CN105125568A - Medicine for treating and preventing renal fibrosis and application of medicine - Google Patents
Medicine for treating and preventing renal fibrosis and application of medicine Download PDFInfo
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- CN105125568A CN105125568A CN201510518433.0A CN201510518433A CN105125568A CN 105125568 A CN105125568 A CN 105125568A CN 201510518433 A CN201510518433 A CN 201510518433A CN 105125568 A CN105125568 A CN 105125568A
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Abstract
The invention belongs to the field of medicine, and particularly provides medicine for treating or preventing renal fibrosis. The medicine comprises chemical compounds Ieodoglucomides A and excipient. The medicine has the advantages that the medicine is high in renal fibrosis inhibitory activity and outstanding in substantiality and is obvious in improvement when used for preventing and treating the renal fibrosis.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind for the treatment of and preventing renal fibrosis medicine and application thereof.
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 Compound I eodoglucomidesA that the present invention relates to is one and delivers (ChadaRajiReddy in 2013, etal., TotalSynthesesoftheProposedStructureforIeodoglucomidesAa ndB, J.Org.Chem.2013, (78) noval chemical compound: 4251-4260.), this compound has brand-new framework types, current purposes only relates to antiinflammatory action (ChadaRajiReddy, etal., TotalSynthesesoftheProposedStructureforIeodoglucomidesAa ndB, J.Org.Chem.2013, (78): 4251-4260.), the purposes of the IeodoglucomidesA that the present invention relates in preparation treatment and preventing renal fibrosis medicine belongs to first public.
Summary of the invention
A kind for the treatment of and preventing renal fibrosis medicine and application thereof are the object of the present invention is to provide.
A kind for the treatment of and preventing renal fibrosis medicine, be made up of Compound I eodoglucomidesA and adjuvant, described Compound I eodoglucomidesA structure is as shown in formula I:
Described treatment and preventing renal fibrosis medicine, adjuvant is dextrin or starch.
Described treatment and the application of preventing renal fibrosis medicine in preparation treatment and preventing renal fibrosis medicine.
The purposes of the IeodoglucomidesA 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 strong for renal fibrosis inhibit activities, possess outstanding substantive distinguishing features, the control simultaneously for renal fibrosis obviously has significant progress.
Detailed description of the invention
The preparation method of Compound I eodoglucomidesA involved in the present invention is see document (ChadaRajiReddy, etal., TotalSynthesesoftheProposedStructureforIeodoglucomidesAa ndB, J.Org.Chem.2013, (78): 4251-4260.)
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 I eodoglucomidesA tablet involved in the present invention:
Get 5 g of compound IeodoglucomidesA and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of Compound I eodoglucomidesA capsule involved in the present invention:
Get 5 g of compound IeodoglucomidesA and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1: Compound I eodoglucomidesA is on the impact of Rats Undergoing Unilateral Urethral Ligation kidney region fibrosis
1.1 material
Benazepril, 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.The raw material got in above-described embodiment 1 is tested.
Laboratory animal: regular grade Wistar rat, male, body weight 150-200g, 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, IeodoglucomidesA intravenous injection 2.5mg/kg group, IeodoglucomidesA intravenous injection 5mg/kg group, IeodoglucomidesA intravenous injection 25mg/kg group, IeodoglucomidesA gavage 5mg/kg group, IeodoglucomidesA gavage 10mg/kg group, IeodoglucomidesA 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 IeodoglucomidesA gavage significantly, compares have notable difference with model control group.
Table 1IeodoglucomidesA 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, IeodoglucomidesA intravenous injection 5mg/kg group, IeodoglucomidesA intravenous injection 25mg/kg group, IeodoglucomidesA gavage 10mg/kg group, IeodoglucomidesA gavage 50mg/kg group reduce FN, HYPP level (comparing with model control group, P<0.05 or 0.01).
Conclusion: IeodoglucomidesA 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 (3)
1. treatment and a preventing renal fibrosis medicine, it is characterized in that, be made up of Compound I eodoglucomidesA and adjuvant, described Compound I eodoglucomidesA structure is as shown in formula I:
2. treat as claimed in claim 1 and preventing renal fibrosis medicine, it is characterized in that, adjuvant is dextrin or starch.
3. treatment and the application of preventing renal fibrosis medicine in treatment and preventing renal fibrosis medicine as claimed in claim 1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510518433.0A CN105125568A (en) | 2015-08-22 | 2015-08-22 | Medicine for treating and preventing renal fibrosis and application of medicine |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510518433.0A CN105125568A (en) | 2015-08-22 | 2015-08-22 | Medicine for treating and preventing renal fibrosis and application of medicine |
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| CN105125568A true CN105125568A (en) | 2015-12-09 |
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| CN201510518433.0A Pending CN105125568A (en) | 2015-08-22 | 2015-08-22 | Medicine for treating and preventing renal fibrosis and application of medicine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107628936A (en) * | 2017-09-30 | 2018-01-26 | 南京正宽医药科技有限公司 | The extracting method of vanillic aldehyde and its application |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101851635A (en) * | 2009-10-10 | 2010-10-06 | 中国人民解放军第四军医大学 | Preparation method for novel fusion protein reversing renal fibrosis and activity detection |
-
2015
- 2015-08-22 CN CN201510518433.0A patent/CN105125568A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101851635A (en) * | 2009-10-10 | 2010-10-06 | 中国人民解放军第四军医大学 | Preparation method for novel fusion protein reversing renal fibrosis and activity detection |
Non-Patent Citations (2)
| Title |
|---|
| CHADA RAJI REDDY等: "Total Syntheses of the Proposed Structure for Ieodoglucomides A and B", 《THE JOURNAL OF ORGANIC CHEMISTRY》 * |
| 王金荣等: "肾纤维化的研究进展", 《医学研究杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107628936A (en) * | 2017-09-30 | 2018-01-26 | 南京正宽医药科技有限公司 | The extracting method of vanillic aldehyde and its application |
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