CN106727533A - A kind of pharmaceutical composition for treating chronic renal failure - Google Patents
A kind of pharmaceutical composition for treating chronic renal failure Download PDFInfo
- Publication number
- CN106727533A CN106727533A CN201710081081.6A CN201710081081A CN106727533A CN 106727533 A CN106727533 A CN 106727533A CN 201710081081 A CN201710081081 A CN 201710081081A CN 106727533 A CN106727533 A CN 106727533A
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- Prior art keywords
- renal failure
- pharmaceutical composition
- chronic renal
- alkyl
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to a kind of pharmaceutical composition for treating chronic renal failure, compound of the described pharmaceutical composition comprising following formula or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：Wherein R1 independently selected from：H, alkyl or halogen.
Description
Technical field
The present invention relates to field of medicaments, specifically, the present invention relates to a kind of pharmaceutical composition for treating chronic renal failure.
Background technology
Chronic renal failure (chronic renal failure, CRF) course of disease is progressive development, but in a certain of the course of disease
In the stage, due to inducements such as infection, hypertension, metabolic acidosis, electrolyte disturbances, drastically disliking can occur in a short time in renal function
Change.It is even serious to threaten patient vitals.This renal function exacerbation, such as treatment in time, often with certain invertibity, or even completely
Return to premalignant renal function level.Therefore, it is the important for the treatment of CRF to control Acute aggravated factors, prevent renal function from drastically deteriorating
Content.At present, the treatment means clinically to CRF are mainly haemodialysis or kidney transplant, have greatly aggravated the warp of patient
Ji burden.
The content of the invention
It is an object of the invention to provide a kind of pharmaceutical composition for treating chronic renal failure.
In order to realize the purpose of the present invention, the present invention provides a kind of pharmaceutical composition for treating chronic renal failure, the medicine
Compound of the compositions comprising following formula or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：
Wherein R1 independently selected from：H, alkyl or halogen.
Preferably, R1 is alkyl.
It is highly preferred that R1 is CH3。
The present invention also provides purposes of the compound in the medicine for preparing treatment chronic renal failure, under the compound has
Array structure：
Wherein R1 independently selected from：H, alkyl or halogen.
Preferably, R1 is alkyl.
It is highly preferred that R1 is CH3。
Medicine of the present invention can be used for treating or mitigating chronic renal failure symptom, and effective component is clearly controllable,
Rapid-action, effect is notable, convenient to take.
Brief Description Of Drawings
Fig. 1 is to nephridial tissue TGF-β1And the influence of PAI-1 protein expressions.
Specific embodiment
It will be appreciated by those skilled in the art that the concept and specific embodiment disclosed in description above can be easy to
With making an amendment or design the basis of the other embodiment for implementing identical purpose of the invention.What those skilled in the art also will be understood that
It is that these equivalent implementation methods are without departing from the spirit and scope of the present invention illustrated in appended claims.
The sign of the medicine of the present invention of experimental example 1
1H NMR(400MHz,CDCl3)δ7.29(m,3H),7.17(m,4H),7.11(m,2H),4.65(m,1H),4.16
(m,2H),3.26(m,3H),2.99(m,2H),2.75(m,1H),2.32(s,3H)；
ESIMS m/z 346([M+Na]+)。
Therapeutic effect of the medicine of the present invention of experimental example 2 for chronic renal failure
60 healthy male SD rats are divided into blank group, model group, positive controls, high, medium and low dose of medicine of the present invention
Amount group, every group 10.Normal group gives chow diet, and remaining each group gives the feed containing 5% adenine, continuously feeds 28d.
Modeling simultaneously, the daily gavage clearing preparation-Niaoduqing of positive controls (be purchased from Kang Chen medicine companies) 4.6gkg-1, high, medium and low dose of medicine of the present invention
Amount group distinguishes gavage 10,5 and 2.5mgkg daily-1Compound in embodiment 1, blank group and the daily gavage physiology of model group
Salt solution.
29th day, the urine of rat 24h is collected with metabolic cage, compare each group urine volume, and urine is detected with Coomassie Brilliant Blue
Protein content in liquid.
