CN105497024A - Application of Herqueiazole to preparing of medicine for preventing or curing pancreas fibrosis - Google Patents
Application of Herqueiazole to preparing of medicine for preventing or curing pancreas fibrosis Download PDFInfo
- Publication number
- CN105497024A CN105497024A CN201510902481.XA CN201510902481A CN105497024A CN 105497024 A CN105497024 A CN 105497024A CN 201510902481 A CN201510902481 A CN 201510902481A CN 105497024 A CN105497024 A CN 105497024A
- Authority
- CN
- China
- Prior art keywords
- herqueiazole
- medicine
- pancreas
- pancreatic gland
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of Herqueiazole to preparing of a medicine for preventing or curing pancreas fibrosis. The usage of the Herqueiazole in the preparing of a medicine for preventing or curing pancreas fibrosis is firstly disclosed, since a skeleton type belongs to a brand new skeleton type and has previously unimagined inhibition activity to pancreas fibrosis without possibility of any teaching given by other compounds, the Herqueiazole has prominent substantive features and has a notable progress in resistance to the pancreas fibrosis.
Description
Technical field
The present invention relates to the novelty teabag of compound H erqueiazole, particularly relate to the application of Herqueiazole in preparation prevention or treatment pancreatic gland fibrosis medicine.
Background technology
The current 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 erqueiazole that the present invention relates to is one and delivers (ElinJulianti in 2013, etal., NewPolyaromaticMetabolitesfromaMarine-DerivedFungusPenic illiumsp..OrganicLetters, 2013, 15 (6) 1286 – 1289.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to cytotoxicity, (ElinJulianti, etal., NewPolyaromaticMetabolitesfromaMarine-DerivedFungusPenic illiumsp..OrganicLetters, 2013, 15 (6) 1286 – 1289.), the purposes of the Herqueiazole that the present invention relates in preparation prevention or treatment pancreatic gland fibrosis medicine is belonged to first public.
Summary of the invention
Technical problem to be solved by this invention is by designing animal experimental technique, the anti-pancreatic gland fibrosis effect of research Herqueiazole.
Described compound H erqueiazole structure is as shown in formula I:
The application of described Herqueiazole in prevention or treatment pancreatic gland fibrosis medicine, Herqueiazole can reduce rat lung hydroxyproline content.
A kind of prevention or treatment pancreatic gland fibrosis medicine, be that active component interpolation adjuvant is prepared from by Herqueiazole, preparation method, for getting 5 g of compound Herqueiazole, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
A kind of prevention or treatment pancreatic gland fibrosis medicine, be that active component adds adjuvant and is prepared from by Herqueiazole, preparation method, for getting 5 g of compound Herqueiazole, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Therefore, the object of this invention is to provide Herqueiazole prevent in preparation or treat the application in the medicine of pancreatic gland fibrosis.
Positive progressive effect of the present invention is: Herqueiazole has the effect of anti-pancreatic gland fibrosis, so the application of Herqueiazole has good DEVELOPMENT PROSPECT.
The purposes of the Herqueiazole that the present invention relates in the anti-pancreatic gland fibrosis medicine of preparation belongs to first public, because framework types belongs to brand-new framework types, and it is unexpectedly strong for pancreatic gland fibrosis inhibit activities, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, for anti-pancreatic gland fibrosis, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of compound H erqueiazole involved in the present invention is see document (ElinJulianti, etal., NewPolyaromaticMetabolitesfromaMarine-DerivedFungusPenic illiumsp..OrganicLetters, 2013,15 (6) 1286 – 1289.)
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 H erqueiazole tablet involved in the present invention:
Get 5 g of compound Herqueiazole to add and prepare 195 grams, dextrin, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound H erqueiazole capsule involved in the present invention:
Get 5 g of compound Herqueiazole and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
One, prevention or treatment pancreatic gland fibrosis experimentation
1 material
1.1 animal Wistar rats, male, body weight 180-200g, Nanjing Medical University's Experimental Animal Center.
1.2Herqueiazole dosage: 0.3mg/kg, 0.9mg/kg, 2.7mg/kg tri-dosage.
