CN103462992B - Application of Aphanamgrandiol A in preparation of medicaments for treating and preventing renal fibrosis - Google Patents
Application of Aphanamgrandiol A in preparation of medicaments for treating and preventing renal fibrosis Download PDFInfo
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- CN103462992B CN103462992B CN201310405546.0A CN201310405546A CN103462992B CN 103462992 B CN103462992 B CN 103462992B CN 201310405546 A CN201310405546 A CN 201310405546A CN 103462992 B CN103462992 B CN 103462992B
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- aphanamgrandiol
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Abstract
The invention provides application of Aphanamgrandiol A in preparation of medicaments for treating or preventing renal fibrosis, and belongs to the technical field of new application of the medicaments. Aphanamgrandiol A has high activity. The application of Aphanamgrandiol A in the preparation of the medicaments for treating or preventing the renal bifrosis is disclosed for the first time, has prominent substantive features, and has significant progress.
Description
Technical field
The present invention relates to the novelty teabag of compd A phanamgrandiol A, particularly relate to the application of Aphanamgrandiol A in preparation treatment and preventing renal fibrosis medicine.
Background technology
Renal fibrosis (comprising kidney region fibrosis and glomerular sclerosis) is the main pathological basis of the kidney damage final stage that a variety of causes causes, renal fibrosis mechanism is comparatively complicated, relevant with many factors, the wherein main and celliferous propagation of extracellular matrix-cell and activation, the conversion of vaso-active substance, cytokine and extracellular matrix is unbalance relevant, and kidney region fibrosis is almost so former or secondary kidney disease proceed to the common pathway of end stage renal failure.
The compd A phanamgrandiol A that the present invention relates to is one and delivers (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 compound has brand-new framework types, current purposes only relates to suppression gastric cancer, ovarian cancer, colon cancer, increment (the Qi Zeng of liver epithelial cancerous cell, 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 and preventing renal fibrosis medicine belongs to first public, belong to brand-new structure type.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report for the treatment of and preventing renal fibrosis activity according in existing Aphanamgrandiol A research, provide the application of Aphanamgrandiol A in preparation treatment and preventing renal fibrosis medicine.
Described compd A phanamgrandiol A structure is as shown in formula I:
The purposes of the Aphanamgrandiol A that the present invention relates in preparation treatment or preventing renal fibrosis medicine belongs to first public, because framework types belongs to brand-new framework types, and it is unexpectedly strong for renal fibrosis inhibit activities, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for renal fibrosis obviously has significant progress.
Detailed description of the invention
The preparation method of compd A phanamgrandiol A involved in the present invention is see 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 by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compd A phanamgrandiol A tablet involved in the present invention:
Get 5 g of compound Aphanamgrandiol A and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compd A phanamgrandiol A capsule involved in the present invention:
Get 5 g of compound Aphanamgrandiol A and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Aphanamgrandiol A is on the impact of Rats Undergoing Unilateral Urethral Ligation kidney region fibrosis
1.1 material benazeprils, Novartis Pharma AG produces; Hydroxyproline (HYP) test kit, biotech firm is built up in Nanjing; Fibronectin (FN) test kit is purchased from Shanghai institute of Biological Products.Laboratory animal: regular grade Wistar rat, male, body weight 150-200g, SD rat, Nanjing Medical University's Experimental Animal Center.
1.2 test methods and result
Rat 90, random point 9 groups, i.e. sham operated rats, model group, benazepril gavage 10mg/kg group, Aphanamgrandiol A intravenous injection 2.5mg/kg group, Aphanamgrandiol A intravenous injection 5mg/kg group, Aphanamgrandiol A intravenous injection 25mg/kg group, Aphanamgrandiol A gavage 5mg/kg group, Aphanamgrandiol A gavage 10mg/kg group, Aphanamgrandiol A gavage 50mg/kg group, animal feeding 1 week, each rat is with after 10% chloral hydrate 3.0mL/kg intraperitoneal injection of anesthesia, by fixing for Rat Right lateral position with on operating-table, with iodine tincture after cropping, 75% alcohol disinfecting field of operation, row left side abdomen otch, successively cut skin, muscle and each layer of stomach wall, expose and be separated left side ureter, sham operated rats only cuts abdominal cavity and free left side ureter, but not ligation and cutting off, other are group rat 4-0 silk thread ligation twice respectively, upper one ligation point is positioned at left inferior pole of kidney level, then ureter is cut off at twice ligation point, layer-by-layer suture, each treated animal is put to death after postoperative 10 days 10% chloral hydrate anesthesia, get blood, measure by Fibronectin and illustrate that mensuration illustrates fibre asphalt mixture (FN).Normal saline leaves and takes left kidney after lavation repeatedly, and nephridial tissue is fixed through the paraformaldehyde buffer of 4%.Cut appropriate nephridial tissue, illustrate by hydroxyproline kit measurement and measure hydroxyproline.
Routine pathology checks 1. perusal: sham operated rats kidney color is scarlet, shows smooth, and peplos gloss, without adhesion.Other are the increase of group Kidney Volume respectively, and color is pale, shows in graininess, similar human body branny kidney, the adhesion of a few regions kidney peplos.2. light microscopy checking: sham operated rats nephron result is clear, glomerular capsule is without expansion or cell infiltration.The large stretch of renal tubular necrosis of model control group, renal interstitial fibroblast proliferation, tubular ectasia, inside has the epithelial cell that a large amount of brown color shading material or necrosis come off, glomerule decreased number, part glomerule fibrosis and with the adhesion of bowman's capsule wall, blister cavities disappears.Administration respectively organizes pathological changes and model control group is similar, but all has morphology in various degree to improve, and especially with the heavy dose of each group of Aphanamgrandiol A gavage significantly, compares have notable difference with model control group.
Table 1Aphanamgrandiol A is on the impact of Rats Undergoing Unilateral Urethral Ligation kidney region fibrosis
* p<0.05, * * p<0.01, compared with model group
T inspection is carried out to each group of FN, HYP.The results are shown in Table 1, Aphanamgrandiol A intravenous injection 5mg/kg group, Aphanamgrandiol A intravenous injection 25mg/kg group, Aphanamgrandiol A gavage 10mg/kg group, Aphanamgrandiol A gavage 50mg/kg group reduce FN, HYPP level (comparing with model control group, P<0.05 or 0.01).
Conclusion: Aphanamgrandiol A significantly can reduce the rising of kidney region fibrosis FN, HYPP level, suppresses kidney region fibrosis, can be used for preparing anti-renal fibrosis medicine.
Claims (1)
- The application of 1.Aphanamgrandiol A in preparation treatment and preventing renal fibrosis medicine, described compd A phanamgrandiol A structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310405546.0A CN103462992B (en) | 2013-09-06 | 2013-09-06 | Application of Aphanamgrandiol A in preparation of medicaments for treating and preventing renal fibrosis |
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| CN201310405546.0A CN103462992B (en) | 2013-09-06 | 2013-09-06 | Application of Aphanamgrandiol A in preparation of medicaments for treating and preventing renal fibrosis |
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| Publication Number | Publication Date |
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| CN103462992A CN103462992A (en) | 2013-12-25 |
| CN103462992B true CN103462992B (en) | 2015-07-01 |
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| CN101073577A (en) * | 2006-05-19 | 2007-11-21 | 山东绿叶天然药物研究开发有限公司 | Use of asiaticoside |
| CN103127089A (en) * | 2012-10-25 | 2013-06-05 | 吴俊华 | Application of Eryngiolide A in medicines curing or preventing kidney fibrosis |
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