CN103463012B - 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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- CN103463012B CN103463012B CN201310470946.XA CN201310470946A CN103463012B CN 103463012 B CN103463012 B CN 103463012B CN 201310470946 A CN201310470946 A CN 201310470946A CN 103463012 B CN103463012 B CN 103463012B
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- tubercle bacillus
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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 novelty teabag of compound F 17-hydroxy-corticosterone luevirosines A, particularly relate to the application of Fluevirosines A in preparation treatment anti-tubercle bacillus drugs.
Background technology
Global morbidity lungy is in increasing trend in recent years, but due to the Case management still not very specification of tuberculosis patient, irregular chemotherapy, abuse antituberculotics, make drug resistance of tuberculosis situation day by day serious, and the change of drug resistance more trends towards multi-medicament drug resistance simultaneously, this causes extreme difficulties to preventing and controlling lungy.Therefore find new antituberculotics, the antituberculotics of especially anti-multidrug resistance is to protection people's health, significant.
The compound F 17-hydroxy-corticosterone luevirosines A that the present invention relates to is one and delivers (Hua Zhang in 2012, et al., Fluevirosines A-C:A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa.Organic Letters, 2013, noval chemical compound 15(1): 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 that the present invention relates in preparation treatment anti-tubercle bacillus drugs belongs to first public.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of anti-anti-tubercle bacillus activity according in existing Fluevirosines A research, provide 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
Inventor first does examination bacterial strain with bacillus calmette-guerin vaccine, the anti-tubercle bacillus activity of disk diffusion method to Fluevirosines A is adopted to carry out preliminary test, according to the result of preliminary test, the present invention uses this compound of solid medium By Dilution to bacillus calmette-guerin vaccine again, the minimal inhibitory concentration of the H37Rv strain of mycobacterium tuberculosis type strain and substance of medicines-resistant branched tubercle bacillus (MDR MTB) three kinds of tulases, experimental result confirms that Fluevirosines A has very strong anti-tubercle bacillus and anti-drug resistance tulase is active, can be used as the lead compound for the treatment of tubercle bacillus affection disease, also can be used for preparation treatment tubercular drugs.The purposes of the Fluevirosines A that the present invention relates in preparation treatment anti-tubercle bacillus drugs belongs to first public, because framework types belongs to brand-new framework types, and it is strong for tulase inhibit activities, possess outstanding substantive distinguishing features, the control simultaneously for tubercle bacillus affection obviously has significant progress.
Detailed description of the invention
The preparation method of compound F 17-hydroxy-corticosterone luevirosines A involved in the present invention is see 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 by 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 g of compound Fluevirosines A, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound F 17-hydroxy-corticosterone luevirosines A capsule involved in the present invention:
Get 5 g of compound Fluevirosines A, add starch 180 grams, mixing, encapsulatedly makes 1000.
Experimental example 1: solid medium By Dilution Fluevirosines A anti-bacillus calmette-guerin vaccine (BCG) absolute concentration
Scraping BCG cultures from inclined-plane, join in 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw test tube cap, high vibration grinding in vortex oscillator, with standard Maxwell opacity tube (MacFarlandNo.1) than turbid, be namely made into bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1mg/ml.
Fluevirosines A DMSO is made into the stock solution of high concentration, by the tween 80 aseptic ultra-pure water dilution stock solution containing 5% to desired concn, the Fluevirosines A diluted is joined 4ml Middlebrook7H11 agar culture medium (this culture medium 121 DEG C of high pressure steam sterilizations 15 minutes by required dosage, be cooled to 50 ~ 55 DEG C), mixing, 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, the isocyatic slant medium of 0.5ug/ml.
Be that bacillus calmette-guerin vaccine (BCG) the bacteria suspension inoculating loop of 1mg/ml dips ring of numbers by concentration, be inoculated in containing in the culture medium of Fluevirosines A series concentration and blank medium slant respectively, be placed in 37 DEG C to cultivate 4 ~ 8 weeks, observation experiment result, result is as shown in table 1.
In the present embodiment, Middlebrook7H9 broth bouillon used and Middlebrook7H11 agar culture medium are the conventional culture medium that those skilled in the art carry out when tulase is cultivated, and its formula adopts conventional formulation.
Experimental example 2 solid medium By Dilution Fluevirosines A Killing Mycobacterium Tuberculosis type strain H37Rv strain absolute concentration
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, high vibration grinding in vortex oscillator, with standard Maxwell opacity tube (MacFarland No.1) than turbid, be namely made into the H37Rv strain bacteria suspension of 1mg/ml.
Fluevirosines A is made into respectively the stock solution of high concentration with DMSO, by the tween 80 aseptic ultra-pure water dilution stock solution containing 5% to desired concn, the Fluevirosines A diluted is joined 4ml Middlebrook7H11 agar culture medium (this culture medium 121 DEG C of high pressure steam sterilizations 15 minutes by required dosage, be cooled to 50 ~ 55 DEG C), mixing, 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, the isocyatic slant medium of 0.5ug/ml.
Be that the H37Rv strain bacteria suspension inoculating loop of 1mg/ml dips ring of numbers by concentration, be inoculated in respectively containing in the culture medium of Fluevirosines A series concentration and blank medium slant, be placed in 37 DEG C and cultivate 4 ~ 8 weeks, observation experiment result, result is as shown in table 1.
The clinical separation of the experimental example 3 solid medium By Dilution Fluevirosines A Ad tuberculosis MTB of resistance to ISRE strain absolute concentration
The clinical separation of the scraping mycobacterium tuberculosis MTB of resistance to ISRE strain (resistance to 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, high vibration grinding in vortex oscillator, with standard Maxwell opacity tube (MacFarlandNo.1) than turbid, be namely made into the bacteria suspension of 1mg/ml.
Fluevirosines A is made into respectively the stock solution of high concentration with DMSO, by the tween 80 aseptic ultra-pure water dilution stock solution containing 5% to desired concn, the Fluevirosines A diluted is joined 4ml Middlebrook7H11 agar culture medium (this culture medium 121 DEG C of high pressure steam sterilizations 15 minutes by required dosage, be cooled to 50 ~ 55 DEG C), mixing, 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, the isocyatic slant medium of 0.5ug/ml.
Be that the clinical separation of the mycobacterium tuberculosis MTB of the resistance to ISRE strain bacteria suspension inoculating loop of 1mg/ml dips ring of numbers by concentration, be inoculated in containing in the culture medium of Fluevirosines A series concentration and blank medium slant respectively, be placed in 37 DEG C to cultivate 4 ~ 8 weeks, 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 is active, can be used as the lead compound for the treatment of tubercle bacillus affection disease, also can be used for preparation treatment tubercular drugs.
Claims (1)
1.Fluevirosines A is preparing the application in anti-tubercle bacillus drugs, and 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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| 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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| CN103463012A CN103463012A (en) | 2013-12-25 |
| CN103463012B true CN103463012B (en) | 2015-05-20 |
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Non-Patent Citations (2)
| Title |
|---|
| Fluevirosines A_C: A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa;Hua Zhang et al;《ORGANIC LETTER》;20121217;第15卷(第1期);120-123 * |
| 生物碱类化合物抗菌活性研究进展;李杨等;《中草药》;20100630;第41卷(第6期);1006-1014 * |
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