CN103356608A - Application of Fluevirosines A in preparing anti-helicobacter pylori medicines - Google Patents
Application of Fluevirosines A in preparing anti-helicobacter pylori medicines Download PDFInfo
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- CN103356608A CN103356608A CN201310338173XA CN201310338173A CN103356608A CN 103356608 A CN103356608 A CN 103356608A CN 201310338173X A CN201310338173X A CN 201310338173XA CN 201310338173 A CN201310338173 A CN 201310338173A CN 103356608 A CN103356608 A CN 103356608A
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Abstract
In-vitro activity tests show that Fluevirosines A has a high anti-helicobacter pylori (Hp) activity. The Fluevirosines A can be used for treating acute and chronic gastritis, gastric ulcer, duodenal ulcer, etc. and for preparing medicines used for treating the acute and chronic gastritis, the gastric ulcer and the duodenal ulcer. The application of the Fluevirosines A in preparing the anti-helicobacter pylori medicines is firstly disclosed. The framework type is a brand-new framework type, and therefore the Fluevirosines A is impossibly revealed by other compounds. The Fluevirosines A has outstanding substantive characteristics. Meanwhile, the Fluevirosines A has significant progress in preventing and treating helicobacter pylori infection.
Description
Technical field
The present invention relates to the new purposes of compound F 17-hydroxy-corticosterone luevirosines A, relate in particular to the application of Fluevirosines A in the preparation Anti-helicobacter pylori drugs.
Background technology
Helicobacter pylori (Helicobacter pylori, Hp) is a kind of Gram-negative spiral bacteria.Studies show that helicobacter pylori is the main pathogenesis of acute and chronic gastritis and Stomach duodenum ulcer, and may be relevant with the morbidity of gastric cancer stomach function regulating mucosa-associated lymphoid tissue (MALT) malignant lymphoma.Therefore, seek the active kind new medicine thing of efficient, safe anti-Hp and become an important and urgent task.
The compound F 17-hydroxy-corticosterone luevirosines A that the present invention relates to is one and delivered (Hua Zhang in 2013, et al., Fluevirosines A-C:A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa.Organic Letters, 2013,15(1): noval chemical compound 120 – 123.), this chemical compound has brand-new framework types, present purposes only has certain cytotoxicity (Hua Zhang to leukemia and lung carcinoma cell, et al., Fluevirosines A-C:A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa.Organic Letters, 2013,15(1): 120 – 123.), the purposes of the Fluevirosines A that the present invention relates in the preparation Anti-helicobacter pylori drugs belongs to open first.
Summary of the invention
The object of the invention is to provides the application of Fluevirosines A in the preparation Anti-helicobacter pylori drugs according to not finding that it has the present situation of the report of anti-helicobactor pylori activity in the existing Fluevirosines A research.
Described compound F 17-hydroxy-corticosterone luevirosines A, structure is shown in formula I:
Formula I
The experiment in vitro of Fluevirosines A shows that Fluevirosines A has very strong anti Helicobacter pylori activity, and paper disk method shows that its antibacterial circle diameter is 17mm (ATCC43504).With agar dilution show it can suppress fully 5 at random clinical strains (Hp001, Hp003, Hp004, Hp018 and Hp036) and the growth of 1 reference culture (ATCC43504), minimal inhibitory concentration (MIC) is 0.31 μ g/ml.Make positive control with the ampicillin, it is 3.5 μ g/ml to the Cmin (MIC) that 6 strains test bacterium suppresses fully.
This result of study shows, the energy force rate ampicillin of the inhibition helicobacter pylori activity of Fluevirosines A is strong, explanation for the diseases such as the closely-related acute and chronic gastritis of helicobacter pylori, duodenal ulcer, Fluevirosines A is the chemical 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 Fluevirosines A that the present invention relates in preparation treatment Anti-helicobacter pylori drugs belongs to open first, because framework types belongs to brand-new framework types, and do not exist by other chemical compounds provide any enlightenment may, possess outstanding substantive distinguishing features, the control that is used for simultaneously helicobacter pylori infections obviously has significant progress.
The specific embodiment
The preparation method of compound F 17-hydroxy-corticosterone luevirosines A involved in the present invention is referring to document (Hua Zhang, et al., Fluevirosines A-C:A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa.Organic Letters, 2013,15(1): 120 – 123.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compound F 17-hydroxy-corticosterone luevirosines A tablet involved in the present invention:
Get 5 and digest compound Fluevirosines A, add dextrin 195 grams, mixing, conventional tabletting are made 1000.
Embodiment 2: the preparation of compound F 17-hydroxy-corticosterone luevirosines A capsule involved in the present invention:
Get 5 and digest compound Fluevirosines A, add starch 195 grams, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
The pharmacological evaluation of Fluevirosines A
1) strains tested
Helicobacter pylori (Helicobacter pylori, Hp) reference culture ATCC43504 is purchased from U.S.'s strain and preserves center (American Type Culture Collection, 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; In continuous gastroscopy to the patient of peptic ulcer, duodenal bulbar inflammation or gastritis verrucosa, be defined as the Hp positive through the RUT experiment first, get again antral gastric mucosa 1-2 piece, be inoculated in after the chopping and contain 8% horse serum, trimethoprim (trimethropin, TMP) in the Columbia selectivity agar culture medium of 1.25g/L, polymyxin (polymyxin) B2500U/L, vancomycin (vancomycin) 10mg/L, in 37 ℃ under little oxygen environment (5%O2,10%CO2 and 85%N2) cultivated 72 hours.Collect antibacterial, through the smear Gram’s staining, after oxidase, catalase and urease are accredited as the positive, the pure culture of going down to posterity, obtained strains is as experimental strain.
