CN103285024A - The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine - Google Patents
The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine Download PDFInfo
- Publication number
- CN103285024A CN103285024A CN2013102539214A CN201310253921A CN103285024A CN 103285024 A CN103285024 A CN 103285024A CN 2013102539214 A CN2013102539214 A CN 2013102539214A CN 201310253921 A CN201310253921 A CN 201310253921A CN 103285024 A CN103285024 A CN 103285024A
- Authority
- CN
- China
- Prior art keywords
- polyflavanostilbene
- tubercle bacillus
- tuberculosis
- preparing
- medicine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
The invention discloses the applications of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine. Aimed at the current situation that the morbidity and mortality of tuberculosis are on the rise due to the high morbidity of tuberculosis and the appearance of multi-drug resistant strain of mycobacterium tuberculosis at present, the invention discovers that Polyflavanostilbene A has obvious activity in suppressing tubercle bacillus, and has good application prospects. The application of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine is disclosed for the first time; and since the skeleton type is a brand new one and the activity in suppressing tubercle bacillus is unexpectedly high, the possibility of any prompt given by other compounds does not exist, and prominent substantive features are provided and a remarkable progress in preventing and treating tubercle bacillus infection.
Description
Technical field
The present invention relates to the new purposes of Compound P olyflavanostilbene A, relate in particular to the application of Polyflavanostilbene A in preparation treatment anti-tubercle bacillus drugs.
Background technology
Global morbidity lungy in recent years is increases trend, estimate according to The World Health Organization (WHO), the whole world is subjected to mycobacterium tuberculosis (Mycobacterium tuberculosis at present, MTB) population of Gan Raning accounts for 1/3rd of world population, and wherein the infected of 5～10% becomes tuberculosis patient.Active tuberculosis patient 1,300,000 examples every year appears in China, about 600,000 examples of infectiousness pulmonary tuberculosis wherein, and wherein about 600,000 examples of infectiousness pulmonary tuberculosis are one of the high burden of global tuberculosis countries.
Come out one after another from antituberculotics, make treatment lungy play epoch-making variation.Yet because the treatment of tuberculosis patient management standard very not still, irregular chemotherapy, the abuse antituberculotics makes tuberculosis drug resistance situation serious day by day, and chemical sproof variation more trends towards multiple medicine drug resistance simultaneously, and this causes very big difficulty for preventing and controlling lungy.Therefore seek new antituberculotics, the antituberculotics of especially anti-multidrug resistance is to the protection people's health, and is significant.
The Compound P olyflavanostilbene A that the present invention relates to is one and delivered (Fushuang Li in 2013, et al., Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters, 2013,3 (15), 674 – 677.) noval chemical compound, this chemical compound has brand-new framework types, present purposes only suppresses alpha-glucosidase activity (Fushuang Li, et al., Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters, 2013,3 (15), 674 – 677.), belong to open first for the purposes of the Polyflavanostilbene A that the present invention relates in preparation treatment anti-tubercle bacillus drugs.
Summary of the invention
The objective of the invention is to provides the application of Polyflavanostilbene A in the anti-anti-tubercle bacillus drugs of preparation according to not finding that it has the present situation of the report of anti-anti-tubercle bacillus activity in the existing Polyflavanostilbene A research.
Described Compound P olyflavanostilbene A structure is shown in formula I:
The inventor does the examination bacterial strain with bacillus calmette-guerin vaccine earlier, adopt disk diffusion method that the anti-tubercle bacillus activity of Polyflavanostilbene A is carried out preliminary test, result according to preliminary test, reuse solid medium dilution method of the present invention has been measured this chemical compound to bacillus calmette-guerin vaccine, the minimal inhibitory concentration of three kinds of tulases of the H37Rv strain of mycobacterium tuberculosis type strain and substance of medicines-resistant branched tubercle bacillus (MDR MTB), experimental result confirms that Polyflavanostilbene A has very strong anti-tubercle bacillus and anti-drug resistance tulase activity, can be used as the lead compound for the treatment of tubercle bacillus affection disease, also can be used for preparation treatment tuberculosis medicine.
