CN105497040A - Application of Astataricusol A in preparing of medicine for treating acute renal failure - Google Patents
Application of Astataricusol A in preparing of medicine for treating acute renal failure Download PDFInfo
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- CN105497040A CN105497040A CN201510897068.9A CN201510897068A CN105497040A CN 105497040 A CN105497040 A CN 105497040A CN 201510897068 A CN201510897068 A CN 201510897068A CN 105497040 A CN105497040 A CN 105497040A
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- renal failure
- acute renal
- astataricusola
- medicine
- astataricusol
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to a new medicine usage of Astataricusol A, namely application of Astataricusol A in preparing of an medicine for treating acute renal failure. The usage of the Astataricusol A in the preparing of the medicine for treating acute renal failure is firstly disclosed, since a skeleton type belongs to a brand new skeleton type and has previously unimagined inhibition activity to acute renal failure without possibility of any teaching given by other compounds, the Astataricusol A has prominent substantive features and has a notable progress in resistance to the acute renal failure.
Description
Technical field
The present invention relates to the novelty teabag of compd A stataricusolA, particularly relate to the application of AstataricusolA in preparation treatment acute renal failure medicine.
Background technology
Acute renal failure (AcuteRenalFailure, ARF) be the clinical syndrome caused by many reasons, be found in clinical departments patient, sickness rate is high and often have serious consequences, its feature is that (a few hours are to a couple of days) siddhi can sharply decline in a short time, clinical manifestation is acute oliguria (urine volume <400mLPd) or anuria (urine volume <100mLPd), in body, nitrogen matter metabolite is discharged and is produced obstacle, there is azotemia rapidly, water and electrolyte, acid base imbalance, and cause each system corresponding function imbalance of whole body.The principal element of acute renal failure is caused to be the sharply minimizing of renal blood flow, and the oxidative stress caused due to nephridial tissue ischemia and cell injury, finally cause the deterioration of renal tissue structural damage and function.There is no the generally acknowledged effective medicine for the treatment of acute renal failure clinically at present, only by correcting water-electrolyte balance, correcting the symptomatic treatment measures such as acidosis and improving symptom, the later stage also needs to maintain body function by hemodialysis.Improving kidney perfusion obstacle and alleviating in Renal tissues damage and have the clinical medicine of obvious curative effects rare.
The compd A stataricusolA that the present invention relates to is one and delivers (Wen-BingZhou in 2013, etal., AstataricusonesA – DandAstataricusolA, FiveNewAnti-HBVShionane-TypeTriterpenesfromAstertataricu sL.f..Molecules2013, 18, 14585-14596.) noval chemical compound, this compound has brand-new framework types, suppress hepatitis B virus (Wen-BingZhou, etal., AstataricusonesA – DandAstataricusolA, FiveNewAnti-HBVShionane-TypeTriterpenesfromAstertataricu sL.f..Molecules2013, 18, 14585-14596.), the purposes of the AstataricusolA that the present invention relates in preparation treatment acute renal failure medicine is belonged to first public, owing to belonging to brand-new structure type, and its activity for treatment acute renal failure is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for acute renal failure obviously has significant progress.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of anti-acute renal failure activity according in existing AstataricusolA research, provide the application of AstataricusolA in the anti-acute renal failure medicine of preparation.
Found by our research, anuria when AstataricusolA can improve acute renal failure or oliguria symptom, the function of protection kidney.
Described compd A stataricusolA, structure is as shown in formula I:
The application of described AstataricusolA in treatment acute renal failure medicine, AstataricusolA can improve renal blood flow amount.
One treats acute renal failure medicine, and be that the active adjuvant that adds is prepared from by AstataricusolA, preparation method, for getting 20 g of compound AstataricusolA, adds the customary adjuvant 180 grams preparing tablet, and mixing, conventional tablet presses makes 1000.
