Targeted photosensitizer and its preparation method, application and antitumor drug containing it

A photosensitizer and targeting technology, which is applied in the field of photosensitizers, can solve the problems of high molecular weight of photosensitizers and reduced photodynamic activity of photosensitizers, and achieve good targeting, good photodynamic activity, and improved water solubility.

Active Publication Date: 2021-02-26
重庆化工职业学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the photosensitizer with the targeting group has a relatively large molecular weight and is not easy to pass through solid tumor tissue; and the photosensitizer is coupled with other molecules through chemical bonds, which reduces the original photodynamic activity of the photosensitizer.

Method used

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  • Targeted photosensitizer and its preparation method, application and antitumor drug containing it
  • Targeted photosensitizer and its preparation method, application and antitumor drug containing it
  • Targeted photosensitizer and its preparation method, application and antitumor drug containing it

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] This embodiment provides a targeted photosensitizer, which is prepared according to the following steps:

[0103] 1) Preparation of photoactive effect molecular intermediates: Equimolar mTHPC, 2-(2-hydroxyalkyl)pyridine dithiopyridine and triphosgene were condensed in the dark, and then separated and purified by column chromatography to obtain carbonate bonds and bis Sulfur-bonded porphin intermediates;

[0104] 2) Preparation of cysteine-polypeptide: starting from Fmoc-arginine and Fmoc-cysteine,

[0105] Weigh the resin and place it in a solid-phase synthesis tube, add dichloromethane to swell, add 20%-40% pyridine-dichloromethane solution, after washing, add equimolar Fmoc-Arg and Fmoc-cysteine, the reaction bottom 2 times the condensing agent, the reaction temperature is room temperature; react for 10 hours, then alternately wash with dichloromethane and absolute ethanol until the by-products are washed clean; repeat the above steps to connect arginine in turn, the...

Embodiment 2

[0115] This embodiment provides a targeted photosensitizer. The difference from Example 1 is that in step 1), equimolar mTHPC, 2-(hydroxymethyl)pyridine dithiopyridine and equimolar triphosgene are used for the light-proof condensation reaction. ; In step 4), react under the condition of 60-80° C. for 6 hours to obtain the targeted photosensitizer.

Embodiment 3

[0117] This example provides a targeted photosensitizer, the difference from Example 1 is that the reaction products are not purified during the preparation of the targeted photosensitizer.

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Abstract

The invention provides a targeted photosensitizer and a preparation method and application thereof, and an anti-tumor drug comprising the targeted photosensitizer, and relates to the field of photosensitizers. The targeted photosensitizer takes folic acid as a tumor target group; a photoactive effector molecule and the folic acid are connected through a carbonate ester bond, a disulfide bond and apeptide chain in sequence; after the targeted photosensitizer enters a tumor cell, the photoactive effector molecule is released through exchange reaction of sulfydryl and the disulfide bond and molecular nucleophilic substitution reaction in a strong reductive environment, so as to exert an effect of photodynamically killing a tumor under the illumination. The preparation method of the targetedphotosensitizer comprises simple steps and is easy to operate; furthermore, no large-sized or complicated instruments are needed, and the preparation method is suitable for expanding large-scale production and preparation.

Description

technical field [0001] The invention relates to the field of photosensitizers, in particular to a targeted photosensitizer, its preparation method, application and antitumor drugs containing the same. Background technique [0002] In photochemical reactions, there is a class of molecules that only absorb photons and transfer energy to those molecules that cannot absorb photons to promote chemical reactions, but they do not participate in chemical reactions and return to their original state. Such molecules are called Photosensitizer. The photochemical reaction initiated by photosensitizer is called photosensitization reaction. Usually, people refer to the photosensitive reaction accompanied by biological effects involving oxygen molecules as photodynamic reaction, and the drugs that can trigger photodynamic reaction to destroy cell structure are called photodynamic drugs, that is, photosensitive drugs. [0003] Photodynamic therapy (PDT) uses photosensitizers to generate s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K41/00A61K47/54A61K47/65A61P35/00
CPCA61K41/0071A61K47/545A61K47/65A61P35/00
Inventor 李鹏熙杨兵刘忠洪
Owner 重庆化工职业学院
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