CN106344577A - Application of Fistulains A in anti-helicobacter pylori drugs - Google Patents
Application of Fistulains A in anti-helicobacter pylori drugs Download PDFInfo
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- CN106344577A CN106344577A CN201610854181.3A CN201610854181A CN106344577A CN 106344577 A CN106344577 A CN 106344577A CN 201610854181 A CN201610854181 A CN 201610854181A CN 106344577 A CN106344577 A CN 106344577A
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- fistulains
- helicobacter pylori
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- General Health & Medical Sciences (AREA)
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Abstract
An in vitro activity experiment shows that Fistulains A has higher anti-helicobacter pylori (Hp) activity, can be used for treating diseases such as acute gastritis, chronic gastritis, gastric ulcer and duodenal ulcer, is applied in preparing drugs for treating the acute gastritis, the chronic gastritis, the gastric ulcer and the duodenal ulcer, has a prominent substantial characteristic, and makes remarkable progress on preventing helicobacter pylori infection at the same time.
Description
Technical field
The present invention relates to the new application of compound fistulains a, more particularly, to fistulains a are preparing anti-pylorus
Application in Helicobacter pylori medicine.
Background technology
Helicobacter pylori is a kind of spiral type, micro- anaerobism, the Gram-negative bar very harsh to growth conditionss requirement
Bacterium.Nineteen eighty-three separates success first from the Mucosa Biopsy of chronic active gastritis patient tissue, be current known can be
The only microbe species of existence in people's stomach.Gastritis that helicobacter pylori disease includes being caused by Helicobacter pylori infection, disappear
Change road ulcer, lymphoproliferative gastric lymphoma etc..The poor prognosis of helicobacter pylori disease are gastric cancer.Therefore, find efficient, peace
Complete anti-hp activity one kind new medicine thing becomes an important and urgent task.
Compound fistulains a according to the present invention be one deliver within 2015 (min zhou, et al.,
fistulains a and b,new bischromones from the bark of cassia fistula,and their
Activities.org.lett.2015,17,2638-2641.) noval chemical compound, this compound has brand-new framework types,
There is antivirus action (min zhou, et al., fistulains a and b, new bischromones from the
Bark of cassia fistula, and their activities.org.lett.2015,17,2638-2641.), for
Purposes in preparing Anti-helicobacter pylori drugs for the fistulains a according to the present invention belongs to first public.
Content of the invention
It is an object of the invention to not finding in studying according to existing fistulains a that it has anti-helicobacter pylori and lives
The present situation of the report of property, there is provided application in preparing Anti-helicobacter pylori drugs for the fistulains a.
Described compound fistulains a, shown in structure such as formula ():
Application in preparing Anti-helicobacter pylori drugs for the described fistulains a, helicobacter pylori is helicobacter pylori
Helicobacter pylori, hp reference culture atcc 43504.
A kind of Anti-helicobacter pylori drugs, add adjuvant by fistulains a for active component and are prepared from, preparation side
Method is to take 5 g of compound fistulains a, adds 195 grams of dextrin, mixes, and Conventional compression makes 1000.
A kind of Anti-helicobacter pylori drugs, add adjuvant by fistulains a for active component and are prepared from, preparation side
Method is to take 5 g of compound fistulains a, adds 195 grams of starch, mixes, and encapsulated makes 1000.
This result of study shows, the ability of the suppression helicobacter pylori activity of fistulains a is stronger than ampicillin,
Illustrate for the diseases such as the acute and chronic gastritis closely related with helicobacter pylori, duodenal ulcer,
Fistulains a is the compound of a great exploitation potential.It can be directly used for treatment and the related drugs of corresponding disease
Preparation.
Purposes in preparation treatment Anti-helicobacter pylori drugs for the fistulains a according to the present invention belongs to public first
Open, because framework types belong to brand-new framework types, and it is unexpectedly strong for helicobacter pylori inhibitory activity, no
There is the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for Helicobacter pylori
The preventing and treating of dye obviously has and significantly improves.
