CN105287501A - Application of Foveospirolide in preparation of tubercle bacillus treating and resisting medicine - Google Patents
Application of Foveospirolide in preparation of tubercle bacillus treating and resisting medicine Download PDFInfo
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- CN105287501A CN105287501A CN201510752639.XA CN201510752639A CN105287501A CN 105287501 A CN105287501 A CN 105287501A CN 201510752639 A CN201510752639 A CN 201510752639A CN 105287501 A CN105287501 A CN 105287501A
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Abstract
The invention discloses application of Foveospirolide in preparation of tubercle bacillus treating and resisting medicine. For the situation that current tuberculosis morbidity is high, mycobacterium tuberculosis multiple-resistant strains appear and tuberculosis morbidity and the death rate are increased, it is found that Foveospirolide has remarkable activity for restraining tubercle bacillus and has quite good application prospects. The application of Foveospirolide in preparation of tubercle bacillus treating and resisting medicine is disclosed for the first time; due to the fact that the framework type belongs to a brand-new framework type, Foveospirolide is unexpectedly high in tubercle bacillus restraining activity, no other compounds give any prompts, remarkable substantive features are achieved, and meanwhile Foveospirolide obviously has a remarkable progress for preventing and treating tuberculous infection.
Description
Technical field
The present invention relates to the novelty teabag of compound F 17-hydroxy-corticosterone oveospirolide, particularly relate to the application of Foveospirolide in preparation treatment anti-tubercle bacillus drugs.
Background technology
Global morbidity lungy is in increasing trend in recent years, estimate according to World Health Organization (WHO) (WHO), the current whole world is by mycobacterium tuberculosis (Mycobacteriumtuberculosis, MTB) population infected accounts for 1/3rd of world population, and wherein the infected of 5 ~ 10% becomes tuberculosis patient.There is active tuberculosis patient 1,300,000 example in China, wherein infectiousness pulmonary tuberculosis about 600,000 example every year, wherein infectiousness pulmonary tuberculosis about 600,000 example, is one of global tuberculosis high burden country.
Come out one after another from antituberculotics, make treatment lungy play epoch-making change.But due to the Case management still not very specification of tuberculosis patient, irregular chemotherapy, abuse antituberculotics, makes 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 oveospirolide that the present invention relates to is one and delivers (PathomSomwong in 2013, etal., NewsesquiterpenesandphenoliccompoundfromFicusfoveolata.F itoterapia, 85 (2013) 1 – 7.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to function of tumor inhibition (PathomSomwong, etal., NewsesquiterpenesandphenoliccompoundfromFicusfoveolata.F itoterapia, 85 (2013) 1 – 7.), the purposes of the Foveospirolide that the present invention relates in preparation treatment anti-tubercle bacillus drugs is belonged to first public, owing to belonging to brand-new structure type, and its activity for anti-tubercle bacillus is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, for anti-tubercle bacillus, obviously there is significant progress simultaneously.
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 Foveospirolide research, provide the application of Foveospirolide in the anti-anti-tubercle bacillus drugs of preparation.
Described compound F 17-hydroxy-corticosterone oveospirolide structure is as shown in formula I:
Inventor first does examination bacterial strain with bacillus calmette-guerin vaccine, the anti-tubercle bacillus activity of disk diffusion method to Foveospirolide 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 (MDRMTB) three kinds of tulases, experimental result confirms that Foveospirolide 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.
Compared with prior art, the present invention has following beneficial effect:
1. the invention provides a kind of Foveospirolide that can be used for antituberculosis treatment, thus expand the kind of anti-tubercle bacillus drugs;
2. the appearance of, tubercule bacillus multiple antibiotic resistant strain high for current incidence of tuberculosis and HIV (human immunodeficiency virus) double infection, make incidence of tuberculosis and mortality rate present situation in rising trend, the present invention finds that Foveospirolide has the feature of anti-tubercle bacillus and drug resistant M bacterium activity, can be used for the preparation of antituberculotics, there is boundless application prospect;
3. the purposes of the Foveospirolide 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 unexpectedly strong for tulase inhibit activities, there is not the possibility being provided any enlightenment by other compounds, 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 oveospirolide involved in the present invention is see document (PathomSomwong, etal., NewsesquiterpenesandphenoliccompoundfromFicusfoveolata.F itoterapia, 85 (2013) 1 – 7.)
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 oveospirolide tablet involved in the present invention:
Get 20 g of compound Foveospirolide, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound F 17-hydroxy-corticosterone oveospirolide capsule involved in the present invention:
Get 20 g of compound Foveospirolide, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Experimental example 1 solid medium By Dilution Foveospirolide anti-bacillus calmette-guerin vaccine (BCG) absolute concentration
Scraping BCG cultures from inclined-plane, join in 3mlMiddlebrook7H9 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.
Foveospirolide 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 Foveospirolide diluted is joined 4mlMiddlebrook7H11 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 Foveospirolide, 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 Foveospirolide 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 Foveospirolide Killing Mycobacterium Tuberculosis type strain H37Rv strain absolute concentration
Scraping mycobacterium tuberculosis type strain H37Rv strain culture from inclined-plane, join in 3mlMiddlebrook7H9 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 H37Rv strain bacteria suspension of 1mg/ml.
Foveospirolide 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 Foveospirolide diluted is joined 4mlMiddlebrook7H11 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 Foveospirolide, 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 Foveospirolide 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 experimental example 3 solid medium By Dilution clinical separation of Foveospirolide Ad tuberculosis resistance to ISREMTB strain absolute concentration
The clinical separation of scraping mycobacterium tuberculosis resistance to ISREMTB strain (resistance to isoniazid, streptomycin, rifampicin, the clinical detached dowel of ethambutol mycobacterium tuberculosis) culture from inclined-plane, join in 3mlMiddlebrook7H9 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.
Foveospirolide 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 Foveospirolide diluted is joined 4mlMiddlebrook7H11 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 Foveospirolide, 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 resistance to ISREMTB strain bacteria suspension inoculating loop of 1mg/ml dips ring of numbers by concentration, be inoculated in containing in the culture medium of Foveospirolide 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 Foveospirolide anti-tubercle bacillus absolute concentration result
Conclusion: Foveospirolide 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)
- The application of 1.Foveospirolide in anti-tubercle bacillus drugs, described compound F 17-hydroxy-corticosterone oveospirolide structure is as shown in formula I:
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510752639.XA CN105287501A (en) | 2015-11-08 | 2015-11-08 | Application of Foveospirolide in preparation of tubercle bacillus treating and resisting medicine |
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| CN201510752639.XA CN105287501A (en) | 2015-11-08 | 2015-11-08 | Application of Foveospirolide in preparation of tubercle bacillus treating and resisting medicine |
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| CN105287501A true CN105287501A (en) | 2016-02-03 |
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Application publication date: 20160203 |