CN110151763A - It examines than treating the application in tubercular drugs as preparation for Buddhist nun - Google Patents
It examines than treating the application in tubercular drugs as preparation for Buddhist nun Download PDFInfo
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- CN110151763A CN110151763A CN201910558802.7A CN201910558802A CN110151763A CN 110151763 A CN110151763 A CN 110151763A CN 201910558802 A CN201910558802 A CN 201910558802A CN 110151763 A CN110151763 A CN 110151763A
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- buddhist nun
- pharmaceutical composition
- macrophage
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
It is highly-safe the invention discloses a kind of application examined than being treated in tubercular drugs for Buddhist nun as preparation, it is high-efficient to kill tuberculosis difference bacillus.It examines than for Buddhist nun, as the application in preparation treatment tubercular drugs, treatment tuberculosis is against mycobacterium tuberculosis drug.A kind of pharmaceutical composition for tuberculotherapy, comprising examining than for Buddhist nun in the pharmaceutical composition.It examines than the drug for Buddhist nun as potential targeting HDT, ratified by FDA, it is highly-safe, with good Development volue, therefore the present invention proposes to examine than that will have very high safety as the main component in antituberculotic for Buddhist nun, and the present invention, which has been found through experiments that examine than that can significantly increase the activity of macrophage in macrophage for Buddhist nun, kills tulase.
Description
Technical field
The present invention relates to technical field of bioengineering, in particular to examine than treating in tubercular drugs for Buddhist nun as preparation
Using.
Background technique
Research and development effectively treat new drug/new departure lungy, with improve therapeutic effect, shorten the course for the treatment of, reduce toxic side effect,
Overcoming clinical drug-resistant is the key subjects and research hotspot of current tuberculosis prevention and control.Developing new antituberculotic is to solve tuberculosis
Drug resistant important thinking.However, a line antituberculotic used is to be researched and developed before more than 40 years now, novel effective resistive connection
Nuclear pharmaceuticals research and development are slow, and these drugs are all to directly act on tulase itself, and there is the risks of crossing drug resistant always.
HDT drug be by improve host's treating tuberculosis be immunized realize treatment tuberculosis purpose, thus for improve tuberculosis treatment effect,
Overcome the problems, such as that drug resistance tuberculosis therapy provides new vision.
It examines than being benzofuran derivatives for Buddhist nun, the sinus rhythm for treating paroxysmal or permanent atrial fibrillation controls
Drug；It examines than blocking a variety of channels (sodium, potassium, calcium) for Buddhist nun, and shows antiadrenergic drug energy characteristic.Examine the anti-rhythm of the heart than replacing Buddhist nun
Not normal effect may be due at least two main functions, it is by inhibiting sodium and potassium channel to extend action potential in cardiac muscular tissue
With the duration of refractory period, by inhibition calcium channel and β 1- adrenergic receptor is blocked, it can be observed that AV conduction and sinus
The reduction of room knot function；Examining can also be by inhibiting alpha 1 adrenergic receptor to cause elevation of the blood pressure than for Buddhist nun.
It examines than being C for Buddhist nun's molecular formula21H21F3IN3O2, molecular weight 531.31, structural formula is as follows:
It examines than there is good Development volue for Buddhist nun and its derivative.
Summary of the invention
It examines the technical problem to be solved in the present invention is to provide a kind of than treating answering in tubercular drugs as preparation for Buddhist nun
With will particularly examine than being applied to highly-safe in the drug for the treatment of tuberculosis difference bacillus for Buddhist nun, kill tuberculosis difference bacillus efficiency
It is high.
In order to solve the above-mentioned technical problem, the present invention adopts the following technical scheme: examining than treating tuberculosis as preparation for Buddhist nun
Application in medicine.
Of the present invention examine than applying for Buddhist nun in treatment tuberculosis is against mycobacterium tuberculosis drug.
A kind of pharmaceutical composition for tuberculotherapy, comprising examining than for Buddhist nun in described pharmaceutical composition.
Also comprising pharmaceutically acceptable auxiliary material in pharmaceutical composition of the present invention.
Pharmaceutical composition of the present invention is oral agents or injection；The oral agents include: tablet, granule, dripping pill,
Soft capsule, suspending agent, at least one of solution and syrup；The injection includes: freeze dried powder, solution-type injection
Agent, at least one of suspension injection and emulsion-type injection.
Compared with prior art, it examines than the drug for Buddhist nun as potential targeting HDT, is ratified by FDA, safety
Height has good Development volue, therefore present invention proposition will be examined than that will have for Buddhist nun as the main component in antituberculotic
There is very high safety, the present invention, which has been found through experiments that, to be examined than that can significantly increase macrophage in macrophage for Buddhist nun
Activity kills tulase.
