CN103340850A - Application of Aphanamgrandiol A in preparation of drugs for treating acute renal failure - Google Patents
Application of Aphanamgrandiol A in preparation of drugs for treating acute renal failure Download PDFInfo
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- CN103340850A CN103340850A CN2013102859725A CN201310285972A CN103340850A CN 103340850 A CN103340850 A CN 103340850A CN 2013102859725 A CN2013102859725 A CN 2013102859725A CN 201310285972 A CN201310285972 A CN 201310285972A CN 103340850 A CN103340850 A CN 103340850A
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- aphanamgrandiol
- renal failure
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Abstract
The invention relates to a new medical application of Aphanamgrandiol A, namely an application of the Aphanamgrandiol A in preparation of drugs for treating acute renal failure. The application of the Aphanamgrandiol A in preparation of drugs for treating acute renal failure is disclosed for the first time, as the framework type belongs to a totally new framework type and the Aphanamgrandiol A has incredible high inhibitory activity to acute renal failure, no other compounds give any prediction, the Aphanamgrandiol A has remarkable substantive features, and simultaneously the Aphanamgrandiol A has a remarkable improvement for resisting acute renal failure.
Description
Technical field
The present invention relates to the new purposes of compd A phanamgrandiol A, relate in particular to the application of Aphanamgrandiol A in preparation treatment acute renal failure medicine.
Background technology
Acute renal failure (Acute Renal Failure, ARF) be the clinical syndrome that is caused by multiple reason, clinical manifestation is acute oliguria (urine amount＜400mLPd) or anuria (urine amount＜100mLPd), nitrogen matter metabolite is discharged and is produced obstacle in the body, occur azotemia rapidly, and cause each system's corresponding function imbalance of whole body.The principal element that causes acute renal failure is the rapid minimizing of renal blood flow, and because oxidative stress and the cell injury that the nephridial tissue ischemia causes finally causes the deterioration of renal tissue structural damage and function.Still there is not at present the effective medicine for the treatment of acute renal failure of generally acknowledging clinically, only can be by correcting water-electrolyte balance, symptomatic treatment measures such as correction acidosis improve symptom, and the later stage also needs to keep the body function by hemodialysis.There is the clinical medicine of obvious curative effects rare aspect the nephridial tissue damage improving renal blood flow perfusion obstacle and alleviate.
The compd A phanamgrandiol A that the present invention relates to is one and delivered (Qi Zeng in 2013, Bin Guan, Jie Ren, et al.Aphanamgrandiol A, a new triterpenoid with a unique carbon skeleton from Aphanamixis grandifolia.Fitoterapia, 86 (2013) 217 – 221.) noval chemical compound, this chemical compound has brand-new framework types, present purposes only relates to inhibition gastric cancer, ovarian cancer, colon cancer, the increment of liver epithelial cancerous cell (Qi Zeng, Bin Guan, Jie Ren, et al.Aphanamgrandiol A, a new triterpenoid with a unique carbon skeleton from Aphanamixis grandifolia.Fitoterapia, 86 (2013) 217 – 221.), the purposes of the Aphanamgrandiol A that the present invention relates in preparation treatment acute renal failure medicine belongs to open first.
Summary of the invention
The objective of the invention is to provides the application of Aphanamgrandiol A in the anti-acute renal failure medicine of preparation according to not finding that it has the present situation of the report of anti-acute renal failure activity in the existing Aphanamgrandiol A research.
By our discovering, the anuria when Aphanamgrandiol A can improve acute renal failure or oliguria symptom, the function of protection kidney.
Described compd A phanamgrandiol A, structure is shown in formula I:
Formula I
The purposes of the Aphanamgrandiol A that the present invention relates in the anti-acute renal failure medicine of preparation belongs to open first, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for acute renal failure, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for anti-acute renal failure simultaneously and obviously have obvious improvement.
