WO2021155795A1 - Composition pharmaceutique et son utilisation - Google Patents

Composition pharmaceutique et son utilisation Download PDF

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Publication number
WO2021155795A1
WO2021155795A1 PCT/CN2021/075001 CN2021075001W WO2021155795A1 WO 2021155795 A1 WO2021155795 A1 WO 2021155795A1 CN 2021075001 W CN2021075001 W CN 2021075001W WO 2021155795 A1 WO2021155795 A1 WO 2021155795A1
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pharmaceutical composition
bacteria
pathogen
virus
formate
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PCT/CN2021/075001
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English (en)
Chinese (zh)
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秦才东
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秦才东
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Priority claimed from CN202011259180.7A external-priority patent/CN114432448A/zh
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Publication of WO2021155795A1 publication Critical patent/WO2021155795A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/02—Local antiseptics

Definitions

  • the present invention relates to the field of medicine. Specifically, the present invention relates to a pharmaceutical composition and its application.
  • the invention is a method and application for inhibiting and controlling the pathogenicity of viruses and bacteria and rapid proliferation of inflammatory cells as effectively as possible by inhibiting the gene synthesis process and increasing the alkalinity of body fluids at the same time.
  • each cell and virus contains a large amount of DNA, RNA and other substances.
  • Tumor cells, bacterial cells, and viruses and inflammatory cells involved in the present invention require a large amount of deoxygenation for rapid replication and proliferation.
  • Ribose, ribose, phosphoric acid, purine, and pyrimidine are essential raw materials for the synthesis of DNA and RNA. Among them, only pyrimidine cannot be obtained directly from food, and the production of a large number of pyrimidine nucleotides can only rely on the way of synthesis.
  • pyrimidine nucleotides In most organisms, there are two ways to synthesize pyrimidine nucleotides, one is de novo synthesis and the other is salvage. In quiescent or fully differentiated cells, the synthesis of pyrimidine nucleotides is mainly produced by the salvage pathway, that is, using free pyrimidine bases or pyrimidine nucleosides in the body as raw materials, passing through pyrimidine phosphoribosyltransferase or pyrimidine nucleoside kinase, etc. The process of catalyzing simple reactions to synthesize pyrimidines.
  • the required amount of pyrimidine nucleotides is much greater than that of normal cells, and its synthesis mainly depends on the de novo synthesis pathway in the cell.
  • the fourth step in the de novo synthesis pathway of pyrimidine nucleotides is catalyzed by dihydroorotate dehydrogenase (DHODH), and the dehydrogenation of dihydroorotate to orotate (pyrimidine derivative) is generated by coenzyme Q, etc.
  • DHODH dihydroorotate dehydrogenase
  • coenzyme Q etc.
  • Coenzymes provide oxidizing power.
  • DHODH is divided into two major families according to its amino acid sequence, coenzyme type, and location in the cell.
  • One type is located in the cytoplasm or the inner side of the cytoplasmic membrane and exists in prokaryotes and lower eukaryotes.
  • Its electron acceptor is fumaric acid (ester) or nicotinamide adenine dinucleotide (NAD).
  • NAD nicotinamide adenine dinucleotide
  • the other is located on the outer surface of the inner mitochondrial membrane of mammals and certain protozoa, and uses Coenzyme Q as an electron acceptor.
  • Human dihydroorotate dehydrogenase (hDHODH) belongs to the second category.
  • virus binding to cell receptors is mainly adsorbed on cell surface molecules through virus adsorption proteins (VAPs), and the receptor is the first cell molecule encountered by the virus. If the VAPs protein of the virus or the corresponding receptor on the cell can be shielded, the virus will not be able to recognize and attach to the surface of the host cell, and the infection will not actually occur.
  • VAPs virus adsorption proteins
  • VAPs and viral receptors you can clamp on both sides to block the binding of the virus to the receptor from two aspects. One is to block the binding site of the virus itself, and the other is to block the receptor. Cut off the binding of the virus to the receptor.
