CN102861008A - Application of Aphanamixoid A in medicine for treating acute renal failure - Google Patents

Application of Aphanamixoid A in medicine for treating acute renal failure Download PDF

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Publication number
CN102861008A
CN102861008A CN2012104143823A CN201210414382A CN102861008A CN 102861008 A CN102861008 A CN 102861008A CN 2012104143823 A CN2012104143823 A CN 2012104143823A CN 201210414382 A CN201210414382 A CN 201210414382A CN 102861008 A CN102861008 A CN 102861008A
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aphanamixoid
renal failure
acute renal
medicine
application
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冯怡
龚霞
吴俊华
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Nanjing University
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Nanjing University
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Abstract

The invention relates to novel medicinal application of Aphanamixoid A, namely application of Aphanamixoid A in preparing a medicine for treating acute renal failure. The application of Aphanamixoid A in preparing the medicine for treating acute renal failure, which is provided by the invention, is disclosed for the first time. The skeleton type belongs to brand-new skeleton type, and the acute renal failure preventing activity of Aphanamixoid A is extremely strong, so that no possibility for providing any prompt by other compounds exists. Aphanamixoid A has outstanding actual characteristics. Meanwhile, Aphanamixoid A has outstanding progress when being used for preventing acute renal failure.

Description

The application of Aphanamixoid A in treatment acute renal failure medicine
Technical field
The present invention relates to the pharmaceutical chemistry field.Particularly, the present invention relates to the novel medical use of Aphanamixoid A, i.e. the application of Aphanamixoid 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 many reasons, be found in the clinical departments patient, sickness rate is high and often have serious consequences, (a few hours are to a couple of days) siddhi can sharply descend its characteristics in a short time, 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, azotemia appears rapidly, water and electrolyte, acid base imbalance, 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.There is no clinically at present the generally acknowledged effective medicine for the treatment of acute renal failure, only can be by correcting water-electrolyte balance, the 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 Renal tissues damage improving the kidney perfusion obstacle and alleviate.
The compd A phanamixoid A that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to insect antifeedant activity (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Aphanamixoid A that the present invention relates in the anti-acute renal failure medicine of preparation, 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 simultaneously anti-acute renal failure and obviously have significant progress.
Summary of the invention
The purpose of this invention is to provide the purposes that Aphanamixoid A is used for the treatment of acute renal failure, namely for the preparation of the purposes for the treatment of the acute renal failure medicine.
Aphanamixoid A of the present invention has obvious therapeutical effect to the acute renal failure disease.
Research by us is found, the anuria when Aphanamixoid A can improve acute renal failure or oliguria symptom, the function of protection kidney.
Described compd A phanamixoid A structure is shown in formula I:
Figure BDA0000230861761
  
The purposes of the Aphanamixoid 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 simultaneously anti-acute renal failure and obviously have significant progress.
The specific embodiment
The preparation method of compd A phanamixoid A involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 phanamixoid A tablet involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A phanamixoid A capsule involved in the present invention:
Get 20 and digest compound Aphanamixoid 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 Aphanamixoid A is to the therapeutical effect of acute renal failure rat
(1) experimental technique
Adopt intramuscular injection glycerol to cause the Acute Renal Failure Rats animal model.Select 60 of the healthy male SD rats of 180 ~ 220g, be divided at random 5 groups: sham operated rats (intramuscular injection normal saline); Model group (intramuscular injection glycerol); Aphanamixoid A I group (0.3 mg/Kg); Aphanamixoid A II group (0.6 mg/Kg); Aphanamixoid A III group (1.2 mg/Kg), each organizes rat immediately tail vein injection saline or Aphanamixoid A 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 Aphanamixoid A or the normal saline, stay rear 6 hours of urine with 4% chloral hydrate intraperitoneal injection of anesthesia, adopt laser Doppler flowmetry to measure after the modeling and the rear bilateral renal blood flow for the treatment of, 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. Aphanamixoid A can increase acute renal failure Mouse Kidney blood flow
Table 1 Aphanamixoid A is on the impact of acute renal failure Mouse Kidney blood flow
Figure BDA0000230861762
* P<0.05vs acute renal failure model group
2. Aphanamixoid A is to the protective effect of acute renal failure Mouse Kidney function tool
The model group rat significantly reduces than rats in sham-operated group twenty-four-hour urine amount, is respectively 4.57 ± 0.74ml and 11.82 ± 2.36ml; Middle and high dosage Aphanamixoid 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 5.48 ± 0.87ml, II group 7.82 ± 1.32ml, III group 9.68 ± 1.50ml.Illustrate that Aphanamixoid 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 25.53 ± 1.62mmol/L, and Cre is 168.56 ± 13.01umol/L, apparently higher than sham operated rats, illustrates that model group animal renal function injury is serious.Middle and high dosage Aphanamixoid 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
Figure BDA0000230861763
* P<0.05vs acute renal failure model group
Conclusion: the anuria when Aphanamixoid 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.Aphanamixoid the application of A in treatment acute renal failure medicine, described compd A phanamixoid A structure is shown in formula I:
Formula I.
CN2012104143823A 2012-10-25 2012-10-25 Application of Aphanamixoid A in medicine for treating acute renal failure Withdrawn CN102861008A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104784176A (en) * 2015-05-12 2015-07-22 南京大学 Application of derivative of Daphmalenine A in preparation of acute renal failure resisting drugs

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102872115A (en) * 2012-10-27 2013-01-16 吴俊华 Application of Houttuynoid A in medicament for treating acute renal failure

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102872115A (en) * 2012-10-27 2013-01-16 吴俊华 Application of Houttuynoid A in medicament for treating acute renal failure

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JIE-YUN CAI ETAL: "Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya", 《ORGANIC LETTERS》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104784176A (en) * 2015-05-12 2015-07-22 南京大学 Application of derivative of Daphmalenine A in preparation of acute renal failure resisting drugs

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Application publication date: 20130109