2) strain culturing
We adopt little aerobic bag (available from Nanjing Medical University) to carry out the strain culturing of HP, and it can produce the needed little aerobic environment of Hp by chemical reaction.
3) biological activity determination
Adopt paper disk method (Microbiological paper method) to measure chemical compound to the inhibitory action of helicobacter pylori, measure the minimum inhibitory concentration (minimal inhibitory concentration, MIC) of test sample with agar dilution.
I. paper disk method experiment
(A) prepare culture medium with the Columbia culture medium for preparing behind high pressure steam sterilization, be cooled to 50-60 ℃, add 8% horse serum or Sheep Blood, mixing is poured in the culture dish of having sterilized, every ware 7-10ml, culture medium thickness are 1.5mm (sterile working).
(B) switching experimental bacteria (being coated with bacterium) is got the bacteria suspension 0.1ml that dilutes good 108CFU/ml (1OD660=108CFU/ml) Hp with microscale sampler and is spread upon equably suitable culture dish surface.Be inverted in 37 ℃ of drying bakers and take out behind the 15min, purpose makes agar surface dry, for subsequent use.
(C) pasting the sample scraps of paper gets 6 μ l testing samples (mass concentration 2mg/ml) with microscale sampler and injects on the round filter paper of having sterilized.Contain the scraps of paper and the blank scraps of paper of contrast of sample with the aseptic nipper tweezer, by the sterile working respectively the scraps of paper be close to and contain the bacterio-agar surface, paste at a certain distance a piece of paper sheet.Every kind of bacterium is cooked 3 wares, and acquired results is asked its meansigma methods.
(D) cultivation places little aerobic bag with each plate, and gas generator is opened in sealing, places 37 ℃ of incubators to cultivate 72h again.
(E) after the survey antibacterial circle diameter takes out flat board, measure respectively each scraps of paper size of antibacterial circle diameter on every side.With reference to the result of matched group, can draw the result of testing sample sensitive experiment.Triplicate.
II. agar dilution is measured MIC
(A) preparation of medicine flat board at first becomes the mother solution of 0.5mg/ml with the chemical compound of test with dimethyl sulfoxide (DMSO) solution preparation, dilutes with sterilized water again, finally is made into 10.0,8.0,6.0,4.5,4.0,3.5,3.0,2.5,2.0,1.5,1.0,0.5 with the concentration series of 0.25 μ g/ml, the concentration of DMSO in medium is less than 1%.The test compounds solution that 1ml is prepared adds in addition 1ml in 50 ℃ 9ml Colombia culture medium and is incubated in the abundant mixing of 50 ℃ horse serum with being incubated, and casts to cool off in the culture dish.
(B) switching experimental bacteria (being coated with bacterium) is drawn the bacteria suspension 0.1ml that dilutes good 1 * 108CFU/ml Hp with microscale sampler and is spread upon equably the culture dish surface, is inverted in and takes out behind the 15min in 37 ℃ of drying bakers, and purpose makes agar surface dry, for subsequent use.
(C) determine that MIC (contains culture dish to be measured: 85%N2,10%CO at little aerobic bag
2And 5%O
2) in, be incubated 37 ℃ and cultivated 72 hours, observe the Hp growing state, contrast with the blank group, take the sample least concentration that do not have bacteria growing fully as minimum inhibitory concentration (minimal inhibitory concentration, MIC) value.Positive control is ampicillin (Ampicillin).
3, the pharmacological results of Fluevirosines A
The experiment in vitro of Fluevirosines A shows that Fluevirosines A has very strong anti Helicobacter pylori activity, and paper disk method shows that its antibacterial circle diameter is 17mm (ATCC43504).With agar dilution show it can suppress fully 5 at random clinical strains (Hp001, Hp003, Hp004, Hp018 and Hp036) and the growth of 1 reference culture (ATCC43504), minimal inhibitory concentration (MIC) is 0.31 μ g/ml.Make positive control with the ampicillin, it is 3.5 μ g/ml to the Cmin (MIC) that 6 strains test bacterium suppresses fully.
Conclusion: it is strong that Fluevirosines A suppresses the energy force rate ampicillin of helicobacter pylori activity, explanation for the diseases such as the closely-related acute and chronic gastritis of helicobacter pylori, duodenal ulcer, Fluevirosines A is the chemical 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 (1)
1.Fluevirosines the application of A in the preparation Anti-helicobacter pylori drugs, described compound F 17-hydroxy-corticosterone luevirosines A structure is shown in formula I:
Formula I.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104761572A (en) * | 2015-03-11 | 2015-07-08 | 暨南大学 | Flueggea suffruticosa-type alkaloid dimer-type compound or pharmaceutically acceptable salt thereof, preparation method and application thereof |
-
2013
- 2013-08-05 CN CN201310338173XA patent/CN103356608A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| HUA ZHANG ET AL: "Fluevirosines A-C: A Biogenesis inspiredexample in the Discovery of New Bioactive Scaffolds from Flueggea virosa. Hua Zhang et al.Organic Letters. 2013,Vol. 15, No. 1 ,120–123.", 《ORGANIC LETTERS》 * |
| RENU SOLANKI: "Some medicinal plants with antibacterial activity. Renu Solanki. Pharmacie Globale (IJCP). 2010, 4 (10),1-4", 《PHARMACIE GLOBALE (IJCP)》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104761572A (en) * | 2015-03-11 | 2015-07-08 | 暨南大学 | Flueggea suffruticosa-type alkaloid dimer-type compound or pharmaceutically acceptable salt thereof, preparation method and application thereof |
| CN104761572B (en) * | 2015-03-11 | 2017-04-12 | 暨南大学 | Flueggea suffruticosa-type alkaloid dimer-type compound or pharmaceutically acceptable salt thereof, preparation method and application thereof |
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Application publication date: 20131023 |