  • the purpose and effect of the present invention is to use a special reducing agent to inhibit the infection and proliferation of viruses, fungi, and bacterial cells, as well as the rapid proliferation of inflammatory cells.
  • An object of the present invention is to provide a pharmaceutical composition.
  • Another object of the present invention is to provide the application of the pharmaceutical composition.
  • the purpose and effect of the present invention is to consider and use the characteristic of adsorbing host cells as the first step in the process of all virus infections, to increase the pH value of body fluids, and to reduce the positive levels carried on the viral ligands or host cell receptors.
  • the number of charges reduces the electrostatic adsorption to host cells or viruses carrying opposite charges, and achieves the effect of inhibiting virus and bacterial infections.
  • the microenvironment of the virus is changed, and it actually provides a condition for dissolving blood clots and phlegm clots in the lungs (anticoagulation effect); on the other hand, considering the single use of increasing alkalinity , It may not be able to effectively prevent viral infections.
  • the existing injection of alkaline baking soda solution has not been found to be able to effectively solve the problem of viral infections. Therefore, the technical method that can be used at the same time is from the perspective of basic substances required for gene synthesis. , Complementing each other's inhibitory effectiveness, two-pronged approach to inhibit viral, fungal, and bacterial infections.
  • the present invention provides a pharmaceutical composition, wherein the pharmaceutical composition comprises formate and/or oxalate.
  • the pharmaceutical composition includes formate and oxalate
  • the mass ratio of formate and oxalate is (0.01:99.99) to (99.99:0.01).
  • the mass ratio of formate and oxalate is (10:90) to (90:10); preferably ( 20:80) to (80:20); more preferably (30:70) to (70:30); more preferably (40:60) to (60:40); still more preferably 50:50.
  • formate and/or oxalate are each independently selected from one or a combination of potassium salt, sodium salt, magnesium salt and calcium salt.
  • the pharmaceutical composition is a solid preparation or a solution preparation.
  • the present invention also provides the application of the pharmaceutical composition in the preparation of drugs for treating and inhibiting pathogens.
  • the pathogen is a pathogen that relies on surface charges to electrostatically attract and adhere to host cells.
  • the pathogen is selected from the group consisting of viruses, fungi, bacteria, chlamydia, mycoplasma, and protease toxoids.
  • the present invention also provides a method for inhibiting pathogens, wherein the method comprises administering the pharmaceutical composition of the present invention to animals or plants.
  • the pharmaceutical composition includes formate and/or oxalate.
  • formate and/or oxalate are each independently selected from one or a combination of potassium salt, sodium salt, magnesium salt and calcium salt.
  • the pharmaceutical composition is a solid preparation or a solution preparation.
  • the pathogen is a pathogen that relies on surface charges to electrostatically attract and adhere to host cells.
  • the pathogen is selected from the group consisting of viruses, fungi, bacteria, chlamydia, mycoplasma, and protease toxoids.
  • the bacteria are selected from anaerobic bacteria or aerobic bacteria.
  • the bacteria are charged bacteria.
  • the virus is an enveloped or non-enveloped virus.
  • the fungus is smut or yeast.
  • the method comprises administering the pharmaceutical composition of the present invention to a mammal by a combination of one or more selected from the following administration modes: oral administration, injection, smearing and spray.
  • low-toxic reducing agents can also be used as a choice for human body surface, plants, and animals when there is no other treatment method.
  • the animal is a mammal.
  • the animal is a human.
  • the pharmaceutical composition inhibits the utilization of dihydroorotic acid and/or the dehydrogenation reaction of dihydroorotic acid in the pyrimidine nucleotide synthesis reaction of the pathogen, and simultaneously increases
  • the pH value of body fluids achieves the inhibition of pathogens.
  • the present invention also provides a method for inhibiting the proliferation of viruses, fungi, bacteria, and inflammatory cells, the method comprising using formate, oxalate, or a mixture of both to inhibit viral, fungal or bacterial infections Or the rapid proliferation of inflammatory cells.
