CN103520172B - The application of Kadcoccitones A in preparation treatment acute renal failure medicine - Google Patents

The application of Kadcoccitones A in preparation treatment acute renal failure medicine Download PDF

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Publication number
CN103520172B
CN103520172B CN201310498460.7A CN201310498460A CN103520172B CN 103520172 B CN103520172 B CN 103520172B CN 201310498460 A CN201310498460 A CN 201310498460A CN 103520172 B CN103520172 B CN 103520172B
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China
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renal failure
acute renal
kadcoccitones
kadcoccitonesa
application
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CN201310498460.7A
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CN103520172A (en
Inventor
陈延翠
刘丽芹
亓颖
孟庆霞
王继仁
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Chen Yancui
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Abstract

Do you the present invention relates to Kadcoccitones? the novel medical use of A, i.e. Kadcoccitones? the application of A in preparation treatment acute renal failure medicine, purposes 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 strong for acute renal failure inhibit activities, possess outstanding substantive distinguishing features, for anti-acute renal failure, obviously there is significant progress simultaneously.

Description

The application of Kadcoccitones A in preparation treatment acute renal failure medicine
Technical field
The present invention relates to the novelty teabag of compound K adcoccitonesA, particularly relate to the application of KadcoccitonesA in preparation treatment acute renal failure medicine.
Background technology
Acute renal failure (AcuteRenalFailure, ARF) is the clinical syndrome caused by many reasons, is found in clinical departments patient, and sickness rate is high and often have serious consequences, and causes 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 compound K adcoccitonesA that the present invention relates to is one and delivers (Cheng-QinLiang in 2012, etal., KadcoccitonesAandB, TwoNew6/6/5/5-FusedTetracyclicTriterpenoidsfromKadsuraco ccinea.OrganicLetters, 2012, 14 (24): 6362 – 6365.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to inhibiting HIV, invalid to kinds of tumors, (Cheng-QinLiang, etal., KadcoccitonesAandB, TwoNew6/6/5/5-FusedTetracyclicTriterpenoidsfromKadsuraco ccinea.OrganicLetters, 2012, 14 (24): 6362 – 6365.), the purposes of the KadcoccitonesA that the present invention relates in preparation treatment acute renal failure medicine belongs to first public.
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 KadcoccitonesA research, provide the application of KadcoccitonesA in the anti-acute renal failure medicine of preparation.
Found by our research, anuria when KadcoccitonesA can improve acute renal failure or oliguria symptom, the function of protection kidney.
Described compound K adcoccitonesA, structure is as shown in formula I:
The purposes of the KadcoccitonesA 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 strong for acute renal failure inhibit activities, 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 compound K adcoccitonesA involved in the present invention is see document (Cheng-QinLiang, etal., KadcoccitonesAandB, TwoNew6/6/5/5-FusedTetracyclicTriterpenoidsfromKadsuraco ccinea.OrganicLetters, 2012,14 (24): 6362 – 6365.)
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 compound K adcoccitonesA tablet involved in the present invention:
Get 5 g of compound KadcoccitonesA, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound K adcoccitonesA capsule involved in the present invention:
Get 5 g of compound KadcoccitonesA, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1:KadcoccitonesA 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, Nanjing Medical University's Experimental Animal Center, is divided into 5 groups at random: sham operated rats (intramuscular injection normal saline); Model group (intramuscular injection glycerol); KadcoccitonesA I group (0.3mg/Kg)); KadcoccitonesA II group (0.6mg/Kg)); KadcoccitonesA III group (1.2mg/Kg)), each group rat tail vein injection saline or KadcoccitonesA 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 KadcoccitonesA 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(all by the operation of test kit description).
(3) experimental result
1.KadcoccitonesA can increase acute renal failure Mouse Kidney blood flow
Table 1KadcoccitonesA is on the impact of acute renal failure Mouse Kidney blood flow
* P<0.05 and acute renal failure model group contrast
2.KadcoccitonesA 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 4.98 ± 0.61ml and 12.74 ± 2.48ml; Middle and high dosage KadcoccitonesA 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 6.25 ± 0.72ml, II group of 7.78 ± 1.34ml, III group of 9.79 ± 1.23ml.Illustrate that KadcoccitonesA 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 28.55 ± 1.92mmol/L, Cre is 169.51 ± 17.51umol/L, apparently higher than sham operated rats, illustrates that model group animal renal function injury is serious.Middle and high dosage KadcoccitonesA 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: KadcoccitonesA 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. The application of 1.KadcoccitonesA in preparation treatment acute renal failure medicine, described compound K adcoccitonesA structure is as shown in formula I:
    Formula I.
CN201310498460.7A 2013-10-22 2013-10-22 The application of Kadcoccitones A in preparation treatment acute renal failure medicine Expired - Fee Related CN103520172B (en)

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Citations (1)

* Cited by examiner, † Cited by third party
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Title
Kadcoccitones A and B, Two New6/6/5/5-Fused Tetracyclic Triterpenoids;Cheng-Qin Liang,et al;《Organic Letters》;20121211;第14卷(第24期);第6362-6365页 *

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