CN102872143A - Application of Houttuynoid D in drug for preventing or treating pancreatic fibrosis - Google Patents
Application of Houttuynoid D in drug for preventing or treating pancreatic fibrosis Download PDFInfo
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- CN102872143A CN102872143A CN2012104196197A CN201210419619A CN102872143A CN 102872143 A CN102872143 A CN 102872143A CN 2012104196197 A CN2012104196197 A CN 2012104196197A CN 201210419619 A CN201210419619 A CN 201210419619A CN 102872143 A CN102872143 A CN 102872143A
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- houttuynoid
- pancreatic fibrosis
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- preventing
- drug
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- 0 CCCCCCCC(CC)OCc(c(O)c(cc1)O)c1C(Oc1cc(O)cc(O)c1C1=O)=C1OC(C1O)OC(C*)C(*)C1O Chemical compound CCCCCCCC(CC)OCc(c(O)c(cc1)O)c1C(Oc1cc(O)cc(O)c1C1=O)=C1OC(C1O)OC(C*)C(*)C1O 0.000 description 1
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Abstract
The invention discloses application of Houttuynoid D in preparing a drug for preventing or treating pancreatic fibrosis. The use of Houttuynoid D in preparing the anti-pancreatic fibrosis drug involved in the invention is disclosed for the first time; as the framework type of Houttuynoid D is a brand new framework type and Houttuynoid D has an unexpectedly high inhibition activity for the pancreatic fibrosis without possibility of giving any implication by other compounds, Houttuynoid D has outstanding substantive features; and simultaneously, the application of Houttuynoid D for preventing the pancreatic fibrosis apparently has obvious progress.
Description
Technical field
The present invention relates to the application of Houttuynoid D in pharmacy, relate in particular to the application of Houttuynoid D in the medicine of preparation prevention or treatment pancreatic gland fibrosis.
Background technology
The present sickness rate of pancreatic gland fibrosis is more and more high, is badly in need of the anti-pancreatic gland fibrosis medicine of research and development high-efficiency low-toxicity.
The compound H outtuynoid D that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid D_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S. D. et al., 2012. Houttuynoid D_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), belong to open first for the purposes of the Houttuynoid D that the present invention relates in the anti-pancreatic gland fibrosis medicine of preparation, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for pancreatic gland fibrosis, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for simultaneously anti-pancreatic gland fibrosis and obviously have significant progress.
Summary of the invention
Technical problem to be solved by this invention is by the designing animal experimental technique, the anti-pancreatic gland fibrosis effect of research Houttuynoid D.
Described compound H outtuynoid D structure is shown in formula I:
Formula I
Therefore, the purpose of this invention is to provide the application of Houttuynoid D in the medicine of preparation prevention or treatment pancreatic gland fibrosis.
Positive progressive effect of the present invention is: Houttuynoid D has the effect of anti-pancreatic gland fibrosis, so the application of Houttuynoid D has good DEVELOPMENT PROSPECT.
The purposes of the Houttuynoid D that the present invention relates in the anti-pancreatic gland fibrosis medicine of preparation belongs to open first, because framework types belongs to brand-new framework types, and it suppresses active unexpectedly strong for pancreatic gland fibrosis, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for simultaneously anti-pancreatic gland fibrosis and obviously have significant progress.
The specific embodiment
The preparation method of compound H outtuynoid D involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid D_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.).
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 H outtuynoid D tablet involved in the present invention:
Get 20 and digest compound Houttuynoid D, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid D capsule involved in the present invention:
Get 20 and digest compound Houttuynoid D, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example:
1 material
1.1 animal Wistar rat is male, body weight 180-200g.
1.2 Houttuynoid D dosage: 0.3mg/kg, 0.9mg/kg, three dosage of 2.7mg/kg.
2 experimental techniques
2.1 modeling method Wistar rat with lumbar injection dl-ethionine 250 mg/ days, continuous 2 months, the pancreas glandular cell can occur and reduce, adipocellular hypertrophy in the matter.
2.2 grouping and medication
Rat model is divided into model group at random, Houttuynoid D 0.3mg/kg, 0.9mg/kg, three dosage groups of 2.7mg/kg, and other establishes the blank group, begins rear administration in modeling, oral continuous 30 days; Dissect animal in the time of 60 days.
2.3 detection index
Weigh 2.3.1 get pancreas when experiment finishes, calculate organ coefficient.