  • the use of dihydroorotic acid and/or dihydrolactic acid in the de novo synthesis of pyrimidine nucleotides necessary for DNA or RNA replication is inhibited by the use of formate and oxalate.
  • the dehydrogenation reaction of clear acid and the increase of the pH value of body fluids at the same time can effectively inhibit the proliferation of viruses, fungi and bacteria, infection and rapid proliferation of inflammatory cells.
  • inhibiting the utilization of dihydroorotic acid and/or the dehydrogenation reaction of dihydroorotic acid in the pyrimidine nucleotide synthesis reaction is by reducing intracellular oxidative coenzyme Q, NAD and The quantity or concentration of at least one of the fumaric acid is achieved.
  • the salt includes, but is not limited to, potassium salt, sodium salt, magnesium salt, and calcium salt.
  • the bacteria are aerobic bacteria or anaerobes.
  • the bacteria are charged bacteria.
  • the virus is an enveloped or non-enveloped virus.
  • the present invention also provides an application of a method for inhibiting the proliferation of viruses, fungi, bacteria, and inflammatory cells.
  • Formate and oxalate are used to inhibit viruses and fungi by oral or injection, smearing, spraying, or compound methods.
  • Bacterial infection and proliferation to achieve the effect of prevention and treatment of various viral, fungal or bacterial infections or rapid proliferation of inflammatory cells.
  • the salt includes, but is not limited to, potassium salt, sodium salt, magnesium salt, and calcium salt.
  • the present invention also provides a method for inhibiting the proliferation of viruses, fungi, bacteria, and inflammatory cells.
  • the method includes using a reducing agent to inhibit the de novo synthesis of pyrimidine nucleotides necessary for DNA or RNA replication.
  • the dihydroorotic acid dehydrogenation reaction is a reaction that is converted into orotic acid under the catalysis of dihydroorotic acid dehydrogenase and a coenzyme.
  • the reducing agent is formate, oxalate or a mixture of both.
  • the bacteria are aerobic bacteria or anaerobes.
  • the salt includes, but is not limited to, potassium salt and sodium salt.
  • the method includes the use of reducing substances by oral administration, injection, smearing, spraying, or compounding to inhibit the rapid proliferation of viruses, fungi, bacteria, and inflammatory cells to achieve protection against various viruses, The prevention and treatment of fungal or bacterial infections or rapid proliferation of inflammatory cells.
  • the mechanism is to inhibit or reduce the synthesis of new DNA or RNA by inhibiting the utilization of dihydroorotic acid and/or dehydrogenation of cells. At the same time increase the pH of body fluids.
  • the reducing substance is formate, oxalate or a mixture of the two, and is used as a solid medicament or a solution or a mixed solution.
  • the method includes using formate and other reducing agents as the prevention of viral, fungal, and bacterial infections in daily life, such as using a low concentration (such as mass/mass concentration 1%-30 %, the same below)
  • the solution is used as a daily mouthwash, a small amount added to daily beverages (such as content of 1%-10%), food (contents of 1% to 5%), a small amount added to personal daily cleaning and hygiene products middle.
  • the beverage can be bottled water, drinking water, fruit juice, alcoholic beverage; the food can be flour, rice noodles, pickled products, sauce products, etc.; the personal daily cleaning and hygiene products such as soap, cleaning liquid, skin care products, etc. .
  • the present invention also provides a method for inhibiting pathogens, wherein the method comprises administering the pharmaceutical composition according to any one of the preceding items of the present invention to a mammal as a prevention of pathogen infection.
  • the pharmaceutical composition is a low-concentration solution as a daily mouthwash; or a small amount is added to daily beverages, foods, and daily personal hygiene products.
  • the beverage can be bottled water, drinking water, fruit juice, alcoholic beverage;
  • the food can be flour, rice noodles, pickled products, sauce products, and the like.
