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 PDFInfo
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- 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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- Prior art keywords
- renal failure
- acute renal
- kadcoccitones
- kadcoccitonesa
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- 208000033626 Renal failure acute Diseases 0.000 title claims abstract description 32
- 201000011040 acute kidney failure Diseases 0.000 title claims abstract description 32
- 208000009304 Acute Kidney Injury Diseases 0.000 title claims abstract description 31
- 208000012998 acute renal failure Diseases 0.000 title claims abstract description 31
- 239000003814 drug Substances 0.000 title claims abstract description 13
- 238000002360 preparation method Methods 0.000 title claims abstract description 12
- 229930185251 kadcoccitone Natural products 0.000 title abstract description 4
- FVIZARNDLVOMSU-UHFFFAOYSA-N ginsenoside K Natural products C1CC(C2(CCC3C(C)(C)C(O)CCC3(C)C2CC2O)C)(C)C2C1C(C)(CCC=C(C)C)OC1OC(CO)C(O)C(O)C1O FVIZARNDLVOMSU-UHFFFAOYSA-N 0.000 claims description 7
- 230000000694 effects Effects 0.000 abstract description 4
- 241000700159 Rattus Species 0.000 description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- 230000006870 function Effects 0.000 description 5
- 210000003734 kidney Anatomy 0.000 description 5
- 210000002700 urine Anatomy 0.000 description 5
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 230000003907 kidney function Effects 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 206010030302 Oliguria Diseases 0.000 description 3
- 230000006378 damage Effects 0.000 description 3
- 238000010255 intramuscular injection Methods 0.000 description 3
- 239000007927 intramuscular injection Substances 0.000 description 3
- 230000008327 renal blood flow Effects 0.000 description 3
- 201000003126 Anuria Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 210000005084 renal tissue Anatomy 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 208000010444 Acidosis Diseases 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 230000007950 acidosis Effects 0.000 description 1
- 208000026545 acidosis disease Diseases 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000002146 bilateral effect Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000005779 cell damage Effects 0.000 description 1
- 208000037887 cell injury Diseases 0.000 description 1
- RNFNDJAIBTYOQL-UHFFFAOYSA-N chloral hydrate Chemical compound OC(O)C(Cl)(Cl)Cl RNFNDJAIBTYOQL-UHFFFAOYSA-N 0.000 description 1
- 229960002327 chloral hydrate Drugs 0.000 description 1
- 208000035850 clinical syndrome Diseases 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- 238000001631 haemodialysis Methods 0.000 description 1
- 230000000322 hemodialysis Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 208000028867 ischemia Diseases 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 230000036542 oxidative stress Effects 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 201000003068 rheumatic fever Diseases 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000002636 symptomatic treatment Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
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
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)
- 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.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310498460.7A CN103520172B (en) | 2013-10-22 | 2013-10-22 | The application of Kadcoccitones A in preparation treatment acute renal failure medicine |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310498460.7A CN103520172B (en) | 2013-10-22 | 2013-10-22 | The application of Kadcoccitones A in preparation treatment acute renal failure medicine |
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| Publication Number | Publication Date |
|---|---|
| CN103520172A CN103520172A (en) | 2014-01-22 |
| CN103520172B true CN103520172B (en) | 2016-02-24 |
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| CN201310498460.7A Expired - Fee Related CN103520172B (en) | 2013-10-22 | 2013-10-22 | The application of Kadcoccitones A in preparation treatment acute renal failure medicine |
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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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2013
- 2013-10-22 CN CN201310498460.7A patent/CN103520172B/en not_active Expired - Fee Related
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 |
|---|
| 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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| Publication number | Publication date |
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| CN103520172A (en) | 2014-01-22 |
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Inventor after: Chen Yancui Inventor after: Liu Liqin Inventor after: Qi Ying Inventor after: Meng Qingxia Inventor after: Wang Jiren Inventor before: The inventor has waived the right to be mentioned |
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Effective date of registration: 20160125 Address after: 271100 Laicheng District People's Hospital, 79 West Street, Laicheng District, Shandong, Laiwu, Fengcheng Applicant after: Chen Yancui Address before: 211200, No. 1, industrial town, crystal Town, Lishui District, Jiangsu, Nanjing Applicant before: Sun Aihua |
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