One treats acute renal failure medicine, is that the active adjuvant that adds is prepared from by AstataricusolA, preparation method for getting 20 g of compound AstataricusolA, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
The purposes of the AstataricusolA that the present invention relates in the anti-acute renal failure medicine of preparation belongs to first public, because framework types belongs to brand-new framework types, and it is unexpectedly strong for acute renal failure inhibit activities, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, for anti-acute renal failure, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of compd A stataricusolA involved in the present invention is see document (Wen-BingZhou, etal., AstataricusonesA – DandAstataricusolA, FiveNewAnti-HBVShionane-TypeTriterpenesfromAstertataricu sL.f..Molecules2013,18,14585-14596.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compd A stataricusolA tablet involved in the present invention:
Get 20 g of compound AstataricusolA, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compd A stataricusolA capsule involved in the present invention:
Get 20 g of compound AstataricusolA, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1AstataricusolA is to the therapeutical effect of acute renal failure rat
(1) experimental technique
Intramuscular injection glycerol is adopted to cause Acute Renal Failure Rats animal model.Select the healthy male SD rat 60 of 180 ~ 220g, be divided into 5 groups at random: sham operated rats (intramuscular injection normal saline); Model group (intramuscular injection glycerol); AstataricusolA I group (0.3mg/Kg)); AstataricusolA II group (0.6mg/Kg)); AstataricusolA III group (1.2mg/Kg)), each group rat tail vein injection saline or AstataricusolA immediately after glycerol modeling, be administered once after 12 and 24 hours again.
(2) observation index
Put into metabolic cage after 60 rat lasts give AstataricusolA or normal saline and collect twenty-four-hour urine, stay latter 6 hours of urine with 4% chloral hydrate intraperitoneal injection of anesthesia, adopt laser Doppler flowmetry to measure after modeling and bilateral renal blood flow after treatment, average as single animal renal blood flow; Get blood and prepare serum, measure blood BUN and Cre; Get kidney, prepare 10% renal cortex homogenate, measure renal cortex homogenate MDA, GSH, NO (all by the operation of test kit description).(3) experimental result
1.AstataricusolA can increase acute renal failure Mouse Kidney blood flow
Table 1AstataricusolA is on the impact of acute renal failure Mouse Kidney blood flow
* P<0.05 and acute renal failure model group contrast
2.AstataricusolA is to the protective effect of acute renal failure Mouse Kidney function tool
Model group rats comparatively rats in sham-operated group twenty-four-hour urine amount significantly reduces, and is respectively 4.82 ± 0.63ml and 12.15 ± 3.15ml; Middle and high dosage AstataricusolA group twenty-four-hour urine amount is significantly higher than model group (P<0.05), the urine volume of three medication therapy groups has dose dependent, be respectively I group of 5.48 ± 0.87ml, II group of 7.90 ± 1.47ml, III group of 19.26 ± 1.76ml.Illustrate that AstataricusolA can improve the oliguria symptom of acute renal failure rat.
Acute renal failure rat intravenous injection normal saline is after 24 hours, and serum BUN is 27.12 ± 1.89mmol/L, Cre is 171.42 ± 15.09umol/L, apparently higher than sham operated rats, illustrates that model group animal renal function injury is serious.Middle and high dosage AstataricusolA dose-dependently can improve the renal function (P<0.05) of acute renal failure rat.In table 2.
The each rats in test groups renal function index of table 2 compares
* P<0.05 and acute renal failure model group contrast
Anuria when conclusion: AstataricusolA can improve acute renal failure or oliguria symptom, the function of protection kidney, can be used for preparing anti-acute renal failure medicine.
Claims (4)
- The application of 1.AstataricusolA in treatment acute renal failure medicine, described compd A stataricusolA structure is as shown in formula I:Formula I.
- 2. the application of AstataricusolA in treatment acute renal failure medicine as claimed in claim 1, it is characterized in that, AstataricusolA can improve renal blood flow amount.
- 3. a treatment acute renal failure medicine, it is characterized in that by AstataricusolA described in claim 1 being that the active adjuvant that adds is prepared from, preparation method, for getting 20 g of compound AstataricusolA, adds the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
- 4. a treatment acute renal failure medicine, it is characterized in that by AstataricusolA described in claim 1 being that the active adjuvant that adds is prepared from, preparation method is for getting 20 g of compound AstataricusolA, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510897068.9A CN105497040A (en) | 2015-12-04 | 2015-12-04 | Application of Astataricusol A in preparing of medicine for treating acute renal failure |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510897068.9A CN105497040A (en) | 2015-12-04 | 2015-12-04 | Application of Astataricusol A in preparing of medicine for treating acute renal failure |
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| Publication Number | Publication Date |
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| CN105497040A true CN105497040A (en) | 2016-04-20 |
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| CN201510897068.9A Pending CN105497040A (en) | 2015-12-04 | 2015-12-04 | Application of Astataricusol A in preparing of medicine for treating acute renal failure |
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2015
- 2015-12-04 CN CN201510897068.9A patent/CN105497040A/en active Pending
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Application publication date: 20160420 |
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| WD01 | Invention patent application deemed withdrawn after publication |