CN102872060B - Application of Gypensapogenin B to preparing drugs for treating or preventing canker sores - Google Patents
Application of Gypensapogenin B to preparing drugs for treating or preventing canker sores Download PDFInfo
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- CN102872060B CN102872060B CN 201210419285 CN201210419285A CN102872060B CN 102872060 B CN102872060 B CN 102872060B CN 201210419285 CN201210419285 CN 201210419285 CN 201210419285 A CN201210419285 A CN 201210419285A CN 102872060 B CN102872060 B CN 102872060B
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- Prior art keywords
- gypensapogenin
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- canker sores
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- 239000003814 drug Substances 0.000 title claims abstract description 12
- NNUMQZNZQGQGCN-AGHUFMIKSA-N gypensapogenin b Chemical compound O=C1C(=C(C)C)CC([C@@H]2[C@@H]3[C@@]([C@@]4(CCC5=C([C@H]6CC[C@H](O6)C5(C)C)[C@H]4CC3)C)(C)CC2)=C1 NNUMQZNZQGQGCN-AGHUFMIKSA-N 0.000 title abstract description 58
- 208000002399 aphthous stomatitis Diseases 0.000 title abstract description 15
- 229940079593 drug Drugs 0.000 title abstract description 5
- 238000002360 preparation method Methods 0.000 claims description 11
- 230000002265 prevention Effects 0.000 claims description 4
- 229930192112 gypensapogenin Natural products 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 abstract description 11
- 230000000694 effects Effects 0.000 abstract description 4
- 208000025865 Ulcer Diseases 0.000 description 14
- 231100000397 ulcer Toxicity 0.000 description 14
- 208000007117 Oral Ulcer Diseases 0.000 description 10
- 230000035876 healing Effects 0.000 description 10
- 230000003203 everyday effect Effects 0.000 description 6
- 241000700159 Rattus Species 0.000 description 4
- 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
- 240000006509 Gynostemma pentaphyllum Species 0.000 description 3
- 235000002956 Gynostemma pentaphyllum Nutrition 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
- 229930182490 saponin Natural products 0.000 description 3
- 150000007949 saponins Chemical class 0.000 description 3
- 235000017709 saponins Nutrition 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 150000003648 triterpenes Chemical class 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
- 239000003153 chemical reaction reagent 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
- INLFWQCRAJUDCR-IQVMEADQSA-N (1R,2S,4S,5'S,6R,7S,8R,9S,12S,13S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icosane-6,2'-oxane] Chemical compound O([C@@H]1[C@@H]([C@]2(CC[C@@H]3[C@@]4(C)CCCCC4CC[C@H]3[C@@H]2C1)C)[C@@H]1C)[C@]11CC[C@H](C)CO1 INLFWQCRAJUDCR-IQVMEADQSA-N 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 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
- 235000003143 Panax notoginseng Nutrition 0.000 description 1
- 241000180649 Panax notoginseng Species 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
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 238000001354 calcination Methods 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
- 230000001472 cytotoxic effect Effects 0.000 description 1
- OORMXZNMRWBSTK-UHFFFAOYSA-N dammaran Natural products C1CCC(C)(C)C2CCC3(C)C4(C)CCC(C(C)CCCC(C)C)C4CCC3C21C OORMXZNMRWBSTK-UHFFFAOYSA-N 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
- 238000011835 investigation 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
- 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
- 238000010998 test method Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
The invention relates to application of Gypensapogenin B to preparing drugs for treating or preventing canker sores. The application of Gypensapogenin B to preparing the drugs for treating the canker sores, disclosed by the invention, is firstly published, the framework type is brand new, the activity of treating the canker sores is unexpectedly strong and the probability of giving any revelation by other compounds does not exist, so that prominent substantive features are provided and a remarkable progress in treating the canker sores is made at the same time.
Description
Technical field
The present invention relates to the application of Gypensapogenin B in preparation treatment or prevention stomatocace medicine.
Background technology
Recurrent oral ulceration is modal disease in the diseases of oral mucosa.The first place of prevalence office diseases of oral mucosa.Sircus(1975) investigation 1587 people, prevalence is 20%.This shows that oral ulcer patient is a very huge colony.The cause of disease complexity of recurrent oral ulceration, still indeterminate so far, may be relevant with factors such as the endocrine regulation of viral infection, bacterial infection and body, immune dysfunctions.
The main treatment measure of oral ulcer comprises topical therapeutic and whole body therapeutic, because the topical therapeutic toxic and side effects is lower, the people who has therefore obtained people can.Though the buccal tablets that use the part that occurs in recent years 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 chemical compound Gypensapogenin B that the present invention relates to is one and delivered (Li in 2012, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178.) new framework compound, this chemical compound has brand-new framework types, present purposes only relates to the cytotoxic activity (Li of human tumor cell line, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178.), belong to open first for the purposes of the Gypensapogenin B that the present invention relates in preparation treatment stomatocace medicine, because framework types belongs to brand-new framework types, and its treatment oral ulcer is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for the treatment of oral ulcer simultaneously and obviously have obvious improvement.
