A kind of n-benzylidene sodium alginate hydrazone compound and its preparation method and application
A technology of sodium alginate and compounds, applied in the direction of drug combination, digestive system, diseases, etc., to achieve good inhibitory effect, great research value and application value
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Embodiment 1
[0037] Embodiment 1 Preparation of a kind of N-benzylidene sodium alginate hydrazone derivative
[0038] The structural unit of N-benzylidene sodium alginate hydrazone compound is shown in formula (I):
[0039] Its molecular weight is 1.1~1.6×10 5 .
[0040] Its concrete preparation route is as follows:
[0041]
[0042] Concrete preparation process is as follows:
[0043] S1. Preparation of sodium alginate dialdehyde (ADA): Take 4.5g of sodium alginate and dissolve it in 400mL of water; take another 2.43g of sodium periodate, dissolve it in 50mL of water, and add it to the sodium alginate solution; Stir and react in the dark for 7 hours; after the reaction is completed, add 7.0 g of ethylene glycol to the system, and the resulting mixture is purified and dialyzed for 2 days to remove unreacted substances and impurities, and freeze-dried for 2 days to obtain sodium alginate dialdehyde (ADA);
[0044] S2. Preparation of sodium alginate hydrazone (HDA): Dissolve 300mg o...
Embodiment 2
[0053] The screening of compound preparation conditions shown in embodiment 2 formula (I)
[0054] This embodiment will investigate three factors altogether, are respectively: reaction temperature is 40 ℃, 45 ℃, 50 ℃, 55 ℃, 60 ℃, reaction time is 2h, 3h, 4h, 5h, 6h, HDA and p-hydroxybenzaldehyde Effects of mass ratios of 1:1, 1:2, 1:4, 1:6, 1:8 on grafting ratio.
[0055] Grafting rate=(the total amount of p-hydroxybenzaldehyde monomer grafted onto the molecule / the total monomer mass of feed intake) × 100%
[0056] 1) Preparation of standard curve: Weigh a certain amount of p-hydroxybenzaldehyde, and configure the concentrations as 30ug / ml, 50ug / ml, 70ug / ml, 90ug / ml, and 110ug / ml respectively. Scan the 30ug / ml p-hydroxybenzaldehyde solution at 210nm-460nm with a UV spectrophotometer to obtain a maximum absorption peak at 252nm. Then the solutions with different concentrations were scanned at 252nm to obtain their absorbance, so as to obtain the regression equation: A=0.0167C...
Embodiment 3
[0070] Example 3 In Vitro Antitumor Activity Experiment
[0071] Test tumor cells: HepG2 (liver cancer cells), SGC-790 (human gastric cancer cells) and, Hela (cervical cancer cells).
[0072] The test method is determined by the MTT method, and the specific test process is as follows:
[0073] Add 100 μL / well of a certain density of tumor cells into the ninety-six-well plate and store at 37°C, 50% CO 2 Incubate the culture for 24 hours to allow the cells to adhere to the wall.
[0074] First suck out the culture solution in the well to be added with the drug, and then add 10 μL / well of the drug solution to be tested. multiple holes. Leave a row of wells without adding drugs as normal control wells. After inoculation, at 37°C, 5% CO 2 Conditions were incubated for 48 hours.
[0075] Add 20 μL / well of MTT solution (5 mg / mL), mix well and mix well at 37°C, 5% CO 2 Incubate under conditions for 4 hours. First pour out the liquid in the well, then add DMSO 100μ / well, and mi...
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