Photodynamic treatment medicament, medical composition and preparation method thereof

A technology of drugs and compounds, which is applied in the field of photodynamic therapy drugs, pharmaceutical compositions and their preparation, can solve the problems of limiting the therapeutic effect of photodynamic therapy and the inability of external light sources to penetrate deep tissues, and achieve the effect of avoiding damage

Active Publication Date: 2012-10-17
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the requirement for external light sources limits the therapeutic effect of photodynamic therapy in deep tissues, because the absorption and scattering effects of biological tissues prevent external light sources from penetrating deep tissues.
Although infrared light can reduce the absorption and scattering effects of biological tissues, the development of photosensitizers that absorb infrared light efficiently (such as two-photon photosensitizers) remains a challenge

Method used

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  • Photodynamic treatment medicament, medical composition and preparation method thereof
  • Photodynamic treatment medicament, medical composition and preparation method thereof
  • Photodynamic treatment medicament, medical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The synthesis of compound OPV shown in embodiment 1, formula I

[0054] For the synthetic route map, see figure 1 .

[0055]

[0056] 1. Synthesis of Compound 2 (Formula 2)

[0057] Add 1.7g of compound 1 (Formula 1), 70mL of acetone deoxygenated, 5.6g of potassium carbonate, 0.14g of 18-crown-6 and 20g of 1,6-dibromohexane into a 250mL single-necked bottle, and heat up to 75°C for 3 days . Add 100mL of water to quench the reaction, then add 100mL of dichloromethane to extract the product, the organic phase is dried with anhydrous magnesium sulfate, and the solvent is evaporated and then separated on a silica gel column (eluent: dichloromethane:petroleum ether=1:5, v / v) Afterwards, 2.5 g of white solid were obtained. Characterization of the product: 1H NMR (400MHz, CDCl3) δ7.27 (s, 1H), 6.98 (s, 1H), 3.95 (m, 4H), 3.43 (m, 4H), 1.91 (m, 4H), 1.82 ( m, 4H), 1.54 (m, 8H).13C NMR (100MHz, CDCl3) δ152.62, 150.50, 124.37, 117.19, 112.66, 33.91, 32.78, 29.82, 29.07, ...

Embodiment 2

[0070] Example 2, the pharmaceutical composition composed of luminol luminescent system and OPV is used for killing cancer cells

[0071] (1) Determination of bioluminescence energy transfer spectrum between luminol and OPV

[0072] Add 3 μL 1 mg / mL HRP (horseradish peroxidase) pH7.0 sodium dihydrogen phosphate solution, 10 μL 20 mM luminol, 10 μL 50 mM p-iodophenol aqueous solution and different concentrations of OPV to 967 μL pH9.0 sodium carbonate buffer (to make the final concentrations of 10 μM, 20 μM, 30 μM, 40 μM and 50 μM respectively), after vortexing for 5 s, add 10 μL of 50 mM hydrogen peroxide aqueous solution and vortex for 2 s to measure the luminescence spectrum immediately, and the spectral range is 370 nm to 700 nm. See figure 2 .

[0073] (2), culture of HeLa cells

[0074] HeLa cells were cultured in DMEM medium containing 10% bovine serum in a constant temperature incubator containing 5% carbon dioxide at 37°C.

[0075] (3), HeLa cell survival analysis...

Embodiment 3

[0079] Example 3. The composite drug composed of luminol luminescent system and OPV is used for tumor suppression in mice

[0080] (1) Formation of HeLa cell tumor model in nude mice

[0081] Will contain 2 x 10 6 200 μL PBS buffer solution of HeLa cells was subcutaneously injected in the axilla of the left forelimb of 14-15 g female nude mice, and 40 mice were inoculated.

[0082] (2), administration in groups

[0083] According to the sequence of injected cells, they were divided into 4 groups, with 10 rats in each group, that is, each group had the first injection and the second injection. The first group is a blank control group, only injected with 100 μL of normal saline; the second group is a positive control group, injected with enzymes and substrates, first injected with 50 μL of HRP (0.01 mg / mL), luminol luminescence enhancer (p-iodophenol , 1.25mM) and luminol (0.5mM) normal saline solution, then injected 50μL hydrogen peroxide normal saline solution (2mM); the th...

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Abstract

The invention discloses a photodynamic treatment medical composition which consists of a photosensitizer and a chemical activator, wherein the photosensitizer is expressed by the formula I; the chemical activator comprises luminol, p-iodophenol, horse radish peroxidase and hydrogen peroxide; and the proportion of the photosensitizer expressed by the formula I, to the luminol to the p-iodophenol to the horse radish peroxidase to the hydrogen peroxide in the composition is 8-12muM:0.4-0.7mM:1-1.5mM:0.01-0.02mg/mL:2-3mM. In the composition of the invention, active oxygen generated by bioluminescence energy transfer between the photosensitizer expressed by the formula I and the luminol is utilized to kill cells and fungi. Compared with the traditional photodynamic treatment method, the composition can be used for treating in deep tissues; and damages to normal tissues, which are caused by long-time irradiation by an external light source, can be avoided; and meanwhile, the composition has a profound influence on the aspects of the clinic treatment of tumors and pathogenic bacteria infection.

Description

technical field [0001] The invention relates to a medicine for photodynamic therapy, a medicine composition and a preparation method thereof. Background technique [0002] Since it was first applied clinically in the 1980s, photodynamic therapy has become a new type of therapy after chemotherapy, surgery and radiation therapy. Photodynamic therapy has been widely used in the clinical treatment of various tumors, ophthalmology and skin-related diseases. Photosensitizer, light source and molecular oxygen are the three most important elements for generating cytotoxic reactive oxygen species in photodynamic therapy. The main advantage of photodynamic therapy is its spatial selectivity in disease treatment, that is, photosensitizers will only be sensitized when excited by selected wavelengths. However, the requirement for external light sources limits the therapeutic effect of photodynamic therapy in deep tissues, because the absorption and scattering effects of biological tiss...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/64A61K38/44A61K41/00A61K45/00A61P31/10A61P35/00A61K31/055A61K31/4178A61K31/502A61K33/40
Inventor 王树袁焕祥刘礼兵
Owner INST OF CHEM CHINESE ACAD OF SCI
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