2 experimental techniques
2.1 modeling method Wistar rats, with lumbar injection dl-ethionine 250mg/ days, continuous 2 months, can occur that pancreas glandular cell reduces, adipocellular hypertrophy in interstitial.
2.2 grouping and medications
Rat model is divided into model group at random, and Herqueiazole0.3mg/kg, 0.9mg/kg, 2.7mg/kg tri-dosage groups, separately establish blank group, start rear administration in modeling, oral continuous 30 days; Animal is dissected when 60 days.
2.3 Testing index
2.3.1 get pancreas at the end of experiment to weigh, calculate organ coefficient.
2.3.2 pancreas hydroxyproline content measures and gets the homogenate in water of 100mg sample, is hydrolyzed 20 hours in 110 DEG C of 10NHCl.HCl nitrogen volatilizees, and hydrolyzate filters after dissolving with distilled water.Get 0.5ml liquid to mix with the 1M periodic acid that 3ml citric acid phosphate buffer (0.15M citric acid adds 0.6M sodium hydrogen phosphate) and 0.5ml are dissolved in 9M phosphoric acid.Add 1.75ml Extraction buffer (5 parts of toluene: 5 parts of 2-methyl isophthalic acid-propanol: 2 parts of 1-propanol), concussion 30min, centrifugal.Organize phase (0.6ml) and Ehrlich, s reagent to mix and place 15min.Measure trap at 565nm, with 4-hydroxyl-1-proline production standard curve calculating concentration, content represents with ug/g tissue.
2.3.3 histological examination pancreatic tissues 10% formalin is fixed, paraffin embedding, microscopy after dyeing.To inflammatory cell infiltration, interstitial edema, fibrosis, pancreas room necrocytosis, and bleeding scoring (0-3 divides).
3 results
3.1Herqueiazole is on the impact of rat pancreas weight and organ coefficient
At the end of experiment, rat put to death, dissect, to weigh in and pancreas weighs and calculates the ratio of itself and body weight, the results are shown in Table 1.Herqueiazole, on the impact of pancreas organ coefficient, compares with model group and has significant difference.
Table 1
3.2 pancreas hydroxyproline contents measure
At the end of experiment, carry out pulmonary's hydroxyproline content mensuration to each group of rat, result is as table 2.
Herqueiazole, on the impact of hydroxyproline content, compares with model group and has significant difference.
Table 2
* represent p<0.05, compare with model group
3.3 histological examination
At the end of experiment, rat put to death, dissect; The embedding of specimen routine, fixing, HE dyeing, microscopy.Result: model group visible pancreas surrounding catheter extensive inflammation reaction in the 60th day; Addicted to middle granulocyte karyolymph cellular infiltration, interstitial edema, hemorrhage and accidental pancreas cystencyte is downright bad; Fibrosis is there is between pancreas cystencyte disappearance position and pancreas bubble.Herqueiazole can reduce inflammatory reaction, tissue edema and fibrosis by dose dependent.Appraisal result is in table 3.
Herqueiazole, on the impact of scoring, compares with model group and has significant difference.
Table 3
* represent p<0.05, * * p<0.01, compares with model group
Conclusion: the present invention on the Fibrotic impact of pancreas in rat, confirms that Herqueiazole has the effect of anti-pancreatic gland fibrosis by Herqueiazole.Therefore, Herqueiazole can be used as the medicine of active component for the preparation of anti-pancreatic gland fibrosis.
Claims (4)
- The application of 1.Herqueiazole in prevention or treatment pancreatic gland fibrosis medicine, described compound H erqueiazole structure is as shown in formula I:
- 2. the application of Herqueiazole in prevention or treatment pancreatic gland fibrosis medicine as claimed in claim 1, is characterized in that Herqueiazole can reduce rat lung hydroxyproline content.