2.3.2 the pancreas hydroxyproline content is measured and got the homogenate in water of 100mg sample, hydrolysis is 20 hours among 110 ℃ of 10 N HCl.HCl volatilizees with nitrogen, and hydrolyzate filters with the distilled water dissolving is rear.Getting 0.5ml liquid mixes with the 1M periodic acid that 3ml citric acid phosphate buffer (the 0.15M citric acid adds the 0.6M sodium hydrogen phosphate) and 0.5ml are dissolved in 9M phosphoric acid.Add the 1.75ml Extraction buffer (5 parts of toluene: 5 parts of 2-methyl isophthalic acid-propanol: 2 parts of 1-propanol), the concussion 30min, centrifugal.Organize phase (0.6ml) and Ehrlich
,The s reagent mix is placed 15min.Measure trap at 565nm, with 4-hydroxyl-1-proline production standard curve calculation concentration, content is with the expression of ug/g tissue.
2.3.3 histological examination pancreas tissue is fixed with 10% formalin, paraffin embedding, microscopy after the dyeing.To inflammatory cell infiltration, interstitial edema, fibrosis, pancreas room necrocytosis, and bleeding scoring (0-3 divides).
3 results
3.1 Houttuynoid D is on the impact of rat pancreas weight and organ coefficient
When experiment finishes, rat is put to death, dissects, weigh in and pancreas is heavy and calculate it and the ratio of body weight, the results are shown in Table 1.Houttuynoid D relatively has significant difference on the impact of pancreas organ coefficient with model group.
Table 1
* represent p＜0.05, compare with model group
3.2 the pancreas hydroxyproline content is measured
During experimental result, each group rat is carried out pulmonary's hydroxyproline content measure result such as table 2.Houttuynoid D relatively has significant difference on the impact of hydroxyproline content with model group.
Table 2
* represent p＜0.05, compare with model group
3.3 histological examination
When experiment finishes, rat is put to death, dissects; The conventional embedding of specimen, fixing, HE dyeing, microscopy.
Result: model group visible pancreas conduit serious inflammatory reaction on every side in the 60th day; Have a liking for middle granulocyte karyolymph cellular infiltration, interstitial edema, hemorrhage and accidental pancreas cystencyte is downright bad; Fibrosis appears between pancreas cystencyte disappearance position and pancreas bubble.
But Houttuynoid D dose dependent reduces inflammatory reaction, tissue edema and fibrosis.Appraisal result sees Table 3.Houttuynoid D relatively has significant difference on the impact of scoring with model group.
Table 3
* represent p＜0.05, compare with model group
Conclusion: the present invention on the Fibrotic impact of pancreas in rat, has confirmed the effect that Houttuynoid D has anti-pancreatic gland fibrosis by Houttuynoid D.Therefore, Houttuynoid D can be used as active component for the preparation of the medicine of anti-pancreatic gland fibrosis.
Claims (1)
1.Houttuynoid D is the application in the hydroxyproline content medicine in reducing the pancreatic gland fibrosis that the dl-ethionine causes, described compound H outtuynoid D structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210419619 CN102872143B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid D in drug for preventing or treating pancreatic fibrosis |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 201210419619 CN102872143B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid D in drug for preventing or treating pancreatic fibrosis |
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| CN102872143A true CN102872143A (en) | 2013-01-16 |
| CN102872143B CN102872143B (en) | 2013-12-18 |
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| CN 201210419619 Expired - Fee Related CN102872143B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid D in drug for preventing or treating pancreatic fibrosis |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1744887A (en) * | 2003-02-04 | 2006-03-08 | 株式会社益力多本社 | Breast cancer-resistant protein inhibitor |
| CN1880328A (en) * | 2006-04-30 | 2006-12-20 | 重庆大学 | Preparation method of hyperin and hypericin of Hypericum perforatum |
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2012
- 2012-10-27 CN CN 201210419619 patent/CN102872143B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1744887A (en) * | 2003-02-04 | 2006-03-08 | 株式会社益力多本社 | Breast cancer-resistant protein inhibitor |
| CN1880328A (en) * | 2006-04-30 | 2006-12-20 | 重庆大学 | Preparation method of hyperin and hypericin of Hypericum perforatum |
Non-Patent Citations (1)
| Title |
|---|
| SHAO-DAN CHEN ET AL.: "Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with NovelSkeletons from Houttuynia cordata", 《ORGANIC LETTERS》 * |
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| CN102872143B (en) | 2013-12-18 |
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Owner name: JIANGSU KANGHENG CHEMICAL CO., LTD. Free format text: FORMER OWNER: WU JUNHUA Effective date: 20141230 |
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Effective date of registration: 20141230 Address after: 226500, Jiangsu, Rugao town (Rugao port area) 8 West Hong Kong Road (Fine Chemical Industry Park) Patentee after: Jiangsu Kangheng Chemical Co., Ltd. Address before: 210009 No. 22, Hankou Road, Gulou District, Jiangsu, Nanjing Patentee before: Wu Junhua |
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Granted publication date: 20131218 Termination date: 20191027 |