CN105412052A - Application of Micranthanone A in preparing drugs for anti-helicobacter pylori - Google Patents
Application of Micranthanone A in preparing drugs for anti-helicobacter pylori Download PDFInfo
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- CN105412052A CN105412052A CN201510961133.XA CN201510961133A CN105412052A CN 105412052 A CN105412052 A CN 105412052A CN 201510961133 A CN201510961133 A CN 201510961133A CN 105412052 A CN105412052 A CN 105412052A
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- helicobacter pylori
- micranthanonea
- micranthanone
- drugs
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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
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
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- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses application of Micranthanone A in preparing drugs for anti-helicobacter pylori, the Micranthanone A can be used for treating diseases such as acute gastritis, chronic gastritis, gastric ulcer, duodenal ulcer and the like, and is applied to preparation of drugs for treating acute gastritis, chronic gastritis, gastric ulcer, duodenal ulcer and the like, due to the fact that a matrix type belongs to a new matrix type, and the inhibitory activity to helicobacter pylori is high, the Micranthanone A has outstanding substantive features, and obviously has remarkable improvement for prevention and treatment of helicobacter pylori infection at the same time.
Description
Technical field
The present invention relates to the novelty teabag of compound MicranthanoneA, particularly relate to MicranthanoneA and preparing the application in Anti-helicobacter pylori drugs.
Background technology
Helicobacter pylori (Helicobacterpylori, Hp) is a kind of Gram-negative spiral bacteria.Research display, helicobacter pylori is the primary pathogenic event of acute and chronic gastritis and taste-blindness rate, and may fall ill relevant with gastric cancer stomach function regulating mucosa-associated lymphoid tissue (MALT) malignant lymphoma.Recently, Hp is classified as I class carcinogen by World Health Organization (WHO), and it plays a leading role in stomach cancer development.Simultaneously the scheme that popular at present treatment Hp infects takes the triple therapy that proton pump inhibitor (PPI) adds two kinds of antibiotic (clarithromycin, amoxicillin, tetracycline, metronidazole etc. select two kinds).The main factor affecting triple therapy is considered to the drug resistance of Hp to antibacterial; Another serious problems are that proton pump inhibitor can bring out dyspepsia, and a large amount of antibacterial then causes the serious destruction of flora in digestive tract.Therefore, find the active kind new medicine thing of efficient, safe anti-Hp and become an important and urgent task.
The compound MicranthanoneA that the present invention relates to is one and delivers (MengkeZhang in 2013, etal., MicranthanoneA, aNewDiterpenewithanUnprecedentedCarbonSkeletonfromRhodod endronmicranthum, OrganicLetters, 2013, 15 (12): 3094 – 3097.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to immunomodulating, (MengkeZhang, etal., MicranthanoneA, aNewDiterpenewithanUnprecedentedCarbonSkeletonfromRhodod endronmicranthum, OrganicLetters, 2013, 15 (12): 3094 – 3097.), the MicranthanoneA that the present invention relates to belongs to first public preparing the purposes in Anti-helicobacter pylori drugs.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of anti-helicobactor pylori activity according in existing MicranthanoneA research, provide MicranthanoneA and preparing the application in Anti-helicobacter pylori drugs.
Described compound MicranthanoneA, structure is as shown in formula I:
The application of described MicranthanoneA in Anti-helicobacter pylori drugs, helicobacter pylori is helicobacter pylori reference culture ATCC43504.
A kind of Anti-helicobacter pylori drugs, be that active component interpolation adjuvant is prepared from by MicranthanoneA, preparation method, for getting 5 g of compound MicranthanoneA, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
A kind of Anti-helicobacter pylori drugs, be that active component adds adjuvant and is prepared from by MicranthanoneA, preparation method, for getting 5 g of compound MicranthanoneA, adds starch 195 grams, mixing, encapsulatedly makes 1000.
