CN102824354A - Application of polydatin in preparation of pharmaceuticals for preventing and treating chronic glomerular diseases - Google Patents
Application of polydatin in preparation of pharmaceuticals for preventing and treating chronic glomerular diseases Download PDFInfo
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- CN102824354A CN102824354A CN2012103596154A CN201210359615A CN102824354A CN 102824354 A CN102824354 A CN 102824354A CN 2012103596154 A CN2012103596154 A CN 2012103596154A CN 201210359615 A CN201210359615 A CN 201210359615A CN 102824354 A CN102824354 A CN 102824354A
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Abstract
The invention relates to a new pharmaceutical application of natural monomeric compound polydatin and specifically relates to an application of polydatin in preparation of pharmaceuticals for preventing and treating chronic glomerular diseases, particularly for preventing and treating progressive chronic glomerular diseases and sertoli cell cytopathic (such as glomerulosclerosis and the like) glomerular diseases. Animal experimental results show that the polydatin has obvious functions of preventing and improving the glomerulus functions and organic cause damages of a fructose model rat, and also has obvious functions of preventing and improving the urine protein and glomerulus sertoli cell damage of a glomerulosclerosis model rat. The polydatin and related adjuvants are mixed to be prepared into healthcare products or pharmaceuticals for preventing and treating glomerular diseases by a conventional preparation method; and the polydatin can be applicable to glomerulosclerosis and other diseases which relate to sertoli cell cytopathy and is capable of delaying and improving the glomerular progressive disease courses of related diseases.
Description
One, technical field:
The present invention relates to the new medicine use of natural plant active component polygonin; Specifically relate to the application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament, the application in particularly relating to the preparation prevention and treating progressive chronic glomerulus disease and podocyte pathological changes relevant (like glomerulosclerosis etc.) renal glomerular disease medicine.
Two, background technology:
Polygonin (Polydatin, CAS 65914-17-2) has another name called piceid or polidatin, is a kind of active skull cap components, and its source comprises dry rhizome and the root of polygonaceae plant Rhizoma Polygoni Cuspidati Polygonum cuspidatum Sieb.et Zucc..
China diabetes prevalence be 9.7%, surpass the world average level 6.4%, become the first in the world diabetes big country.China diabetes high-risk group is up to 1.5 hundred million people.Along with the increase year by year of diabetic nephropathy sickness rate, in the complication of diabetes, the sickness rate of chronic glomerulus disease has risen to first.
Turn to the ratio of renal failure in latter stage (needing dialysis) very high after the diabetic nephropathy morbidity; Similar with it, when other chronic glomerulus disease turned to dialysis along with course of disease progress, social significant problems such as medical expense is surging can appear equally.Therefore, very strong to chronic glomerulus PD relevant prevention and healing potion demand.
With regard to the chronic glomerulus disease, podocyte (podocyte) pathological changes is crucial pathology affair in its incidence and development process.Podocyte is the visceral layer epithelial cell that is positioned at the GCBM outside, gains the name because of its endochylema forms pseudopodium appearance projection on the basement membrane surface.Slit membrane between the podocytic process (split mernbrane) is last one barrier of glomerular filtration, so the podocyte damage will cause albuminuria to occur.Along with to the going deep into of podocyte biological study, especially after finding some specific proteins molecules that podocyte is expressed, podocyte has been considered to participate in the key cells of various constitutionales or secondary glomerulopathy progress.The constitutional podocyte is sick often falls ill with the form of expression of minute lesion, FSGS and membranous nephropathy; And Secondary cases podocyte disease is common in infection dependency, drug-associated, metal species drug-associated, LADA, cancer-related, renal transplantation dependency membranous nephropathy.
The medicine of specific aim target does not appear becoming with glomerulopathy at present both at home and abroad as yet; Change to dialysis for suppressing or postpone the course of disease, clinical medicament commonly used comprises: steroid medicine, anticoagulant, immunosuppressant, Angiotensin class etc.Said medicine improvement effect is limited, and side effect is obvious.