  • the personal daily hygiene products such as soap, cleansing liquid, skin care products and the like.
  • the present invention also provides a method for adjusting the pH value of human body fluids, wherein the method comprises administering to the human body any of the aforementioned pharmaceutical compositions of the present invention.
  • the body fluid is blood and/or urine.
  • composition of the present invention inhibits pathogens as follows:
  • the inventor of the present application found that the isoelectric point of most viruses is between pH 4-5.5, and that of most bacteria is pH 3-4. Therefore, most viruses and bacteria carry negative charges under physiological conditions. Since the virus itself does not provide energy for metabolism, the attachment and binding of virus ligands to specific receptors on the cell membrane as the initial step of virus replication can only passively rely on the electrostatic attraction between the ligand and the receptor.
  • cell receptors when cell receptors are positively charged, they can only selectively accept viruses with negatively charged ligands. Similarly, when cell receptors are negatively charged, they can only selectively accept viruses with positively charged ligands. . It can be reasonably expected that if the nature and quantity of surface charges of viruses, fungi, bacteria or cell receptors can be actively adjusted, then whether the viruses, fungi, bacteria and cells can bind or the probability of binding can also be adjusted accordingly.
  • the charge of the surface proteins of viruses or cells comes from the hydrolysis reaction of amino and carboxyl groups on amino acid residues, where amino groups tend to carry positive charges and carboxyl groups tend to carry negative charges.
  • the reaction is affected by the pH value of the solution, so if the pH value of the solution (saliva, gastric juice or blood and other body fluids) can be actively adjusted, it can actively affect the charge state of viruses, bacteria, cell surfaces, and the electrostatic attraction between each other. size. Increase the pH of the solution. If there are undissociated carboxyl groups on the negatively charged amino acid residues, the negatively charged amino acid residues will continue to increase the number of negative charges until all the carboxyl groups on the amino acid residues are dissociated.
  • the present invention further uses reducing substances to inhibit the synthesis of pyrimidine derivatives by the dehydrogenation reaction of dihydroorotic acid in pyrimidine de novo synthesis.
  • the most important advantage of the present invention is that it has found reducing substances such as sodium formate, which can increase the alkalinity of body fluids through intermediate reactions, and can inhibit chemical reactions in the de novo synthesis of pyrimidines.
  • Sodium formate has the following tendency to react in an ionic manner in an aqueous solution (or body fluid):
  • reducing oxalate has a similar dehydrogenation reaction and can also form alkaline carbonate.
  • the salt can be sodium salt, potassium salt, magnesium salt, calcium salt and the like.
  • the above-mentioned reduced coenzyme Q is oxidized and restored to oxidized coenzyme Q in the cell.
  • the presence of sodium formate can at least reduce the amount or concentration of oxidative coenzyme Q, NAD, and fumaric acid, thus inhibiting dihydrogen
  • the effect of orotic acid is converted into orotic acid, thereby inhibiting the synthesis efficiency and quantity of pyrimidine nucleotides.
  • reducing sodium formate changes the chemical potential in the cell, thereby affecting the catalytic activity of the oxidizing coenzyme. According to the Nernst equation, this change is concentration-dependent.
  • the tricarboxylic acid cycle can provide a large amount of coenzyme NAD.
  • the effect of sodium formate on coenzyme NAD is weakened or ignored, so it does not affect the glycolytic part of normal cells. , Does not affect the tricarboxylic acid cycle.
  • reducing agents such as sodium formate do not affect the synthesis of pyrimidine nucleotides required for normal cell repair or division.
  • NADPH (Sodium formate + water) "dehydrogenation," the dehydrogenation is transferred to the oxidizing coenzyme NADP, which is converted into the reducing coenzyme NADPH.
  • NADPH is mainly derived from the intracellular pentose phosphate pathway and is not affected by sodium formate reducing agent.
  • Aerobic bacteria will continue to proliferate under suitable conditions.
