ml of distilled water, stirred to dissolve, added triethylamine to adjust the pH to 9, and obtained carboxymethyl chitosan solution. Weigh 2.2g norcantharidin (0.012 mol), dissolve it in 10ml acetone to obtain norcantharidin acetone solution. Add the norcantharidin acetone solution dropwise into the carboxymethyl chitosan solution under stirring, react at room temperature and ...
Embodiment 2
[0038] Embodiment 2: Chitosan-based norcantharidin derivatives inhibit the growth of tumor tissue
[0039] The experimental animals were Kunming mice, half male and half male, weighing 18-20 g. Resuscitate mouse liver cancer cells H22, after routine culture of cells, adjust the cell density to 1.0×10 with normal saline 7 / ml, inoculated in the abdominal cavity of primary mice, 0.5 ml / only. Five to seven days after inoculation, the cells were subcultured in the abdominal cavity for 3 consecutive generations. H22 tumor-bearing mice with good growth in the abdominal cavity were taken and sacrificed by cervical dislocation. The ascites tumor fluid was extracted under sterile conditions, centrifuged, and the cell density was adjusted to 2.0×10 with normal saline. 7 / ml, inoculated subcutaneously in the left forelimb armpit of normal mice, 0.2 ml each, to make mouse H22 tumor-bearing models.
[0040] After 24 hours of modeling, tumor-bearing mice were randomly divided into gro...
Embodiment 3
[0053] Embodiment 3: excretion of chitosan-based norcantharidin derivatives
[0054] Taking rats as experimental animals, they were randomly divided into 7 groups, with 3 rats in each group:
[0055] Normal saline control group: give normal saline;
[0056] Experiment 1 group: give chitosan-based norcantharidin derivative 1 physiological saline solution;
[0057] Experiment 2 group: give chitosan-based norcantharidin derivative 2 physiological saline solution;
[0058] Experiment 3 group: give chitosan-based norcantharidin derivative 3 physiological saline solution;
[0059] Experiment 4 group: give chitosan-based norcantharidin derivative 4 physiological saline solution;
[0060] Experimental group 5: given the physiological saline solution of chitosan-based norcantharidin derivative 5;
[0061] Experiment 6 group: give chitosan-based norcantharidin derivative 6 physiological saline solution;
[0062] Norcantharidin control group: Norcantharidin normal saline solution wa...
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