Compared with prior art, the present invention has following beneficial effect:
1. the invention provides a kind of Polyflavanostilbene A that can be used for the sick treatment of tuberculosis, thereby enlarged the kind of anti-tubercle bacillus drugs;
2. at the appearance of present incidence of tuberculosis height, tubercule bacillus multiple antibiotic resistant strain and HIV (human immunodeficiency virus) double infection, make incidence of tuberculosis and mortality rate present situation in rising trend, the present invention finds that Polyflavanostilbene A has the characteristics of anti-tubercle bacillus and drug resistance tulase activity, can be used for the preparation of antituberculotics, have boundless application prospect;
3. the purposes of the Polyflavanostilbene A that the present invention relates in preparation treatment anti-tubercle bacillus drugs belongs to open first, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for tulase, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for tubercle bacillus affection simultaneously obviously has obvious improvement.
The specific embodiment
The preparation method of Compound P olyflavanostilbene A involved in the present invention is referring to document (Fushuang Li, et al., Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters, 2013,3 (15), 674 – 677.)
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 P olyflavanostilbene A tablet involved in the present invention:
Get 5 and digest compound Polyflavanostilbene A, add dextrin 195 grams, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of Compound P olyflavanostilbene A capsule involved in the present invention:
Get 5 and digest compound Polyflavanostilbene A, add starch 195 grams, mixing is encapsulatedly made 1000.Experimental example 1 solid medium dilution method is measured the anti-bacillus calmette-guerin vaccine of Polyflavanostilbene A (BCG) absolute concentration
Scrape from the inclined-plane and to get the bacillus calmette-guerin vaccine culture, join in the 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw the test tube lid, high vibration grinds on the vortex oscillation device, with standard Maxwell opacity tube (MacFarlandNo.1) than turbid, namely be made into bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1mg/ml.
Polyflavanostilbene A is made into the stock solution of high concentration with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Polyflavanostilbene A that dilution is good joins the 4mlMiddlebrook7H11 agar culture medium by required dosage, and (this culture medium is 121 ℃ of high pressure steam sterilizations 15 minutes, be cooled to 50～55 ℃), mixing, make and contain Polyflavanostilbene A, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, 0.75ug/ml, the isocyatic slant medium of 0.5ug/ml.
Bacillus calmette-guerin vaccine (BCG) bacteria suspension that with concentration is 1mg/ml dips in the peek ring with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Polyflavanostilbene A series concentration, place 37 ℃ to cultivate for 4～8 weeks, the observation experiment result, the result is as shown in table 1.
Culture medium commonly used when used Middlebrook7H9 broth bouillon and Middlebrook7H11 agar culture medium carry out the tulase cultivation for those skilled in the art in the present embodiment, its prescription adopts conventional formulation to get final product.
Experimental example 2 solid medium dilution methods are measured Polyflavanostilbene A Killing Mycobacterium Tuberculosis type strain H37Rv strain absolute concentration
Scrape from the inclined-plane and to get mycobacterium tuberculosis type strain H37Rv strain culture, join in the 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw the test tube lid, high vibration grinds on the vortex oscillation device, with standard Maxwell opacity tube (MacFarland No.1) than turbid, namely be made into the H37Rv strain bacteria suspension of 1mg/ml.
Polyflavanostilbene A is made into the stock solution of high concentration respectively with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Polyflavanostilbene A that dilution is good joins the 4mlMiddlebrook7H11 agar culture medium by required dosage, and (this culture medium is 121 ℃ of high pressure steam sterilizations 15 minutes, be cooled to 50～55 ℃), mixing, make and contain Polyflavanostilbene A, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, 0.75ug/ml, the isocyatic slant medium of 0.5ug/ml.
The H37Rv strain bacteria suspension that with concentration is 1mg/ml dips in the peek ring with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Polyflavanostilbene A series concentration, place 37 ℃ to cultivate for 4～8 weeks, the observation experiment result, the result is as shown in table 1.
Experimental example 3 solid medium dilution methods are measured the clinical separation of the Polyflavanostilbene A tuberculosis mycobacterium MTB of anti-ISRE strain absolute concentration
Scrape from the inclined-plane and to get the clinical separation of the mycobacterium tuberculosis MTB of anti-ISRE strain (anti-isoniazid, streptomycin, rifampicin, the clinical detached dowel of ethambutol mycobacterium tuberculosis) culture, join in the 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw the test tube lid, high vibration grinds on the vortex oscillation device, with standard Maxwell opacity tube (MacFarland No.1) than turbid, namely be made into the bacteria suspension of 1mg/ml.