  • the coenzymes NAD and NADPH in aerobic bacteria cells will not be affected by reducing agents, but the proliferation of aerobic bacteria or DNA replication depends on pyrimidine nucleosides.
  • the de novo synthesis reaction of acid provides reducing agents such as sodium formate with an opportunity and method to inhibit the growth of aerobic bacteria.
  • the reason is that the bacterial DHODH is located inside the cytoplasm or cytoplasmic membrane. Therefore, the NAD provided by the oxidation reaction in the mitochondria has no or only a small effect on the amount of the coenzyme NAD of DHODH.
  • the present invention breaks through the traditional technical habit of dealing with viruses only by focusing on the virus itself. Indirectly, the present invention controls the rapid replication of host cells' genes, which also controls the virus, and also breaks through the original inhibition of de novo synthesis of pyrimidine nucleotides in cells. The way of thinking cannot or did not think of the limitations of thinking that can be directly applied to non-cellular viruses.
  • Reducing agents such as sodium formate inhibit or reduce the quantity and concentration of oxidative coenzyme Q, NAD, and fumaric acid, and reduce the efficiency and quantity of pyrimidine nucleotide synthesis, and therefore, can indirectly inhibit the replication of viral DNA or RNA.
  • the number of virus replication, infectivity, and destructive power are limited, and the reaction preparation that inhibits the conversion of dihydroorotic acid into orotic acid becomes a broad-spectrum antidote to the virus.
  • the material and energy consumption of the host cell is expected to increase sharply, which may change the cell's respiratory metabolism to aerobic glycolysis.
  • lactic acid, a metabolite of respiratory reaction accumulates in the blood, and the acidic blood environment promotes the formation of embolism, which leads to various embolism problems.
  • the virus causing cell cancer may be related to the long-term change of the cell respiration pattern by the virus.
  • reducing agents such as sodium formate can not only inhibit the glycolytic respiratory reaction of cancer cells and anaerobic bacteria by inhibiting coenzyme NAD, but also inhibit the de novo synthesis of pyrimidine nucleotides by inhibiting oxidative coenzyme Q, NAD and fumaric acid.
  • the present invention also has the advantage of controlling the replication and synthesis of viral genes, cancer cells, bacterial cells, and inflammatory cells by controlling the synthesis reaction of gene replication, and solves the global drug resistance caused by gene mutation from the source. problem.
  • One of the advantages of the present invention is that because the pH value of body fluid can be increased, it helps to alleviate the problem of phlegm plug caused by pneumonia caused by virus or bacterial infection.
  • the synthesis of pyrimidine nucleotides is essential for virus replication by host cells, and for the proliferation and metabolism of cancer cells, bacterial cells, and inflammatory cells. Therefore, the method for inhibiting viruses, bacteria, and inflammatory cells of the present invention
  • the use of reducing agents such as formate, oxalate or a mixture of both not only increases the alkalinity of body fluids, hinders the electrostatic attraction contact between the virus and the host cell, but also inhibits the pyrimidine nucleus necessary for DNA or RNA replication
  • the utilization of dihydroorotic acid and/or the dehydrogenation reaction of dihydroorotic acid in the de novo synthesis reaction of uronic acid realizes the inhibition of viral and bacterial infection and proliferation, and the inhibition of the proliferation of inflammatory cells.
  • the method of the present invention for inhibiting viruses, bacteria, and inflammatory cells is to use the characteristic of adsorbing host cells as the first step in the infection process of all viruses, increase the pH value of body fluids, and reduce the viral ligands or host cell receptors carried The number of positive charges reduces the electrostatic adsorption to host cells or viruses carrying opposite charges. At the same time, it has the effect of inhibiting the de novo synthesis path of pyrimidine in virus or bacterial gene replication, and overcomes the effect of inhibiting the de novo synthesis path of pyrimidine alone to inhibit virus or bacterial infection.
  • Chlamydia and protease toxoids also use their outer surface membrane proteins to adhere to host cells as the first step to cause disease.
