CN103462951A - Application of scopariusins in preparation of medicine treating or preventing canker sore - Google Patents
Application of scopariusins in preparation of medicine treating or preventing canker sore Download PDFInfo
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- CN103462951A CN103462951A CN201310470463XA CN201310470463A CN103462951A CN 103462951 A CN103462951 A CN 103462951A CN 201310470463X A CN201310470463X A CN 201310470463XA CN 201310470463 A CN201310470463 A CN 201310470463A CN 103462951 A CN103462951 A CN 103462951A
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- Prior art keywords
- scopariusins
- canker sore
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- preparation
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- 229930191324 scopariusin Natural products 0.000 title claims abstract description 31
- 208000020670 canker sore Diseases 0.000 title claims abstract description 13
- 239000003814 drug Substances 0.000 title claims abstract description 12
- 238000002360 preparation method Methods 0.000 title claims abstract description 11
- 238000011282 treatment Methods 0.000 claims abstract description 11
- 150000001875 compounds Chemical class 0.000 claims description 11
- 230000000694 effects Effects 0.000 abstract description 4
- 239000011159 matrix material Substances 0.000 abstract 2
- 208000025865 Ulcer Diseases 0.000 description 14
- 231100000397 ulcer Toxicity 0.000 description 14
- 230000035876 healing Effects 0.000 description 10
- 208000007117 Oral Ulcer Diseases 0.000 description 6
- 208000002399 aphthous stomatitis Diseases 0.000 description 6
- 230000003203 everyday effect Effects 0.000 description 6
- 241000700159 Rattus Species 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
- 241000554617 Isodon scoparius Species 0.000 description 3
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 3
- 230000003592 biomimetic effect Effects 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 229940046011 buccal tablet Drugs 0.000 description 3
- ZFYQTYYYCYTQSH-YWMUFLPLSA-N isoscoparin N Natural products COC(=O)C=C(/C)C[C@H](O)[C@@]1(C)[C@H](C)CCC2=C1CCCC2(C)C ZFYQTYYYCYTQSH-YWMUFLPLSA-N 0.000 description 3
- BDHATPNMGPTWJB-OAHLLOKOSA-N scopariusin A Natural products COC(=O)C=C(/C)CC1=C(C)[C@H](C)CCC2=C1CCCC2(C)C BDHATPNMGPTWJB-OAHLLOKOSA-N 0.000 description 3
- 238000003786 synthesis reaction Methods 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
- 229940079593 drug Drugs 0.000 description 2
- 239000000203 mixture 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
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 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
- 241000700157 Rattus norvegicus Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 238000001354 calcination Methods 0.000 description 1
- 239000002775 capsule Substances 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
- 235000019425 dextrin Nutrition 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 208000026278 immune system disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000011221 initial treatment Methods 0.000 description 1
- 239000004325 lysozyme Substances 0.000 description 1
- 229960000274 lysozyme Drugs 0.000 description 1
- 235000010335 lysozyme Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 201000001441 melanoma Diseases 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
- 238000011552 rat model Methods 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
- 239000003826 tablet Substances 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
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides the application of scopariusins in preparation of the medicine treating or preventing the canker sore. The application is disclosed for the first time. The matrix type of the scopariusins belongs to a brand new matrix type. The scopariusins has the advantages of being high in activity of treatment of the canker sore and prominent in substantive features, and makes remarkable progress in treatment of the canker sore.
Description
Technical field
The present invention relates to the new purposes of compound S copariusins, relate in particular to the application of Scopariusins 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) investigate 1587 people, prevalence is 20%.As can be seen here, the oral ulcer patient is a very huge colony.The cause of disease complexity of recurrent oral ulceration, still indefinite so far, may infect with viral infection, antibacterial and the factors such as the endocrine regulation of body, immune dysfunction relevant.The primary treatment measure of oral ulcer comprises topical therapeutic and whole body therapeutic, and because the topical therapeutic toxic and side effects is lower, the people who has therefore obtained people can.Although the buccal tablets that the part occurred is in recent years used carries, easy to use, mouthfeel and compliance are better, and as lysozyme buccal tablet, watermelon crystal buccal tablet, cydiodine etc., these medicines emphasize particularly on different fields at aspects such as sterilization, antiinflammatory, pain relievings.
The compound S copariusins the present invention relates to is one and within 2013, delivers (Min Zhou, et al., Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodon scoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.Organic Letters, 2013, 15(2): noval chemical compound 314 – 317.), this compound has brand-new framework types, research finds that melanoma cell etc. is not had to significant inhibitory action (Min Zhou, et al., Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodon scoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.Organic Letters, 2013, 15(2): 314 – 317.), the purposes of the Scopariusins the present invention relates in preparation treatment or preventing canker sore medicine belongs to open first.
Summary of the invention
The object of the invention is to, according in existing Scopariusins research, not finding that it has the present situation of the report for the treatment of or preventing canker sore, provides the application of Scopariusins in preparation treatment or preventing canker sore medicine.
Described compound S copariusins structure is as shown in formula I:
The purposes of the Scopariusins the present invention relates in preparation treatment or preventing canker sore medicine belongs to open first, because framework types belongs to brand-new framework types, and its treatment or preventing canker sore are active strong, possess outstanding substantive distinguishing features, be used for the treatment of or preventing canker sore obviously has significant progress simultaneously.
