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Preparation of series of water-soluble polymers based on Rylene compound and biomedical application of water-soluble polymer as optothermal reagent
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A technology of water-soluble polymers and compounds, applied in medical preparations containing active ingredients, pharmaceutical formulas, echo/ultrasonic imaging agents, etc., to achieve excellent water solubility, high biocompatibility, and stable photothermal conversion effects
Active Publication Date: 2017-08-11
BEIJING UNIV OF CHEM TECH
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However, due to the strong hydrophobicity of phenolines when they are not modified, if this high-performance material is introduced into the biological field for photothermal therapy, the first problem to be solved is water solubility and biocompatibility.
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[0051] 2. the product NHCOC (CH 3 ) 2 Br (271mg, 0.38mmol) and TDI-4Al (50mg, 0.038mmol) were added t...
Embodiment 2
[0059] 1. QDI-6Br (60mg, 0.042mmol) and p-ethyl hydroxyphenol (30mg, 0.22mmol) were added to the 2 CO 3 React with NMP solvent in a reaction flask at 115°C for 48h. After the reaction is over, remove NMP. After precipitation in n-hexane, the product is separated by column chromatography (dichloromethane) to obtain an intermediate product marked as QDI-4OH;
[0060]
[0061] 2. Mix the product QDI-4OH (50mg, 0.03mmol) of step 1 and PEG-COOH (240mg) with a molecular weight of 2000 in dichloromethane, and react in HOBt and DIC system at room temperature for more than 60h; precipitate in ice ether to obtain the final Product QDI-PEG;
[0062]
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Abstract
The invention relates to preparation of a series of water-soluble polymers based on a Rylene compound and biomedical application of the water-soluble polymer as an optothermal reagent. Through chemical modification on imide positions and 'bay' positions of the Rylene compound, and through leading of polar multi-branching or linear polymers, the water solubility of a hydrophobic benzene ring framework is sharply improved, and a series of water-soluble polymers which are based on the Rylene compound and have water-soluble performance and an optothermal function are obtained. Based on the characteristics that the Rylene compound absorbs heat energy and is effectively converted into heat energy, photoacoustic imaging of a target product in mouse tumors and optothermal reagent application are successfully achieved. The water-soluble polymers based on the Rylene compound have high biocompatibility, and have low toxicity to mouse organs and blood; when the water-soluble polymers enter the depth of tumor tissue, under the radiation of oriented laser, the temperature of partial tumor can be efficiently raised, the purpose of precisely and efficiently conducting thermal treatment is achieved, and no obvious thermal damages exist in other normal tissue.
Description
technical field [0001] The invention belongs to the technical field of photothermal reagents, and in particular relates to the preparation of a series of water-soluble polymers based on phenoline compounds and their application in biomedicine as photothermal reagents. The invention obtains the water-soluble polymer based on the phenoline compound which can be used as a photothermal reagent through the chemical modification of the imide position and the "bay position" of the phenoline compound. Background technique [0002] Tumor has become one of the most important diseases that endanger human health. At present, the treatment methods for cancer mainly focus on surgery, chemotherapy and radiotherapy: surgery is a fast treatment method, but due to the lack of inhibition of tumor cell activity and incomplete physical removal of lesions, it is often accompanied by high recurrence and incurable hidden dangers Chemotherapy and radiotherapy can effectively inhibit the activity an...
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