CN103520181B - The application of Phyllanthoid A in preparation treatment and preventing renal fibrosis medicine - Google Patents
The application of Phyllanthoid A in preparation treatment and preventing renal fibrosis medicine Download PDFInfo
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- CN103520181B CN103520181B CN201310495999.7A CN201310495999A CN103520181B CN 103520181 B CN103520181 B CN 103520181B CN 201310495999 A CN201310495999 A CN 201310495999A CN 103520181 B CN103520181 B CN 103520181B
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Abstract
Do you the invention provides Phyllanthoid? the application of A in the medicine preparing treatment or preventing renal fibrosis, belong to technical field of new application of medicine, belong 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.
Description
Technical field
The present invention relates to the novelty teabag of compound PhyllanthoidA, particularly relate to the application of PhyllanthoidA 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 compound PhyllanthoidA that the present invention relates to is one and delivers (Jian-QiangZhao in 2013, etal., TwoNewHighlyOxygenatedandRearrangedLimonoidsfromPhyllant huscochinchinensis.OrganicLetters, 2013, 15(10) 2414 – 2417.) noval chemical compound, this compound has brand-new framework types, current purposes only suppresses breast cancer cell increment (Jian-QiangZhao, etal., TwoNewHighlyOxygenatedandRearrangedLimonoidsfromPhyllant huscochinchinensis.OrganicLetters, 2013, 15(10) 2414 – 2417.), the purposes of the PhyllanthoidA that the present invention relates in preparation treatment and preventing renal fibrosis medicine belongs to first public.
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 PhyllanthoidA research, provide the application of PhyllanthoidA in preparation treatment and preventing renal fibrosis medicine.
Described compound PhyllanthoidA structure is as shown in formula I:
The purposes of the PhyllanthoidA 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 PhyllanthoidA involved in the present invention is see document (Jian-QiangZhao, etal., TwoNewHighlyOxygenatedandRearrangedLimonoidsfromPhyllant huscochinchinensis.OrganicLetters, 2013,15(10) 2414 – 2417.)
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 PhyllanthoidA tablet involved in the present invention:
Get 5 g of compound PhyllanthoidA and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound PhyllanthoidA capsule involved in the present invention:
Get 5 g of compound PhyllanthoidA and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:PhyllanthoidA 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.
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, PhyllanthoidA intravenous injection 2.5mg/kg group, PhyllanthoidA intravenous injection 5mg/kg group, PhyllanthoidA intravenous injection 25mg/kg group, PhyllanthoidA gavage 5mg/kg group, PhyllanthoidA gavage 10mg/kg group, PhyllanthoidA 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 PhyllanthoidA gavage significantly, compares have notable difference with model control group.
Table 1PhyllanthoidA 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, PhyllanthoidA intravenous injection 5mg/kg group, PhyllanthoidA intravenous injection 25mg/kg group, PhyllanthoidA gavage 10mg/kg group, PhyllanthoidA gavage 50mg/kg group reduce FN, HYPP level (comparing with model control group, P<0.05 or 0.01).
Conclusion: PhyllanthoidA 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.PhyllanthoidA in preparation treatment and preventing renal fibrosis medicine, described compound PhyllanthoidA structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310495999.7A CN103520181B (en) | 2013-10-21 | 2013-10-21 | The application of Phyllanthoid A in preparation treatment and preventing renal fibrosis medicine |
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| CN201310495999.7A CN103520181B (en) | 2013-10-21 | 2013-10-21 | The application of Phyllanthoid A in preparation treatment and preventing renal fibrosis medicine |
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| Publication Number | Publication Date |
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| CN103520181A CN103520181A (en) | 2014-01-22 |
| CN103520181B true CN103520181B (en) | 2016-02-17 |
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| CN201310495999.7A Expired - Fee Related CN103520181B (en) | 2013-10-21 | 2013-10-21 | The application of Phyllanthoid A in preparation treatment and preventing renal fibrosis medicine |
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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
- 2013-10-21 CN CN201310495999.7A patent/CN103520181B/en not_active Expired - Fee Related
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 |
|---|
| Two New Highly Oxygenated and Rearranged Limonoids from Phyllanthus cochinchinensis;Jian-Qiang Zhao,et al;《Organic Letters》;20130502;第15卷(第10期);1 * |
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| CN103520181A (en) | 2014-01-22 |
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Inventor after: Jia Yong Inventor after: Chi Kun Inventor after: Fu Haixia Inventor after: Xian Yuxin Inventor before: The inventor has waived the right to be mentioned |
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Effective date of registration: 20151231 Address after: 266000 Donghai Road, Shandong, Qingdao, China, No. 5 Applicant after: Qingdao Municipal Hospital Address before: 211200, No. 1, industrial town, crystal Town, Lishui District, Jiangsu, Nanjing Applicant before: Sun Aihua |
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