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Amphiphilic block polymer with anti-tumor activity of folic acid targeting ph-reduction dual response and its preparation and application
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A technology with anti-tumor activity and dual response, applied in the field of biomedicine and polymer chemistry, can solve problems such as cell damage, achieve the effects of promoting inhibition, good application prospects, and reducing damage
Inactive Publication Date: 2018-08-10
NORTHWEST NORMAL UNIVERSITY
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Among them, radiotherapy and chemotherapy are extremely important non-surgical treatments, but while radiotherapy and chemotherapy kill tumor cells, they also cause serious damage to normal cells in the body.
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Embodiment 1
[0074] (1) compound Preparation: Weigh 3.08 g of bis(2-hydroxyethyl) disulfide and dissolve it in 30 mL of dichloromethane, add 4 g of triethylamine as an acid-binding agent and stir for 20 minutes. 1.08 g of methacryloyl chloride was added, and the stirring reaction was continued for 24 hours. After the reaction is complete, the reaction solution is washed three times with 100 mmol / l pH phosphate buffer of 8.0 and distilled water, the organic layer is dried with anhydrous sodium sulfate, and then the solvent is rotary evaporated, and the crude product is purified by silica gel chromatography to obtain 1.62 g of white solid, compound , and the yield was 73%.
[0075] 1 H NMR (400 MHz, CDCl 3 , δ, ppm): 6.13 (s, 1H, CH H = C(CH 3 )CO-), 5.59(s, 1H, C H H = C(CH 3 )CO-), 4.41 (t, J = 6.6Hz, 2H, -COOC H 2 CH 2 SSCH 2CH 2 OH), 3.87(t, J = 6.5Hz, 2H, -COOCH 2 CH 2 SSCH 2 C H 2 OH), 2.96 (t, J = 6.7Hz, 2H, -COOCH 2 C H 2 SSCH 2 CH 2 OH), 2.87 (t, J = 5.8Hz,...
Embodiment 2
[0091] (1) compound , , , , , and compound The preparation: with embodiment 1.
[0092] (2) Target compound Preparation: take 0.11g compound (Mn=1.18×10 4 g / mol), 24mg of folic acid monomer and 26mg of AIBN were dissolved in 3ml of DMSO in a Schlenk flask, filled with nitrogen in an ice bath for 30 minutes, then put the Schlenk flask into a constant temperature oil bath, and reacted at 60°C for 24 hours. The reaction solution was precipitated with ether to obtain 0.104g light yellow powder compound , and the yield was 58%. Mn: 1.42×10 4 .
[0093] 1 H NMR (400 MHz, DMSO-d6, δ, ppm): 8.65 (–CH – of FA heterocyclic),8.12-7.95 (4H, m, phenyl group of acid labile PEG-macroRAFT), 7.66 (–CH 2 NHC 6 H 2 h 2 CONHCH(COOH)CH 2 CH 2 CO–of FA), 6.65 (–CH 2 NHC 6 h 2 H 2 CONHCH (COOH) CH 2 CH 2 CO–of FA), 4.46 (–C H 2 NHC 6 h 4 CONHCH(COOH)CH 2 CH 2 CO– of FA), 4.41 (2H, t, -COOCH 2 CH 2 SSCH 2 C H 2 COOC 6 h 2 (OCH 3 ) 3 of MAOHD-TMOBA...
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Abstract
The invention provides an amphiphilic block copolymer having folate-targeted pH-reduction dual-response and antineoplastic activity and preparation as well as application thereof; through RAFT polymerization, a functionalized disulfide monomer, methoxy polyethylene glycol responding by acid stimulation and functionalized folic acid form a macromolecular block copolymer, i.e. a disulfide monomer-acidity PEG-folic acid copolymer, being good in biocompatibility. The copolymer has pH and reduction dual stimulus-response, and is provided with a folic acid active targeting polymer drug carrying micelle, and can effectively release adriamycin amycin at a target site. The micelle with intelligent responsibility has low cytotoxicity, is biodegradable, has a proper drug carrying level, and can promote a great quantity of drugs to be more quickly accumulated at a tumor tissue part, thus effects in acidic cytoplasm and between cytoplasm and cell nuclei with high reducibility are achieved, and therefore the amphiphilic block copolymer as a drug carrier has a good application prospect in preparing antineoplastic drugs.
Description
technical field [0001] The invention belongs to the field of macromolecular chemistry, and relates to an amphiphilic block polymer (methacryloyl dithioethanol-trimethoxybenzoic acid)-hydrazone, which has anti-tumor activity with dual response to folic acid targeting pH and reduction Bond-polyethylene glycol-polyfolate; the invention also relates to the preparation of the amphiphilic block copolymer and its application as a drug carrier in the preparation of antitumor drugs, belonging to the field of polymer chemistry and biomedical application technology. Background technique [0002] Cancer has become one of the major threats to human health, and it is on the rise. The main methods of treating cancer today include radiotherapy, chemotherapy, surgical therapy and gene therapy. Among them, radiotherapy and chemotherapy are extremely important non-surgical treatments, but while killing tumor cells, radiotherapy and chemotherapy also cause serious damage to normal cells in the...
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