CN103446109A - Applications of Sarcaboside B in medicament against mycobacterium tuberculosis - Google Patents
Applications of Sarcaboside B in medicament against mycobacterium tuberculosis Download PDFInfo
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- CN103446109A CN103446109A CN 201310428810 CN201310428810A CN103446109A CN 103446109 A CN103446109 A CN 103446109A CN 201310428810 CN201310428810 CN 201310428810 CN 201310428810 A CN201310428810 A CN 201310428810A CN 103446109 A CN103446109 A CN 103446109A
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Abstract
The invention discloses applications of Sarcaboside B in preparing a medicament against mycobacterium tuberculosis. Aiming at the current situation that the occurrence of high tuberculosis incidence and multi-medicament-resistant strains of mycobacterium tuberculosis causes the rise trend of tuberculosis incidence and death rate, people discover that the Sarcaboside B has the remarkable mycobacterium tuberculosis inhibition activity and excellent application prospects. The applications of the Sarcaboside B in preparing the medicament against mycobacterium tuberculosis are disclosed for the first time. As a skeleton type of the Sarcaboside B belongs to a brand-new skeleton type, the Sarcaboside B has unexpectedly strong mycobacterium tuberculosis inhibition activity, and the possibility of giving any inspiration by other compounds does not exist. The Sarcaboside B has significantly substantive characteristics, as well as obviously prominent progress in the prevention and treatment of the mycobacterium tuberculosis infection.
Description
Technical field
The present invention relates to the medical compounds application, be specifically related to the application of Sarcaboside B in preparing anti-tubercle bacillus drugs.
Background technology
Global morbidity lungy in recent years is increases trend, according to the World Health Organization (WHO), estimate, the whole world is subject to mycobacterium tuberculosis (Mycobacterium tuberculosis at present, MTB) population infected 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, be one of the high burden of global tuberculosis country.
Come out one after another from antituberculotics, make treatment lungy play epoch-making variation.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.
Summary of the invention
The compound S arcaboside B the present invention relates to is one and within 2012, delivers (Li, X.et al., 2012.Two New-Skeleton Compounds from Sarcandra glabra.Helvetica Chimica Acta95 (6), 998-1002.) New skeleton compound, this compound has brand-new framework types, at present not about active report, purposes for the Sarcaboside 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, possesses outstanding substantive distinguishing features, control for tubercle bacillus affection simultaneously obviously has significant progress.
Summary of the invention
The object of the invention is to, according in existing Sarcaboside B research, not finding that it has the present situation of the report of tuberculosis activity, provides the application of Sarcaboside B in preparing anti-tubercle bacillus drugs.
Described compound S arcaboside B structure is as shown in formula I:
Formula I
The object of the invention is achieved by the following technical programs:
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 Sarcaboside 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 Sarcaboside 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.
Compared with prior art, the present invention has following beneficial effect:
1. the invention provides a kind of Sarcaboside B that can be used for the sick treatment of tuberculosis, thereby enlarged 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 Sarcaboside B has the characteristics of anti-tubercle bacillus and drug resistance tulase activity, can be used for the preparation of antituberculotics, there is boundless application prospect;
3. the purposes of the Sarcaboside 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 arcaboside B involved in the present invention is referring to document (Li, X.et al., 2012.Two New-Skeleton Compounds from Sarcandra glabra.Helvetica Chimica Acta95 (6), 998-1002.).
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 arcaboside B tablet involved in the present invention:
Get 20 and digest compound Sarcaboside B, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound S arcaboside B capsule involved in the present invention:
Get 20 and digest compound Sarcaboside B, add the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The experimental example 1 anti-bacillus calmette-guerin vaccine of solid medium By Dilution Sarcaboside 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 (MacFarland No.1).
Sarcaboside 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 Sarcaboside B that diluted is joined to 4ml Middlebrook7H11 agar culture medium (this culture medium 121 ℃ of high pressure steam sterilizations 15 minutes, be cooled to 50～55 ℃) by required dosage, mix, make containing Sarcaboside 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, the isocyatic slant medium of 0.5ug/ml.
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 Sarcaboside 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 Sarcaboside 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).
Sarcaboside 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 Sarcaboside 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 Sarcaboside 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 Sarcaboside B 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 Sarcaboside 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 (MacFarland No.1).
Sarcaboside 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 Sarcaboside B that diluted is joined to 4ml Middlebrook7H11 agar culture medium (this culture medium 121 ℃ of high pressure steam sterilizations 15 minutes, be cooled to 50～55 ℃) by required dosage, mix, make containing Sarcaboside 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, the isocyatic slant medium of 0.5ug/ml.
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 Sarcaboside 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 Sarcaboside B anti-tubercle bacillus absolute concentration result
Conclusion: Sarcaboside 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.Sarcaboside the application of B in anti-tubercle bacillus drugs, described compound S arcaboside B structure as
formula Ishown in:
formula I.
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| CN 201310428810 CN103446109A (en) | 2013-09-18 | 2013-09-18 | Applications of Sarcaboside B in medicament against mycobacterium tuberculosis |
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Application publication date: 20131218 |