CN107281190A - A kind of medicine for treating digestive tract ulcer - Google Patents
A kind of medicine for treating digestive tract ulcer Download PDFInfo
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- CN107281190A CN107281190A CN201710555111.2A CN201710555111A CN107281190A CN 107281190 A CN107281190 A CN 107281190A CN 201710555111 A CN201710555111 A CN 201710555111A CN 107281190 A CN107281190 A CN 107281190A
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- bufalin
- resibufogenin
- cinobufagin
- digestive tract
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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
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
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- Chemical & Material Sciences (AREA)
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- 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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract
The present invention relates to drug field, and in particular to a kind of medicine for treating digestive tract ulcer.Described medicine includes resibufogenin, Cinobufagin or Bufalin；Or including the combination of resibufogenin, Cinobufagin and Bufalin, the weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1 ~ 2:1~4:1~3.Present invention research finds that resibufogenin, three kinds of compounds of Cinobufagin or Bufalin have the effect for the treatment of digestive tract ulcer, therefore can be used three kinds of compounds as the medicine for the treatment of digestive tract ulcer；In addition, the present invention further study show that will resibufogenin, Cinobufagin and Bufalin be combined after can produce the effect of obviously synergistic treatment digestive tract ulcer, and three be combined after can mutually be attenuated；It is especially 1 by weight by resibufogenin, Cinobufagin and Bufalin:1~3:After 1 ~ 2 mixing, the effect of its synergistic treatment digestive tract ulcer is most obvious.
Description
Technical field
The present invention relates to drug field, and in particular to a kind of medicine for treating digestive tract ulcer.
Background technology
Peptic ulcer refers mainly to betide stomach and duodenal chronic ulcer, is a frequently-occurring disease, common disease.Ulcer
Various factors is formed with, wherein acidic gastric juice is the Fundamentals of ulcer formation to the digestion of mucous membrane, is hence obtained one's name.Stomach is burst
Ulcer is most common one kind in digestive tract ulcer, and be primarily referred to as that stomach lining caused by peptic digest liquid autodigestion exceedes mucous membrane
The tissue damage of muscle layer.Its typical performance is hungry uncomfortable, glutted belch, pantothenic acid or the chronic middle Upper abdominal pain of timing after the meal,
Can there are melena and spitting blood when serious.
The dried venom of toads is the secretion of toad ear rear gland and epidermal gland, white milky liquid or pale yellow syrup, poisonous.The dried venom of toads
Slurries are extracted, are dried, are painted, can be used as medicine after sealing preserve.With detoxifying, ease pain, have one's ideas straightened out, a variety of functions such as antitumor and by
Extensive use.But because the dried venom of toads has certain toxicity, therefore, it also limit its clinical practice.
It is existing studies have found that, substantial amounts of arenobufagin class, steroid and alkaloids chemical composition, ester are contained in the dried venom of toads
Bufotalin, Cinobufagin and Bufalin are the arenobufagin class material in the dried venom of toads.But the open dried venom of toads is not had been reported that at present
Or the specific composition in the dried venom of toads is used to treat digestive tract ulcer.Using bufanolide as starting point, a kind of chemistry of exploitation
Definite ingredients, the efficient, anti-inflammatory drug of low toxicity have wide market prospects.
The content of the invention
The technical problems to be solved by the invention are to provide a kind of medicine for treating digestive tract ulcer.
Above mentioned problem to be solved by this invention, is achieved by the following technical programs：
The application of resibufogenin, Cinobufagin or Bufalin in the medicine for preparing treatment digestive tract ulcer.
The application of resibufogenin, Cinobufagin and Bufalin combination in the medicine for preparing treatment digestive tract ulcer.
Preferably, the weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1~2:1~4:1~3.
It is further preferred that the weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1:1~4:1~
3。
It is further preferred that the weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1:1~3:1
~2.
Invention shows that resibufogenin, Cinobufagin and Bufalin have treatment alimentary canal by lot of experiments
The effect of ulcer.Further study showed that can be produced obviously after resibufogenin, Cinobufagin and Bufalin combination
Can mutually it be attenuated after the effect of synergistic treatment digestive tract ulcer, and three's combination.Therefore, by resibufogenin, magnificent dried venom of toads poison
It can make to treat the medicine of digestive tract ulcer after base and Bufalin or three's combination.
A kind of medicine for treating digestive tract ulcer, includes resibufogenin, Cinobufagin or Bufalin.
Preferably, the medicine of described treatment digestive tract ulcer, includes resibufogenin, Cinobufagin and Bufalin
Combination, the weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1~2:1~4:1~3.
