CN103006639A - Application of aphanamixoid A in preparing antituberculosis medicament - Google Patents
Application of aphanamixoid A in preparing antituberculosis medicament Download PDFInfo
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- CN103006639A CN103006639A CN2012104701726A CN201210470172A CN103006639A CN 103006639 A CN103006639 A CN 103006639A CN 2012104701726 A CN2012104701726 A CN 2012104701726A CN 201210470172 A CN201210470172 A CN 201210470172A CN 103006639 A CN103006639 A CN 103006639A
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Abstract
The invention discloses an application of aphanamixoid A in preparing an antituberculosis medicament. Regarding the current situation that the tuberculosis incidence rate and death rate are in a rising trend due to the high incidence rate of current tuberculosis and occurrence of multiple-resistant strain of mycobacterium tuberculosis, the invention discovers that aphanamixoid A has remarkable activity of inhibiting tuberculosis, and has a high application prospect. The application of aphanamixoid A in preparing a medicament for treating tuberculosis belongs to first disclosure, which has prominent substantial characteristics because the frame model belongs to a brand-new frame model, and has unexpectedly strong inhibiting activity to tuberculosis without the possibility of giving any revelation by other compounds, and the prevention and treatment of aphanamixoid A for tuberculosis infection has a remarkable progress.
Description
Technical field
The present invention relates to the medical compounds application, be specifically related to the application of Aphanamixoid A in the preparation anti-tubercle bacillus drugs.
Background technology
In recent years global morbidity lungy 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 wherein about 600,000 examples of infectiousness pulmonary tuberculosis 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 because 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 chemical sproof variation more trends towards simultaneously drug resistance of multi-medicament, 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 compd A phanamixoid A that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to insect antifeedant activity (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Aphanamixoid A 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 chemical compounds, possess 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 Aphanamixoid A in the preparation anti-tubercle bacillus drugs according to not finding that it has the present situation of the report of tuberculosis activity in the existing Aphanamixoid A research.
Described compd A phanamixoid A structure is shown in formula I:
The object of the invention is achieved by the following technical programs:
The inventor does the examination bacterial strain with bacillus calmette-guerin vaccine first, adopt disk diffusion method that the anti-tubercle bacillus activity of Aphanamixoid A is carried out preliminary test, result according to preliminary test, the present invention use again the solid medium By Dilution this chemical 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 Aphanamixoid A 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 Aphanamixoid A 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 Aphanamixoid A 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 Aphanamixoid A 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 chemical 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 compd A phanamixoid A involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 compd A phanamixoid A tablet involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A phanamixoid A capsule involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
The experimental example 1 anti-bacillus calmette-guerin vaccine of solid medium By Dilution Aphanamixoid A (BCG) absolute concentration
Scraping bacillus calmette-guerin vaccine culture from the inclined-plane, join in the 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw test tube cap, high vibration grinds on the vortex oscillation device, with standard Maxwell opacity tube (MacFarland No.1) than turbid, namely be made into bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1 mg/ml.
Aphanamixoid A 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 Aphanamixoid A that dilution is good joins 4 ml Middlebrook7H11 agar culture mediums 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 Aphanamixoid A, 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, the isocyatic slant medium of 0.5 ug/ml.
Be that bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1 mg/ml dips ring of numbers with inoculating loop with concentration, be inoculated in respectively on the culture medium and blank medium slant that contains Aphanamixoid A series concentration, place 37 ℃ to cultivate for 4 ~ 8 weeks, the observation experiment result, the result is as shown in table 1.
Culture medium commonly used when used Middlebrook7H9 broth bouillon and Middlebrook7H11 agar culture medium carry out the tulase cultivation for those skilled in the art in the present embodiment, its prescription adopts conventional formulation to get final product.
Experimental example 2 solid medium By Dilution Aphanamixoid A Killing Mycobacterium Tuberculosis type strain H37Rv strain absolute concentrations
Scraping mycobacterium tuberculosis type strain H37Rv strain culture from the inclined-plane, join in the 3 ml Middlebrook7H9 broth bouillons, add a small amount of bead, screw test tube cap, high vibration grinds on the vortex oscillation device, with standard Maxwell opacity tube (MacFarland No.1) than turbid, namely be made into the H37Rv strain bacteria suspension of 1 mg/ml.
Aphanamixoid A 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 Aphanamixoid A that dilution is good joins 4 ml Middlebrook7H11 agar culture mediums 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 Aphanamixoid A, 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, the isocyatic slant medium of 0.5 ug/ml.
Be that the H37Rv strain bacteria suspension of 1 mg/ml dips ring of numbers with inoculating loop with concentration, be inoculated in respectively on the culture medium and blank medium slant that contains Aphanamixoid A series concentration, place 37 ℃ to cultivate for 4 ~ 8 weeks, the observation experiment result, the result is as shown in table 1.
The clinical separation of the experimental example 3 solid medium By Dilution Aphanamixoid A tuberculosis mycobacteriums MTB of anti-ISRE strain 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 the inclined-plane, join in the 3 ml Middlebrook7H9 broth bouillons, add a small amount of bead, screw test tube cap, high vibration grinds on the vortex oscillation device, with standard Maxwell opacity tube (MacFarland No.1) than turbid, namely be made into the bacteria suspension of 1mg/ml.
Aphanamixoid A 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 Aphanamixoid A 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 Aphanamixoid A, 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, the isocyatic slant medium of 0.5 ug/ml.
Be that the clinical separation of the mycobacterium tuberculosis MTB of the anti-ISRE strain bacteria suspension of 1mg/ml dips ring of numbers with inoculating loop with concentration, be inoculated in respectively on the culture medium and blank medium slant that contains Aphanamixoid A series concentration, place 37 ℃ to cultivate for 4 ~ 8 weeks, the observation experiment result, the result is as shown in table 1.
Table 1 solid medium By Dilution Aphanamixoid A anti-tubercle bacillus absolute concentration result
Conclusion: Aphanamixoid A 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.Aphanamixoid the application of A in the preparation anti-tubercle bacillus drugs, described compd A phanamixoid A structure is shown in formula I:
Formula I.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103432139A (en) * | 2013-09-11 | 2013-12-11 | 杨文君 | Application of compound in preparation of antituberculosis medicament |
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- 2012-11-19 CN CN2012104701726A patent/CN103006639A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| JY CAI,ET AL: "Aphanamixoid A, a potent defensive limonoid, with a new carbon skeleton from Aphanamixis polystachya", 《ORGANIC LETTERS》 * |
| 宋艳丽，康文艺: "抗耐药结核杆菌药用植物成分研究进展", 《中成药》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103432139A (en) * | 2013-09-11 | 2013-12-11 | 杨文君 | Application of compound in preparation of antituberculosis medicament |
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