CN103263428A - Application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments - Google Patents
Application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments Download PDFInfo
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- CN103263428A CN103263428A CN2013102173087A CN201310217308A CN103263428A CN 103263428 A CN103263428 A CN 103263428A CN 2013102173087 A CN2013102173087 A CN 2013102173087A CN 201310217308 A CN201310217308 A CN 201310217308A CN 103263428 A CN103263428 A CN 103263428A
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Abstract
The invention discloses an application of polyflavanostilbene A in preparation of anti-tuberculosis bacteria medicaments. The invention is designed against the current situation that the incidence rate and the mortality rate of tuberculosis are in a rising trend due to high incidence rate of the tuberculosis and the appearance of multiple-resistant strains of tuberculosis bacteria and finds that the polyflavanostilbene A has significant inhibition activity against the tuberculosis bacteria and further has good application prospects. The use of the polyflavanostilbene A in the preparation of the anti-tuberculosis bacteria medicaments, disclosed by the invention, belongs to the first disclosure, as the framework type belongs to the brand new framework type, the strong inhibition activity against the tuberculosis bacteria is unexpected, the possibility of giving any notices by other compounds does not exist, and the polyflavanostilbene A has prominent substantial characteristics; and simultaneously, the polyflavanostilbene A obviously has a significant progress in control of infection of the tuberculosis bacteria.
Description
Technical field
The present invention relates to the new purposes of Compound P olyflavanostilbene A, relate in particular to the application of Polyflavanostilbene A 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), at present the whole world be subjected to mycobacterium tuberculosis (Mycobacterium tuberculosis, MTB) population of Gan Raning accounts for 1/3rd of world population, 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 tuberculosis drug resistance situation serious day by day, and chemical sproof variation more trends towards multiple medicine 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.
The Compound P olyflavanostilbene A that the present invention relates to is one and delivered (Fushuang Li in 2013, et al., 2013.Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters 3 (15), 674 – 677.) noval chemical compound, this chemical compound has brand-new framework types, also do not find its pharmacologically active (Fushuang Li, et al., 2013.Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters 3 (15), 674 – 677.), belong to open first for the purposes of the Polyflavanostilbene A that the present invention relates in the preparation anti-tubercle bacillus drugs, owing to belong to brand-new structure type, and it is active unexpectedly strong for anti-tubercle bacillus, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for anti-tubercle bacillus simultaneously and obviously have obvious improvement.
Summary of the invention
The objective of the invention is to provides the application of Polyflavanostilbene A in the preparation anti-tubercle bacillus drugs according to not finding that it has the present situation of the report of anti-tubercle bacillus activity in the existing Polyflavanostilbene A research.
Described Compound P olyflavanostilbene 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 earlier, adopt disk diffusion method that the anti-tubercle bacillus activity of Polyflavanostilbene A is carried out preliminary test, result according to preliminary test, reuse solid medium dilution method of the present invention has been measured 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 Polyflavanostilbene A 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 Polyflavanostilbene A that can be used for the sick treatment of tuberculosis, thereby enlarged the kind of anti-tubercle bacillus drugs;
2. at the appearance of present incidence of tuberculosis height, tubercule bacillus multiple antibiotic resistant strain and HIV (human immunodeficiency virus) double infection, make incidence of tuberculosis and mortality rate present situation in rising trend, the present invention finds that Polyflavanostilbene 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 Polyflavanostilbene 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 tubercle bacillus affection simultaneously obviously has obvious improvement.
The specific embodiment
The preparation method of Compound P olyflavanostilbene A involved in the present invention is referring to document (Fushuang Li, et al., 2013.Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters 3 (15), 674 – 677.)
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 P olyflavanostilbene A tablet involved in the present invention:
Get 20 and digest compound Polyflavanostilbene A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of Compound P olyflavanostilbene A capsule involved in the present invention:
Get 20 and digest compound Polyflavanostilbene 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.