It is further preferred that the weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1:1~4:1~
3。
It is further preferred that the weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1:1~3:1
~2.
Preferably, the formulation of the medicine of described treatment digestive tract ulcer is liquid injection agent, powder-injection, tablet, capsule
Agent, soft capsule, powder, pill, oral liquid, paste, granule or dressing.
Preferably, described medicine also includes pharmaceutically acceptable carrier.
Beneficial effect：Present invention research finds that resibufogenin, three kinds of compounds of Cinobufagin or Bufalin have and controlled
The effect of digestive tract ulcer is treated, therefore can be used three kinds of compounds as the medicine for the treatment of digestive tract ulcer；In addition, this hair
It is bright further study show that will resibufogenin, Cinobufagin and Bufalin be combined after can produce obviously synergistic treatment
Can mutually it be attenuated after the effect of digestive tract ulcer, and three's combination.Especially by resibufogenin, Cinobufagin and toadpoison
Spirit is 1 by weight:1~3:After 1~2 mixing, the effect of its synergistic treatment digestive tract ulcer is most obvious.
Embodiment
The present invention is explained further below in conjunction with specific embodiment, but embodiment does not do any type of limit to the present invention
It is fixed.
The Antiulcer activity of embodiment 1 is tested
Modeling：Take 200g ± 20g Wistar male rats 300, fasting 48h, free water.Anesthetized rat, opens abdomen
Chamber, exposure stomach, injection 0.1mL volume fractions are 10% at 0.5mm under rat serous coat (body of stomach and pyloric antrum intersection)
Acetic acid.Suturing them, reduction stomach.Postoperative rat free water, next day starts normal raising.
Wistar rats after modeling success are divided into 1 group of blank control group and 14 groups of experimental groups, every group 20；Blank pair
Distilled water gavage was used after the 3rd day according to group, medicine to be measured was added distilled water to be configured to solution progress gavage by experimental group after the 3rd day
It is administered (dosage is 10mg/kg)；Successive administration puts to death rat after 7 days, opens abdomen, full stomach and takes out.1% Fu Er is injected into stomach
Malin 15ml, then stomach is soaked in 15min fixations stomach ectonexine in 1% formalin.Stomach is cut off along greater curvature, stomach is turned up,
Gastric content is removed, stomach is flattened on glass plate, corresponding mucosal surface observation ulcer is formed at injection acetic acid solution position
Situation.It has been observed that being injected under rat stomach serous coat after acetic acid, gastric tissue is damaged, and ulcer is oval or circle, central concave,
The micro- protuberance of surrounding.Each administration group has quality ulcer function, and the degree that the gastric tissue of administration group is impaired is substantially slight.Specific system
Reckon by the piece table 1.
The medication composition of each experimental group is as follows：
Resibufogenin is used alone in experimental group 1；
Cinobufagin is used alone in experimental group 2；
Bufalin is used alone in experimental group 3；
Experimental group 4 is 1 using weight ratio:2 resibufogenin and Cinobufagin；
Experimental group 5 is 2 using weight ratio:1.5 Cinobufagin and Bufalin；
Experimental group 6 is 1 using weight ratio:1.5 resibufogenin and Bufalin；
Experimental group 7 is 1 using weight ratio:2:1.5 resibufogenin, Cinobufagin and Bufalin；
Experimental group 8 is 1 using weight ratio:3:2 resibufogenin, Cinobufagin and Bufalin；
Experimental group 9 is 1 using weight ratio:1:1 resibufogenin, Cinobufagin and Bufalin；
Experimental group 10 is 1 using weight ratio:1:2 resibufogenin, Cinobufagin and Bufalin；
Experimental group 11 is 1 using weight ratio:4:3 resibufogenin, Cinobufagin and Bufalin；
Experimental group 12 is 1 using weight ratio:3:3 resibufogenin, Cinobufagin and Bufalin；
Experimental group 13 is 2 using weight ratio:1:1 resibufogenin, Cinobufagin and Bufalin；
Experimental group 14 is 2 using weight ratio:4:3 resibufogenin, Cinobufagin and Bufalin；
The test effect of the present embodiment drug therapy digestive tract ulcer of table 1.
As can be seen from Table 1, stomach can effectively be suppressed by resibufogenin, Cinobufagin or Bufalin being used alone
The generation of ulcer, illustrates that resibufogenin, Cinobufagin or Bufalin have the effect for the treatment of gastric ulcer.In addition, by ester toad
It is same after malicious aglucon, Cinobufagin or Bufalin combination of two that there is treatment ulcer function, but and there are no collaboration quality stomach
Ulcer function.