Three, summary of the invention:
The object of the present invention is to provide the new medical use of natural plant active component polygonin; Specifically relate to the application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament, particularly relate to preparation and be used for progressive chronic glomerulus disease and comprise the prevention of glomerulosclerosis and the application of medicine.
Technical solution of the present invention:
The application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament is provided.
The application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is that glomerular podocyte is sick.
The application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is a FGS.
The application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is an IgA nephropathy.
The application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is a membranous nephropathy.
The application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is a membrano proliferative glomerulonephritis.
This application has comprised with the polygonin being major ingredient; Be equipped with the pharmaceutic adjuvant (excipient, cosolvent, controlled release agent etc.) that those skilled in the art knows, process the dosage form (comprising oral liquid, injection, capsule, tablet, granule, microcapsule etc.) that those skilled in the art knows with conventional formulation method.
Advantage of the present invention is; Provide the polygonin that progressive chronic glomerulus disease is had definite improvement and therapeutical effect to prepare medicament (health product or medicine), be used for prevention and treat progressive chronic glomerulus disease and podocyte pathological changes relevant (like glomerulosclerosis etc.) renal glomerular disease.The present invention has 3 significantly progressive and advantages: 1, definite ingredients (polygonin); 2, with clearly defined objective (renal glomerular disease); 3, regulating action clear and definite (obviously improving and therapeutical effect).
The present invention utilizes animal model on biochemical function and histiocyte level, scientifically to estimate and proved definite improvement and the therapeutical effect of polygonin to the chronic glomerulus disease.
Polygonin involved in the present invention does not make significant difference to normal control animal chronic glomerulus disease association index, has good safety.
Essence for a better understanding of the present invention will be explained its application in preparation prevention and treatment chronic glomerulus disease medicament with the pharmacological evaluation and the result of polygonin below.
Four, description of drawings:
Fig. 1: PAS coloration result (fructose causes glomerule pathological changes rat model)
The left figure of last row: normal control; Figure among the last row: normal control+polygonin; The right figure of last row: normal control+pioglitazone;
The left figure of following row: fructose model; Figure among the following row: fructose model+polygonin; The right figure of following row: fructose model+pioglitazone.
Fig. 2: TEM results (fructose causes glomerule pathological changes rat model)
The left figure of last row: normal control; Figure among the last row: normal control+polygonin; The right figure of last row: normal control+pioglitazone;
The left figure of following row: fructose model; Figure among the following row: fructose model+polygonin; The right figure of following row: fructose model+pioglitazone.
Fig. 3: TEM results (amycin causes the glomerulosclerosis rat model)
Left figure: normal control; Middle figure: model contrast; Right figure: model+polygonin.
Five, the specific embodiment: following examples are only as the usefulness of further setting forth invention, can not be used for limiting the present invention.
Embodiment 1: polygonin is to the therapeutical effect that improves of fructose rat model glomerule pathological changes.
Laboratory animal: the SD rat, the 200-220 gram, male.
The medicine preparation: selecting polygonin content for use is the prevention that is used for renal glomerular disease of 20mg/ sheet or the tablet of treatment, and ultra-sonic dispersion is used for gastric infusion in normal saline, and dosage is 7.5mg/kg.
Experimental apparatus: High speed refrigerated centrifuge, histotome, ELIASA, spectrophotometer, optical microscope, transmission electron microscope etc.
Experimental model: fructose rat model.
Experimental technique:
1, the foundation of model: animal conformed after 1 week, was divided into model group and normal group at random, 30 every group.The modeling of fructose rat model: drinking water gives 10% fructose soln; Normal group gives tap water, 70 days modeling cycles.
2, model group and normal group are set up polygonin and pioglitazone administration group, 10 every group respectively after 4 weeks of modeling.Irritate stomach every day and give polygonin (7.5mg/kg) and pioglitazone (4mg/kg).This medicine continued for 6 weeks, and animal pattern continues to give 10% fructose soln during the administration.
