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Application of piperidinium-2,3-dihydroxy-5-((2R,3R)-3,5,7-trihydroxy-4-oxochroman-2-yl)phenolate (PDTOP) in preparation of medicines for treating or preventing diseases of respiratory system

A technology for respiratory diseases and phenol theophyllic acid, applied in the field of phenolic theophyllic acid and its preparation and application, can solve problems such as unknown mechanism of action, and achieve the effect of preventing the spread of influenza and preventing invasion

Active Publication Date: 2016-08-31
梁京
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the mechanism of action is unknown

Method used

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  • Application of piperidinium-2,3-dihydroxy-5-((2R,3R)-3,5,7-trihydroxy-4-oxochroman-2-yl)phenolate (PDTOP) in preparation of medicines for treating or preventing diseases of respiratory system
  • Application of piperidinium-2,3-dihydroxy-5-((2R,3R)-3,5,7-trihydroxy-4-oxochroman-2-yl)phenolate (PDTOP) in preparation of medicines for treating or preventing diseases of respiratory system
  • Application of piperidinium-2,3-dihydroxy-5-((2R,3R)-3,5,7-trihydroxy-4-oxochroman-2-yl)phenolate (PDTOP) in preparation of medicines for treating or preventing diseases of respiratory system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1. preparation of phenol theophyllic acid

[0032] The phenol theophyllic acid (PDTOP) of the present invention is a synthetic flavonoid compound. Also known as phenol dihydromyricetin (English name: Piperidinium2,3-dihydroxy-5-((2R,3R)-3,5,7-trihydroxy-4-oxochroman-2-yl)phenolate, PDTOP)

[0033] The chemical formula is:

[0034] The preparation method of phenol theophyllic acid of the present invention:

[0035] Add five millimoles (5mmol, 1.6g) of dihydromyricetin to 20 milliliters of methanol and dissolve for 30 minutes, place the dissolved solution in an ice bath, and titrate with 5.5 millimoles of piperidine in the presence of argon at -10°C Add dihydromyricetin methanol solution, leave it for 20 minutes to make it react completely, then, concentrate the reaction solution under low pressure vacuum situation, after filtering, wash three times with methanol to obtain phenotheophylline (about 2g).

[0036] The preparation method of dihydromyricetin: ...

Embodiment 2

[0043] Embodiment 2. The animal experiment of preventing and treating smog

[0044] Experimental animals: conventional experimental white mice, male / female, with a body weight of 300 / 275 grams, respectively. 6 groups;

[0045] Experimental drug: phenol theophyllic acid;

[0046] Experimental drug dosage and configuration:

[0047] 1) 0.5 mg / kg body weight; or

[0048] or

[0049]3) Put 1 gram of agar into 100 milliliters of experimental water, boil it, add 0.05 grams of phenol theophyllic acid, stir well, let it cool until it becomes frozen. Give 1cm 3 Agar jelly (containing 0.5 mg phenol theophyllic acid element). or

[0050] 4) Measuring metabolic rate: 1cm 3 Agar jelly contains 0.2 grams of phenol theophyllic acid. or

[0051] 5) For toxicity determination: 1cm 3 Agar jelly contains 0.2 grams of phenol theophyllic acid.

[0052] (Note: at 500mg / 1cm 3 Give 75000 grams of body weight as the standard, 500 mg / 75000 grams of body weight=x / 300 grams of experimental w...

Embodiment 3

[0064] Embodiment 3. The experiment of phenol theophyllic acid anti-influenza A (H1N1) virus infection

[0065] Influenza A (H1N1) virus 252 (± 34) micrograms per milliliter of particles was used to determine the antiviral effect of phenol theophylline. H1N1 virus particles were co-incubated with dog kidney cells for a total of 2 hours in a medium containing phenocin and washed 3 times. Filter through a filter and remove unbound compounds with common culture medium. Virus particles were harvested and analyzed using a direct binding assay—the phenolic acid-bound and unbound fractions of the virus were then compared.

[0066] The results showed that phenol theophyllic acid had obvious dose-dependent inhibitory effect on H1N1 virus infection ( figure 2 ). 50% inhibitory concentration (IC) of phenol theophyllic acid to H1N1 50 ) is 2.4 micrograms / ml (8μM), and 100% inhibits the concentration of H1N1 virus infection (IC 100 ) micrograms / ml (27 μM).

[0067] The mechanism of p...

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PUM

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Abstract

The invention discloses piperidinium-2,3-dihydroxy-5-((2R,3R)-3,5,7-trihydroxy-4-oxochroman-2-yl)phenolate (PDTOP) and a preparation method thereof, and applications thereof in treatment or prevention on diseases of a respiratory system. The applications include: a mask with a PDTOP layer attached thereto; a sprayer filled with a PDTOP solution; PDTOP oral tablets; and PDTOP oral liquid. These applications can avoid or greatly reduce damage on health due to haze for people who are exposed to haze, can reduce at least infection on lung and upper respiratory, lung diseases and cancer incidence. In addition, these applications have advantages in all industrial environments with dust. In a high-occurrence season of influenza, a PDTOP preparation can effectively prevent invasion of the influenza to human body and prevent spread of the influenza.

Description

technical field [0001] The invention relates to a phenol theophyllic acid and its preparation and application. The product is used for personal protection in polluted areas, virus-infected areas, toxic chemical work areas and various dust work environments. Background technique [0002] The composition of haze is very complex, including hundreds of atmospheric chemical particulate matter. Among them, aerosol particles with a diameter of less than 10 microns are mainly harmful to health, such as mineral particles, sea salt, sulfate, nitrate, organic aerosol particles, fuel and vehicle exhaust, etc., which can directly enter and adhere to the human respiratory tract and alveoli Among them, especially submicron particles will be deposited in the upper and lower respiratory tract and alveoli respectively, causing acute rhinitis and acute bronchitis and other diseases. For patients with chronic respiratory diseases such as bronchial asthma, chronic bronchitis, obstructive emphys...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P11/00A61P11/06A61P31/04A61P31/12A61P11/02
CPCA61K31/352
Inventor 梁京
Owner 梁京
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