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Serial drug capable of catalyzing decomposition of hydrogen dioxide by phytochromes

A technology of catalytic decomposition and hydrogen peroxide, applied in the direction of active ingredients of peroxides, drug combinations, and photodisintegration of drugs in the body, etc., can solve problems such as decreased photofrin content, weakened therapeutic effect, and difficulty in implementing continuous and repeated treatments

Inactive Publication Date: 2014-04-16
WUXI ZHAOZHEN RADIATION TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(2) PDT rapidly destroys photofrin during the treatment, causing the content of photofrin to drop rapidly, and the therapeutic effect is weakened accordingly
[0035] Continuous and repeated treatment: traditional PDT is difficult to implement continuous and repeated treatment due to the destruction of photofrin, often with the help of interventional methods

Method used

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  • Serial drug capable of catalyzing decomposition of hydrogen dioxide by phytochromes
  • Serial drug capable of catalyzing decomposition of hydrogen dioxide by phytochromes
  • Serial drug capable of catalyzing decomposition of hydrogen dioxide by phytochromes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0109] Example 1: Weak bases and OH radicals catalyze H 2 o 2 decomposition reaction

[0110] experimental method:

[0111] (1) Take a 10ml vacuum bottle and completely seal the vacuum bottle with Kodak photosensitive film light-proof paper.

[0112] (2) Different concentrations of H 2 o 2 (in DMF:H 2 O=1:5) into a sealed vacuum bottle.

[0113] (3) Add 5 uM of 9,10 dimethylanthracene (DMA). DMA is a 1 o 2 The specific indicator (probe), DMA has strong fluorescent properties, binding 1 o 2 After that, an endorperoxide that does not have fluorescent properties is formed, therefore, 1 o 2 The amount of production is inversely proportional to the content of DMA.

[0114] (4) 50MeV X-ray irradiation vacuum bottle, dose 5Gy, start H 2 o 2 Decomposition reaction; stop X-ray irradiation to terminate the reaction.

[0115] (5) Or add 0.1mM FeCl 3 (FeCl 3 ·6H 2 O) and 0.1mM Vit-C, decompose H 2 o 2 generate, start H 2 o 2 Decomposition reaction for 5 minutes, 20%...

Embodiment 2

[0120] Example 2: Weak base and photofrin catalyzed H 2 o 2 decomposition reaction

[0121] experimental method:

[0122] (1) Take a 10ml vacuum bottle and completely seal the vacuum bottle with Kodak photosensitive film light-proof paper.

[0123] (2) Different concentrations of H 2 o 2 (in DMF:H 2 O=1:5) into a sealed vacuum bottle.

[0124] (3) Add 5 uM of 9,10 dimethylanthracene (DMA). DMA is a 1 o 2 The specific indicator (probe), DMA has strong fluorescent properties, binding 1 o 2 After that, an endorperoxide that does not have fluorescent properties is formed, therefore, 1 o 2 The amount of production is inversely proportional to the content of DMA.

[0125] (4) Add 15uM Haematoporphyrin derivative, and react at 25°C for 8 hours.

[0126] Experimental results:

[0127] As a result, with OH catalyzed H 2 o 2 The decomposition reaction is similar, when H 2 o 2 At concentrations lower than or equal to 0.15%, hematoporphyrin alone does not significantly ...

Embodiment 3

[0131] Embodiment 3: photofrin and physical method catalyze H 2 o 2 Decomposition reaction (RCDT method)

[0132] experimental method:

[0133] (1) Take a 10ml vacuum bottle and completely seal the vacuum bottle with Kodak photosensitive film light-proof paper.

[0134] (2) Different concentrations of H 2 o 2 (in DMF:H 2 O=1:5) into a sealed vacuum bottle.

[0135] (3) Add 5 uM of 9,10 dimethylanthracene (DMA). DMA is a 1 o 2 The specific indicator (probe), DMA has strong fluorescent properties, binding 1 o 2 After that, an endorperoxide that does not have fluorescent properties is formed, therefore, 1 o 2 The amount of production is inversely proportional to the content of DMA.

[0136] (4) Add 15uM Haematoporphyrin derivative (HPD), or 15uM acidified porphyrin (Protoporphyrin IX, PpIX).

[0137] (5) 10MeV X-ray irradiates the vacuum bottle for about 1 minute, the dose is 5Gy, and the H 2 o 2 decomposition reaction. Irradiation was stopped to terminate the re...

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Abstract

In the invention, phytochromes are activated in focuses such as tumors, vascular patches and skin diseases, in a fixed-point and fixed-quantity way by a specific means through the utilization of the specific affinity action of the phytochromes on the focuses, the decomposition reaction of H2O2 is catalyzed by the phytochromes to generate <1>O2, and the apoptosis or the necrosis of pathological cells is caused, thereby achieving the purpose of treating the diseases. A corresponding serial novel drug is screened, developed and used for CDT (Chemodynamic Therapy) or RCDT (Radiochemodynamic Therapy). The invention relates to the serial novel drug which is used for CDT and RCDT. The serial novel drug can catalyze the chemical reaction of decomposing the H2O2 to generate the <1>O2, does not have obvious side effect on the normal tissues and organs of a human body, and meanwhile, has the capability of affiliating the focuses. The phytochromes are used as a catalyst, and the acting mechanism, the usage, the therapeutic effect and the like of the phytochromes are completely different from those of traditional photo-dynamic therapy. Oxygen and visual light are not needed, and a completely independent novel drug series can be formed.

Description

technical field [0001] The present invention relates to a kind of in vivo decomposing hydrogen peroxide (H 2 o 2 ) to produce singlet oxygen ( 1 o 2 ) series of new drugs for the treatment of diseases or beauty, which can be used for "Chemodynamic Therapy" (Chemodynamic Therapy, CDT), or for "Radiochemodynamic Therapy" (Radiochemodynamic Therapy, RCDT) through radiation. Radiation directly excites phytochrome to realize the treatment method "Radiodynamic Therapy, Radiodynamic Therapy RDT". Background technique: [0002] Traditional photodynamic therapy (PDT) utilizes the specific affinity of photofrin to tumors, vascular plaques and skin diseases, and then irradiates the lesion with visible light of a specific wavelength that can be absorbed by photofrin. After absorbing light energy, the O 2 change into 1 o 2 , 1 o 2 And then lead to apoptosis or necrosis of diseased cells, so as to achieve therapeutic effect. However, due to the poor tissue penetration of visible...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K45/00A61K31/409A61P35/00A61P9/00A61P29/00A61P27/02A61P13/08A61P17/00A61K33/40A61K33/00
CPCA61K41/0052A61K31/409A61K41/0057A61K31/495A61P9/00A61P13/08A61P17/00A61P27/02A61P29/00A61P35/00A61K38/42A61K49/20A61K51/08A61K41/0042
Inventor 曾骏孙启银
Owner WUXI ZHAOZHEN RADIATION TECH
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