3, collect the blood urine specimen, be used to detect biochemical indicator: serum creatinine, blood urea nitrogen level and urinaryalbumin and UCr ratio.
4, separate renal tissue on the sacrifice of animal ice platform, be divided into two parts, fix through formaldehyde and glutaraldehyde respectively, conventional section.Under optical microscope (PAS dyeing) and transmission electron microscope, observe the change of glomerule tectology respectively.
Experimental result:
A: renal function biochemical indicator
+++P<0.001 with normally+the normal saline group relatively;
*P<0.01,
* *P<0.001 all be significantly higher than normal rats with fructose model+normal saline group comparison fructose rat model serum creatinine, blood urea nitrogen level and urinaryalbumin and UCr ratio; Wherein serum creatinine and blood urea nitrogen level raise, and explain that fructose rat model filtration capacity of the kidney descends; Urinaryalbumin and UCr ratio raise and then point out fructose rat model kidney filtration barrier to be damaged; Above-mentioned two kinds of renal function filtering function obstacles are all explained fructose kidney of rats bead generation functional lesion.Polygonin can be alleviated the glomerule function damage that fructose causes significantly, and its effect surpasses positive control medicine pioglitazone, and the intact animal gives polygonin and then These parameters all do not found significant change.
B: nephridial tissue structural damage
Shown in accompanying drawing 1: om observation presents tangible positive reaction to model group kidney of rats bead PAS dyeing, prompting fructose rat glomerular mesangium substrate hypertrophy; The polygonin administration can effectively improve the inductive glomerular mesangium substrate of fructose hypertrophy; With respect to the normal control animal, polygonin administration treated animal glomerular mesangium is not seen significant change.
Shown in accompanying drawing 2: transmission electron microscope observing merges to model group podocyte podocytic process and becomes flat, partial fusion, disappearance, and GBM (GBM) thickens; The polygonin administration can effectively alleviate above-mentioned podocyte and the GBM pathologic changes; With respect to the normal control animal, polygonin administration treated animal glomerular podocyte is not seen significant change.
Show through renal function index and organizational structure testing result; Polygonin has significant protection improvement effect for fructose rat model glomerule function and structural damage; Its effectiveness and pioglitazone are suitable, and its effect is mainly reflected in the protection for glomerular podocyte and film function.The polygonin administration does not make significant difference for intact animal's glomerule function and structure, explains that it is used for the prevention of renal glomerular disease and the safety of medicine.
Embodiment 2: polygonin amycin is caused the glomerulosclerosis rat the glomerule pathological changes improve therapeutical effect.
Laboratory animal: the SD rat, the 200-220 gram, male.
The medicine preparation: selecting polygonin content for use is the prevention that is used for renal glomerular disease of 20mg/ sheet or the tablet of treatment, and ultra-sonic dispersion is used for gastric infusion in normal saline, and dosage is 75mg/kg.Adriamycin vial (trade name: Pharmorubicin RD pin; Pharmacia Corp of Soviet Union).
Experimental technique: focal segmental glomerulosclerosis is a common primary glomerulopathy, mainly be since glomerular hemodynamics cause the podocyte damage unusually, be prone to progress and be whole chronic renal failure in latter stage.
1, the foundation of model: animal conformed after 1 week, was divided into model group and normal group at random, 30 every group.The model group rat is through tail vein injection amycin 2.5mg/kg (being dissolved among the normal saline 0.5mL); Normal group tail vein injection saline 0.5mL.Behind the 20d, repeat aforesaid operations.
2, behind the 2nd injection amycin 1 day, the treatment group was irritated stomach every day and is given polygonin (7.5mg/kg) administration and continued for 12 weeks.
3, collect the blood urine specimen, be used to detect biochemical indicator: serum creatinine, blood urea nitrogen level and urinaryalbumin and UCr ratio.