Polyflavanostilbene A is made into the stock solution of high concentration respectively with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Polyflavanostilbene A that dilution is good joins the 4mlMiddlebrook7H11 agar culture medium by required dosage, and (this culture medium is 121 ℃ of high pressure steam sterilizations 15 minutes, be cooled to 50～55 ℃), mixing, make and contain Polyflavanostilbene A, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, 0.75ug/ml, the isocyatic slant medium of 0.5ug/ml.
The clinical separation of the mycobacterium tuberculosis MTB of the anti-ISRE strain bacteria suspension that with concentration is 1mg/ml dips in the peek ring with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Polyflavanostilbene A series concentration, place 37 ℃ to cultivate for 4～8 weeks, the observation experiment result, the result is as shown in table 1.
Table 1 solid medium dilution method is measured Polyflavanostilbene A anti-tubercle bacillus absolute concentration result
Conclusion: Polyflavanostilbene A has very strong anti-tubercle bacillus and anti-drug resistance tulase activity, can be used as the lead compound for the treatment of tubercle bacillus affection disease, also can be used for preparation treatment tuberculosis medicine.
Claims (1)
1.Polyflavanostilbene the application of A in the preparation anti-tubercle bacillus drugs, described Compound P olyflavanostilbene A structure is shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102539214A CN103285024A (en) | 2013-06-22 | 2013-06-22 | The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102539214A CN103285024A (en) | 2013-06-22 | 2013-06-22 | The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103285024A true CN103285024A (en) | 2013-09-11 |
Family
ID=49086914
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013102539214A Pending CN103285024A (en) | 2013-06-22 | 2013-06-22 | The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103285024A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103263428A (en) * | 2013-06-03 | 2013-08-28 | 南京正亮医药科技有限公司 | Application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments |
-
2013
- 2013-06-22 CN CN2013102539214A patent/CN103285024A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103263428A (en) * | 2013-06-03 | 2013-08-28 | 南京正亮医药科技有限公司 | Application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103263428A (en) | Application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments | |
| CN105250270A (en) | Application of Cyanogramide to preparation of medicine for resisting mycobacterium tuberculosis | |
| CN103285010A (en) | Application of compound in preparation of medicaments for resisting tubercle bacillus | |
| CN103285024A (en) | The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine | |
| CN103356629A (en) | Application of Myriberine A in preparing antituberculous medicines | |
| CN102872049B (en) | Application of gypensapogenin A in anti-tubercle bacillus drugs | |
| CN102872087B (en) | Application of Houttuynoid A in medicines for inhibiting tubercle bacillus | |
| CN102872091B (en) | Application of Houttuynoid E in anti-tubercle bacillus medicine | |
| CN102872152B (en) | Application of Houttuynoid D in tubercle bacillus resistant medicament | |
| CN103462976B (en) | Incarviatone A is preparing the application in anti-tubercle bacillus drugs | |
| CN103446129B (en) | Lycojaponicumin A is preparing the application in anti-tubercle bacillus drugs | |
| CN103006639A (en) | Application of aphanamixoid A in preparing antituberculosis medicament | |
| CN103479631B (en) | Lycojaponicumin B is preparing the application in anti-tubercle bacillus drugs | |
| CN103446145B (en) | Lycojaponicumin C is preparing the application in anti-tubercle bacillus drugs | |
| CN102872104B (en) | The application of Houttuynoid C in anti-tubercle bacillus drugs | |
| CN103381156B (en) | Chukrasone B is preparing the application in anti-tubercle bacillus drugs | |
| CN103446109A (en) | Applications of Sarcaboside B in medicament against mycobacterium tuberculosis | |
| CN103446107A (en) | Applications of Sarcaboside A in medicament against mycobacterium tuberculosis | |
| CN103381169A (en) | Applications of Chukrasone A in anti-tubercle bacillus medicines | |
| CN105287501A (en) | Application of Foveospirolide in preparation of tubercle bacillus treating and resisting medicine | |
| CN102872055B (en) | Application of gypensapogenin B in anti-tubercle bacillus drugs | |
| CN103463012B (en) | Application of fluevirosines A in preparation of medicine inhibiting tubercle bacillus | |
| CN102885845A (en) | Application of Houttuynoid B in medicament for resisting tubercle bacillus | |
| CN105496998A (en) | Application of Perovskone B to preparation of drug for treating tongue cancer | |
| CN103432139A (en) | Application of compound in preparation of antituberculosis medicament |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20130911 |