CN103705500A - Applications of Myrtucommuacetalone in medicines treating renal insufficiency - Google Patents
Applications of Myrtucommuacetalone in medicines treating renal insufficiency Download PDFInfo
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- CN103705500A CN103705500A CN201310642417.3A CN201310642417A CN103705500A CN 103705500 A CN103705500 A CN 103705500A CN 201310642417 A CN201310642417 A CN 201310642417A CN 103705500 A CN103705500 A CN 103705500A
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- myrtucommuacetalone
- renal insufficiency
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- medicines
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- 239000003814 drug Substances 0.000 title claims abstract description 19
- 208000001647 Renal Insufficiency Diseases 0.000 title claims abstract description 13
- 201000006370 kidney failure Diseases 0.000 title claims abstract description 13
- 229940079593 drug Drugs 0.000 title abstract description 13
- 150000001875 compounds Chemical class 0.000 claims description 13
- 230000000694 effects Effects 0.000 abstract description 7
- 230000005764 inhibitory process Effects 0.000 abstract 1
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 16
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 11
- 229960004316 cisplatin Drugs 0.000 description 11
- 210000002966 serum Anatomy 0.000 description 9
- 229940109239 creatinine Drugs 0.000 description 8
- PNNCWTXUWKENPE-UHFFFAOYSA-N [N].NC(N)=O Chemical compound [N].NC(N)=O PNNCWTXUWKENPE-UHFFFAOYSA-N 0.000 description 7
- 210000004369 blood Anatomy 0.000 description 7
- 239000008280 blood Substances 0.000 description 7
- 238000002360 preparation method Methods 0.000 description 7
- 239000007924 injection Substances 0.000 description 6
- 238000002347 injection Methods 0.000 description 6
- 210000003734 kidney Anatomy 0.000 description 6
- XPCFTKFZXHTYIP-PMACEKPBSA-N Benazepril Chemical compound C([C@@H](C(=O)OCC)N[C@@H]1C(N(CC(O)=O)C2=CC=CC=C2CC1)=O)CC1=CC=CC=C1 XPCFTKFZXHTYIP-PMACEKPBSA-N 0.000 description 5
- 229960004530 benazepril Drugs 0.000 description 5
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 4
- 230000006378 damage Effects 0.000 description 4
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 240000005125 Myrtus communis Species 0.000 description 3
- 235000013418 Myrtus communis Nutrition 0.000 description 3
- 230000006052 T cell proliferation Effects 0.000 description 3
- 208000020832 chronic kidney disease Diseases 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- 239000013641 positive control Substances 0.000 description 3
- 230000001681 protective effect Effects 0.000 description 3
- 230000009692 acute damage Effects 0.000 description 2
- 239000004202 carbamide Substances 0.000 description 2
- 235000013877 carbamide Nutrition 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 231100000915 pathological change Toxicity 0.000 description 2
- 230000036285 pathological change Effects 0.000 description 2
- 208000009304 Acute Kidney Injury Diseases 0.000 description 1
- 208000037157 Azotemia Diseases 0.000 description 1
- 239000002083 C09CA01 - Losartan Substances 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 1
- 206010018367 Glomerulonephritis chronic Diseases 0.000 description 1
- 208000002682 Hyperkalemia Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 238000012449 Kunming mouse Methods 0.000 description 1
- 206010027336 Menstruation delayed Diseases 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 210000005252 bulbus oculi Anatomy 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 208000033679 diabetic kidney disease Diseases 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 208000028208 end stage renal disease Diseases 0.000 description 1
- 201000000523 end stage renal failure Diseases 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000003176 fibrotic effect Effects 0.000 description 1
- 206010061989 glomerulosclerosis Diseases 0.000 description 1
- 230000001631 hypertensive effect Effects 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 230000008676 import Effects 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 230000002427 irreversible effect Effects 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- KJJZZJSZUJXYEA-UHFFFAOYSA-N losartan Chemical compound CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C=2[N]N=NN=2)C=C1 KJJZZJSZUJXYEA-UHFFFAOYSA-N 0.000 description 1
- 229960004773 losartan Drugs 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 239000013642 negative control Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 208000037922 refractory disease Diseases 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 208000009852 uremia Diseases 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses applications of Myrtucommuacetalone in medicines preventing and/or treating renal insufficiency, belongs to the technical field of new applications of medicines, and is disclosed for the first time. The skeleton type belongs to a brand new skeleton type. Myrtucommuacetalone has strong inhibition activity to renal insufficiency, has outstanding substantive features and has substantial progress in controlling renal insufficiency obviously.