Specific embodiment
The preparation method of compound fistulains a involved in the present invention referring to document (min zhou, et al.,
fistulains a and b,new bischromones from the bark of cassia fistula,and their
activities.org.lett.2015,17,2638-2641.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to concrete reality
Apply any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound fistulains a tablet involved in the present invention:
Take 20 g of compound fistulains a, 180 grams of the customary adjuvant of tablet is prepared in addition, mix, conventional tablet presses
Make 1000.
Embodiment 2: the preparation of compound fistulains a capsule involved in the present invention:
Take 20 g of compound fistulains a, customary adjuvant such as 180 grams of the starch of capsule is prepared in addition, mix, dress
Capsule makes 1000.
To further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The pharmacological evaluation of embodiment 3:fistulains a
1) strains tested
Helicobacter pylori (helicobacter pylori, hp) reference culture atcc 43504 is purchased from U.S.'s fungi preservation
Center (american type culture collection, atcc).15 plants of hp clinical strains pick up from Jiangsu Prov. People's Hospital
Gastroenterology dept., clinical laboratory of Jiangsu TCM Hospital and Nanjing Children's Hospital Dndoscope Laboratory accept gastroscopic patient；In continuous gastroscope
Patient to peptic ulcer, duodenal bulbar inflammation or gastritis verrucosa in inspection, is first defined as hp sun through RUT experiment
Property person, then take antral gastric mucosa 1-2 block, be inoculated in after chopping containing 8% horse serum, trimethoprim (trimethropin,
Tmp) 1.25g/l, polymyxin (polymyxin) b2500u/l, the columbia of vancomycin (vancomycin) 10mg/l
In selectivity agar culture medium, in 37 DEG C of (5%o2,10%co2 and 85%n2) culture 72 hours under micro- oxygen environment.Collect thin
Bacterium, through smear Gram’s staining, after oxidase, catalase and urease are accredited as the positive, passes on pure culture, obtained strains are as reality
Test bacterial strain.
2) strain culturing
We carry out the strain culturing of hp using micro- aerobic bag (purchased from Shanghai Medical Univ), and it can be produced by chemical reaction
Micro- aerobic environment required for raw hp.
3) biological activity determination
The inhibitory action to helicobacter pylori for the compound is measured using paper disk method, measures test sample with agar dilution
Minimum inhibitory concentration (mic).
I. paper disk method experiment
A the columbia preparing culture medium after high pressure steam sterilization, is cooled to 50-60 DEG C by () preparation culture medium,
Plus 8% horse serum or Sheep Blood, mix and be poured in sterilized culture dish, every ware 7-10ml, culture medium thickness are 1.5mm
(sterile working).
B () switching experimental bacteria (applying bacterium) takes the 108cfu/ml (1od660=108cfu/ml) having diluted with microscale sampler
The bacteria suspension 0.1ml of hp is equably applied to suitable culture dish surface.Take out after being inverted in 15min in 37 DEG C of drying bakers, mesh
Make agar surface be dried, standby.
C () patch sample scraps of paper microscale sampler takes 6 μ l testing sample (mass concentration 2mg/ml) injections sterilized
On circle filter paper.Contain the scraps of paper and the comparison virgin paper sheet of sample with aseptic nipper tweezer, the scraps of paper are close to respectively by sterile working
Surface containing bacterio-agar, pastes a piece of paper piece at a certain distance.Every kind of bacterium is cooked 3 wares, and acquired results seek its meansigma methods.
D each plate is placed in micro- aerobic bag for () culture, sealing is opened gas generator, then is placed in 37 DEG C of incubators
Culture 72h.
E () surveys antibacterial circle diameter taking-up flat board after, measure the size of antibacterial circle diameter around each scraps of paper respectively.With reference to comparison
The result of group, can draw the result of testing sample sensitive experiment.In triplicate.