  • the proliferation and replication also involve gene synthesis. Therefore, the method of the present invention is also suitable for similar electrostatic attraction by surface charges.
  • Various pathogens that adhere to host cells Mycoplasma adheres to the surface of epithelial cells and red blood cells through its own adhesion protein. Therefore, in the present invention, mycoplasma can be used as a generalized bacteria or generalized virus that can carry charges. Because it can adhere to red blood cells, mycoplasma carries a positive charge and is therefore easily neutralized by an environment with increased pH.
  • Fig. 1 is a photograph of the surface of the water chestnut in Example 4.
  • the left picture shows the water chestnut surface immersed in the dihydroorotic acid solution alone, and the right picture is the water chestnut surface immersed in the dihydroorotic acid solution and added with sodium formate.
  • Figure 2 is a photograph of the surface of the dough surface of Example 5 added with dihydroorotic acid (the upper part of the figure) and both dihydroorotic acid and sodium formate (the lower part of the figure).
  • Oxalate also has a similar reaction as described above.
  • B is an oxidative substance (such as active free radicals) or an oxidative reaction process that can accept electrons in human body fluids or cells.
  • the above reaction not only inactivates free radicals or participates in redox reactions, such as inhibiting the de novo synthesis of pyrimidine, but also provides the human body with hydroxide anions that increase pH.
  • the individual specific dosage or the dosage required for direct injection because it is to adjust the pH value of body fluids, and everyone’s initial pH value is different, and the total amount of body fluids is also not the same. Therefore, it is necessary to achieve the same The pH level, the required dosage or injection volume are different. For the actual operation of all the embodiments, it can be increased or decreased according to the pH value of urine or blood. For example, when the pH value of urine is lower than 5.5, the dosage can be increased by 1 gram per day until the pH value of urine is not high. Is below 8 (the upper limit of the normal value), or the pH of the blood is not higher than 7.87.
  • Four hospital blood tests during the continuous use period The report showed that the blood pH value reached 7.57, 7.76, 7.87, and 7.77. During the period, the body felt good, indicating that the pH value of the blood of patients taking formate can be significantly increased, and can reach 7.87.
  • the above phenomenon shows that sodium formate itself inhibits the proliferation of smut fungus, and also inhibits the utilization and conversion of the added dihydroorotic acid of smut fungus. Because the smut is a fungus, it is an aerobic bacteria, so sodium formate will not affect its respiratory metabolism. What can affect should be the reaction of dihydroorotic acid dehydrogenation to orotic acid, thereby inhibiting the pyrimidine nucleus The synthesis of glycosides leads to the obstacles to the synthesis of DNA by smut fungus.
  • the coenzyme of the dihydroorotic acid dehydrogenation reaction in Zizania smut cells may be coenzyme NAD or coenzyme Q.
  • the above test can at least prove that reducing substances such as sodium formate can inhibit one of the coenzyme NAD or coenzyme Q of DHODH. After replacing the above sodium formate with sodium oxalate, similar experimental results were obtained.
  • the pH value of the dough added with sodium formate was about 3 according to the test paper, and the pH value of the dough added with dihydroorotic acid was about 4.
  • the dough (top of Figure 2) to which dihydroorotic acid was added alone was covered with a layer of turquoise mycelium about 5-10 mm thick, and dihydroorotic acid and dihydroorotic acid were added at the same time.
  • the surface of the sodium formate dough (bottom of Figure 2) is still the original milky white of the dough (the red part left on the surface of the dough is the color left by the wet pH test paper when the test is pressed, and the pH test shows that the pH is about 4). See there are hyphae. It shows that sodium formate has a long-lasting inhibitory effect on the proliferation of yeast bacteria (see Figure 2), because it inhibits the proliferation of bacteria by inhibiting the pyrimidine synthesis pathway in gene synthesis. Therefore, as long as the yeast has a long-lasting inhibitory effect, reducing agents such as A Acid salts have the same or similar inhibitory effect on the proliferation of other bacteria.