Animal was put to death in 30th day, kidney is taken out rapidly, shredded, add liquid nitrogen grinding, adding cell pyrolysis liquid (will
0.2422g Tris are dissolved in 20mL distilled water, and it is 8.0 to adjust its pH value, is subsequently adding 0.149g EDTA and 0.16g SDS)
Extract proteins, are quantified with BCA methods to albumen.Tissue homogenate supernatant is diluted into 2000 μ gmL by physiological saline again-1's
Concentration, adds 4X sample-loading buffers, the water-bath 5min in boiling water to be stored at a temperature of -40 DEG C；10 μ L albumen are taken in constant pressure 80V
Under carry out PAGE gel (10%) electrophoresis, electrophoresis time 30min, then shift to 120V, remove gel, transferring film 1h under 200mA,
Pvdf membrane is closed with confining liquid at room temperature again, overnight.Pvdf membrane is cut, 1 is added:250 TGF-β1, PAI-1 and GAPDH mono-
It is anti-, 1h is incubated at room temperature, then is rinsed 3 times with TBST, each 5min；Add 1:5000 secondary antibody, is incubated 45min at room temperature,
TBST is rinsed 3 times, each 5min；Developed the color through ECL, darkroom exposure 2min, developing fixing.
The software kits of experimental result application SPSS 16.0 are analyzed, and the data obtained measurement data uses mean ± standard deviationRepresent, multigroup is compared and use variance analysis, compare two-by-two using LSD methods, P<0.05 has statistics for difference
Meaning.
Influence to CRF rat 24h urine volume and Urine proteins
Modeling the 29th day, compares with model group, and the high, medium and low dosage group of medicine of the present invention dramatically increases rat 24h urine volume,
And significantly reduce urine albumen amount (P<0.05).There was no significant difference with the high, medium and low dosage group of medicine of the present invention for positive controls.
It can be seen that medicine of the present invention can improve the symptom of chronic renal failure, as a result see the table below.
Note：Compare with model group, * P<0.05
To nephridial tissue TGF-β1And the influence of PAI-1 protein expressions
Western blot band photodensitometries show, compare with model group, the high, medium and low dosage group of medicine of the present invention
TGF-β in nephridial tissue1And PAI-1 protein expressions significantly reduce (P<0.05).Positive controls are high, medium and low with medicine of the present invention
There was no significant difference for dosage group.Show that medicine of the present invention plays certain protective role to kidney, as a result see the table below and Fig. 1.
Note：Compare with model group, * P<0.05.
Claims (6)
1. a kind of pharmaceutical composition for treating chronic renal failure, it is characterised in that chemical combination of the described pharmaceutical composition comprising following formula
Thing or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：
Wherein R1 independently selected from：H, alkyl or halogen.
2. it is according to claim 1 treatment chronic renal failure pharmaceutical composition, it is characterised in that R1 is alkyl.
3. it is according to claim 1 treatment chronic renal failure pharmaceutical composition, it is characterised in that R1 is CH3。
4. compound prepare treatment chronic renal failure medicine in purposes, it is characterised in that the compound has following
Structure：
Wherein R1 independently selected from：H, alkyl or halogen.
5. purposes according to claim 4, it is characterised in that R1 is alkyl.
6. purposes according to claim 5, it is characterised in that R1 is CH3。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710081081.6A CN106727533A (en) | 2017-02-15 | 2017-02-15 | A kind of pharmaceutical composition for treating chronic renal failure |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710081081.6A CN106727533A (en) | 2017-02-15 | 2017-02-15 | A kind of pharmaceutical composition for treating chronic renal failure |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106727533A true CN106727533A (en) | 2017-05-31 |
Family
ID=58958440
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710081081.6A Pending CN106727533A (en) | 2017-02-15 | 2017-02-15 | A kind of pharmaceutical composition for treating chronic renal failure |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106727533A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105764897A (en) * | 2013-10-01 | 2016-07-13 | 美国陶氏益农公司 | Use of macrocylic picolinamides as fungicides |
-
2017
- 2017-02-15 CN CN201710081081.6A patent/CN106727533A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105764897A (en) * | 2013-10-01 | 2016-07-13 | 美国陶氏益农公司 | Use of macrocylic picolinamides as fungicides |
Non-Patent Citations (1)
| Title |
|---|
| 张玲等: "黄连碱对慢性肾功能衰竭大鼠的治疗作用及其机制研究", 《中国现代应用药学》 * |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170531 |
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