CN102872104B - The application of Houttuynoid C in anti-tubercle bacillus drugs - Google Patents
The application of Houttuynoid C in anti-tubercle bacillus drugs Download PDFInfo
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- CN102872104B CN102872104B CN201210419108.5A CN201210419108A CN102872104B CN 102872104 B CN102872104 B CN 102872104B CN 201210419108 A CN201210419108 A CN 201210419108A CN 102872104 B CN102872104 B CN 102872104B
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- houttuynoid
- tubercle bacillus
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Abstract
The invention discloses Houttuynoid C and prepare the application in anti-tubercle bacillus drugs.The present invention is directed to that current incidence of tuberculosis is high, the appearance of tubercule bacillus multiple antibiotic resistant strain, make incidence of tuberculosis and mortality rate present situation in rising trend, find that Houttuynoid C has the activity significantly suppressing tulase, there is good application prospect.The purposes of the Houttuynoid C 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.
Description
Technical field
The present invention relates to medical compounds application, be specifically related to Houttuynoid C and preparing the application in anti-tubercle bacillus drugs.
Background technology
Global morbidity lungy is in increasing trend in recent years, estimate according to the World Health Organization (WHO), the current whole world is by mycobacterium tuberculosis (Mycobacterium tuberculosis, 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.
Summary of the invention
The compound H outtuynoid C that the present invention relates to is one and delivers (Chen in 2012, S.D.et al., 2012.Houttuynoid C_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletonsfrom Houttuynia cordata.Organic Letters14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to anti-herpes simplex virus activity (Chen, S.D.etal., 2012.Houttuynoid C_E, Anti-Herpes Simplex Virus Active Flavonoids with NovelSkeletons from Houttuynia cordata.Organic Letters14 (7), 1772 – 1775.), the purposes of the Houttuynoid C that the present invention relates in preparation treatment anti-tubercle bacillus drugs is belonged 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, possesses outstanding substantive distinguishing features, control simultaneously for tubercle bacillus affection obviously has significant progress.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of anti-tubercular according in existing Houttuynoid C research, provide Houttuynoid C and preparing the application in anti-tubercle bacillus drugs.
Described compound H outtuynoid C-structure is as shown in formula I:
The object of the invention is achieved by the following technical programs:
Inventor first does examination bacterial strain with bacillus calmette-guerin vaccine, the anti-tubercle bacillus activity of disk diffusion method to Houttuynoid C 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 Houttuynoid C 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 Houttuynoid C 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 Houttuynoid C 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 Houttuynoid C 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 H outtuynoid C involved in the present invention is see document (Chen, S.D.et al., 2012.Houttuynoid C_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons fromHouttuynia cordata.Organic Letters14 (7), 1772 – 1775.).
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 H outtuynoid C tablet involved in the present invention:
Get 20 g of compound Houttuynoid C, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound H outtuynoid C capsule involved in the present invention:
Get 20 g of compound Houttuynoid C, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1 solid medium By Dilution Houttuynoid C 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 (MacFarland No.1) than turbid, be namely made into bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1mg/ml.
Houttuynoid C 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 Houttuynoid C diluted is joined 4ml Middlebrook7H11 agar culture medium (this culture medium 121 DEG C of high pressure steam sterilizations 15 minutes, be cooled to 50 ~ 55 DEG C) by required dosage, mixing, make containing HouttuynoidC, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, the isocyatic slant medium of 0.75ug/ml, 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 HouttuynoidC 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 Houttuynoid C 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.
Houttuynoid C 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 Houttuynoid C diluted is joined 4ml Middlebrook7H11 agar culture medium (this culture medium 121 DEG C of high pressure steam sterilizations 15 minutes, be cooled to 50 ~ 55 DEG C) by required dosage, mixing, make containing Houttuynoid C, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, the isocyatic slant medium of 0.75ug/ml, 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 Houttuynoid C 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 Houttuynoid clinical separation of C Ad tuberculosis resistance to ISREMTB 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 (MacFarland No.1) than turbid, be namely made into the bacteria suspension of 1mg/ml.
Houttuynoid C 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 Houttuynoid C diluted is joined 4ml Middlebrook7H11 agar culture medium (this culture medium 121 DEG C of high pressure steam sterilizations 15 minutes, be cooled to 50 ~ 55 DEG C) by required dosage, mixing, make containing Houttuynoid C, concentration is respectively 6.0ug/ml, 4.0ug/ml, 3.0ug/ml, 2.0ug/ml, 1.5ug/ml, 1.0ug/ml, the isocyatic slant medium of 0.75ug/ml, 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 Houttuynoid C 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 Houttuynoid C anti-tubercle bacillus absolute concentration result
Conclusion: Houttuynoid C 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.Houttuynoid C is preparing the application in anti-tubercle bacillus drugs, described compound H outtuynoid C-structure as
formula Ishown in:
formula I.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210419108.5A CN102872104B (en) | 2012-10-27 | 2012-10-27 | The application of Houttuynoid C in anti-tubercle bacillus drugs |
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| CN201210419108.5A CN102872104B (en) | 2012-10-27 | 2012-10-27 | The application of Houttuynoid C in anti-tubercle bacillus drugs |
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| CN102872104A CN102872104A (en) | 2013-01-16 |
| CN102872104B true CN102872104B (en) | 2015-08-19 |
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- 2012-10-27 CN CN201210419108.5A patent/CN102872104B/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| Chen,S.D. et al.Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.《Organic Letters》.2012,第14卷(第7期),第1772-1775页. * |
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