  • the acidic dihydroorotic acid (pKa 3.41) is converted to use synthetic pyrimidine nucleotides, as it is consumed, the pH value of the dough increases; while the dough added with sodium formate or sodium oxalate, the reducing agent inhibits the dihydrogen
  • the consumption reaction of orotic acid should be to inhibit and slow down the dehydrogenation conversion reaction of dihydroorotic acid in yeast cells, so the pH value of the dough basically remains unchanged or slowly increases.
  • the inhibition of fermentation by sodium formate and sodium oxalate should not be by inhibiting glycolysis, but by inhibiting the dehydrogenation reaction of dihydroorotic acid, that is, inhibiting the dehydrogenation reaction of dihydroorotic acid.
  • the coenzyme NAD or coenzyme Q The higher the concentration of reducing agent such as sodium formate, the stronger the inhibitory effect of coenzyme, therefore, the inhibitory effect is dose-dependent.
  • mitochondria can provide a large amount of coenzyme NAD products, according to the fact that the bacterial dihydroorotate dehydrogenase is located in the cytoplasm or inside the cytoplasmic membrane, it can be expected that the tricarboxylic acid cycle in the mitochondria will not be directly Influencing the catalytic reaction of DHODH here, in particular, does not directly affect the mutual conversion reaction between the coenzyme NAD-NADH of dihydroorotate dehydrogenase.
  • the aqueous solution of sodium formate reduces the oxidized coenzyme Q10, reduces the hydrophobic carbonyl group in the coenzyme to a hydrophilic hydroxyl group, increases the solubility of the coenzyme, and promotes the miscibility of the reducing coenzyme fine particles with the aqueous solution to form a colloid.
  • reducing agents such as sodium formate have the effect of inhibiting various viruses, in line with the theory of charge neutralization and the anticipation of the theory of inhibiting viral gene replication.
  • the neutralization of charge plus the inhibition of gene synthesis increases the effectiveness of a single action. It can be presumed that according to the same principle, it can also have the effect of inhibiting other viruses.
  • reducing agents such as formate can also be used to prevent viral and bacterial infections, such as using a low concentration (for example, 1%-30% by weight) solution as a daily routine
  • a low concentration (for example, 1%-30% by weight) solution as a daily routine
  • a small amount of mouthwash is added to daily beverages (for example, the content is 1%-10% by weight), food (the content is 1% to 5% by weight), and a small amount is added to personal daily cleaning and hygiene products.
  • the beverage can be bottled water, drinking water, fruit juice, alcoholic beverage; the food can be flour, rice noodles, pickled products, sauce products, etc.; the personal daily cleaning and hygiene products such as soap, cleaning liquid, skin care products, etc. .
  • Hepatitis B virus including its satellite virus, hepatitis D virus (HDV), like other enveloped viruses or non-enveloped viruses, must bind to cell surface receptor molecules to infect host cells.
  • the N-terminal of the hepatitis B virus ligand carries a positive charge, while the host cell receptor correspondingly carries a negative charge.
  • a hepatitis B virus carrier took 1 g of sodium formate a day. After half a year, the indicators were checked, and the somatosensory and indicators were all improved.
  • the reduction of the virus charge coupled with the inhibitory effect of the reducing agent on the de novo synthesis of pyrimidine in gene synthesis, has the effect of inhibiting the replication of hepatitis B virus.
  • hemagglutinin HA or a protein similar to hemagglutinin can be found on the surface of measles virus, mumps virus, parainfluenza virus, rubella, and many other bacteria and viruses as a ligand for the virus to invade host cells, thus increasing body fluids Alkalinity can also reduce the pathogenicity of these viruses by reductively inhibiting the de novo pyrimidine synthesis pathway in the process of gene replication.
  • influenza virus adheres and binds to host cells through hemagglutinin HA, and then enters the cell. It is known that the surface of red blood cells is negatively charged, and it is naturally speculated that hemagglutinin HA, as a viral ligand, carries a positive charge.