4, separate renal tissue on the sacrifice of animal ice platform, the fixing section of glutaraldehyde.Transmission electron microscope is observed the glomerule tectology down and is changed.
Experimental result:
A: urine protein index
+++P<0.001 compare with the normal control group;
* *P<0.001 compare with the glomerular sclerosis model control group
B: nephridial tissue structural damage
Shown in accompanying drawing 3: transmission electron microscope observing merges to model group rat foot process of glomerular podocyte and becomes flat, partial fusion, disappearance, and GBM (GBM) thickens.The polygonin administration can effectively alleviate above-mentioned podocyte and the GBM pathologic changes.Show; Polygonin has tangible prevention protection and improves therapeutical effect for glomerulosclerosis rat model glomerule function and structural damage; Its effect is mainly reflected in the protection for the glomerular podocyte structure, explains that it is used to prepare podocyte pathological changes relevant glomerulosclerosis and the prevention of other renal glomerular disease or the effectiveness and the specific aim of medicine.
Embodiment 3:
Polygonin according to the conventional formulation method, is added entry and an amount of solubilizing agent (PEG400) dissolving, packing, sterilization, the chronic glomerulus disease prevention that is prepared into polygonin content and is 20mg/ml is used oral liquid with treatment;
According to the conventional formulation method, the soft capsule material is selected gelatin and sorbitol for use with polygonin, and the chronic glomerulus disease prevention that is prepared into polygonin content and is the 20mg/ grain is used capsule with treatment;
Polygonin according to the conventional formulation method, is added the excipient cyclodextrin, and mix homogeneously is granulated, tabletting, and tablet is used in the chronic glomerulus disease prevention and the treatment that are prepared into polygonin content and are the 20mg/ sheet.
Claims (7)
1. the application of polygonin in preparation prevention and treatment chronic glomerulus disease medicament.
2. the application of polygonin according to claim 1 in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is that glomerular podocyte is sick.
3. the application of polygonin according to claim 1 in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is a FGS.
4. the application of polygonin according to claim 1 in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is an IgA nephropathy.
5. the application of polygonin according to claim 1 in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is a membranous nephropathy.
6. the application of polygonin according to claim 1 in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that described chronic glomerulus disease is a membrano proliferative glomerulonephritis.
7. the application of polygonin according to claim 1 in preparation prevention and treatment chronic glomerulus disease medicament is characterized in that the adjuvant that described polygonin is equipped with corresponding dosage form processes oral liquid, capsule, tablet, granule or microcapsule with conventional formulation method.
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| CN2012103596154A CN102824354A (en) | 2012-09-24 | 2012-09-24 | Application of polydatin in preparation of pharmaceuticals for preventing and treating chronic glomerular diseases |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN110179773A (en) * | 2019-07-04 | 2019-08-30 | 合肥师范学院 | Dendrophnol prevents and treats the application in Chronic glomerular disease drug in preparation |
| CN114949046A (en) * | 2022-05-11 | 2022-08-30 | 武汉儿童医院 | New application of giant knotweed rhizome |
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| CN101780062A (en) * | 2010-03-22 | 2010-07-21 | 张爱华 | Application of resveratrol to treating kidney disease |
| CN102631358A (en) * | 2012-04-25 | 2012-08-15 | 中山大学 | Application of polydatin in preparing medicament for treating diabetic nephropathy |
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| CN101780062A (en) * | 2010-03-22 | 2010-07-21 | 张爱华 | Application of resveratrol to treating kidney disease |
| CN102631358A (en) * | 2012-04-25 | 2012-08-15 | 中山大学 | Application of polydatin in preparing medicament for treating diabetic nephropathy |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110179773A (en) * | 2019-07-04 | 2019-08-30 | 合肥师范学院 | Dendrophnol prevents and treats the application in Chronic glomerular disease drug in preparation |
| CN114949046A (en) * | 2022-05-11 | 2022-08-30 | 武汉儿童医院 | New application of giant knotweed rhizome |
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