As can be seen from Table 1, after resibufogenin, Cinobufagin or Bufalin three being combined, it is to rat
Ulcer rates be used alone significantly lower than resibufogenin, Cinobufagin or Bufalin or any combination.This
Illustrate that obvious synergistic treatment gastric ulcer effect can be produced after combining resibufogenin, Cinobufagin or Bufalin three.
Especially shown in experimental group 7~10, its ulcer rates to rat is less than 25%, this explanation resibufogenin, magnificent dried venom of toads poison
Base and Bufalin are 1 by weight:1~3:1~2, which is combined rear its, cooperates with the effect of quality gastric ulcer optimal.
In summary, resibufogenin, Cinobufagin or Bufalin can disappear separately as active ingredient for treatment
Change road ulcer, can also two-by-two mix and treat digestive tract ulcer as active ingredient, it is particularly possible to will make after their three's combinations
It is used for treating digestive tract ulcer for active ingredient.
The cytotoxicity test of the medicine of the present invention of embodiment 2
By Hep-2 cell culture in 96 well culture plates, after cell monolayer length is good, what addition maintaining liquid had diluted is
The μ L of row concentration samples solution 100, in 5%CO2, cultivate 3 days in 37 DEG C of incubators；Then 10 μ lMTT solution, MTT solution are added
Concentration be 5mg/mL, configured with cushioning liquid, continue cultivate 4 hours；Sample solution is suctioned out, dimethyl sulfoxide is added, at room temperature,
96 orifice plates are placed in micro- emptying aperture plate oscillator and vibrated 10 minutes；The OD values in each hole are determined with ELIASA, measurement wavelength is
570nm, reference wavelength is 630nm, calculates median lethal toxic concentration (CC of the sample to cell50).Every group sets 4 balance pipes,
Every group of experiment is repeated 3 times.Result of calculation, draws curve, obtains half toxic concentration (CC50)。
Testing sample is respectively：Resibufogenin；Bufalin；Cinobufagin；Resibufogenin：Cinobufagin (1:
2)；Cinobufagin：Bufalin (2:1.5)；Resibufogenin：Bufalin (1:1.5)；Resibufogenin：Cinobufagin：Toad
Malicious spirit (1:2:1.5)；Resibufogenin：Cinobufagin：Bufalin (1:3:2)；Resibufogenin：Cinobufagin：Toadpoison
Spirit (1:1:1)；Resibufogenin：Cinobufagin：Bufalin (1:1:2)；Resibufogenin：Cinobufagin：Bufalin (1:
4:3)；Resibufogenin：Cinobufagin：Bufalin (1:3:3)；Resibufogenin：Cinobufagin：Bufalin (2:1:1)；
Aforementioned proportion is weight ratio.
The cytotoxicity test test result of table 2.
| Sample | CC50It is worth (μM) |
| Resibufogenin | 17.42 |
| Bufalin | 25.15 |
| Cinobufagin | 21.38 |
| Resibufogenin：Cinobufagin (1:2) | 19.98 |
| Cinobufagin：Bufalin (2:1.5) | 24.03 |
| Resibufogenin：Bufalin (1:1.5) | 22.38 |
| Resibufogenin：Cinobufagin：Bufalin (1:2:1.5) | 68.21 |
| Resibufogenin：Cinobufagin：Bufalin (1:3:2) | 66.44 |
| Resibufogenin：Cinobufagin：Bufalin (1:1:1) | 65.34 |
| Resibufogenin：Cinobufagin：Bufalin (1:1:2) | 65.95 |
| Resibufogenin：Cinobufagin：Bufalin (1:4:3) | 62.25 |
| Resibufogenin：Cinobufagin：Bufalin (1:3:3) | 60.38 |
| Resibufogenin：Cinobufagin：Bufalin (2:1:1) | 61.14 |
As can be seen that resibufogenin, Cinobufagin and Bufalin or the group of the two is used alone from the data of table 2
Close, its CC to cell50Value is far smaller than the combination of resibufogenin, Cinobufagin and Bufalin three, this explanation ester toad
After malicious aglucon, Cinobufagin and Bufalin three combination the cytotoxicity after three's combination is greatly reduced, can occur phase
Mutual attenuation.
Embodiment 3 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 1:2:1.5 mixing are as active ingredient, then
Powder-injection is made by the conventional method of pharmaceutical field.
Embodiment 4 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 1:3:Then 2 mixing press as active ingredient
Powder-injection is made in the conventional method of pharmaceutical field.
Embodiment 5 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 1:1:Then 1 mixing presses as active ingredient
Liquid injection agent is made in the conventional method of pharmaceutical field.
