CN103599104B - Application of Caesanines D in drug for treating or preventing dental ulcer - Google Patents
Application of Caesanines D in drug for treating or preventing dental ulcer Download PDFInfo
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- CN103599104B CN103599104B CN201310618334.0A CN201310618334A CN103599104B CN 103599104 B CN103599104 B CN 103599104B CN 201310618334 A CN201310618334 A CN 201310618334A CN 103599104 B CN103599104 B CN 103599104B
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- caesanines
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- ulcer
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- dental ulcer
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- 239000003814 drug Substances 0.000 title claims abstract description 12
- 208000025865 Ulcer Diseases 0.000 title abstract description 18
- 231100000397 ulcer Toxicity 0.000 title abstract description 18
- 229940079593 drug Drugs 0.000 title abstract description 5
- 238000011282 treatment Methods 0.000 claims abstract description 11
- 238000002360 preparation method Methods 0.000 claims abstract description 10
- 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 8
- 230000000694 effects Effects 0.000 abstract description 4
- 230000035876 healing Effects 0.000 description 9
- 208000020670 canker sore Diseases 0.000 description 7
- 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 5
- 239000006189 buccal tablet Substances 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 235000015162 Caesalpinia sappan Nutrition 0.000 description 3
- 244000306301 Caesalpinia sappan Species 0.000 description 3
- 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
- 229930002147 cassane Natural products 0.000 description 3
- 229930004069 diterpene Natural products 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
- 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
- 230000000721 bacterilogical 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
- 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
- 238000000034 method 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
- 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
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses application of Caesanines D in preparation of a drug for treating or preventing dental ulcer for the first time. Caesanines D has a brand new type of skeleton, has high activity on treatment of dental ulcer as well as outstanding substantial characteristics, and also shows a remarkable progress on treatment of dental ulcer.
Description
Technical field
The present invention relates to the novelty teabag of Compound C aesanines D, particularly relate to the application of Caesanines D 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 C aesanines D that the present invention relates to is one and delivers (Jingyu Zhang in 2013, et al., Caesanines AD, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan.Organic Letters, 2013, 15 (18): 4726 – 4729.) noval chemical compound, this compound has brand-new framework types, current purposes finds antibacterial (the Jingyu Zhang of its energy, et al., Caesanines AD, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan.Organic Letters, 2013, 15 (18): 4726 – 4729.), the purposes of the Caesanines D 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 Caesanines D research, provide the application of Caesanines D in preparation treatment or preventing canker sore medicine.
Described Compound C aesanines D structure is as shown in formula I:
Formula I
The purposes of the Caesanines D 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 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.
The preparation method of Compound C aesanines D involved in the present invention is see document (Jingyu Zhang, et al., Caesanines AD, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan.Organic Letters, 2013,15 (18): 4726 – 4729.), prepare Compound C aesanines D according to the method described above.
Embodiment 1: the preparation of Compound C aesanines D tablet involved in the present invention:
Get 5 g of compound Caesanines D and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of Compound C aesanines D capsule involved in the present invention:
Get 5 g of compound Caesanines D 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:Caesanines D anti-oral ulcer
1, test objective: manufacture Oral ulcer model with phenol, gives the Caesanines D of Oral ulcer model rat certain number of times every day, and whether observe Caesanines D 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); Caesanines D high dose group (4 times/day, 0.5mg/ time); Dosage (4 times/day, 0.1mg/ time) in Caesanines D; Caesanines D low dose group (4 times/day, 0.02mg/ time); Positive controls: cydiodine group (4 times/day, 0.5mg/ time).Caesanines D 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): Caesanines D 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 Caesanines D, dosage group compares with model group, within the 3rd day, plays off-test from administration, and corresponding every day compares significant difference; Caesanines D low dose group compares with model group, within the 5th day, plays off-test from administration, and corresponding every day compares significant difference; In Caesanines D, 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 Caesanines D low dose group play off-test on the 1st day from administration, and ulcer does not heal; And Caesanines D 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 Caesanines D, 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
Caesanines D has the effect obviously promoting oral ulcer healing.
Claims (1)
- The application of 1.Caesanines D in preparation treatment stomatocace medicine, described Compound C aesanines D structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310618334.0A CN103599104B (en) | 2013-11-28 | 2013-11-28 | Application of Caesanines D in drug for treating or preventing dental ulcer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310618334.0A CN103599104B (en) | 2013-11-28 | 2013-11-28 | Application of Caesanines D in drug for treating or preventing dental ulcer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103599104A CN103599104A (en) | 2014-02-26 |
| CN103599104B true CN103599104B (en) | 2015-06-17 |
Family
ID=50117413
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310618334.0A Active CN103599104B (en) | 2013-11-28 | 2013-11-28 | Application of Caesanines D in drug for treating or preventing dental ulcer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103599104B (en) |
-
2013
- 2013-11-28 CN CN201310618334.0A patent/CN103599104B/en active Active
Non-Patent Citations (1)
| Title |
|---|
| Caesanines A-D, New Cassane Diterpenes with Unprecedented N Bridge from Caesalpinia sappan;Zhang Jingyu et al.,;《Organic Letters》;20130920;第15卷(第18期);p.4726-4729 * |
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| Publication number | Publication date |
|---|---|
| CN103599104A (en) | 2014-02-26 |
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Inventor after: Song Xiuxiang Inventor after: Zang Xiaoguo Inventor after: Li Aifang Inventor after: Li Qiang Inventor before: Li Qiang |
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Free format text: CORRECT: INVENTOR; FROM: LI QIANG TO: SONG XIUXIANG ZANG XIAOGUO LI AIFANG LI QIANG |
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Effective date of registration: 20170930 Address after: 226500 Jiangsu city of Nantong province Rugao City, Dong Chen Zhen Hong Bridge neighborhood 4 groups Patentee after: Rugao Chengdong hospital Address before: 266000 Shandong province Qingdao City Red Road No. 31 North Building 201 Patentee before: Li Qiang |
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Effective date of registration: 20191209 Address after: Room 306, building 3, business center, No. 82, Huayuan West Road, Chuzhou, Anhui Patentee after: CHUZHOU TIANSHUN PRODUCTIVITY PROMOTION Co.,Ltd. Address before: 226500 Jiangsu city of Nantong province Rugao City, Dong Chen Zhen Hong Bridge neighborhood 4 groups Patentee before: Rugao Chengdong hospital |
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Effective date of registration: 20221213 Address after: 276000 No. 95, Huaxia Road, economic and Technological Development Zone, Linyi City, Shandong Province Patentee after: SHANDONG TIANCHENG STEEL STRUCTURE Co.,Ltd. Address before: 239000 incubation workshop, room 306, building 3, entrepreneurship center, No.82 Huayuan West Road, Chuzhou City, Anhui Province Patentee before: CHUZHOU TIANSHUN PRODUCTIVITY PROMOTION Co.,Ltd. |