The specific embodiment
The preparation method of compd A phanamgrandiol A involved in the present invention is referring to document (Qi Zeng, Bin Guan, Jie Ren, et al.Aphanamgrandiol A, a new triterpenoid with a unique carbon skeleton from Aphanamixis grandifolia.Fitoterapia, 86 (2013) 217 – 221.)
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 phanamgrandiol A tablet involved in the present invention:
Get 5 and digest compound Aphanamgrandiol A, add dextrin material 195 grams, mixing, conventional tabletting are made 1000.
Embodiment 2: the preparation of compd A phanamgrandiol A capsule involved in the present invention:
Get 5 and digest compound Aphanamgrandiol A, add starch 195 grams, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
The therapeutical effect of the acute renal failure rat of experimental example 1Aphanamgrandiol A
(1) experimental technique
Adopt intramuscular injection glycerol to cause the acute renal failure rat animal model.Select 60 of the healthy male SD rats of 180～220g for use, be divided into 5 groups at random: sham operated rats (intramuscular injection normal saline); Model group (intramuscular injection glycerol); Aphanamgrandiol A I group (0.3mg/Kg)); Aphanamgrandiol A II group (0.6mg/Kg)); Aphanamgrandiol A III group (1.2mg/Kg)), each organizes rat tail vein injection saline or Aphanamgrandiol A immediately after the glycerol modeling, is administered once after 12 and 24 hours again.
(2) observation index
60 rat lasts give to put into metabolic cage collection twenty-four-hour urine behind Aphanamgrandiol A or the normal saline, stay back 6 hours of urine with 4% chloral hydrate intraperitoneal injection of anesthesia, adopt laser Doppler flowmetry to measure after the modeling and treatment back bilateral renal blood flow amount, 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.Aphanamgrandiol A can increase acute renal failure mice renal blood flow
The influence of the acute renal failure mice of table 1Aphanamgrandiol A renal blood flow
* P＜0.05 contrasts with the acute renal failure model group
2.Aphanamgrandiol the acute renal failure mice of A renal function tool protective effect
The model group rat significantly reduces than sham operated rats rat twenty-four-hour urine amount, is respectively 4.86 ± 0.26ml and 11.43 ± 2.53ml; Middle and high dosage Aphanamgrandiol A group twenty-four-hour urine amount is significantly higher than model group (P＜0.05), and the urine measurer of three medication therapy groups has dose dependent, is respectively I group 5.16 ± 0.65ml, II group 7.93 ± 1.43ml, III group 9.86 ± 1.39ml.Illustrate that Aphanamgrandiol A 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 28.73 ± 1.62mmol/L, and Cre is 171.63 ± 14.37umol/L, apparently higher than sham operated rats, illustrates that model group animal renal function injury is serious.Middle and high dosage Aphanamgrandiol A can improve the renal function (P＜0.05) of acute renal failure rat in dose dependent ground.See Table 2.
Each rats in test groups renal function index of table 2 relatively
* P＜0.05 contrasts with the acute renal failure model group
Conclusion: the anuria when Aphanamgrandiol A can improve acute renal failure or oliguria symptom, the function of protection kidney can be used for preparing anti-acute renal failure medicine.
Claims (1)
1.Aphanamgrandiol the application of A in preparation treatment acute renal failure medicine, described compd A phanamgrandiol A structure is shown in formula I:
Formula I.
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101965184A (en) * | 2008-01-11 | 2011-02-02 | 里亚塔医药公司 | Synthetic triterpenoid compound and method in order to cure the disease |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101965184A (en) * | 2008-01-11 | 2011-02-02 | 里亚塔医药公司 | Synthetic triterpenoid compound and method in order to cure the disease |
Non-Patent Citations (1)
| Title |
|---|
| QI ZENG ET AL.: "Aphanamgrandiol A, a new triterpenoid with a unique carbon skeleton from Aphanamixis grandifolia", 《FITOTERAPIA》 * |
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Application publication date: 20131009 |