CN103356653B - The application of Chukrasone A in preparation treatment or preventing canker sore medicine - Google Patents
The application of Chukrasone A in preparation treatment or preventing canker sore medicine Download PDFInfo
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- CN103356653B CN103356653B CN201310279228.4A CN201310279228A CN103356653B CN 103356653 B CN103356653 B CN 103356653B CN 201310279228 A CN201310279228 A CN 201310279228A CN 103356653 B CN103356653 B CN 103356653B
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- Prior art keywords
- chukrasone
- day
- chukrasonea
- preparation treatment
- treatment
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- 238000011282 treatment Methods 0.000 title claims abstract description 15
- 239000003814 drug Substances 0.000 title claims abstract description 13
- 238000002360 preparation method Methods 0.000 title claims abstract description 12
- 208000020670 canker sore Diseases 0.000 title claims abstract description 6
- HZUBWSRMDOJYPS-WPCVKUBSSA-N chukrasone A Natural products C=1([C@@H]2OC(=O)C[C@H]3[C@@]4(O)[C@H](O)C(=O)[C@@]5(O)[C@@H](OC(=O)C(C)C)C(C)(C)[C@@H]([C@]5([C@H]4[C@H](OC(C)=O)C[C@]32C)C)CC(=O)OC)C=COC=1 HZUBWSRMDOJYPS-WPCVKUBSSA-N 0.000 title description 2
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 claims description 6
- 208000007117 Oral Ulcer Diseases 0.000 abstract description 12
- 208000002399 aphthous stomatitis Diseases 0.000 abstract description 12
- 150000001875 compounds Chemical class 0.000 abstract description 7
- 229930187319 chukrasone Natural products 0.000 abstract 2
- 208000025865 Ulcer Diseases 0.000 description 14
- 231100000397 ulcer Toxicity 0.000 description 14
- 230000035876 healing Effects 0.000 description 9
- 230000003203 everyday effect Effects 0.000 description 6
- 241000700159 Rattus Species 0.000 description 5
- 239000002671 adjuvant Substances 0.000 description 4
- 239000006189 buccal tablet Substances 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 3
- 229940046011 buccal tablet Drugs 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 206010002091 Anaesthesia Diseases 0.000 description 2
- 206010028034 Mouth ulceration Diseases 0.000 description 2
- 230000037005 anaesthesia Effects 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 210000002200 mouth mucosa Anatomy 0.000 description 2
- 230000000306 recurrent effect Effects 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 244000241235 Citrullus lanatus Species 0.000 description 1
- 235000012828 Citrullus lanatus var citroides Nutrition 0.000 description 1
- 240000001624 Espostoa lanata Species 0.000 description 1
- 235000009161 Espostoa lanata Nutrition 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 102000016943 Muramidase Human genes 0.000 description 1
- 108010014251 Muramidase Proteins 0.000 description 1
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 description 1
- 102000004257 Potassium Channel Human genes 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000000721 bacterilogical effect Effects 0.000 description 1
- 238000001354 calcination Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- RNFNDJAIBTYOQL-UHFFFAOYSA-N chloral hydrate Chemical compound OC(O)C(Cl)(Cl)Cl RNFNDJAIBTYOQL-UHFFFAOYSA-N 0.000 description 1
- 229960002327 chloral hydrate Drugs 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 208000026278 immune system disease Diseases 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 238000011221 initial treatment Methods 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 229960000274 lysozyme Drugs 0.000 description 1
- 235000010335 lysozyme Nutrition 0.000 description 1
- 239000004325 lysozyme Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000036407 pain Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 108020001213 potassium channel Proteins 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Do you the present invention relates to Chukrasone? the application of A in preparation treatment or preventing canker sore medicine.The Chukrasone that the present invention relates to? the purposes of A in preparation treatment stomatocace medicine belongs to first public, because framework types belongs to brand-new framework types, and its treatment oral ulcer is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for the treatment of oral ulcer simultaneously and obviously there is significant progress.
Description
Technical field
The present invention relates to the application of ChukrasoneA in preparation treatment or preventing canker sore medicine.
