Water-soluble cationic benzylidene cyclopentanone photosensitizer and preparation method and application of photosensitizer in photodynamic sterilization

Abstract

The invention discloses a water-soluble cationic benzylidene cyclopentanone photosensitizer and a synthetic method and application of the photosensitizer in photodynamic sterilization. The photosensitizer has a simple molecular structure, has a determined chemical structure, has appropriate fat-to-water ratio, has fat-water amphipathy, has mild reaction condition for synthesis, and is easy to prepare and purify. The operation is simple. The photosensitizer has high biological photodynamic activity within the 350-600 nm wavelength range, can be used for selective photodynamic inactivation of pathogenic microorganisms and avoids from damaging host cells and tissues as much as possible, has a broad-spectrum antibacterial property, and has a great application prospect in the aspect of photodynamic sterilization.

Description

technical field [0001] The present invention relates to the field of photodynamic therapy. More specifically, it relates to a preparation method of a water-soluble cationic benzylidene cycloalkanone photosensitizer and its application in photodynamic sterilization. Background technique [0002] The discovery of antibiotics once made human beings think that the era of microbial infection was about to be bid farewell. However, with the widespread use and continuous upgrading of antibiotics, clinical pathogenic bacteria infections have not been completely controlled. On the contrary, many pathogenic bacteria or opportunistic pathogens have mutated into those with effective resistance to antibiotics under the pressure of the living environment. Multidrug-resistant bacteria that kill drug-resistant mechanisms. The high mortality rate and high medical expenses caused by infections caused by multidrug-resistant bacteria make the work of antimicrobial infections face a severe test...

AI Technical Summary

Problems solved by technology

However, with the widespread use and continuous upgrading of antibiotics, clinical pathogenic bacteria infections have not been completely controlled. On the contrary, many pathogenic bacteria or opportunistic pathogens have mutated into those with effective resistance to antibiotics under the pressure of the living environment. Multidrug Resistant Bacteria

The high mortality rate and high medical costs caused by infections caused by multi-drug resistant bacteria make the work of antimicrobial infections face a severe test

In 2010, the British medical journal "The Lancet" announced that the "super bacteria" carrying the "New Delhi metalloproteinase-1 (NDM-1)" gene can tolerate almost all antibiotics, but the commonly used anti-infective drugs and methods have limited efficacy against such infections

[0006] At present, there are currently existing photosensitizers for clinical photodynamic therapy such as hematoporphyrin derivatives HpD, photofrin, verteporfin, etc. These photosensitizers have different degrees of unclear effective components, unclear absorption and metabolism mechanisms in vivo, and poor metabolism. And other issues

However, the photosensitizer phenothiazine dye methylene blue (MB), which is used in clinical practice, easily forms dimers on the surface of bacteria, which seriously affects the efficiency of photodynamic inactivation.

Images