Biological photosensitizer, and preparation method and application thereof

A photosensitizer and biological technology, applied in the field of biomedicine, can solve the problems of patients' heavy physical and mental burden, and achieve the effect of promoting skin repair, efficient and fast killing, and promoting tissue healing.

Inactive Publication Date: 2018-06-08
THE THIRD XIANGYA HOSPITAL OF CENT SOUTH UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These mild or severe toxic reactions are reflected in the skin and perineum, which have highe...

Method used

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  • Biological photosensitizer, and preparation method and application thereof
  • Biological photosensitizer, and preparation method and application thereof
  • Biological photosensitizer, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: the synthesis of EtNBSe-PDT

[0039] To prepare intermediate product A, the reaction conditions are: heating to a temperature of 70-100°C for 16-24 hours in an organic solvent containing an inorganic base, wherein the molar ratio of the two reactants is 1:1.

[0040] The reaction scheme is as follows:

[0041]

[0042] To prepare intermediate product B, the reaction conditions are: in benzene solvent, 50-60 degrees Celsius, and the molar ratio of the two reactants is 1:4-4.5. The reaction scheme is as follows:

[0043]

[0044] Preparation of EtNBSe-PDT: The intermediate product A obtained in step (1) and the intermediate product B obtained in step (2) are reacted to obtain the final product, wherein the molar ratio of the two reactants is 1:3.2-4.5, and the reactant Use ethanol with a volume of 200-300 times as a solvent, heat and reflux for 24-48 hours under the protection of argon, after the reaction is completed, cool to room temperature, remov...

Embodiment 2

[0045] Example 2: EtNBSe-PDT causes apoptosis in epithelial cancer Example

[0046]Annexin V is a reagent for detecting cell apoptosis. In normal cells, phosphatidylserine is only distributed on the inner side of the lipid bilayer of the cell membrane. In the early stage of cell apoptosis, the membrane phosphatidylserine (PS) is turned from the inner side of the lipid membrane to outside. Therefore, Annexin V is a sensitive indicator for detecting early cell apoptosis. PI (propidium iodide) is a nuclear staining reagent that can stain DNA. Although PI cannot pass through the living cell membrane, it can pass through the damaged cell membrane and stain the nucleus. Therefore, the combination of Annexin V and PI can stain live and dead cells at the same time. According to flow cytometry analysis, under the action of EtNBSe-PDT, the number of apoptotic cells increased significantly compared with the blank group, which proved that EtNBSe-PDT can induce tumor cell apoptosis to ac...

Embodiment 3

[0052] Embodiment 3: EtNBSe-PDT inhibits Wnt signal embodiment

[0053] The Wnt signaling pathway mainly refers to the classic Wnt signaling pathway mediated by β-Catenin. When there is no Wnt signal, GSK3β can add a phosphate group to the serine / threonine residue at the N-terminal of β-Catenin, and the phosphorylated β-Catenin is covalently modified by β-TRCP ubiquitination, and is released by the proteasome ( proteasome) degradation. However, PP2A dephosphorylated GSK3β in the Wnt pathway, which can significantly promote Wnt signaling. Therefore, whether Wnt signaling is activated can be directly understood by measuring the phosphorylation status of GSK3β, β-Catenin and PP2A. As a highly conserved signaling pathway in evolution, the Wnt signaling pathway plays an important role in various biological processes such as growth, development, metabolism and stem cell maintenance, and is closely related to tumor growth. According to the analysis of Western Blot results, in EtNBS...

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PUM

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Abstract

The invention discloses a biological photosensitizer, and a preparation method and application thereof. The photosensitizer has the targeting ability of the photosensitizer and the characteristic of killing tumour cells, can also activate an epidermal growth factor receptor in a tissue of a living body, can kill tumour tissues, and meanwhile, can promote tissue healing; the biological photosensitizer can kill squamous-cell carcinoma efficiently and quickly, and can promote skin repairing; side effects of drug reaction are extremely low.

Description

technical field [0001] The invention relates to a biological photosensitizer and its preparation method and application, belonging to the field of biological medicine. Background technique [0002] Squamous cell carcinoma is a type of skin cancer. Its main features are: it is a blemish-like raised mass at the beginning, the base is hard, the outer surface is rough like cauliflower, telangiectasia can be seen, and spike-like cutin is common on the top. [0003] Photodynamic therapy (Photodynamic Therapy, PDT) came out in the 1970s. Its core strategy is to use specific wavelengths of light to irradiate photosensitizers selectively accumulated in lesions. Photosensitizers are activated to generate cytotoxic singlet oxygen and Reactive oxygen species, thereby killing cells. [0004] Photodynamic therapy has been successfully used in the treatment of early tumors, superficial tumors, and other non-tumor diseases such as port wine stains and condyloma acuminata during the develo...

Claims

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Application Information

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IPC IPC(8): C07D421/14A61K41/00A61P35/00A61P17/00
CPCA61K41/0057C07D421/14
Inventor 康健王臻黄进华陈静宋相志柳岸鲁建云谭丽娜曾庆海周细平吴林钰赵海福支从钢
Owner THE THIRD XIANGYA HOSPITAL OF CENT SOUTH UNIV
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