The specific embodiment
The preparation method of compound S copariusins involved in the present invention is referring to document (Min Zhou, et al., Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodon scoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.Organic Letters, 2013,15(2): 314 – 317.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound S copariusins tablet involved in the present invention:
Get 5 and digest compound Scopariusins and add dextrin 195 grams, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound S copariusins capsule involved in the present invention:
Get 5 and digest compound Scopariusins and add starch 195 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The experimental study of test example 1:Scopariusins anti-oral ulcer
1, test objective: whether manufacture the oral ulcer model with phenol, give the Scopariusins of the certain number of times of oral ulcer rat model every day, observing Scopariusins has the effect that reduces ulcer.
2, tested medicine and reagent
Cydiodine (Beijing Sihuan Medicine Science and Technology Co., Ltd); Phenol
Animal: the Wistar rat, male, body weight 240～280g, Nanjing Medical University's Experimental Animal Center.
3, test method
Get 50 of rats, male, body weight 240～280g, 10% chloral hydrate anesthesia, dosage: 0.35ml/100g, after anesthesia, by the plastic dropper of 90% phenol cotton balls, (internal diameter: 3mm) lower end is flat on the cheek film at the about 1mm of rats with left bicker place, calcination 30min, be shown in the white infringement that this locates about 3mm.Grouping immediately after 24 hours,, divide 5 groups, i.e. model group (4 times/days of adjuvants, containing medicine) by 10 every group; Scopariusins high dose group (4 times/days, 0.5mg/ time); Dosage in Scopariusins (4 times/days, 0.1mg/ time); Scopariusins low dose group (4 times/days, 0.02mg/ time); Positive controls: cydiodine group (4 times/days, 0.5mg/ time).Scopariusins and cydiodine buccal tablet be pulverize before use, and administration be take flap coverage as degree.Successive administration 5 days, observe ulcer area size (in the diameter of ulcer) and ulcer healing situation (being considered as healing without macroscopic ulcer) next day before administration and after each administration, and first administration to last administration is recorded as respectively 1,2,3,4,5,6 day.The ulcer area size is checked with t, and ulcer healing rate is checked with X2.4, result of the test
Ulcer area is (table 1) relatively: Scopariusins high dose group and model group relatively, play off-test on the 3rd day from administration, and significant difference is relatively arranged corresponding every day; Cydiodine group and model group relatively, play off-test on the 3rd day from administration, and significant difference is relatively arranged corresponding every day; In Scopariusins, dosage group and model group relatively, play off-test on the 3rd day from administration, and significant difference is relatively arranged corresponding every day; Scopariusins low dose group and model group relatively, play off-test on the 5th day from administration, and significant difference is relatively arranged corresponding every day; In Scopariusins, dosage group and cydiodine group relatively, play off-test on the 1st day from administration, and significant difference is relatively arranged corresponding every day.
The impact of table 1 on the rat ulcer area
Annotate: compare * p<0.05, * p<0.01 with model group.
Healing rate (table 2): model group and Scopariusins low dose group play off-test on the 1st day from administration, and ulcer is healing not; And the Scopariusins high dose group just had ulcer healing from administration the 4th day, to off-test, reach 90%; The cydiodine group, from administration the 4th day, has ulcer healing, to off-test, reaches 60%; In Scopariusins, the dosage group, from administration the 5th day, has ulcer healing, to off-test, reaches 40%.
The impact of table 2 on the rat ulcer healing time
Annotate: compare * p<0.05, * p<0.01 with model group.
5, conclusion
Scopariusins has the effect of obvious promotion oral ulcer healing.
Claims (1)
1.Scopariusins the application in preparation treatment or preventing canker sore medicine, described compound S copariusins structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310470463.XA CN103462951B (en) | 2013-10-10 | 2013-10-10 | Application of scopariusins in preparation of medicine treating or preventing canker sore |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310470463.XA CN103462951B (en) | 2013-10-10 | 2013-10-10 | Application of scopariusins in preparation of medicine treating or preventing canker sore |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103462951A true CN103462951A (en) | 2013-12-25 |
| CN103462951B CN103462951B (en) | 2015-04-01 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310470463.XA Expired - Fee Related CN103462951B (en) | 2013-10-10 | 2013-10-10 | Application of scopariusins in preparation of medicine treating or preventing canker sore |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107669782A (en) * | 2017-10-04 | 2018-02-09 | 南京正宽医药科技有限公司 | A kind of Chinese medicinal granule product for reducing blood glucose and preparation method thereof |
-
2013
- 2013-10-10 CN CN201310470463.XA patent/CN103462951B/en not_active Expired - Fee Related
Non-Patent Citations (2)
| Title |
|---|
| BUCHBAUER G ET AL.: "二萜的生物活性", 《国外医学药学分册》 * |
| MIN ZHOU ET AL.: "Scopariusins, A New Class of ent-Halimane Diterpenoids Isolated from Isodon scoparius, and Biomimetic Synthesis of Scopariusin A and Isoscoparin N", 《ORGANIC LETTERS》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107669782A (en) * | 2017-10-04 | 2018-02-09 | 南京正宽医药科技有限公司 | A kind of Chinese medicinal granule product for reducing blood glucose and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN103462951B (en) | 2015-04-01 |
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Address after: 225300 Jiangsu City, Gaogang District, city road, No. 58, No. Patentee after: Zibo Qidingli Patent Information Consulting Co., Ltd. Address before: Industrial Park No. 87 Yu Bridge 255086 Shandong province Zibo high tech Zone Wanjie Road Room 301 Patentee before: Zibo Qidingli Patent Information Consulting Co., Ltd. |
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