The experiment in vitro of MicranthanoneA shows, MicranthanoneA has very strong anti Helicobacter pylori activity, and it is 17mm (ATCC43504) that paper disk method shows its antibacterial circle diameter.With agar dilution display, it can suppress the growth of 5 random clinical strains (Hp001, Hp003, Hp004, Hp018 and Hp036) and 1 reference culture (ATCC43504) completely, and minimal inhibitory concentration (MIC) is 0.46 μ g/ml.Make positive control with ampicillin, its Cmin (MIC) suppressed completely 6 strain test bacterium is 5.9 μ g/ml.
This result of study shows, the energy force rate ampicillin of the suppression helicobacter pylori activity of MicranthanoneA is strong, illustrate for the diseases such as the closely-related acute and chronic gastritis of helicobacter pylori, duodenal ulcer, MicranthanoneA is the compound of a great exploitation potential for its.It can be directly used in the treatment of corresponding disease and the preparation of related drugs.
The purposes of the MicranthanoneA that the present invention relates in preparation treatment Anti-helicobacter pylori drugs belongs to first public, because framework types belongs to brand-new framework types, and it is strong for helicobacter pylori inhibit activities, possess outstanding substantive distinguishing features, the control simultaneously for helicobacter pylori infections obviously has significant progress.
Detailed description of the invention
The preparation method of compound MicranthanoneA involved in the present invention is see document (MengkeZhang, etal., MicranthanoneA, aNewDiterpenewithanUnprecedentedCarbonSkeletonfromRhodod endronmicranthum, OrganicLetters, 2013,15 (12): 3094 – 3097.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound MicranthanoneA tablet involved in the present invention:
Get 5 g of compound MicranthanoneA, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound MicranthanoneA capsule involved in the present invention:
Get 5 g of compound MicranthanoneA, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The pharmacological evaluation of experimental example 3:MicranthanoneA
1) strains tested: helicobacter pylori reference culture ATCC43504 is purchased from U.S.'s Culture Collection (AmericanTypeCultureCollection, ATCC).15 strain Hp clinical strains are picked up from Jiangsu Prov. People's Hospital Gastroenterology dept., clinical laboratory of Jiangsu TCM Hospital and Nanjing Children's Hospital Dndoscope Laboratory and are accepted gastroscopic patient; To the patient of peptic ulcer, duodenal bulbar inflammation or gastritis verrucosa in continuous gastroscopy, first be defined as Hp positive through RUT experiment, get antral gastric mucosa 1-2 block again, be inoculated in the Columbia selectivity agar culture medium containing 8% horse serum, trimethoprim 1.25g/L, Polymyxin B2 500U/L, vancomycin 10mg/L after chopping, in 37 DEG C under micro-oxygen environment (5%O2,10%CO2 and 85%N2) cultivate 72 hours.Collect antibacterial, through smear Gram’s staining, after oxidase, catalase and urease are accredited as the positive, pure culture of going down to posterity, obtained strains is as experimental strain.
2) strain culturing: we adopt micro-aerobic bag (purchased from Shanghai Medical Univ) to carry out the strain culturing of HP, it produces the micro-aerobic environment required for Hp by chemical reaction.
3) biological activity determination: adopt paper disk method to measure compound to the inhibitory action of helicobacter pylori, measure the minimum inhibitory concentration of test sample with agar dilution.
I. paper disk method experiment: (A) prepares culture medium by the Columbia culture medium for preparing after high pressure steam sterilization, be cooled to 50-60 DEG C, add 8% horse serum or Sheep Blood, mixing is poured in the culture dish of sterilizing, every ware 7-10ml, culture medium thickness is 1.5mm (sterile working).(B) experimental bacteria of transferring (being coated with bacterium) gets diluted 10 with microscale sampler
8cFU/ml (1OD660=10
8cFU/ml), the bacteria suspension 0.1ml of Hp spreads upon suitable culture dish surface equably.Be inverted in 37 DEG C of drying bakers and take out after 15min, object makes agar surface dry, for subsequent use.(C) paste sample scraps of paper microscale sampler to get 6 μ l testing samples (mass concentration 2mg/ml) and inject on the round filter paper of sterilizing.With aseptic nipper tweezer containing the scraps of paper of sample and the blank scraps of paper of contrast, by sterile working respectively the scraps of paper be close to containing bacterio-agar surface, paste a piece of paper sheet at a certain distance.Often kind of bacterium is cooked 3 wares, and acquired results asks its meansigma methods.(D) cultivate each plate is placed in micro-aerobic bag, sealing, opens gas generator, then is placed in 37 DEG C of incubators and cultivates 72h.(E), after surveying antibacterial circle diameter taking-up flat board, the size of antibacterial circle diameter around each scraps of paper is measured respectively.With reference to the result of matched group, the result of testing sample sensitive experiment can be drawn.In triplicate.
