CN105326836A - Application of Alistonitrine A in preparing pancreatic fibrosis prevention or treatment medicine - Google Patents
Application of Alistonitrine A in preparing pancreatic fibrosis prevention or treatment medicine Download PDFInfo
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- CN105326836A CN105326836A CN201510777345.2A CN201510777345A CN105326836A CN 105326836 A CN105326836 A CN 105326836A CN 201510777345 A CN201510777345 A CN 201510777345A CN 105326836 A CN105326836 A CN 105326836A
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- alistonitrine
- pancreatic fibrosis
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- alistonitrinea
- treatment medicine
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Abstract
The invention discloses application of Alistonitrine A in preparing pancreatic fibrosis prevention or treatment medicine. The application of Alistonitrine A in preparing the pancreatic fibrosis prevention or treatment medicine is disclosed for the first time; as Alistonitrine A is of a bran-new skeleton type and has unexpectedly-strong inhibitory activity on pancreatic fibrosis, the possibility of gaining inspiration from other compounds does not exist, and Alistonitrine A has prominent substantial characteristics; meanwhile, Alistonitrine A obviously has remarkable progress when applied to resisting pancreatic fibrosis.
Description
Technical field
The present invention relates to the novelty teabag of compd A listonitrineA, particularly relate to the application of AlistonitrineA 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 compd A listonitrineA that the present invention relates to is one and delivers (Guo-YuanZhu in 2014, etal., AlistonitrineA, aCagedMonoterpeneIndoleAlkaloidfromAlstoniascholaris.Org anicLetters, 2014, 16, noval chemical compound 1080-1083.), this compound has brand-new framework types, current purposes only relates to (the Guo-YuanZhu such as treatment dysentery, etal., AlistonitrineA, aCagedMonoterpeneIndoleAlkaloidfromAlstoniascholaris.Org anicLetters, 2014, 16, 1080-1083.), the purposes of the AlistonitrineA that the present invention relates in preparation prevention or treatment pancreatic gland fibrosis medicine is belonged to first public, owing to belonging to brand-new structure type, and its for prevention or treatment pancreatic gland fibrosis active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, for prevention or treatment pancreatic gland fibrosis, obviously there is significant progress simultaneously.
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 AlistonitrineA.
Described compd A listonitrineA structure is as shown in formula I:
Therefore, the object of this invention is to provide AlistonitrineA prevent in preparation or treat the application in the medicine of pancreatic gland fibrosis.
Positive progressive effect of the present invention is: AlistonitrineA has the effect of anti-pancreatic gland fibrosis, so the application of AlistonitrineA has good DEVELOPMENT PROSPECT.
The purposes of the AlistonitrineA 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 compd A listonitrineA involved in the present invention is see document (Guo-YuanZhu, etal., AlistonitrineA, aCagedMonoterpeneIndoleAlkaloidfromAlstoniascholaris.Org anicLetters, 2014,16,1080-1083.)
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 compd A listonitrineA tablet involved in the present invention:
Get 20 g of compound AlistonitrineA and add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compd A listonitrineA capsule involved in the present invention:
Get 20 g of compound AlistonitrineA add prepare capsule customary adjuvant as starch 180 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.
1.2AlistonitrineA 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 AlistonitrineA0.3mg/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
3.1AlistonitrineA 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.AlistonitrineA, on the impact of pancreas organ coefficient, compares with model group and has significant difference.
Table 1
* represent p<0.05, compare with model group
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.AlistonitrineA, 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.AlistonitrineA can reduce inflammatory reaction, tissue edema and fibrosis by dose dependent.Appraisal result is in table 3.AlistonitrineA, 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 AlistonitrineA has the effect of anti-pancreatic gland fibrosis by AlistonitrineA.Therefore, AlistonitrineA can be used as the medicine of active component for the preparation of anti-pancreatic gland fibrosis.
Claims (1)
- The application of 1.AlistonitrineA in prevention or treatment pancreatic gland fibrosis medicine, described compd A listonitrineA structure is as shown in formula I:Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510777345.2A CN105326836A (en) | 2015-11-13 | 2015-11-13 | Application of Alistonitrine A in preparing pancreatic fibrosis prevention or treatment medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510777345.2A CN105326836A (en) | 2015-11-13 | 2015-11-13 | Application of Alistonitrine A in preparing pancreatic fibrosis prevention or treatment medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105326836A true CN105326836A (en) | 2016-02-17 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN201510777345.2A Pending CN105326836A (en) | 2015-11-13 | 2015-11-13 | Application of Alistonitrine A in preparing pancreatic fibrosis prevention or treatment medicine |
Country Status (1)
| Country | Link |
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| CN (1) | CN105326836A (en) |
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- 2015-11-13 CN CN201510777345.2A patent/CN105326836A/en active Pending
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Application publication date: 20160217 |