CN103462980A - Application of spirooliganones B in preparation of medicine inhibiting tubercle bacillus - Google Patents
Application of spirooliganones B in preparation of medicine inhibiting tubercle bacillus Download PDFInfo
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- CN103462980A CN103462980A CN2013104646047A CN201310464604A CN103462980A CN 103462980 A CN103462980 A CN 103462980A CN 2013104646047 A CN2013104646047 A CN 2013104646047A CN 201310464604 A CN201310464604 A CN 201310464604A CN 103462980 A CN103462980 A CN 103462980A
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- tubercle bacillus
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Abstract
The invention discloses the application of spirooliganones B in preparation of the medicine inhibiting the tubercle bacillus. The spirooliganones B has remarkable activity in inhibiting the tubercle bacillus and good application prospects, and belongs to a brand new matrix type. The spirooliganones B has the advantages of being high in inhibitory activity for the tubercle bacillus and prominent in substantive features, and makes remarkable progress in prevention and treatment of infection of the tubercle bacillus.
Description
Technical field
The present invention relates to the new purposes of compound S pirooliganones B, relate in particular to the application of Spirooliganones B in preparation treatment anti-tubercle bacillus drugs.
Background technology
Global morbidity lungy in recent years is increases trend, yet due to the treatment of tuberculosis patient management standard very not still, irregular chemotherapy, the abuse antituberculotics, make the drug resistance of tuberculosis situation day by day serious, and the variation of drug resistance more trends towards multi-medicament drug resistance simultaneously, and this causes very big difficulty to preventing and controlling lungy.Therefore find new antituberculotics, the antituberculotics of especially anti-multidrug resistance is to the protection people's health, significant.
The compound S pirooliganones B the present invention relates to is one and within 2013, delivers (Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013, 15(17): noval chemical compound 4450 – 4453.), this compound has brand-new framework types, current purposes finds that it can suppress Coxsackie B virus 3 and influenza A virus H3N2(Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013, 15(17): 4450 – 4453.), the purposes of the Spirooliganones B the present invention relates in preparation treatment anti-tubercle bacillus drugs belongs to open first.
Summary of the invention
The object of the invention is to, according in existing Spirooliganones B research, not finding that it has the present situation of the report of anti-anti-tubercle bacillus activity, provides the application of Spirooliganones B in the anti-anti-tubercle bacillus drugs of preparation.
Described compound S pirooliganones B structure is as shown in formula I:
The inventor first does the examination bacterial strain with bacillus calmette-guerin vaccine, adopt disk diffusion method to carry out preliminary test to the anti-tubercle bacillus activity of Spirooliganones B, result according to preliminary test, the present invention use again the solid medium By Dilution this 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 Spirooliganones B 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.The purposes of the Spirooliganones B 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 do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for tubercle bacillus affection simultaneously obviously has significant progress.
The specific embodiment
The preparation method of compound S pirooliganones B involved in the present invention is referring to document (Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013,15(17): 4450 – 4453.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound S pirooliganones B tablet involved in the present invention:
Get 5 and digest compound Spirooliganones B, add dextrin 195 grams, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound S pirooliganones B capsule involved in the present invention:
Get 5 and digest compound Spirooliganones B, add starch 180 grams, mix, encapsulatedly make 1000.
Experimental example 1: the anti-bacillus calmette-guerin vaccine of solid medium By Dilution Spirooliganones B (BCG) absolute concentration
Scraping bacillus calmette-guerin vaccine culture from inclined-plane, join in 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw test tube cap, on the vortex oscillation device, high vibration grinds, than turbid, be made into bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1mg/ml with standard Maxwell opacity tube (MacFarlandNo.1).
Spirooliganones B is made into to the stock solution of high concentration with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 containing 5%, the Spirooliganones B that diluted is joined to 4ml Middlebrook7H11 agar culture medium by required dosage, and (this culture medium is 121 ℃ of high pressure steam sterilizations 15 minutes, be cooled to 50 ~ 55 ℃), mix, make containing Spirooliganones B, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, 0.75ug/ml, 0.5ug/ml isocyatic slant medium.
