CN103381159A - Applications of Chukrasone B in medicines used for treating or preventing renal fibrosis - Google Patents
Applications of Chukrasone B in medicines used for treating or preventing renal fibrosis Download PDFInfo
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- CN103381159A CN103381159A CN 201310281056 CN201310281056A CN103381159A CN 103381159 A CN103381159 A CN 103381159A CN 201310281056 CN201310281056 CN 201310281056 CN 201310281056 A CN201310281056 A CN 201310281056A CN 103381159 A CN103381159 A CN 103381159A
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Abstract
The invention provides applications of Chukrasone B in preparation of medicines used for treating or preventing renal fibrosis, and belongs to the field of medicine new application technology. Applications of Chukrasone B in preparation of medicines used for treating or preventing renal fibrosis are disclosed for the first time. Due to the fact that skeleton type belongs to completely novel skeleton type, and Chukrasone B has an unexpectedly high inhibitory activity on renal fibrosis, probability of other compounds giving any revelation for Chukrasone B does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in treating or preventing renal fibrosis.
Description
Technical field
The present invention relates to a kind of new medicine use, relate to particularly the application of Chukrasone B in the medicine of preparation treatment or preventing renal fibrosis.
Background technology
Renal fibrosis (comprising kidney region fibrosis and glomerular sclerosis) is the main pathological basis of the kidney damage final stage that causes of a variety of causes, the renal fibrosis mechanism is comparatively complicated, relevant with many factors, wherein main and the celliferous propagation of extracellular matrix cell and activation, vaso-active substance, cytokine and extracellular matrix conversion are unbalance relevant, so kidney region fibrosis is almost the common pathway that former or secondary kidney disease proceed to end stage renal failure.
the Compound C hukrasone B that the present invention relates to is one and delivered (Liu in 2012, H. B. et al., 2012. Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to potassium-channel and suppresses active (Liu, H. B. et al., 2012. Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.), belong to open first for the purposes of the Chukrasone B that the present invention relates in preparation treatment or preventing renal fibrosis medicine, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for renal fibrosis, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the control that is used for simultaneously renal fibrosis obviously has significant progress.
Summary of the invention
The invention provides the application of Chukrasone B in the medicine of preparation prevention or treatment renal fibrosis.
Described Compound C hukrasone B structure is as shown in formula I:
Formula I
The purposes of the Chukrasone B that the present invention relates in preparation treatment or preventing renal fibrosis medicine belongs to open first, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for renal fibrosis, there is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously renal fibrosis obviously has significant progress.
The specific embodiment
The preparation method of Compound C hukrasone B involved in the present invention is referring to document (Liu, H. B. et al., 2012. Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of Compound C hukrasone B tablet involved in the present invention:
Get 20 and digest compound Chukrasone B, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of Compound C hukrasone B capsule involved in the present invention:
Get 20 and digest compound Chukrasone B, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The impact of test Chukrasone B on the 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 available from the Shanghai institute of Biological Products.
Laboratory animal: regular grade Wistar rat, male, body weight 150-200g, SD rat.
1.2 test method and result
90 of rats, divide 9 groups at random, it is sham operated rats, model group, benazepril gavage 10mg/kg group, Chukrasone B intravenous injection 2.5 mg/kg groups, Chukrasone B intravenous injection 5 mg/kg groups, Chukrasone B intravenous injection 25 mg/kg groups, Chukrasone B gavage 5mg/kg group, Chukrasone B gavage 10mg/kg group, Chukrasone B gavage 50mg/kg group, 1 week of animal feeding, each rat with 10% chloral hydrate 3.0mL/kg intraperitoneal injection of anesthesia after, with the Rat Right lateral position fixing with operating-table on, use 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 separate the left side ureter, sham operated rats is only cut abdominal cavity and free left side ureter, but not ligation and cutting off, other respectively organize rat 4-0 silk thread ligation twice, upper one ligation point is positioned at left inferior pole of kidney level, then cut off ureter at twice ligation point, layer-by-layer suture, postoperative was put to death each treated animal after 10% chloral hydrate anesthesia in 10 days, get blood, press Fibronectin and measure explanation mensuration explanation fiber connexin (FN).Normal saline is left and taken left kidney after lavation repeatedly, and nephridial tissue is fixed through 4% paraformaldehyde buffer.Cut appropriate nephridial tissue, press the explanation of hydroxyproline kit measurement and measure hydroxyproline.
Routine pathology is learned and to be examined 1. perusal: sham operated rats kidney color is scarlet, shows smoothly, and peplos gloss is without adhesion.Other respectively organize the Kidney Volume increase, and color is pale, shows to be 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, and glomerular capsule is without expansion or cell infiltration.The large stretch of renal tubular necrosis of model control group, the hyperplasia of kidney interstitial fibers, tubular ectasia, in a large amount of brown color shading materials or the downright bad epithelial cell that comes off are arranged, the 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 heavy dose of each group of Chukrasone B gavage significantly, with model control group, notable difference is arranged relatively.
The impact of table 1 Chukrasone B on the Rats Undergoing Unilateral Urethral Ligation kidney region fibrosis
* p＜0.05, compare with model group in * * p＜0.01
FN, HYP carry out the T check to each group.The results are shown in Table 1, Chukrasone B intravenous injection 5 mg/kg organize, Chukrasone B intravenous injection 25 mg/kg organize, Chukrasone B gavage 10mg/kg organizes, Chukrasone B gavage 50mg/kg group reduces FN, HYPP level (comparing P＜0.05 or 0.01 with model control group).
Conclusion: Chukrasone B can significantly 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)
1.Chukrasone the application of B in treatment or the medicine of preventing renal fibrosis, described Compound C hukrasone B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN 201310281056 CN103381159A (en) | 2013-07-04 | 2013-07-04 | Applications of Chukrasone B in medicines used for treating or preventing renal fibrosis |
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| CN 201310281056 CN103381159A (en) | 2013-07-04 | 2013-07-04 | Applications of Chukrasone B in medicines used for treating or preventing renal fibrosis |
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| CN103381159A true CN103381159A (en) | 2013-11-06 |
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| CN 201310281056 Pending CN103381159A (en) | 2013-07-04 | 2013-07-04 | Applications of Chukrasone B in medicines used for treating or preventing renal fibrosis |
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Application publication date: 20131106 |