CN103479624B - Application of Racemosins A in preparation of oral ulcer treatment or prevention medicines - Google Patents
Application of Racemosins A in preparation of oral ulcer treatment or prevention medicines Download PDFInfo
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- CN103479624B CN103479624B CN201310470511.5A CN201310470511A CN103479624B CN 103479624 B CN103479624 B CN 103479624B CN 201310470511 A CN201310470511 A CN 201310470511A CN 103479624 B CN103479624 B CN 103479624B
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- Prior art keywords
- racemosins
- day
- oral ulcer
- preparation
- ulcer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- QZUNAFWZEXJWGD-UHFFFAOYSA-N racemosin Natural products C1=CC(=O)OC2=C1C(OC)=C1C=CC(C)(C)OC1=C2OC QZUNAFWZEXJWGD-UHFFFAOYSA-N 0.000 title claims abstract description 29
- 238000011282 treatment Methods 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
- 208000007117 Oral Ulcer Diseases 0.000 title abstract description 10
- 208000002399 aphthous stomatitis Diseases 0.000 title abstract description 10
- 229940079593 drug Drugs 0.000 title abstract description 5
- 230000002265 prevention Effects 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims description 11
- 208000020670 canker sore Diseases 0.000 claims description 9
- 230000000694 effects Effects 0.000 abstract description 4
- 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
- 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
- 241001290352 Caulerpa racemosa Species 0.000 description 3
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 3
- 229930013930 alkaloid Natural products 0.000 description 3
- 229940046011 buccal tablet Drugs 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
- 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
- 206010029260 Neuroblastoma Diseases 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
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000000721 bacterilogical effect Effects 0.000 description 1
- 238000001354 calcination Methods 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000005779 cell damage Effects 0.000 description 1
- 208000037887 cell injury Diseases 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
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 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
- 208000015181 infectious disease Diseases 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
- 230000036407 pain Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 108090000765 processed proteins & peptides 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
- 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
Abstract
The invention relates to an application of Racemosins A in the preparation of oral ulcer treatment or prevention medicines for the first time. The Racemosins A has a brand new skeleton type, has a strong treatment activity against the oral ulcer, has prominent substantive characteristics, and is a substantial improvement in the treatment of the oral ulcer.
Description
Technical field
The present invention relates to the novelty teabag of compound R acemosins A, particularly relate to the application of Racemosins A 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, 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 R acemosins A that the present invention relates to is one and delivers (Ding-Quan Liu in 2013, et al., Racemosins A and B, two novel bisindole alkaloids from the green alga Caulerpa racemosa.Fitoterapia, 91 (2013): 15 – 20.) noval chemical compound, this compound has brand-new framework types, and current purposes finds that it can weaken beta-amyloyd peptide
25-35(A β
25 – 35) human neuroblastoma cells SH-SY5Y cell injury (the Ding-Quan Liu that causes, et al., Racemosins A and B, two novel bisindole alkaloids from the green alga Caulerpa racemosa.Fitoterapia, 91 (2013): 15 – 20.), the purposes of the Racemosins A that the present invention relates in preparation treatment or preventing canker sore medicine belongs to first public.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report for the treatment of or preventing canker sore according in existing Racemosins A research, provide the application of Racemosins A in preparation treatment or preventing canker sore medicine.
Described compound R acemosins A structure is as shown in formula I:
Formula (1)
The purposes of the Racemosins A that the present invention relates in preparation treatment or preventing canker sore medicine belongs to first public, because framework types belongs to brand-new framework types, and its treatment or preventing canker sore active strong, possess outstanding substantive distinguishing features, to be used for the treatment of or preventing canker sore obviously has significant progress simultaneously.
Detailed description of the invention
The preparation method of compound R acemosins A involved in the present invention is see document (Ding-Quan Liu, et al., Racemosins A and B, two novel bisindole alkaloids from the green alga Caulerpa racemosa.Fitoterapia, 91 (2013): 15 – 20.)