Embodiment 6 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 1:1:Then 1 mixing presses as active ingredient
Tablet is made in the conventional method of pharmaceutical field.
Embodiment 7 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 1:4:Then 3 mixing press as active ingredient
Capsule is made in the conventional method of pharmaceutical field.
Embodiment 8 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 2:1:Then 1 mixing presses as active ingredient
Powder is made in the conventional method of pharmaceutical field.
Embodiment 9 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 2:4:Then 3 mixing press as active ingredient
Oral liquid is made in the conventional method of pharmaceutical field.
Embodiment 10 treats the medicine of digestive tract ulcer
By Bufalin, resibufogenin and telecinobufagin by weight 2:3:Then 2 mixing press as active ingredient
Oral liquid is made in the conventional method of pharmaceutical field.
Claims (10)
1. the application of resibufogenin, Cinobufagin or Bufalin in the medicine for preparing treatment digestive tract ulcer.
2. the application of resibufogenin, Cinobufagin and Bufalin combination in the medicine for preparing treatment digestive tract ulcer.
3. application according to claim 2, it is characterised in that described resibufogenin, Cinobufagin and Bufalin
Weight ratio be 1 ~ 2:1~4:1~3.
4. application according to claim 3, it is characterised in that described resibufogenin, Cinobufagin and Bufalin
Weight ratio be 1:1~4:1~3.
5. application according to claim 3, it is characterised in that described resibufogenin, Cinobufagin and Bufalin
Weight ratio be 1:1~3:1~2.
6. a kind of medicine for treating digestive tract ulcer, it is characterised in that include resibufogenin, Cinobufagin or Bufalin；
The weight ratio of described resibufogenin, Cinobufagin and Bufalin is 1 ~ 2:1~4:1~3.
7. the medicine for the treatment of digestive tract ulcer according to claim 6, it is characterised in that described resibufogenin, China
The weight ratio of bufalin and Bufalin is 1:1~4:1~3.
8. the medicine for the treatment of digestive tract ulcer according to claim 7, it is characterised in that described resibufogenin, China
The weight ratio of bufalin and Bufalin is 1:1~3:1~2.
9. the medicine of the treatment digestive tract ulcer according to any one of claim 6 ~ 8, it is characterised in that described treatment disappears
Change road ulcer medicine formulation for liquid injection agent, powder-injection, tablet, capsule, soft capsule, powder, pill, oral liquid,
Paste, granule or dressing.
10. the medicine of the treatment digestive tract ulcer according to any one of claim 6 ~ 8, it is characterised in that described medicine
Also include pharmaceutically acceptable carrier.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710555111.2A CN107281190A (en) | 2017-07-10 | 2017-07-10 | A kind of medicine for treating digestive tract ulcer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710555111.2A CN107281190A (en) | 2017-07-10 | 2017-07-10 | A kind of medicine for treating digestive tract ulcer |
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| Publication Number | Publication Date |
|---|---|
| CN107281190A true CN107281190A (en) | 2017-10-24 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710555111.2A Pending CN107281190A (en) | 2017-07-10 | 2017-07-10 | A kind of medicine for treating digestive tract ulcer |
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| Country | Link |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101564418A (en) * | 2009-05-26 | 2009-10-28 | 华中科技大学 | Pharmaceutical composition for treating oral ulcer and Behcet syndrome |
| CN105125592A (en) * | 2015-10-12 | 2015-12-09 | 北京诺康达医药科技有限公司 | Medicine containing toad venom lipid-soluble substances and preparation method thereof |
-
2017
- 2017-07-10 CN CN201710555111.2A patent/CN107281190A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101564418A (en) * | 2009-05-26 | 2009-10-28 | 华中科技大学 | Pharmaceutical composition for treating oral ulcer and Behcet syndrome |
| CN105125592A (en) * | 2015-10-12 | 2015-12-09 | 北京诺康达医药科技有限公司 | Medicine containing toad venom lipid-soluble substances and preparation method thereof |
Non-Patent Citations (4)
| Title |
|---|
| ZE-JUN WANG 等: "Resibufogenin and Cinobufagin Activate Central Neurons through an Ouabain-Like Action", 《TOAD VENOMS ACT ON NEURONS》 * |
| 张存良: "华蟾素穴位注射治疗顽固性呃逆的临床疗效观察", 《中医临床研究》 * |
| 苏永华 等: "华蟾素注射液中蟾毒内酯类成分含量检测", 《中成药》 * |
| 许锡元: "放疗同时口服华始索液治疗溃疡型食管癌35例分析", 《中国抗癌协会会议论文集》 * |
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Application publication date: 20171024 |