CN106265689A - Friedolanostanes application in preparation prevention or treatment pancreatic gland fibrosis medicine - Google Patents
Friedolanostanes application in preparation prevention or treatment pancreatic gland fibrosis medicine Download PDFInfo
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- CN106265689A CN106265689A CN201610803223.0A CN201610803223A CN106265689A CN 106265689 A CN106265689 A CN 106265689A CN 201610803223 A CN201610803223 A CN 201610803223A CN 106265689 A CN106265689 A CN 106265689A
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- friedolanostanes
- pancreatic gland
- gland fibrosis
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- preparation prevention
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- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- 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)
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Abstract
The invention discloses Friedolanostanes application in preparation prevention or treatment pancreatic gland fibrosis medicine.The Friedolanostanes that the present invention relates to purposes in preparing anti-pancreatic gland fibrosis medicine belongs to first public, owing to framework types belongs to brand-new framework types, and it is unexpectedly strong for pancreatic gland fibrosis inhibitory activity, there is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for anti-pancreatic gland fibrosis and obviously have the most progressive.
Description
Technical field
The present invention relates to the new application of compound Friedolanostanes, particularly relate to Friedolanostanes in system
Application in standby prevention or treatment pancreatic gland fibrosis medicine.
Background technology
The current sickness rate of pancreatic gland fibrosis is the highest, is badly in need of the anti-pancreatic gland fibrosis medicine of research and development high-efficiency low-toxicity.
The compound Friedolanostanes that the present invention relates to be one within 2014, deliver (Saranyoo Klaiklay,
et al.,Friedolanostanes and xanthones from the twigs of Garcinia
Hombroniana.Phytochemistry, 85 (2013) 161 166.) noval chemical compound, this compound has brand-new skeleton
Type, current purposes merely relates to treat (Saranyoo Klaiklay, et al., the Friedolanostanes such as dysentery
and xanthones from the twigs of Garcinia hombroniana.Phytochemistry,85(2013)
161 166.), the Friedolanostanes for the present invention relates in preparation prevention or treats in pancreatic gland fibrosis medicine
Purposes belongs to first public, and owing to belonging to brand-new structure type, and it is strong for prevention or treatment pancreatic gland fibrosis activity
Obtain unexpected, there is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for
Prevention or treatment pancreatic gland fibrosis obviously have the most progressive.
Summary of the invention
The technical problem to be solved is, by designing animal experimental technique, to study Friedolanostanes
Anti-pancreatic gland fibrosis effect.
Described compound Friedolanostanes structure is as shown in formula I:
Therefore, it is an object of the invention to provide Friedolanostanes at preparation prevention or the medicine for the treatment of pancreatic gland fibrosis
Application in thing.
The most progressive effect of the present invention is: Friedolanostanes has the effect of anti-pancreatic gland fibrosis, so
The application of Friedolanostanes has good DEVELOPMENT PROSPECT.
The Friedolanostanes that the present invention relates to purposes in preparing anti-pancreatic gland fibrosis medicine belongs to public first
Opening, owing to framework types belongs to brand-new framework types, and it is unexpectedly strong for pancreatic gland fibrosis inhibitory activity, no
There is the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for anti-pancreatic gland fibrosis
Obviously have the most progressive.
Detailed description of the invention
The preparation method of compound Friedolanostanes involved in the present invention sees document (Saranyoo
Klaiklay, et al., Friedolanostanes and xanthones from the twigs of Garcinia
hombroniana.Phytochemistry,85(2013)161–166.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Execute any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound Friedolanostanes tablet involved in the present invention:
Take 20 g of compound Friedolanostanes additions and prepare the customary adjuvant 180 grams of tablet, mixing, Conventional compression
Machine makes 1000.
Embodiment 2: the preparation of compound Friedolanostanes capsule involved in the present invention:
Take 20 g of compound Friedolanostanes additions and prepare the customary adjuvant such as starch 180 grams of capsule, mixing,
Encapsulated make 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
One, prevent or treat pancreatic gland fibrosis experimentation
1 material
1.1 animal Wistar rats, male, body weight 180-200g.
1.2Friedolanostanes dosage: tri-dosage of 0.3mg/kg, 0.9mg/kg, 2.7mg/kg.