Detailed description of the invention
Fig. 1 is to test various concentration in 1 experimental group to examine than the data and control group for Buddhist nun's influence macrophage survival rate
The survival rate data of middle macrophage；Wherein, " * * ", which is represented, has significant difference, and " ns " represents no statistical difference.
Fig. 2 is to test various concentration in 2 experimental groups to examine in data and control group than influencing tulase survival rate for Buddhist nun
Tulase survival rate data.
Specific embodiment
The present invention will be further described in detail with reference to the accompanying drawings and detailed description.The present invention is real by two groups
It tests to measure and examine than having the function of that the activity for enhancing macrophage carrys out Antituberculous mycobacteria in macrophage for Buddhist nun.With
The conventional means that technological means used in lower experiment is well known to those skilled in the art, all raw materials are versatile material.
Experiment 1
The differentiation of one .U937 macrophage (number BNCC100967):
1. the U937 macrophage of suspension is incubated in the RPMI-1640 culture medium containing 10%FBS (fetal calf serum),
And being placed on temperature is 37 DEG C, contains 5%CO2Cell incubator in cultivate.
2. PMA (the cool acetic acid of Buddhist Bo Rou Beans) overnight incubation of final concentration of 20ng/ml is added, it is thin to be divided into macrophage
Born of the same parents.
3. being cleaned twice with PBS (phosphate buffer), after pancreatin digestion, being resuspended, 96 porocyte culture plates are added
In, make the cell number 1x10 in every hole4It is a；
The measurement of two, cell survival rates:
1. examining than for Buddhist nun's solution, making to examine than existing for Buddhist nun for various concentration is added after above-mentioned U937 macrophage culture for 24 hours
Ultimate density in macrophage culture plate in each hole is 100umol/L, 10umol/L, 1umo/L, and each concentration weighs respectively
Multiple at least 3 times experiments.
It is examined with above-mentioned than for Buddhist nun's volume 2. being added using DMSO (dimethyl sulfoxide) as parallel control experiment, in control group
Identical DMSO equally repeats at least 3 times experiments respectively.
3 are added (the water-soluble tetrazolium salts examination of 10ul WST-1 solution after 48h into all holes of experimental group and control group
Agent), continue to cultivate 4h under conditions of temperature is 37 DEG C.
4. finally utilizing the OD450nm light absorption value of microplate reader measurement experiment group and control group；
Three, cell survival rates are calculated according to following formula:
Cell survival rate %=[A/A0] × 100, wherein A0For the light absorption value of DMSO control, A is at various concentration drug
The light absorption value of reason.
As shown in Figure 1, various concentration is examined than for influence of the Buddhist nun to the survival rate of macrophage；Wherein, " * * " representative has
Significant difference, " ns " represent no statistical difference.
Experimental result is shown, is examined than being 100umol/L, 10umol/L, 1umol/L, corresponding macrophage for Buddhist nun's concentration
Survival rate is respectively as follows: 34%, 108%, 100%；When examine than for Buddhist nun's concentration be 10umol/L when, the survival rate of macrophage with it is right
No statistical difference is compared according to group, it was demonstrated that is examined under this concentration than not having toxicity to macrophage for Buddhist nun.
Experiment 2:
The differentiation of one .U937 macrophage (number BNCC100967):
1. the U937 macrophage of suspension is incubated in the RPMI-1640 culture medium containing 10%FBS (fetal calf serum),
And being placed on temperature is 37 DEG C, contains 5%CO2Cell incubator in cultivate.
2. the PMA overnight incubation of final concentration of 20ng/ml is added, it is divided into macrophage.It is cleaned twice with PBS,
After pancreatin digestion, being resuspended, it is added in 96 porocyte culture plates, makes the cell number 1x10 in every hole4It is a；
The intracellular bactericidal activity measurement of two:
1. tubercle bacillus affection macrophage is added, is added in experimental group and examines ratio after above-mentioned U937 macrophage culture for 24 hours
Make its final concentration of 100umol/L, 10umol/L, 1umol/L for Buddhist nun, each concentration repeats at least 3 times experiments respectively.
2. be added and examine using DMSO as parallel control experiment, in control group it is DMSO more identical than for Buddhist nun's volume, respectively
Repeat at least 3 times experiments.
3. sucking culture medium after 4h, cleaned twice with PBS, the RPMI-1640 culture of 10%FBS (fetal calf serum) is added
Then 0.01%SDS (lysate) is added in base 72h, lytic cell, is coated on 7H10 plate after gradient dilution, calculates after 3 weeks
Bacterium colony；
4. result using 10umol/L as shown in Fig. 2, when being examined than handling for Buddhist nun, the tulase to survive in cell is only compareed
The 7.2% of the tulase to survive in group, i.e., survival rate of the survival rate of tulase relative to tulase in control group in experimental group
It is very low；And according to experiment 1, is examined under this concentration than there is no apparent cytotoxicity to macrophage for Buddhist nun, can be used
Antituberculotic in exploitation efficiently, less toxic.