Description
Technical field
The present invention relates to the new purposes of compound Myrtucommuacetalone, relate in particular to the application of Myrtucommuacetalone 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.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 at last chronic renal insufficiency and irreversible end stage renal failure (being uremia).If be used for the treatment of clinically drug main Benazepril and the Losartan of renal insufficiency at present, but main dependence on import, this class drug price is expensive, and toxic and side effects is larger.As cause part patient hyperkalemia, unsurmountable cough, hypotensive activity strong not etc.
The compound Myrtucommuacetalone the present invention relates to is one and within 2013, delivers (M.Iqbal Choudhary, et al., New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis.Organic Letters, 2013, 15 (8): 862 – 1865.) noval chemical compound, this compound has brand-new framework types, current purposes finds that it can suppress NO and discharge (M.Iqbal Choudhary, et al., New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis.Organic Letters, 2013, 15 (8): 862 – 1865.), the purposes of the Myrtucommuacetalone 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, and with after induced by Cisplatin acute injury of kidney 3 days, model group serum creatinine, blood urea nitrogen significantly raise.Myrtucommuacetalone1.25mg/kg dosage group can reduce serum creatinine, urea level, and its action intensity is suitable with positive drug Benazepril10mg/kg dosage group.
After modeling group 5 days, model group serum creatinine, blood urea nitrogen still kept higher level.Myrtucommuacetalone1.25mg/kg dosage group can reduce serum creatinine, is obviously better than positive drug Benazepril10mg/kg dosage group.Myrtucommuacetalone0.625mg/kg dosage group reduces blood urea nitrogen level, suitable with the effect of positive drug Benazepril5mg/kg dosage group.
After 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 is still significantly higher than negative control group, Myrtucommuacetalone0.625mg/kg, 1.25m/kg dosage group can reduce blood urea nitrogen level, are better than positive drug.
Experimental result shows, the Mouse Kidney damage that Myrtucommuacetalone causes cisplatin has certain protective effect, acts on suitable with positive control drug Benazepril.
Described compound Myrtucommuacetalone structure is as shown in formula I:
The purposes of the Myrtucommuacetalone 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 strong for renal insufficiency therapeutic activity, possess outstanding substantive distinguishing features, the control for renal insufficiency simultaneously obviously has significant progress.
Term: BUN: carbamide is difficult
Cre: creatinine
The specific embodiment
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
The preparation method of compound Myrtucommuacetalone involved in the present invention is referring to document (M.Iqbal Choudhary, et al., New Inhibitors of ROS Generation and T-Cell Proliferation from Myrtus communis.Organic Letters, 2013,15 (8): 862 – 1865.), prepare according to the method described above compound Myrtucommuacetalone.
Embodiment 1: the preparation of compound Myrtucommuacetalone tablet involved in the present invention:
Get 5 and digest compound Myrtucommuacetalone and add 195 grams, dextrin, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound Myrtucommuacetalone capsule involved in the present invention:
Get 5 and digest compound Myrtucommuacetalone and add 195 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
The impact research of experimental example 1:Myrtucommuacetalone on acute renal injury in mice model
1, the foundation of cisplatin induced mice acute injury of kidney model: get male Kunming KM mice, 16～18g, is divided into solvent control group and cisplatin model group, administration group, totally 6 groups, 8 every group at random by body weight.Matched group intraperitoneal injection of saline, cisplatin is with physiological saline solution, and lumbar injection, by 7mg/kg drug administration by injection.The compounds of this invention starts oral administration in first 2 days in injection cisplatin, once a day, is administered five times altogether; Positive control drug benazepril Benazepril(K), while oral administration when injection cisplatin, once a day, being administered three times altogether, (effect that starts administration for first 2 days at injection cisplatin is not as good as administration simultaneously, the effect being administered five times is not as good as three times), above each administration volume is 0.4ml/20g.After injection cisplatin, the 3rd day eyeball got blood, detects serum BUN, Cre, and weigh with test kit.