  • Increasing the alkalinity of body fluids will reduce the number of positive charges carried by hemagglutinin HA and reduce the pathogenicity of the virus.
  • the inhibitory effect of reducing agents on the de novo pyrimidine synthesis pathway will weaken the pathogenic effect and pathogenic symptoms of viral infections. .
  • the effect of taking potassium formate on a person with advanced AIDS is provided.
  • the patient took 3 grams of potassium formate (taken in 3 times) every day. After 3 days, the appetite was significantly increased, and the breathing, physical fitness, and body feeling gradually improved, which had the effect of relieving symptoms. .
  • CD4 molecule is a single-chain transmembrane protein mainly present on the surface of T cells.
  • the isoelectric point of chicken CD4 molecule is 10.1 (under physiological conditions, it is positively charged). It is speculated that it has great similarities with mammalian CD4 molecules.
  • the most noteworthy extracellular region of CD4 is its N-terminal (positively charged) two Ig-like regions, because they are binding regions with MHCII and are also HIV (human immunodeficiency virus) gp120 binding sites (for human CD4). In terms of).
  • the CD4 molecule is the primary receptor for the HIV virus to enter human cells.
  • MHC II should also be able to bind to CD4 only if it carries a negative charge. This inference is consistent with the previously speculated MHC II isoelectric point of 6.89.
  • a patient with cervical polyps is provided. Without other treatment, he simply took 15 ml of sodium formate saturated solution plus 15 ml of potassium formate saturated solution twice a day. After taking 30 days, the polyp was about 6 mm The size is so large that the endoscopy disappears.
  • the human papillomavirus HPV genome encodes E1, E2, E3, E4, E5, E6, E7, and L1, L2 capsid proteins, respectively.
  • the E1-E4 proteins are associated with host cell keratin through their N-terminal leucine-rich motifs. Therefore, the virus adsorption protein VAP is E1, and its N-terminus carries a positive charge, and the receptor keratin protein carries a negative charge.
  • a middle-aged man has a piece of local neurodermatitis on his neck (diagnosed by the hospital) with a size of 2 cm in diameter. He sweats in the summer and itching every day. The prescription drugs of hormones do not work for half a year. After 10 ml 3 times a day for 2 weeks, he basically recovered. It is estimated that the inhibition of pyrimidine synthesis inhibits the de novo pyrimidine synthesis step in gene synthesis required for rapid proliferation of inflammatory cells.
  • the hospital medical record diagnosis of an elderly man is erythema with unclear trunk and limb boundaries, papules, scratches, dry and cracked skin, and itching for about 1 year.
  • the symptoms of itching have not been controlled.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Birds (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une composition pharmaceutique comprenant du formiate et/ou de l'oxalate, et l'utilisation de la composition pharmaceutique dans l'inhibition d'infections provoquée par des agents pathogènes.
PCT/CN2021/075001 2020-02-03 2021-02-03 Composition pharmaceutique et son utilisation WO2021155795A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN202010100912 2020-02-03
CN202010100912.1 2020-02-03
CN202011259180.7A CN114432448A (zh) 2020-11-03 2020-11-03 一种抑制病毒、细菌的方法和应用
CN202011259180.7 2020-11-03

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WO2021155795A1 true WO2021155795A1 (fr) 2021-08-12

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109549952A (zh) * 2017-09-27 2019-04-02 秦才东 一种抑制细胞糖酵解过程的方法及应用
CN110559284A (zh) * 2018-06-06 2019-12-13 秦才东 一种增加血液碱性、溶解含酯及脂沉积物的方法及应用

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109549952A (zh) * 2017-09-27 2019-04-02 秦才东 一种抑制细胞糖酵解过程的方法及应用
CN110559284A (zh) * 2018-06-06 2019-12-13 秦才东 一种增加血液碱性、溶解含酯及脂沉积物的方法及应用

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