CN103463012A - Application of fluevirosines A in preparation of medicine inhibiting tubercle bacillus - Google Patents
Application of fluevirosines A in preparation of medicine inhibiting tubercle bacillus Download PDFInfo
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- CN103463012A CN103463012A CN201310470946XA CN201310470946A CN103463012A CN 103463012 A CN103463012 A CN 103463012A CN 201310470946X A CN201310470946X A CN 201310470946XA CN 201310470946 A CN201310470946 A CN 201310470946A CN 103463012 A CN103463012 A CN 103463012A
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Abstract
The invention discloses the application of fluevirosines A in preparation of the medicine inhibiting the tubercle bacillus. The fluevirosines A has remarkable activity for inhibiting the tubercle bacillus and good application prospect. The fluevirosines A belongs to a brand new matrix type, has the advantages of being high in inhibitory activity to 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 F 17-hydroxy-corticosterone luevirosines A, relate in particular to the application of Fluevirosines A 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 F 17-hydroxy-corticosterone luevirosines A the present invention relates to is one and within 2012, delivers (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): noval chemical compound 120 – 123.), this compound has brand-new framework types, current 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 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 Fluevirosines A research, not finding that it has the present situation of the report of anti-anti-tubercle bacillus activity, provides the application of Fluevirosines A in the anti-anti-tubercle bacillus drugs of preparation.
Described compound F 17-hydroxy-corticosterone luevirosines A structure is as shown in formula I:
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 Fluevirosines A, 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 Fluevirosines 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.The purposes of the Fluevirosines A 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 strong for tulase, possess outstanding substantive distinguishing features, the control for tubercle bacillus affection simultaneously 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 subject to any restriction of specific embodiment, but be 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, mix, conventional tabletting is 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 180 grams, mix, encapsulatedly make 1000.
Experimental example 1: the anti-bacillus calmette-guerin vaccine of solid medium By Dilution Fluevirosines A (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).
Fluevirosines A 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 Fluevirosines A 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 Fluevirosines 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, 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 Fluevirosines A 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 Fluevirosines A 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).
Fluevirosines A 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 Fluevirosines A 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 Fluevirosines 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, 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 Fluevirosines A series concentration, and be placed in 37 ℃ and cultivate 4～8 weeks, the observation experiment result, result is as shown in table 1.
The clinical separation of the experimental example 3 solid medium By Dilution Fluevirosines A tuberculosis mycobacterium MTB of anti-ISRE strain 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).
Fluevirosines A 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 Fluevirosines A 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 Fluevirosines 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, 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 Fluevirosines A 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 Fluevirosines A anti-tubercle bacillus absolute concentration result
Conclusion: Fluevirosines 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.Fluevirosines the application of A in preparing anti-tubercle bacillus drugs, described compound F 17-hydroxy-corticosterone luevirosines A structure is as shown in formula I:
Formula I.
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| CN201310470946.XA CN103463012B (en) | 2013-10-11 | 2013-10-11 | Application of fluevirosines A in preparation of medicine inhibiting tubercle bacillus |
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| CN103463012B CN103463012B (en) | 2015-05-20 |
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Non-Patent Citations (2)
| Title |
|---|
| HUA ZHANG ET AL: "Fluevirosines A_C: A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa", 《ORGANIC LETTER》 * |
| 李杨等: "生物碱类化合物抗菌活性研究进展", 《中草药》 * |
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