Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of fat-soluble photosensitizer and its preparation method and application

A photosensitizer, fat-soluble technology, applied in the medical and biomedical fields, can solve the problems of difficult to achieve therapeutic effect, limited concentration and retention time of photosensitizer, weak fat-solubility, etc. Medicinal properties and the effect of reducing side effects of drugs

Active Publication Date: 2021-03-19
THE THIRD XIANGYA HOSPITAL OF CENT SOUTH UNIV
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Secondly, the aggregation concentration of existing photosensitizers in skin tumor tissues needs to be improved. For example, China invented "Photosensitizer Sodium Chlorophyllin Derivatives and Its Preparation Method and Application", application number: 201210169784.1; the sodium chlorophyllin used Salt derivatives are combined with traditional photosensitizers. Although water-soluble sodium chlorophyllin enhances the penetration ability of photosensitizers, due to its poor fat solubility, the enrichment concentration and retention time of photosensitizers in tumor tissues are greatly limited. limitations, it is still difficult to achieve a good therapeutic effect

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of fat-soluble photosensitizer and its preparation method and application
  • A kind of fat-soluble photosensitizer and its preparation method and application
  • A kind of fat-soluble photosensitizer and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: the synthetic route of fat-soluble photosensitizer is as follows:

[0047] (1) Combine 1-naphthylamine with chlorine-containing compounds Reaction in the ethanol solvent of 55 ℃-60 ℃, obtains intermediate product A, and its reaction formula is:

[0048] ;

[0049] Tetracarboxy compound Reaction with KOH or NaOH solution to obtain intermediate product B;

[0050] (2) React intermediate product A and intermediate product B in an ethanol solvent at a molar ratio of 2-2.5:3-4 to obtain intermediate product C. The reaction formula is:

[0051]

[0052] ;

[0053] (3) Reaction of vitamin E and intermediate product C in acetone solvent to obtain fat-soluble photosensitizer ( figure 1 ), the reaction formula is:

[0054] .

[0055] The following is the hydrogen spectrum of the final product ( figure 2 ) and carbon spectra ( image 3 ), which proves that the present invention successfully obtains the above-mentioned target product.

Embodiment 2

[0056] Example 2: Test of inhibition of skin tumor cell activity by long-acting fat-soluble photodynamic external preparations containing vitamin E fragments

[0057] MTT method is a method to detect cell survival and growth. The detection principle is that succinate dehydrogenase in the mitochondria of living cells can reduce exogenous MTT to water-insoluble blue-purple crystalline formazan (Formazan) and deposit in the cells, while dead cells do not have this function. Dimethyl sulfoxide (DMSO) can dissolve formazan in cells, and its light absorption value is measured at a wavelength of 490nm with an enzyme-linked immunosorbent detector, which can indirectly reflect the number of living cells.

[0058] (1) Experimental method

[0059] The squamous cell carcinoma A-431 cell line was cultured in DMEM medium with 10% calf serum, added with 100 IU / L penicillin and 100 mg / L streptomycin, and placed in a constant temperature incubator at 37°C and 5% CO2 Routine culture in medium...

Embodiment 3

[0063] Example 3: Long-acting fat-soluble photodynamic preparation containing vitamin E fragments induces apoptosis in skin tumors

[0064] 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.

[0065] (1) Experimental method

[0066] The squamous cell carcinoma A-431 cell line was cultured in DMEM medium with 10% calf serum, added with 100 IU / L penicill...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
strengthaaaaaaaaaa
Login to View More

Abstract

The invention discloses a fat-soluble photosensitizer, and a preparation method and application thereof. According to the invention, vitamin E derivatives and inorganic salts of the derivatives are combined with a photosensitizer for treating skin tumors, and skin collagen fibers can be repaired with the help of the protective effect of the vitamin E on healthy skins while tumor cells can be effectively killed, so that the side effects of medicines are greatly reduced. According to the fat-soluble photosensitizer disclosed by the invention, the drug metabolism rate is slowed, so that the drugeffect is more durable. The photosensitizer containing the vitamin E derivatives can generate more free radicals, so that the tumor cells can be killed more efficiently and quickly. The required dosage is far lower than a required dosage of 5-ALA used in the market, antibiotics are not contained, drug resistance is not generated, and the photosensitizer is safe, non-toxic, economical and practical.

Description

technical field [0001] The invention relates to a fat-soluble photosensitizer and its preparation method and application, belonging to the fields of medical treatment and biomedicine. Background technique [0002] Cutaneous squamous cell carcinoma is a type of skin tumor. Its main features are: it starts as a blemish-like raised mass, with a hard base, a rough surface like a cauliflower, visible telangiectasia, and spike-like cutin at the top. Skin squamous cell carcinoma co-infected with viscous pus, foul smell and pain. Its malignancy is high, and it is easy to transfer, and regional lymph node metastasis is more common, which seriously affects the physical and mental health of patients. [0003] The anti-cancer principle of Photodynamic Therapy (PDT) is a treatment method that mainly affects the target tissue and has dual selectivity. Its dual selectivity is based on the difference in the concentration of the photosensitizer in normal and target tissues, and the direct...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D421/12A61K41/00A61P35/00A61P17/00
CPCA61K41/0057C07D421/12
Inventor 王臻康健黄进华陈静柳岸宋相志郭克华马思祺吴梦媛向亚平丁澍郭爱元陈则夷朱宏王海蓉杨茜妍王萍
Owner THE THIRD XIANGYA HOSPITAL OF CENT SOUTH UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com