Experimental example 1 solid medium dilution method is measured the anti-bacillus calmette-guerin vaccine of Polyflavanostilbene A (BCG) absolute concentration
Scrape from the inclined-plane and to get the bacillus calmette-guerin vaccine culture, join in the 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw the test tube lid, high vibration grinds on the vortex oscillation device, with standard Maxwell opacity tube (MacFarlandNo.1) than turbid, namely be made into bacillus calmette-guerin vaccine (BCG) bacteria suspension of 1mg/ml.Polyflavanostilbene 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 Polyflavanostilbene 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 Polyflavanostilbene A, 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.
Bacillus calmette-guerin vaccine (BCG) bacteria suspension that with concentration is 1mg/ml dips in the peek ring with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Polyflavanostilbene 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 dilution methods are measured Polyflavanostilbene A Killing Mycobacterium Tuberculosis type strain H37Rv strain absolute concentration
Scrape from the inclined-plane and to get mycobacterium tuberculosis type strain H37Rv strain culture, join in the 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw the test tube lid, 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 1mg/ml.
Polyflavanostilbene A is made into the stock solution of high concentration respectively with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Polyflavanostilbene 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 Polyflavanostilbene A, 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 H37Rv strain bacteria suspension that with concentration is 1mg/ml dips in the peek ring with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Polyflavanostilbene A series concentration, place 37 ℃ to cultivate for 4～8 weeks, the observation experiment result, the result is as shown in table 1.
Experimental example 3 solid medium dilution methods are measured the clinical separation of the Polyflavanostilbene A tuberculosis mycobacterium MTB of anti-ISRE strain absolute concentration
Scrape from the inclined-plane and to get the clinical separation of the mycobacterium tuberculosis MTB of anti-ISRE strain (anti-isoniazid, streptomycin, rifampicin, the clinical detached dowel of ethambutol mycobacterium tuberculosis) culture, join in the 3ml Middlebrook7H9 broth bouillon, add a small amount of bead, screw the test tube lid, 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.
Polyflavanostilbene A is made into the stock solution of high concentration respectively with DMSO, dilute stock solution to desired concn with the aseptic ultra-pure water of the tween 80 that contains 5%, the Polyflavanostilbene 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 Polyflavanostilbene A, 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 with concentration is 1mg/ml dips in the peek ring with inoculating loop, be inoculated in respectively on the culture medium and blank medium slant that contains Polyflavanostilbene 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 dilution method is measured Polyflavanostilbene A anti-tubercle bacillus absolute concentration result
Conclusion: Polyflavanostilbene A 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.Polyflavanostilbene the application of A in the preparation anti-tubercle bacillus drugs, described Compound P olyflavanostilbene A structure is shown in formula I:
Formula I.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103285024A (en) * | 2013-06-22 | 2013-09-11 | 李正梅 | The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine |
| CN104122348A (en) * | 2014-08-06 | 2014-10-29 | 山东蓝星东大化工有限责任公司 | Preparation method of high-viscosity standard solution for quantification of headspace gas chromatography external standard method |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102872049A (en) * | 2012-10-26 | 2013-01-16 | 吴俊华 | Application of gypensapogenin A to anti-tubercle bacillus drugs |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102872049A (en) * | 2012-10-26 | 2013-01-16 | 吴俊华 | Application of gypensapogenin A to anti-tubercle bacillus drugs |
Non-Patent Citations (2)
| Title |
|---|
| FUSHUANG LI等: "Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum", 《ORGANIC LETTERS》 * |
| 黄英俊等: "狭叶红景天的化学成分及其抑制结核分枝杆菌生长活性的研究", 《中国中药杂志》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103285024A (en) * | 2013-06-22 | 2013-09-11 | 李正梅 | The pplication of Polyflavanostilbene A in preparing an anti-tubercle bacillus medicine |
| CN104122348A (en) * | 2014-08-06 | 2014-10-29 | 山东蓝星东大化工有限责任公司 | Preparation method of high-viscosity standard solution for quantification of headspace gas chromatography external standard method |
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Application publication date: 20130828 |