Background technology
Recurrent oral ulceration is modal disease in diseases of oral mucosa.The first place of prevalence office diseases of oral mucosa.Sircus (1975) investigates 1587 people, and prevalence is 20%.As can be seen here, oral ulcer patient is a very huge colony.The cause of disease of recurrent oral ulceration is complicated, still indefinite so far, may be relevant with the factor such as the endocrine regulation of viral infection, bacteriological infection and body, immune dysfunction.
The primary treatment measure of oral ulcer comprises topical therapeutic and whole body therapeutic, and because topical therapeutic toxic and side effects is lower, the people therefore obtaining people can.Although the buccal tablets that the local that occurs in recent years uses carries, easy to use, mouthfeel and compliance better, as lysozyme buccal tablet, watermelon crystal buccal tablet, cydiodine etc., these medicines emphasize particularly on different fields in sterilization, antiinflammatory, pain relieving etc.
The Compound C hukrasoneA that the present invention relates to is one and delivers (Liu in 2012, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to potassium-channel inhibit activities (Liu, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.), the purposes of the ChukrasoneA that the present invention relates in preparation treatment stomatocace medicine is belonged to first public, because framework types belongs to brand-new framework types, and its treatment oral ulcer is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, be used for the treatment of oral ulcer simultaneously and obviously there is significant progress.
Summary of the invention
The invention provides the application of ChukrasoneA in preparation treatment or preventing canker sore medicine.
Described Compound C hukrasoneA structure is as shown in formula I:
The purposes of the ChukrasoneA that the present invention relates in preparation treatment stomatocace medicine belongs to first public, because framework types belongs to brand-new framework types, and its treatment oral ulcer is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for the treatment of oral ulcer simultaneously and obviously there is significant progress.
Detailed description of the invention
The preparation method of Compound C hukrasoneA involved in the present invention is see document (Liu, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.).
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 C hukrasoneA tablet involved in the present invention:
Get 20 g of compound ChukrasoneA, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasoneA capsule involved in the present invention:
Get 20 g of compound ChukrasoneA, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The experimental study of test example 1ChukrasoneA anti-oral ulcer
1, test objective: manufacture Oral ulcer model with phenol, gives the ChukrasoneA of Oral ulcer model rat certain number of times every day, and whether observe ChukrasoneA has the effect reducing ulcer.
2, test medicine and reagent
Cydiodine (Beijing Sihuan Medicine Science and Technology Co., Ltd); Phenol
Animal: Wistar rat, male, body weight 240 ~ 280
3, test method
Get rat 50, male, body weight 240 ~ 280g, 10% chloral hydrate anesthesia, dosage: 0.35ml/100g, after anesthesia, plastic dropper (internal diameter: the 3mm) lower end of 90% phenol cotton balls being flat on rats with left bicker is about on the cheek film at 1mm place, calcination 30min, namely sees the white infringement of this place about 3mm.Divide into groups immediately after 24 hours, often organize 10, divide 5 groups, i.e. model group (adjuvant 4 times/day, not drug containing); ChukrasoneA high dose group (4 times/day, 0.5mg/ time); Dosage (4 times/day, 0.1mg/ time) in ChukrasoneA; ChukrasoneA low dose group (4 times/day, 0.02mg/ time); Positive controls: cydiodine group (4 times/day, 0.5mg/ time).ChukrasoneA and cydiodine buccal tablet pulverize before use, administration is degree of being with flap coverage.Successive administration 5 days, after the front and each administration of administration, next day observes ulcer area size (diameter in ulcer) and ulcer healing situation (being considered as healing without macroscopic ulcer), and first administration is recorded as 1,2,3,4,5,6 day respectively to last administration.Ulcer area size t checks, ulcer healing rate X
2inspection.