II. agar dilution measures MIC:(A) first compound dimethyl sulfoxide (DMSO) solution preparation of test is become the mother solution of 0.5mg/ml, then with sterilized water dilution, is finally made into 10.0 by the preparation of Drug plates, 8.0,6.0,4.5,4.0,3.5,3.0,2.5,2.0,1.5,1.0, the concentration series of 0.5 and 0.25 μ g/ml, DMSO concentration is in media as well less than 1%.The test compounds solution prepared by 1ml separately adds in the 9ml Columbia medium of 50 DEG C the horse serum that 1ml is incubated in 50 DEG C and fully mixes with being incubated, and casts in culture dish to cool.(B) experimental bacteria of transferring (being coated with bacterium) draws diluted 1 × 10 with microscale sampler
8the bacteria suspension 0.1ml of CFU/mlHp spreads upon culture dish surface equably, is inverted in 37 DEG C of drying bakers and takes out after 15min, and object makes agar surface dry, for subsequent use.(C) determine that test dish (contains: 85%N2,10%CO at micro-aerobic bag by MIC
2and 5%O
2) in, be incubated 37 DEG C and cultivate 72 hours, observe Hp growing state, contrast with blank group, there is no the sample least concentration of bacteria growing completely for minimum inhibitory concentration value.Positive control is ampicillin.
4) the pharmacological results of MicranthanoneA: experiment in vitro shows, MicranthanoneA has very strong anti Helicobacter pylori activity, and it is 17mm (ATCC43504) that paper disk method shows its antibacterial circle diameter.With agar dilution display, it can suppress the growth of 5 random clinical strains (Hp001, Hp003, Hp004, Hp018 and Hp036) and 1 reference culture (ATCC43504) completely, and minimal inhibitory concentration (MIC) is 0.46 μ g/ml.Make positive control with ampicillin, its Cmin (MIC) suppressed completely 6 strain test bacterium is 5.9 μ g/ml.
Conclusion: MicranthanoneA suppresses the energy force rate ampicillin of helicobacter pylori activity strong, illustrate for the diseases such as the closely-related acute and chronic gastritis of helicobacter pylori, duodenal ulcer, MicranthanoneA is the compound of a great exploitation potential for its.It can be directly used in the treatment of corresponding disease and the preparation of related drugs.
Claims (4)
- The application of 1.MicranthanoneA in Anti-helicobacter pylori drugs, described compound MicranthanoneA structure is as shown in formula I:
- 2. the application of MicranthanoneA in Anti-helicobacter pylori drugs as claimed in claim 1, is characterized in that helicobacter pylori is helicobacter pylori reference culture ATCC43504.
- 3. an Anti-helicobacter pylori drugs, it is characterized in that by MicranthanoneA described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound MicranthanoneA, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
- 4. an Anti-helicobacter pylori drugs, it is characterized in that by MicranthanoneA described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound MicranthanoneA, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510961133.XA CN105412052A (en) | 2015-12-20 | 2015-12-20 | Application of Micranthanone A in preparing drugs for anti-helicobacter pylori |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510961133.XA CN105412052A (en) | 2015-12-20 | 2015-12-20 | Application of Micranthanone A in preparing drugs for anti-helicobacter pylori |
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| Publication Number | Publication Date |
|---|---|
| CN105412052A true CN105412052A (en) | 2016-03-23 |
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| CN201510961133.XA Pending CN105412052A (en) | 2015-12-20 | 2015-12-20 | Application of Micranthanone A in preparing drugs for anti-helicobacter pylori |
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| CN (1) | CN105412052A (en) |
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2015
- 2015-12-20 CN CN201510961133.XA patent/CN105412052A/en active Pending
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Application publication date: 20160323 |