Claims (5)
1. examining than treating the application in tubercular drugs as preparation for Buddhist nun.
2. application according to claim 1, it is characterised in that: the treatment tuberculosis is Killing Mycobacterium Tuberculosis
Drug.
3. a kind of pharmaceutical composition for tuberculotherapy, it is characterised in that: comprising examining than for Buddhist nun in described pharmaceutical composition.
4. pharmaceutical composition according to claim 3, it is characterised in that: described pharmaceutical composition also includes pharmaceutically may be used
The auxiliary material of receiving.
5. pharmaceutical composition according to claim 3, it is characterised in that: described pharmaceutical composition is oral agents or injection
Agent；
The oral agents include: tablet, granule, dripping pill, soft capsule, suspending agent, at least one in solution and syrup
Kind；
The injection includes: freeze dried powder, solution type injection agent, in suspension injection and emulsion-type injection extremely
Few one kind.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910558802.7A CN110151763A (en) | 2019-06-26 | 2019-06-26 | It examines than treating the application in tubercular drugs as preparation for Buddhist nun |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910558802.7A CN110151763A (en) | 2019-06-26 | 2019-06-26 | It examines than treating the application in tubercular drugs as preparation for Buddhist nun |
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| Publication Number | Publication Date |
|---|---|
| CN110151763A true CN110151763A (en) | 2019-08-23 |
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| CN201910558802.7A Pending CN110151763A (en) | 2019-06-26 | 2019-06-26 | It examines than treating the application in tubercular drugs as preparation for Buddhist nun |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110664811A (en) * | 2019-09-18 | 2020-01-10 | 深圳市第三人民医院 | Application of afatinib in anti-mycobacterium tuberculosis drugs |
| CN111110655A (en) * | 2020-01-20 | 2020-05-08 | 山东大学 | Nano composite and preparation method and application thereof |
| CN113975276A (en) * | 2021-12-01 | 2022-01-28 | 中南大学 | Application of cobicistinib in preparation of medicine for treating ischemia/reperfusion injury and cell protection medicine |
| WO2023082397A1 (en) * | 2021-11-15 | 2023-05-19 | 中国科学院深圳先进技术研究院 | A-fabp protein inhibitor and use thereof |
Citations (4)
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| WO2013001372A2 (en) * | 2011-06-30 | 2013-01-03 | University Of Oslo | Methods and compositions for inhibition of activation of regulatory t cells |
| WO2017049036A1 (en) * | 2015-09-16 | 2017-03-23 | Emory University | Use of kinase inhibitors to manage tuberculosis and other infectious diseases |
| CN108135854A (en) * | 2015-06-30 | 2018-06-08 | 基因泰克公司 | Tablet and the method for being used to form tablet are released immediately containing drug |
| CN108420822A (en) * | 2017-02-15 | 2018-08-21 | 四川大学 | The antibacterial new application of Ceritinib |
-
2019
- 2019-06-26 CN CN201910558802.7A patent/CN110151763A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013001372A2 (en) * | 2011-06-30 | 2013-01-03 | University Of Oslo | Methods and compositions for inhibition of activation of regulatory t cells |
| CN108135854A (en) * | 2015-06-30 | 2018-06-08 | 基因泰克公司 | Tablet and the method for being used to form tablet are released immediately containing drug |
| WO2017049036A1 (en) * | 2015-09-16 | 2017-03-23 | Emory University | Use of kinase inhibitors to manage tuberculosis and other infectious diseases |
| CN108420822A (en) * | 2017-02-15 | 2018-08-21 | 四川大学 | The antibacterial new application of Ceritinib |
Non-Patent Citations (1)
| Title |
|---|
| HUYNH HH等: "Development and Validation of a Simultaneous Quantification Method of 14 Tyrosine Kinase Inhibitors in Human Plasma Using LC-MS/MS", 《THER DRUG MONIT》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110664811A (en) * | 2019-09-18 | 2020-01-10 | 深圳市第三人民医院 | Application of afatinib in anti-mycobacterium tuberculosis drugs |
| CN111110655A (en) * | 2020-01-20 | 2020-05-08 | 山东大学 | Nano composite and preparation method and application thereof |
| WO2023082397A1 (en) * | 2021-11-15 | 2023-05-19 | 中国科学院深圳先进技术研究院 | A-fabp protein inhibitor and use thereof |
| CN113975276A (en) * | 2021-12-01 | 2022-01-28 | 中南大学 | Application of cobicistinib in preparation of medicine for treating ischemia/reperfusion injury and cell protection medicine |
| CN113975276B (en) * | 2021-12-01 | 2023-03-07 | 中南大学 | Application of cobicistinib in preparation of medicines for treating ischemia/reperfusion injury and cytoprotective medicines |
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Application publication date: 20190823 |
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