CN103330704A - Application of Aphanamgrandiol A in preparation of drugs treating renal insufficiency - Google Patents
Application of Aphanamgrandiol A in preparation of drugs treating renal insufficiency Download PDFInfo
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- CN103330704A CN103330704A CN2013102805443A CN201310280544A CN103330704A CN 103330704 A CN103330704 A CN 103330704A CN 2013102805443 A CN2013102805443 A CN 2013102805443A CN 201310280544 A CN201310280544 A CN 201310280544A CN 103330704 A CN103330704 A CN 103330704A
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- aphanamgrandiol
- renal insufficiency
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- treating renal
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- HHBRPINXMMKYCM-SRBOSORUSA-N NCC(C1)[C@@H]1N=O Chemical compound NCC(C1)[C@@H]1N=O HHBRPINXMMKYCM-SRBOSORUSA-N 0.000 description 1
Abstract
Belonging to the technical field of new drug uses, the invention discloses application of Aphanamgrandiol A in drugs preventing and/or treating renal insufficiency. The uses of the Aphanamgrandiol A in preparation of drugs preventing and treating renal insufficiency are disclosed for the first time. As its skeleton belongs to a brand new skeleton type and the Aphanamgrandiol A has unexpected strong inhibitory activity on renal insufficiency, there exists no possibility that any enlightenment can be provided by other compounds. With outstanding substantive features, the Aphanamgrandiol A obviously has significant progress in prevention and treatment of renal insufficiency at the same time.
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 renal insufficiency medicine.
Background technology
Chronic renal disease (comprising each chronic nephritis, diabetic nephropathy and hypertensive cerebral renal damage etc.) is a kind of the most common chronic refractory disease.The nephridial tissue pathological changes all can from early lesion make progress gradually between glomerular sclerosis and/or kidney Fibrotic late period pathological changes.If can not get effective treatment, cause chronic renal insufficiency and irreversible end stage renal failure (being uremia) at last.If be used for the treatment of drug main Benazepril and the Losartan of renal insufficiency at present clinically, but main dependence on import, this class drug price costliness, toxic and side effects is bigger.As cause part patient hyperkalemia, unsurmountable cough, hypotensive activity strong etc. inadequately.
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 renal insufficiency medicine belongs to open first.
Summary of the invention
The present invention shows by pharmacological evaluation, causes after the chmice acute injury of kidney 3 days with cisplatin, and model group serum creatinine, blood urea nitrogen significantly raise.Aphanamgrandiol A1.25mg/kg dosage group can reduce serum creatinine, urea level, and its action intensity is suitable with positive drug Benazepril10mg/kg dosage group.
After the modeling group 5 days, model group serum creatinine, blood urea nitrogen still kept higher level.Aphanamgrandiol A1.25mg/kg dosage group can reduce serum creatinine, obviously is better than positive drug Benazepril10mg/kg dosage group.Aphanamgrandiol A0.625mg/kg dosage group reduces the blood urea nitrogen level, and is suitable with the effect of positive drug Benazepril5mg/kg dosage group.
Behind the modeling type 7 days, model group and administration group serum creatinine level were recovered normal (Benazepril10mg/kg dosage group serum creatinine level is lower than normal level).But model group blood urea nitrogen level still is significantly higher than negative control group, and Aphanamgrandiol A0.625mg/kg, 1.25m/kg dosage group can reduce the blood urea nitrogen level, are better than positive drug.
Experimental result shows that the mice injury of kidney that the cisplatin of Aphanamgrandiol A causes has the certain protection effect, acts on suitable with positive control drug Benazepril.
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 preparation prevention, treatment renal insufficiency medicine belongs to open first, because framework types belongs to brand-new framework types, and it is unexpectedly strong for the renal insufficiency therapeutic activity, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for renal insufficiency simultaneously obviously has obvious improvement.Term: BUN: the difficult Cre of carbamide: creatinine
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 adding dextrin 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 and add starch 195 grams, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
1, the foundation of cisplatin induced mice acute injury of kidney model
Get male Kunming KM mice, 16～18g is divided into positive controls and cisplatin model group, administration group, totally 6 groups, 8 every group at random by body weight.Matched group intraperitoneal injection of saline, cisplatin are with physiological saline solution, and lumbar injection is pressed the 7mg/kg drug administration by injection.The compounds of this invention once a day, is administered five times altogether in injection cisplatin beginning in preceding 2 days oral administration; Positive control drug Benazepril(K), while oral administration when the injection cisplatin once a day, is administered three times altogether (in the too late administration simultaneously of effect of injection cisplatin beginning in preceding 2 days administration, too late three times of the effect that is administered five times), each administration volume is 0.4ml/20g more than.Behind the injection cisplatin the 3rd day, 5 days, 7 days respectively eyeball get blood, detect serum BUN, Cre with test kit, and weigh.
2, result of study
The protective effect of the mice injury of kidney that table 1Aphanamgrandiol A cisplatin causes (after the modeling 3 days)
* compare with model group P＜0.05
The protective effect of the mice injury of kidney that table 2Aphanamgrandiol A cisplatin causes (after the modeling 5 days)
* compare with model group P＜0.05
The protective effect of the mice injury of kidney that table 3Aphanamgrandiol A cisplatin causes (after the modeling 7 days)
* compare with model group P＜0.05
Above-mentioned experimental result shows, after modeling 3 days, model group serum result, blood urea nitrogen significantly raise, and Aphanamgrandiol A1.25mg/kg dosage group can reduce serum creatinine, urea nitrogen levels, and effect is suitable with the effect of positive drug Benazepril10mg/kg dosage group.
Behind the modeling type 5 days, model group serum result, blood urea nitrogen still kept higher level, and Aphanamgrandiol A1.25mg/kg dosage group can reduce serum creatinine, obviously is better than positive drug Benazepril10mg/kg dosage group.Aphanamgrandiol A0.625mg/kg dosage group can reduce urea nitrogen levels, and is suitable with the effect of positive drug Benazepril5mg/kg dosage group.After the modeling 7 days, model group and each administration group serum creatinine level are recovered normal (Benazepril10mg/kg dosage group serum creatinine level is lower than normal level), model group blood urea nitrogen level still is significantly higher than negative control group, Aphanamgrandiol A0.625mg/kg, 1.25mg/kg dosage group can reduce the blood urea nitrogen level, are better than positive drug Benazepril.
Conclusion: the mice injury of kidney that the cisplatin of Aphanamgrandiol A causes has the certain protection effect, acts on quite with positive control drug Benazepril, can be used for preparation prevention, treatment renal insufficiency medicine.
Claims (1)
1.Aphanamgrandiol the application of A in preparation treatment renal insufficiency medicine, described compd A phanamgrandiol A structure is shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102805443A CN103330704A (en) | 2013-07-05 | 2013-07-05 | Application of Aphanamgrandiol A in preparation of drugs treating renal insufficiency |
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| CN2013102805443A CN103330704A (en) | 2013-07-05 | 2013-07-05 | Application of Aphanamgrandiol A in preparation of drugs treating renal insufficiency |
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| CN103330704A true CN103330704A (en) | 2013-10-02 |
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| CN2013102805443A Pending CN103330704A (en) | 2013-07-05 | 2013-07-05 | Application of Aphanamgrandiol A in preparation of drugs treating renal insufficiency |
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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
- 2013-07-05 CN CN2013102805443A patent/CN103330704A/en active Pending
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: 20131002 |