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A preparation method of a porphyrin photosensitizer with visualized photodynamic therapy properties

A technology for visualizing light and photosensitizers, which can be used in medical preparations containing active ingredients, organic chemistry, preparations for in vivo tests, etc., which can solve the problems of photosensitizer marketization, unenvironmental preparation process, and increased preparation costs. , to achieve the effect of not affecting cell viability, uniform size and easy operation

Active Publication Date: 2017-11-03
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, nearly ten new photosensitizers have been approved for marketing or are under clinical research, and more and more photosensitizers are being researched and prepared. Most photosensitizers are prepared by chemical synthesis and other methods. In addition to the high cost, the preparation process Problems such as not being environmentally friendly, and the increase in preparation costs caused by the multi-step reaction synthesis of molecules have also become a serious obstacle to the marketization of photosensitizers
In order to meet the needs of marketization, it is of great research significance to seek a photosensitizer with simple preparation method and low price, and it also poses a huge challenge for researchers.

Method used

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  • A preparation method of a porphyrin photosensitizer with visualized photodynamic therapy properties
  • A preparation method of a porphyrin photosensitizer with visualized photodynamic therapy properties
  • A preparation method of a porphyrin photosensitizer with visualized photodynamic therapy properties

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preparation example Construction

[0033] According to one aspect of the present invention, there is provided a method for preparing a porphyrin photosensitizer with visualized photodynamic therapy properties, the method comprising the following three steps:

[0034] Step 1: Add water-soluble porphyrin and soluble nitrate into water, and mix well.

[0035] In the above step one, the water-soluble porphyrin is represented by formula I:

[0036]

[0037] Among them, R is a polar group, especially, it is preferably a sulfoarene group, an N-alkylpyridyl group and its derivatives, an aminoarene group, a quaternary ammonium arene group or a carboxyarene group.

[0038] When R is a sulfonic acid aromatic hydrocarbon group, R is selected from one of the following structural formulas:

[0039]

[0040] Wherein, X is Cl, Me, OMe or F.

[0041] When R is N-alkylpyridyl and derivatives thereof, R is selected from one of the following structural formulas:

[0042]

[0043] When R is an amino aromatic hydrocarbon...

Embodiment 1

[0090] 1) 0.12g water-soluble porphyrin and 0.048g bismuth nitrate are added in 100ml water, mix well, wherein, water-soluble porphyrin is shown by following formula:

[0091] Among them, R is

[0092] 2) Select 10mol / l hydrochloric acid to adjust the pH of the system in step 1) to 2.5;

[0093] 3) The pH-adjusted system was left standing for 12 hours at room temperature and protected from light to obtain a reaction system containing a porphyrin photosensitizer.

[0094] After scanning electron microscope test, the obtained porphyrin photosensitizer is a nano-aggregate, its morphology is a rod-like structure, and the average size is about 400nm, such as figure 1 Shown; Tested by transmission electron microscopy, the aggregate is a hollow structure, such as figure 2 shown.

Embodiment 2

[0096] 1) 0.12g water-soluble porphyrin and 0.04g chromium nitrate are added in 100ml water, mix well, wherein, water-soluble porphyrin is shown by following formula:

[0097] Among them, R is

[0098] 2) Select 10mol / l hydrochloric acid to adjust the pH of the system in step 1) to 2.8;

[0099] 3) The pH-adjusted system was left to stand for 16 hours at room temperature and protected from light to obtain a reaction system containing a porphyrin photosensitizer.

[0100] Through scanning electron microscope test, the average size of the obtained porphyrin photosensitizer is 400nm.

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Abstract

The invention discloses a preparation method of a porphyrin photosensitizer with visible photodynamic therapy properties. The method comprises reacting water-soluble porphyrin molecules and soluble nitrates under the conditions of acidity, light avoidance and room temperature to obtain a porphyrin photosensitizer containing The reaction system of the porphyrin photosensitizer, after the system is processed, the porphyrin photosensitizer is obtained, which is a nano-aggregate and has the characteristics of cell imaging and photodynamic therapy. In addition, the preparation method provided by the present invention has a simple process, does not require complicated synthesis steps and post-processing steps, is easy to operate, and has relatively low cost, and therefore, is easy to popularize in production.

Description

technical field [0001] The invention relates to the field of preparation of nanomaterials, in particular to a preparation method of a photosensitizer, and more particularly to a preparation method of a porphyrin photosensitizer, which has the characteristic of visual dynamic therapy. Background technique [0002] Photodynamic effect refers to the change of function or shape of cells or biomolecules in the body under the action of light and the participation of photosensitizers. In severe cases, cells can be damaged or necrotic. Since this action must be attended by oxygen, it is also called photosensitization-oxidation. In chemistry, this action is called photosensitization, and in biology and medicine, it is called photodynamic action. [0003] The method of using the above-mentioned photodynamic effect to treat diseases is called photodynamic therapy (PDT). Photodynamic therapy is a clinical approach that can cure early cancers and reduce tumor size in advanced cancers. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/22A61K41/00A61K49/00A61P35/00
Inventor 黄建滨赵蔷阎云
Owner PEKING UNIV
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