2 experimental techniques
2.1 modeling method Wistar rats, with lumbar injection dl-ethionine 250mg/ days, continuous 2 months, may occur in which pancreas
Dirty glandular cell reduces, the adipocellular hypertrophy of interstitial.
2.2 packet and medications
Rat model is randomly divided into model group, Friedolanostanes 0.3mg/kg, 0.9mg/kg, 2.7mg/kg tri-
Individual dosage group, separately sets blank group, is administered after modeling starts, oral continuous 30 days；Animal is dissected when 60 days.
2.3 Testing index
2.3.1 take pancreas at the end of experiment to weigh, calculate organ coefficient.
2.3.2 pancreas hydroxyproline content measures and takes 100mg sample and be homogenized in water, and in 110 DEG C of 10N HCl, hydrolysis 20 is little
Time.HCl nitrogen volatilizees, and hydrolyzate filters after dissolving with distilled water.Take 0.5ml liquid and 3ml citric acid phosphate buffer
(0.15M citric acid adds 0.6M disodium hydrogen phosphate) and 0.5ml are dissolved in the 1M periodic acid mixing of 9M phosphoric acid.Add 1.75ml and extract buffering
Liquid (5 parts of toluene: 5 parts of 2-methyl isophthalic acid-propanol: 2 parts of 1-propanol), shakes 30min, centrifugal.Tissue phase (0.6ml) and Ehrlich,
15min is placed in the mixing of s reagent.Measure trap at 565nm, make standard curve with 4-hydroxyl-1-proline and calculate concentration, content
Represent with ug/g tissue.
2.3.3 histological examination pancreatic tissues is fixed with 10% formalin, paraffin embedding, microscopy after dyeing.To inflammation
Cellular infiltration, interstitial edema, fibrosis, pancreas room necrocytosis, and bleeding scoring (0-3 divides).
3 results
3.1 Friedolanostanes are on rat pancreas weight and the impact of organ coefficient
At the end of experiment, rat put to death, dissect, weigh in and pancreas weighs and calculate the ratio of itself and body weight, result
It is shown in Table 1.The Friedolanostanes impact on 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 content measures
At the end of experiment, each group of rat is carried out pulmonary's hydroxyproline content mensuration, result such as table 2.
The Friedolanostanes impact on 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
Pancreas surrounding catheter extensive inflammation reaction seen from 60th day；Addicted to middle granulocyte karyolymph cellular infiltration, interstitial edema is hemorrhage and even
See that pancreas cystencyte is downright bad；Between pancreas cystencyte disappearance position and pancreas bubble, fibrosis occurs.Friedolanostanes can dose-dependant
Property reduce inflammatory reaction, tissue edema and fibrosis.Appraisal result is shown in Table 3.The Friedolanostanes impact on scoring, with
Model group compares significant difference.
Table 3
* represent p < 0.05, * * p < 0.01, compare with model group
Conclusion: the present invention by Friedolanostanes impact Fibrotic on pancreas in rat it was confirmed
Friedolanostanes has the effect of anti-pancreatic gland fibrosis.Therefore, Friedolanostanes can use as active component
In the medicine preparing anti-pancreatic gland fibrosis.
Claims (1)
1.Friedolanostanes application in prevention or treatment pancreatic gland fibrosis medicine, described compound
Friedolanostanes structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610803223.0A CN106265689A (en) | 2016-09-06 | 2016-09-06 | Friedolanostanes application in preparation prevention or treatment pancreatic gland fibrosis medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610803223.0A CN106265689A (en) | 2016-09-06 | 2016-09-06 | Friedolanostanes application in preparation prevention or treatment pancreatic gland fibrosis medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106265689A true CN106265689A (en) | 2017-01-04 |
Family
ID=57710832
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610803223.0A Pending CN106265689A (en) | 2016-09-06 | 2016-09-06 | Friedolanostanes application in preparation prevention or treatment pancreatic gland fibrosis medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106265689A (en) |
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2016
- 2016-09-06 CN CN201610803223.0A patent/CN106265689A/en active Pending
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| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170104 |
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| WD01 | Invention patent application deemed withdrawn after publication |