- 3. a prevention or treatment pancreatic gland fibrosis medicine, it is characterized in that by Herqueiazole described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound Herqueiazole, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
- 4. a prevention or treatment pancreatic gland fibrosis medicine, it is characterized in that by Herqueiazole described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound Herqueiazole, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510902481.XA CN105497024A (en) | 2015-12-08 | 2015-12-08 | Application of Herqueiazole to preparing of medicine for preventing or curing pancreas fibrosis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510902481.XA CN105497024A (en) | 2015-12-08 | 2015-12-08 | Application of Herqueiazole to preparing of medicine for preventing or curing pancreas fibrosis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105497024A true CN105497024A (en) | 2016-04-20 |
Family
ID=55705585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510902481.XA Pending CN105497024A (en) | 2015-12-08 | 2015-12-08 | Application of Herqueiazole to preparing of medicine for preventing or curing pancreas fibrosis |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105497024A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106577698A (en) * | 2016-12-04 | 2017-04-26 | 徐州得铸生物科技有限公司 | Sterilizing composition for preventing and treating sclerotinia rot of colza |
-
2015
- 2015-12-08 CN CN201510902481.XA patent/CN105497024A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106577698A (en) * | 2016-12-04 | 2017-04-26 | 徐州得铸生物科技有限公司 | Sterilizing composition for preventing and treating sclerotinia rot of colza |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN104147019A (en) | Application of O-(tetrahydropyrrole) ethyl derivative of cleistanone in preparation of medicines for preventing or treating pancreatic fibrosis | |
| CN105497024A (en) | Application of Herqueiazole to preparing of medicine for preventing or curing pancreas fibrosis | |
| CN103381167B (en) | The application of Chukrasone A in the medicine of preparation prevention pancreatic gland fibrosis | |
| CN103393669B (en) | The application of Chukrasone B in the medicine of preparation prevention pancreatic gland fibrosis | |
| CN105326836A (en) | Application of Alistonitrine A in preparing pancreatic fibrosis prevention or treatment medicine | |
| CN105395560A (en) | Application of Astataricusol A in preparation of drugs for prevention or treatment of pancreatic fibrosis | |
| CN105287489A (en) | Application of Furanocyclocommunin in preparation of pancreatic fibrosis preventing or treating medicine | |
| CN103356580A (en) | Application of Sarcaboside A in medicine for preventing pancreatic fibrosis | |
| CN102861028B (en) | Application of Gypensapogenin B in medicine for preventing or treating pancreatic fibrosis | |
| CN102872143B (en) | Application of Houttuynoid D in drug for preventing or treating pancreatic fibrosis | |
| CN102872126B (en) | Application of Houttuynoid E in medicament for preventing or treating pancreatic fibrosis | |
| CN102872054B (en) | Application of gypensapogenin A in preparing medicine for pancreatic fibrosis prevention and treatment drugs | |
| CN102872124B (en) | Application of Houttuynoid A in medicament for preventing or treating pancreatic fibrosis | |
| CN102872127B (en) | Application of Houttuynoid C in medicament for preventing or treating pancreatic fibrosis | |
| CN106265689A (en) | Friedolanostanes application in preparation prevention or treatment pancreatic gland fibrosis medicine | |
| CN106344565A (en) | Application of Ternatusine A in preparation of drugs for preventing or treating pancreatic fibrosis | |
| CN103393659A (en) | Application of Sarcaboside B to medicament for prevention of pancreatic fibrosis | |
| CN103340875A (en) | Application of compound in preparation of medicine for preventing or treating pancreatic fibrosis | |
| CN103120660A (en) | Application of Eryngiolide A in medicine for preventing or treating pancreatic fibrosis | |
| CN103120686A (en) | Application of Aphanamixoid A in medicine for preventing or treating pancreatic fibrosis | |
| CN103285005A (en) | Application of compound in preparation of medicaments for preventing or treating pancreatic fibrosis | |
| CN106344556A (en) | Application of Fistulains B in drugs for pancreatic fibrosis prevention or treatment | |
| CN102872120A (en) | Application of Houttuynoid B in medicament for preventing or treating pancreatic fibrosis | |
| CN105193791A (en) | Composition and application thereof in medicine for preventing or treating pancreatic fibrosis | |
| CN104739846A (en) | Application of O-(1H-tetrazole) ethyl derivative of cleistanone to preparing drug for preventing or treating pancreatic fibrosis |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160420 |
|
| WD01 | Invention patent application deemed withdrawn after publication |