4, result of the test
Ulcer area compares (table 1): ChukrasoneA high dose group compares with model group, within the 3rd day, plays off-test from administration, and corresponding every day compares significant difference; Cydiodine group compares with model group, within the 3rd day, plays off-test from administration, and corresponding every day compares significant difference; In ChukrasoneA, dosage group compares with model group, within the 3rd day, plays off-test from administration, and corresponding every day compares significant difference; ChukrasoneA low dose group compares with model group, within the 5th day, plays off-test from administration, and corresponding every day compares significant difference; In ChukrasoneA, dosage group compares with cydiodine group, within the 1st day, plays off-test from administration, and corresponding every day compares significant difference.
Table 1 is on the impact of rat ulcer area
Note: compare with model group, * p<0.05, * p<0.01.
Healing rate (table 2): adjuvant group and ChukrasoneA low dose group play off-test on the 1st day from administration, and ulcer does not heal; And ChukrasoneA high dose group was from administration the 4th day, just there is ulcer healing, to off-test, reach 90%; Cydiodine group, from administration the 4th day, has ulcer healing, to off-test, reaches 60%; In ChukrasoneA, dosage group was from administration the 5th day, had ulcer healing, to off-test, reached 40%.
Table 2 is on the impact of rat ulcer healing time
Note: compare with model group, * p<0.05, * p<0.01.
5, conclusion
ChukrasoneA has the effect obviously promoting oral ulcer healing.
Claims (1)
1.ChukrasoneA preparation treatment or preventing canker sore medicine in application, described Compound C hukrasoneA structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310279228.4A CN103356653B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in preparation treatment or preventing canker sore medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310279228.4A CN103356653B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in preparation treatment or preventing canker sore medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103356653A CN103356653A (en) | 2013-10-23 |
| CN103356653B true CN103356653B (en) | 2015-11-25 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310279228.4A Expired - Fee Related CN103356653B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in preparation treatment or preventing canker sore medicine |
Country Status (1)
| Country | Link |
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| CN (1) | CN103356653B (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101322714A (en) * | 2008-07-25 | 2008-12-17 | 中国科学院昆明植物研究所 | Anti-herpes simplex virus I-form medicament composition and uses thereof |
-
2013
- 2013-07-04 CN CN201310279228.4A patent/CN103356653B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101322714A (en) * | 2008-07-25 | 2008-12-17 | 中国科学院昆明植物研究所 | Anti-herpes simplex virus I-form medicament composition and uses thereof |
Non-Patent Citations (1)
| Title |
|---|
| Chukrasone A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis;Liu,H.B.et al.;《Organic Letters》;20121231;第14卷(第17期);第4438–4441页 * |
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| Publication number | Publication date |
|---|---|
| CN103356653A (en) | 2013-10-23 |
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| C06 | Publication | ||
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| C41 | Transfer of patent application or patent right or utility model | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20151028 Address after: 266000 Licang, Qingdao, No. nine East water road, No. 320, No. Applicant after: Gu Xiangmao Address before: 210009 Gulou District, Jiangsu, Nanjing Gu Ping Kong, No. 4 Applicant before: Ding Shengyu |
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| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CB03 | Change of inventor or designer information |
Inventor after: Chai Liyun Inventor after: Yu Ling Inventor before: Ding Shengyu |
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Effective date of registration: 20170322 Address after: 457600 Puyang County, Zhejiang Province, the county paper mill family hospital No. 1 Patentee after: Chai Liyun Patentee after: Yu Ling Address before: 266000 Licang, Qingdao, No. nine East water road, No. 320, No. Patentee before: Gu Xiangmao |
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| CB03 | Change of inventor or designer information |
Inventor after: Cao Liping Inventor after: Yang Zechun Inventor before: Chai Liyun Inventor before: Yu Ling |
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Effective date of registration: 20180131 Address after: 046000 Shanxi Hsinying Changzhi City Street No. 50 Building No. 4 26 Co-patentee after: Yang Zechun Patentee after: Cao Liping Address before: No. 1, family hospital of Tai Qian County paper mill in Tai Qian County, Puyang, Henan Co-patentee before: Yu Ling Patentee before: Chai Liyun |
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| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20151125 Termination date: 20180704 |
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| CF01 | Termination of patent right due to non-payment of annual fee |