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Use of novel amine compound modified protoporphyrin

A protoporphyrin, application technology, applied in the application field of new amine compound modified protoporphyrin, can solve the problem of narrow antibacterial spectrum of photosensitizer

Inactive Publication Date: 2014-02-26
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In previous reports, the photosensitizers used as antibacterial drugs have a narrow antibacterial spectrum, some are effective against Gram-negative bacteria, and some are effective against Gram-positive bacteria. The photosensitizers we designed have broad-spectrum characteristics and can Effectively kill different types of bacteria and prevent the emergence of drug-resistant bacteria, which has practical significance for the promotion of PACT therapy

Method used

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  • Use of novel amine compound modified protoporphyrin
  • Use of novel amine compound modified protoporphyrin
  • Use of novel amine compound modified protoporphyrin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] N,N-dimethylethylenediamine and N,N-diethylethylenediamine or N-(2-aminoethyl)-trimethylammonium iodide or N-(2-aminoethyl)-tri Photodynamic therapy effect of ethylammonium iodide modified protoporphyrin on in vitro cultured methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa. N,N-dimethylethylenediamine and N,N-diethylethylenediamine or N-(2-aminoethyl)-trimethylammonium iodide or N-(2-aminoethyl)-tri The structural formula of ethyl ammonium iodide modified protoporphyrin is:

[0028]

[0029] Wherein M=H, Fe, Mn, Cu, Zn, Co or Mg;

[0030]

[0031] Experimental steps:

[0032] (1) Preparation of liquid medicine: Accurately weigh appropriate amount of N,N-dimethylethylenediamine and N,N-diethylethylenediamine or N-(2-aminoethyl)-trimethyl iodide Ammonium or N-(2-aminoethyl)-triethylammonium iodide modified protoporphyrin, dissolved in 1ml LB liquid medium, and prepared a series of drug solutions with decreasing concentrations in LB li...

Embodiment 2

[0042] N, N-dimethylethylenediamine modified protoporphyrin P-H photodynamic antibacterial mouse in vivo experimental steps include:

[0043] Studies based on in vitro bacterial levels have shown that the photosensitive drugs we designed can effectively kill Gram-negative bacteria (MRSA) and Gram-positive bacteria (Pseudomonas aeruginosa) under light, so in animal experiments we combined MRSA and Pseudomonas aeruginosa The suspension of bacilli was mixed in equal amounts (10 10 CFU) were inoculated into mouse skin wounds to establish an infection model. This model is more serious and more realistic than a single bacterial species infection, and can effectively confirm the broad-spectrum of our photosensitizing drugs.

[0044] 40 adult BALB / c female mice weighing 20-22 g were selected and provided by Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., license number SCXK (Beijing) 2009-0007. Placed in an experimental environment with room temperature of 20-25°C, r...

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Abstract

The present invention discloses a use of N,N-dimethylethylenediamine or N,N-diethylethylenediamine or N-(2-aminoethyl)-trimethyl ammonium iodide or N-(2-aminoethyl)-triethyl ammonium iodide modified protoporphyrin. The N,N-dimethylethylenediamine or N,N-diethylethylenediamine or N-(2-aminoethyl)-trimethyl ammonium iodide or N-(2-aminoethyl)-triethyl ammonium iodide modified protoporphyrin has the following structure. Experiment results show that: the N,N-dimethylethylenediamine or N,N-diethylethylenediamine or N-(2-aminoethyl)-trimethyl ammonium iodide or N-(2-aminoethyl)-triethyl ammonium iodide modified protoporphyrin has a good in vitro photodynamic antibacterial performance, and provides good treatment effects for photodynamic treatments of mice infections caused by bacteria, fungi and the like.

Description

technical field [0001] The present invention relates to N,N-dimethylethylenediamine or N,N-diethylethylenediamine or N-(2-aminoethyl)-trimethylammonium iodide or N-(2-aminoethyl )-triethylammonium iodide modified protoporphyrin purposes. Background technique [0002] In recent years, the abuse of antibiotics has led to the emergence and spread of drug-resistant bacteria, and produced some multi-drug resistant bacteria, namely "superbugs". Since "super bacteria" are resistant to almost all antibiotics, its potential explosive epidemic has caused panic all over the world. Scientists are working hard to find new drugs and new means to defeat super bacteria, and research and development of new Anti-infection strategies have also become imminent. [0003] Photodynamic antimicrobial chemotherapy (PACT) is one of the most promising new treatments [1-3] . PACT is an oxidative damage mechanism based on the synergistic action of light, photosensitizer and oxygen. A single drug wil...

Claims

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Application Information

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IPC IPC(8): C07D487/22A61K41/00A61K31/409A61P31/04
CPCC07D487/22A61K41/0071
Inventor 刘天军赵占娟郭江红
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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