CN102872115B - Application of Houttuynoid A in preparing medicament for treating acute renal failure - Google Patents
Application of Houttuynoid A in preparing medicament for treating acute renal failure Download PDFInfo
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- CN102872115B CN102872115B CN 201210419374 CN201210419374A CN102872115B CN 102872115 B CN102872115 B CN 102872115B CN 201210419374 CN201210419374 CN 201210419374 CN 201210419374 A CN201210419374 A CN 201210419374A CN 102872115 B CN102872115 B CN 102872115B
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Abstract
The invention relates to the new medical use of Houttuynoid A, namely application of Houttuynoid A in preparing a medicament for treating acute renal failure. The use of Houttuynoid A in preparing the medicament for treating the acute renal failure involved in the invention is disclosed for the first time; as the framework type of Houttuynoid A is a brand new framework type and Houttuynoid A has an unexpectedly high inhibition activity for the acute renal failure without possibility of giving any implication by other compounds, Houttuynoid A has outstanding substantive features; and simultaneously, the application of Houttuynoid A for preventing acute renal failure apparently has obvious progress.
Description
Technical field
The present invention relates to the pharmaceutical chemistry field.Particularly, the present invention relates to the novel medical use of Houttuynoid A, i.e. the application of Houttuynoid 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), in body, nitrogen matter metabolite is discharged and is produced obstacle, 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 sharply minimizing of renal blood flow, and the oxidative stress and the cell injury that cause due to the nephridial tissue ischemia, 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 Renal tissues damage improving the kidney perfusion obstacle and alleviate.
the compound H outtuynoid A that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid A_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S. D. et al., 2012. Houttuynoid A_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), belong to open first for the purposes of the Houttuynoid 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 compounds, possesses 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 Houttuynoid 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.
Houttuynoid A of the present invention has obvious therapeutical effect to the acute renal failure disease.
Research by us is found, the anuria when Houttuynoid A can improve acute renal failure or oliguria symptom, the function of protection kidney.
Described compound H outtuynoid A structure is as shown in formula I:
Formula I
The purposes of the Houttuynoid 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 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 compound H outtuynoid A involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid A_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.).
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 compound H outtuynoid A tablet involved in the present invention:
Get 20 and digest compound Houttuynoid A, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid A capsule involved in the present invention:
Get 20 and digest compound Houttuynoid A, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The therapeutical effect of experimental example 1 Houttuynoid A to the 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); Houttuynoid A I group (0.3 mg/Kg)); Houttuynoid A II group (0.6 mg/Kg)); Houttuynoid A III group (1.2 mg/Kg)), each organizes rat tail vein injection saline or Houttuynoid 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 after Houttuynoid A or normal saline, stay rear 6 hours of urine with 4% chloral hydrate intraperitoneal injection of anesthesia, reach the rear bilateral renal blood flow for the treatment of after adopting laser Doppler flowmetry to measure modeling, average as single animal renal blood flow; Get blood and prepare serum, measure blood BUN and Cre; Get kidney, preparation 10% renal cortex homogenate is measured renal cortex homogenate MDA, GSH, NO(all by the operation of test kit description).
(3) experimental result
1. Houttuynoid A can increase acute renal failure Mouse Kidney blood flow
The impact of table 1 Houttuynoid A on acute renal failure Mouse Kidney blood flow
* P＜0.05vs acute renal failure model group
2. Houttuynoid 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 Houttuynoid 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 Houttuynoid 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 Houttuynoid A energy dose dependent ground improves the renal function (P＜0.05) of acute renal failure rat.See Table 2.
Each rats in test groups renal function index of table 2 relatively
* P＜0.05vs acute renal failure model group
Conclusion: the anuria when Houttuynoid 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.Houttuynoid the application of A in preparation treatment acute renal failure medicine, described compound H outtuynoid A structure as
Formula IShown in:
Formula I.
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| CN102872115B true CN102872115B (en) | 2013-05-15 |
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| CN102861008A (en) * | 2012-10-25 | 2013-01-09 | 南京大学 | Application of Aphanamixoid A in medicine for treating acute renal failure |
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Non-Patent Citations (2)
| Title |
|---|
| Chen, Shao-Dan等.Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.《Organic Letters》.2012,第14卷(第7期),1772-1775. |
| Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata;Chen, Shao-Dan等;《Organic Letters》;20120313;第14卷(第7期);1772-1775 * |
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