Ii. agar dilution measures mic
A compound dimethyl sulfoxide (dmso) solution of test is configured to 0.5mg/ by the preparation of () Drug plates first
The mother solution of ml, then with sterilized water dilution, finally it is made into 10.0,8.0,6.0,4.5,4.0,3.5,3.0,2.5,2.0,1.5,1.0,
The concentration series of 0.5 and 0.25 μ g/ml, dmso concentration in media as well is less than 1%.The test compound that 1ml is prepared is molten
Liquid separately adds, in 50 DEG C of 9ml Columbia medium, the horse serum that 1ml is incubated in 50 DEG C and fully mixes with being incubated, and casts into culture
Cool down in ware.
B the bacteria suspension of the 1 × 108cfu/ml hp having diluted is drawn in () switching experimental bacteria (applying bacterium) with microscale sampler
0.1ml is equably applied to culture dish surface, takes out after being inverted in 15min in 37 DEG C of drying bakers, and purpose makes agar surface be dried,
Standby.
C () determines that test dish (is contained: 85%n2,10%co by mic in micro- aerobic bag2And 5%o2) in, it is incubated 37 DEG C
Culture 72 hours, is observed hp growing state, is contrasted with blank group, be minimum with the sample least concentration not having bacteria growing completely
Mlc (mic) value.Positive control is ampicillin.
Experiment in vitro shows, fistulains a has very strong anti Helicobacter pylori activity, and paper disk method shows its suppression
Bacterium loop diameter is 16mm (atcc43504).Show that it can completely inhibit 5 random clinical strains with agar dilution
(hp001, hp003, hp004, hp018 and hp036) and the growth of 1 reference culture (atcc43504), minimal inhibitory concentration
(mic) it is 0.56 μ g/ml.Make positive control with ampicillin, its Cmin (mic) to 6 plants of test bacterium complete inhibitions
For 3.3 μ g/ml.
Conclusion: fistulains a suppress helicobacter pylori activity ability stronger than ampicillin, illustrate for imprison
For the diseases such as the closely related acute and chronic gastritis of door pylori, duodenal ulcer, fistulains a is one
The compound of great exploitation potential.It can be directly used for the treatment of corresponding disease and the preparation of related drugs.
Claims (4)
- Application in Anti-helicobacter pylori drugs for the 1.fistulains a, described compound fistulains a structure such as formula Shown in ():
- 2. application in Anti-helicobacter pylori drugs for the fistulains a as claimed in claim 1 is it is characterised in that pylorus spiral shell Bacillus is helicobacter pylori helicobacter pylori, hp reference culture atcc 43504.
- 3. a kind of Anti-helicobacter pylori drugs are it is characterised in that added for active component by fistulains a described in claim 1 Plus adjuvant is prepared from, preparation method is to take 5 g of compound fistulains a, adds 195 grams of dextrin, mixes, Conventional compression Make 1000.
- 4. a kind of Anti-helicobacter pylori drugs are it is characterised in that added for active component by fistulains a described in claim 1 Plus adjuvant is prepared from, preparation method is to take 5 g of compound fistulains a, adds 195 grams of starch, mixes, encapsulated system Become 1000.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610854181.3A CN106344577A (en) | 2016-09-27 | 2016-09-27 | Application of Fistulains A in anti-helicobacter pylori drugs |
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| CN201610854181.3A CN106344577A (en) | 2016-09-27 | 2016-09-27 | Application of Fistulains A in anti-helicobacter pylori drugs |
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| CN201610854181.3A Pending CN106344577A (en) | 2016-09-27 | 2016-09-27 | Application of Fistulains A in anti-helicobacter pylori drugs |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105294720A (en) * | 2015-05-08 | 2016-02-03 | 云南民族大学 | Dimerization chromone alkaloid compound as well as preparation method and application thereof |
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- 2016-09-27 CN CN201610854181.3A patent/CN106344577A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105294720A (en) * | 2015-05-08 | 2016-02-03 | 云南民族大学 | Dimerization chromone alkaloid compound as well as preparation method and application thereof |
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Application publication date: 20170125 |