CN102872091B - Application of Houttuynoid E in anti-tubercle bacillus medicine - Google Patents
Application of Houttuynoid E in anti-tubercle bacillus medicine Download PDFInfo
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- CN102872091B CN102872091B CN 201210418720 CN201210418720A CN102872091B CN 102872091 B CN102872091 B CN 102872091B CN 201210418720 CN201210418720 CN 201210418720 CN 201210418720 A CN201210418720 A CN 201210418720A CN 102872091 B CN102872091 B CN 102872091B
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Abstract
The invention discloses application of Houttuynoid E in preparing an anti-tubercle bacillus medicine. Aimed at the current situation that the morbidity and mortality of tuberculosis are on the rise due to the high morbidity of tuberculosis and the appearance of multi-drug resistant strain of mycobacterium tuberculosis at present, the invention discovers that Houttuynoid E has obvious activity in suppressing tubercle bacillus, and has good application prospects. The application of Houttuynoid E in preparing an anti-tubercle bacillus medicine is disclosed for the first time; and since the skeleton type is a brand new one and the activity in suppressing tubercle bacillus is unexpectedly strong, the possibility of any other compound offering any inspiration does not exist, outstanding substantial characteristics are obtained, and an obvious progress is made in preventing and treating tubercle bacillus infection.
Description
Technical field
The present invention relates to the medical compounds application, be specifically related to the application of Houttuynoid E in the preparation anti-tubercle bacillus drugs.
Background technology
Global morbidity lungy in recent years is increases trend, estimate according to the World Health Organization (WHO), the whole world is subjected to the population of mycobacterium tuberculosis (Mycobacterium tuberculosis, MTB) infection to account for 1/3rd of world population at present, 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 about 600,000 examples of infectiousness pulmonary tuberculosis wherein are one of the high burden of global tuberculosis countries.
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 makes 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 for preventing and controlling lungy.Therefore seek new antituberculotics, the antituberculotics of especially anti-multidrug resistance is to the protection people's health, and is significant.
Summary of the invention
the compound H outtuynoid E that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid E_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S. D. et al., 2012. Houttuynoid E_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), belong to open first for the purposes of the Houttuynoid E that the present invention relates in preparation treatment anti-tubercle bacillus drugs, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for tulase, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the control that is used for simultaneously tubercle bacillus affection obviously has significant progress.
Summary of the invention
The object of the invention is to provides the application of Houttuynoid E in the preparation anti-tubercle bacillus drugs according to not finding that it has the present situation of the report of tuberculosis activity in existing Houttuynoid E research.
Described compound H outtuynoid E 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 Houttuynoid E, 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 Houttuynoid E has very strong anti-tubercle bacillus and the 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 tuberculosis medicine.
Compared with prior art, the present invention has following beneficial effect:
1. the invention provides a kind of Houttuynoid E 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 present 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 E has the characteristics of anti-tubercle bacillus and drug resistance tulase activity, can be used for the preparation of antituberculotics, have boundless application prospect;
3. the purposes of the Houttuynoid E that 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 is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously tubercle bacillus affection obviously has significant progress.
The specific embodiment
The preparation method of compound H outtuynoid E involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid E_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compound H outtuynoid E tablet involved in the present invention:
Get 20 and digest compound Houttuynoid E, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid E capsule involved in the present invention:
Get 20 and digest compound Houttuynoid E, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The experimental example 1 anti-bacillus calmette-guerin vaccine of solid medium By Dilution Houttuynoid E (BCG) absolute concentration
Scraping bacillus calmette-guerin vaccine culture from the inclined-plane, join in 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw test tube cap, high vibration grinds on the vortex oscillation device, than turbid, namely be made into bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1mg/ml with standard Maxwell opacity tube (MacFarland No.1).
Houttuynoid E is made into the stock solution of high concentration with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Houttuynoid E that dilution is good joins 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 ℃), mixing, make and contain Houttuynoid E, concentration is respectively 6.0 ug/ml, 4.0 ug/ml, 3.0 ug/ml, 2.0 ug/ml, 1.5 ug/ml, 1.0 ug/ml, 0.75 ug/ml, 0.5 the isocyatic slant medium of ug/ml.
Bacillus calmette-guerin vaccine (BCG) bacteria suspension that is 1 mg/ml with concentration dips ring of numbers with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Houttuynoid E series concentration, be placed in 37 ℃ and cultivated for 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 Houttuynoid E Killing Mycobacterium Tuberculosis type strain H37Rv strain absolute concentrations
Scraping mycobacterium tuberculosis type strain H37Rv strain culture from the inclined-plane, join in 3 ml Middlebrook7H9 broth bouillons, add a small amount of bead, screw test tube cap, high vibration grinds on the vortex oscillation device, than turbid, namely be made into the H37Rv strain bacteria suspension of 1 mg/ml with standard Maxwell opacity tube (MacFarland No.1).
Houttuynoid E is made into respectively the stock solution of high concentration with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Houttuynoid E that dilution is good joins 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 ℃), mixing, make and contain Houttuynoid E, concentration is respectively 6.0 ug/ml, 4.0 ug/ml, 3.0 ug/ml, 2.0 ug/ml, 1.5 ug/ml, 1.0 ug/ml, 0.75 ug/ml, 0.5 the isocyatic slant medium of ug/ml.
The H37Rv strain bacteria suspension that is 1mg/ml with concentration dips ring of numbers with inoculating loop, is inoculated in respectively on the culture medium and blank medium slant that contains Houttuynoid E series concentration, and be placed in 37 ℃ and cultivated for 4 ~ 8 weeks, the observation experiment result, result is as shown in table 1.
The experimental example 3 clinical separation of the solid medium By Dilution Houttuynoid E tuberculosis mycobacterium MTB of anti-ISRE strain absolute concentrations
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 the inclined-plane, join in 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw test tube cap, high vibration grinds on the vortex oscillation device, than turbid, namely be made into the bacteria suspension of 1mg/ml with standard Maxwell opacity tube (MacFarland No.1).
Houttuynoid E is made into respectively the stock solution of high concentration with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Houttuynoid E that dilution is good joins 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 ℃), mixing, make and contain Houttuynoid E, concentration is respectively 6.0 ug/ml, 4.0 ug/ml, 3.0 ug/ml, 2.0 ug/ml, 1.5 ug/ml, 1.0 ug/ml, 0.75 ug/ml, 0.5 the isocyatic slant medium of ug/ml.
The clinical separation of the mycobacterium tuberculosis MTB of the anti-ISRE strain bacteria suspension that is 1mg/ml with concentration dips ring of numbers with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Houttuynoid E series concentration, be placed in 37 ℃ and cultivated for 4 ~ 8 weeks, the observation experiment result, result is as shown in table 1.
Table 1 solid medium By Dilution Houttuynoid E anti-tubercle bacillus absolute concentration result
Conclusion: Houttuynoid E has very strong anti-tubercle bacillus and the 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 tuberculosis medicine.
Claims (1)
1.Houttuynoid E is in the application of preparation in anti-tubercle bacillus drugs, described compound H outtuynoid E structure as
Formula IShown in:
Formula I.
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Non-Patent Citations (2)
| Title |
|---|
| Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata;Shao-Dan Chen等;《Organic Letters》;20120313;第14卷(第7期);1 * |
| Shao-DanChen等.HouttuynoidsA-E Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.《Organic Letters》.2012 |
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