2, result of study
The protective effect of the Mouse Kidney damage that table 1Myrtucommuacetalone causes cisplatin (after modeling 3 days)
* P<0.05, with model group comparison
Above-mentioned experimental result shows, after modeling 3 days, model group serum result, blood urea nitrogen significantly raise, and Myrtucommuacetalone1.25mg/kg dosage group can reduce serum creatinine, urea nitrogen levels, and effect is suitable with the effect of positive drug Benazepril10mg/kg dosage group.
The damage of Mouse Kidney that conclusion: Myrtucommuacetalone causes cisplatin has certain protective effect, act on quite with positive control drug Benazepril, can be used for preparation to prevent, treat renal insufficiency medicine.
Claims (1)
- The application of 1.Myrtucommuacetalone in treatment renal insufficiency medicine, described compound Myrtucommuacetalone structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310642417.3A CN103705500B (en) | 2013-12-04 | 2013-12-04 | Myrtucommuacetalone application in treatment renal insufficiency medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310642417.3A CN103705500B (en) | 2013-12-04 | 2013-12-04 | Myrtucommuacetalone application in treatment renal insufficiency medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103705500A true CN103705500A (en) | 2014-04-09 |
| CN103705500B CN103705500B (en) | 2016-07-06 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201310642417.3A Expired - Fee Related CN103705500B (en) | 2013-12-04 | 2013-12-04 | Myrtucommuacetalone application in treatment renal insufficiency medicine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107417697A (en) * | 2016-05-23 | 2017-12-01 | 暨南大学 | A kind of phloroglucin derivative and its application in antibacterials are prepared |
-
2013
- 2013-12-04 CN CN201310642417.3A patent/CN103705500B/en not_active Expired - Fee Related
Non-Patent Citations (4)
| Title |
|---|
| M.IQBAL CHOUDHARY等: "new inhibitors of ROS generation and T-cell proliferation from Myrtus communis", 《ORGANIC LETTERS》, vol. 15, no. 8, 3 April 2013 (2013-04-03), pages 1862 - 1865 * |
| 凌关庭: "氧化.疾病.抗氧化（VI）", 《粮食与油脂》, no. 2, 31 December 2004 (2004-12-31), pages 54 - 57 * |
| 张刘峰 译: "氧化应激与肾功能不全：机制、临床预后和治疗", 《中华高血压杂志》, vol. 18, no. 4, 30 April 2010 (2010-04-30), pages 395 - 396 * |
| 张刘锋 译: "氧化应激与肾功能不全：机制、临床预后和治疗", 《中华高血压杂志》, vol. 18, no. 3, 31 March 2010 (2010-03-31), pages 296 - 297 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107417697A (en) * | 2016-05-23 | 2017-12-01 | 暨南大学 | A kind of phloroglucin derivative and its application in antibacterials are prepared |
| CN107417697B (en) * | 2016-05-23 | 2019-07-19 | 暨南大学 | A kind of phloroglucin derivative and its application in preparation antibacterials |
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| Publication number | Publication date |
|---|---|
| CN103705500B (en) | 2016-07-06 |
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Legal Events
| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Zhao Nana Inventor after: Liu Fujun Inventor after: Sui Meixiang Inventor after: Li Zhongcheng Inventor before: Chen Jun |
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| COR | Change of bibliographic data | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20160602 Address after: 266109 10-4-101, 480 Hua Cheng Road, Chengyang District, Shandong, Qingdao Applicant after: Li Zhongcheng Address before: 213000 West -256-1, building 4, West Taihu international wisdom garden, Wujin Economic Development Zone, Jiangsu, Changzhou Applicant before: CHANGZHOU KELIXIN MEDICAL DEVICES Co.,Ltd. |
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| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
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| TR01 | Transfer of patent right |
Effective date of registration: 20201029 Address after: No.369, Changjiang street, juancheng County, No. 26, sunbin North Road, juancheng County, Heze City, Shandong Province Patentee after: JUANCHENG PEOPLE'S Hospital Address before: 266109 10-4-101, 480 Hua Cheng Road, Chengyang District, Shandong, Qingdao Patentee before: Li Zhongcheng |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20160706 Termination date: 20211204 |