The bacillus calmette-guerin vaccine that is 1mg/ml by concentration (BCG) bacteria suspension dips ring of numbers with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant containing Spirooliganones B series concentration, be placed in 37 ℃ and cultivate 4 ~ 8 weeks, the observation experiment result, result is as shown in table 1.
Culture medium commonly used when in the present embodiment, Middlebrook7H9 broth bouillon used and Middlebrook7H11 agar culture medium carry out the tulase cultivation for those skilled in the art, its formula adopts conventional formulation to get final product.
Experimental example 2 solid medium By Dilution Spirooliganones B Killing Mycobacterium Tuberculosis type strain H37Rv strain absolute concentrations
Scraping mycobacterium tuberculosis type strain H37Rv strain culture from inclined-plane, join in 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw test tube cap, on the vortex oscillation device, high vibration grinds, than turbid, be made into the H37Rv strain bacteria suspension of 1mg/ml with standard Maxwell opacity tube (MacFarland No.1).
Spirooliganones B is made into respectively to the stock solution of high concentration with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 containing 5%, the Spirooliganones B that diluted is joined to 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 ℃), mix, make containing Spirooliganones B, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, 0.75ug/ml, 0.5ug/ml isocyatic slant medium.
The H37Rv strain bacteria suspension that is 1mg/ml by concentration dips ring of numbers with inoculating loop, is inoculated in respectively on the culture medium and blank medium slant containing the SpirooliganonesB series concentration, and be placed in 37 ℃ and cultivate 4 ~ 8 weeks, the observation experiment result, result is as shown in table 1.
The anti-ISREMTB strain of the experimental example 3 solid medium By Dilution Spirooliganones B clinical separation of tuberculosis mycobacterium absolute concentration
The clinical separation of the scraping mycobacterium tuberculosis MTB of anti-ISRE strain (anti-isoniazid, streptomycin, rifampicin, the clinical detached dowel of ethambutol mycobacterium tuberculosis) culture from inclined-plane, join in 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw test tube cap, on the vortex oscillation device, high vibration grinds, than turbid, be made into the bacteria suspension of 1mg/ml with standard Maxwell opacity tube (MacFarlandNo.1).
Spirooliganones B is made into respectively to the stock solution of high concentration with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 containing 5%, the Spirooliganones B that diluted is joined to 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 ℃), mix, make containing Spirooliganones B, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, 0.75ug/ml, 0.5ug/ml isocyatic slant medium.
The clinical separation of the mycobacterium tuberculosis MTB of the anti-ISRE strain bacteria suspension that is 1mg/ml by concentration dips ring of numbers with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant containing Spirooliganones B series concentration, being placed in 37 ℃ cultivates 4 ~ 8 weeks, the observation experiment result, result is as shown in table 1.
Table 1 solid medium By Dilution Spirooliganones B anti-tubercle bacillus absolute concentration result
Conclusion: Spirooliganones B 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.Spirooliganones the application of B in preparing anti-tubercle bacillus drugs, described compound S pirooliganones B structure is as shown in formula I:
Formula I.
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| CN2013104646047A CN103462980A (en) | 2013-10-08 | 2013-10-08 | Application of spirooliganones B in preparation of medicine inhibiting tubercle bacillus |
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| CN2013104646047A CN103462980A (en) | 2013-10-08 | 2013-10-08 | Application of spirooliganones B in preparation of medicine inhibiting tubercle bacillus |
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2013
- 2013-10-08 CN CN2013104646047A patent/CN103462980A/en active Pending
Non-Patent Citations (4)
| Title |
|---|
| ROELOF A. DE PAUS等: "The influence of influenza virus infections on the development of tuberculosis", 《TUBERCULOSIS》 * |
| SHUANG-GANG MA,ET AL.: "Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum", 《ORGANIC LETTERS》 * |
| SVEN LOFGR;EN AND ALICE CALLANS.: "Asian Influenza and Pulnionarg Tuberculosis", 《ACTA MEDICA SCANDINAVICA》 * |
| 唐文照: "少药八角果实及茎皮化学成分和药理活性研究", 《中国博士学位论文全文数据库，医药卫生科技辑（月刊 ）》 * |
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Application publication date: 20131225 |