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 R acemosins A tablet involved in the present invention:
Get 5 g of compound Racemosins A and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound R acemosins A capsule involved in the present invention:
Get 5 g of compound Racemosins A and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The experimental study of test example 1:Racemosins A anti-oral ulcer
1, test objective: manufacture Oral ulcer model with phenol, gives the RacemosinsA of Oral ulcer model rat certain number of times every day, and whether observe Racemosins A 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 ~ 280g, Nanjing Medical University's Experimental Animal Center.
3, test method
Get rat 50, male, body weight 240 ~ 280g, 10% chloral hydrate anesthesia, dosage: 0.35ml/100g, is flat on rats with left bicker by plastic dropper (internal diameter: the 3mm) lower end of 90% phenol cotton balls after anesthesia and is about on the cheek film at 1mm place, calcination 30min, is namely shown in 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); Racemosins A high dose group (4 times/day, 0.5mg/ time); Dosage (4 times/day, 0.1mg/ time) in Racemosins A; Racemosins A low dose group (4 times/day, 0.02mg/ time); Positive controls: cydiodine group (4 times/day, 0.5mg/ time).Racemosins A 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, and ulcer healing rate X2 checks.
4, result of the test
Ulcer area compares (table 1): Racemosins A 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 Racemosins A, dosage group compares with model group, within the 3rd day, plays off-test from administration, and corresponding every day compares significant difference; Racemosins A low dose group compares with model group, within the 5th day, plays off-test from administration, and corresponding every day compares significant difference; In Racemosins A, 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): model group and Racemosins A low dose group play off-test on the 1st day from administration, and ulcer does not heal; And Racemosins A 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 Racemosins A, 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
Racemosins A has the effect obviously promoting oral ulcer healing.
Claims (1)
- The application of 1.Racemosins A in preparation treatment or preventing canker sore medicine, described compound R acemosinsA structure is as shown in formula I:Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310470511.5A CN103479624B (en) | 2013-10-10 | 2013-10-10 | Application of Racemosins A in preparation of oral ulcer treatment or prevention medicines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310470511.5A CN103479624B (en) | 2013-10-10 | 2013-10-10 | Application of Racemosins A in preparation of oral ulcer treatment or prevention medicines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103479624A CN103479624A (en) | 2014-01-01 |
| CN103479624B true CN103479624B (en) | 2015-06-17 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310470511.5A Expired - Fee Related CN103479624B (en) | 2013-10-10 | 2013-10-10 | Application of Racemosins A in preparation of oral ulcer treatment or prevention medicines |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103479624B (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1160347A (en) * | 1994-10-12 | 1997-09-24 | 辉瑞研究及发展公司 | Use of indole drivs. for treatment of dermatological disorders peripheral neuropathied, arthritis, headache, orofacial pain, allergic or chronic obstructive airways desease, glaucoma and ocular....... |
-
2013
- 2013-10-10 CN CN201310470511.5A patent/CN103479624B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1160347A (en) * | 1994-10-12 | 1997-09-24 | 辉瑞研究及发展公司 | Use of indole drivs. for treatment of dermatological disorders peripheral neuropathied, arthritis, headache, orofacial pain, allergic or chronic obstructive airways desease, glaucoma and ocular....... |
Non-Patent Citations (1)
| Title |
|---|
| Racemosins A and B, two novel bisindole alkaloids from the green alga Caulerpa racemosa;Ding-quan Liu,et al.;《Fitoterapia》;20130824;第91卷;15-20 * |
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| CN103479624A (en) | 2014-01-01 |
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Effective date of registration: 20151224 Address after: 223471, Jiangsu County, Lianshui Province, South Town, South set industrial concentration area Patentee after: Lianshui county strong wood products Co., Ltd. Address before: Sanjiang street Shengzhou city Zhejiang province 312400 Shaoxing City Tong Community Sanjiang Street No. 186 yuan Patentee before: SHENGZHOU NUOMIKE IMPORT AND EXPORT CO., LTD. |
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