Summary of the invention
The invention provides the application of Gypensapogenin B in preparation treatment or prevention stomatocace medicine.
Described chemical compound Gypensapogenin B structure is shown in formula I:
The purposes of the Gypensapogenin B that the present invention relates in preparation treatment stomatocace medicine belongs to open first, because framework types belongs to brand-new framework types, and its treatment oral ulcer is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for the treatment of oral ulcer simultaneously and obviously have obvious improvement.
The specific embodiment
The preparation method of chemical compound Gypensapogenin B involved in the present invention is referring to document (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50,173 – 178. and Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45 (3): 167-171.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of chemical compound Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of chemical compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
The anti-oral ulcer experimental study of test example 1 Gypensapogenin B
1, test objective: whether make the oral ulcer model with phenol, give the Gypensapogenin B of the certain number of times of oral ulcer rat model every day, observing Gypensapogenin B has the effect that reduces ulcer.
2, be subjected to reagent thing and reagent
Cydiodine (Beijing Sihuan Medicine Science and Technology Co., Ltd); Phenol
Animal: the Wistar rat, male, body weight 240 ~ 280
3, test method
Get 50 of rats, male, body weight 240 ~ 280g, 10% chloral hydrate anesthesia, dosage: 0.35ml/100g, (internal diameter: 3mm) lower end is flat on the cheek film at the about 1mm of rats with left bicker place with the plastic dropper of 90% phenol cotton balls after the anesthesia, calcination 30min namely sees the white infringement of the about 3mm in this place.Grouping immediately, divides 5 groups, i.e. model group (adjuvant 4 times/day does not contain medicine) by 10 every group after 24 hours; Gypensapogenin B high dose group (4 times/day, 0.5mg/ time); Dosage among the Gypensapogenin B (4 times/day, 0.1mg/ time); Gypensapogenin B low dose group (4 times/day, 0.02mg/ time); Positive controls: cydiodine group (4 times/day, 0.5mg/ time).Gypensapogenin B and cydiodine buccal tablet be pulverize before use, and administration is degree of being with the flap coverage.Observe ulcer area size (in the diameter of ulcer) and ulcer healing situation (do not have macroscopic ulcer and be considered as healing) next day after reaching each administration before the successive administration 5 days, administration, and first administration to last administration is recorded as 1,2,3,4,5,6 day respectively.Ulcer area size is checked with t, ulcer healing rate X
2Check.
4, result of the test
The ulcer area is (table 1) relatively: Gypensapogenin B high dose group and model group relatively played off-test on the 3rd day from administration, and significant difference is relatively arranged corresponding every day; Cydiodine group and model group relatively played off-test on the 3rd day from administration, and significant difference is relatively arranged corresponding every day; Dosage group and model group relatively played off-test on the 3rd day from administration among the Gypensapogenin B, and significant difference is relatively arranged corresponding every day; Gypensapogenin B low dose group and model group relatively played off-test on the 5th day from administration, and significant difference is relatively arranged corresponding every day; Dosage group and cydiodine group relatively played off-test on the 1st day from administration among the Gypensapogenin B, and significant difference is relatively arranged corresponding every day.
The influence of table 1 pair rat ulcer area
Annotate: compare * p＜0.05, * p＜0.01 with model group.
Healing rate (table 2): adjuvant group and Gypensapogenin B low dose group played off-test on the 1st day from administration, and ulcer is healing not; And Gypensapogenin B high dose group just has ulcer healing from administration the 4th day, to off-test, reaches 90%; The cydiodine group has ulcer healing from administration the 4th day, to off-test, reaches 60%; The dosage group has ulcer healing from administration the 5th day among the Gypensapogenin B, to off-test, reaches 40%.
The influence of table 2 pair rat ulcer healing time
Annotate: compare * p＜0.05, * p＜0.01 with model group.
5, conclusion
Gypensapogenin B has the effect of obvious promotion oral ulcer healing.
Claims (1)
1.Gypensapogenin the application of B in preparation treatment or prevention stomatocace medicine, described chemical compound Gypensapogenin B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210419285 CN102872060B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B to preparing drugs for treating or preventing canker sores |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210419285 CN102872060B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B to preparing drugs for treating or preventing canker sores |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102872060A CN102872060A (en) | 2013-01-16 |
| CN102872060B true CN102872060B (en) | 2013-08-28 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201210419285 Expired - Fee Related CN102872060B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B to preparing drugs for treating or preventing canker sores |
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| Country | Link |
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| CN (1) | CN102872060B (en) |
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2012
- 2012-10-26 CN CN 201210419285 patent/CN102872060B/en not_active Expired - Fee Related
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| Publication number | Publication date |
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| CN102872060A (en) | 2013-01-16 |
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Owner name: JIANGSU XIN NEOLITHIC BASALT FIBER CO., LTD. Free format text: FORMER OWNER: WU JUNHUA Effective date: 20131209 |
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Free format text: CORRECT: ADDRESS; FROM: 210009 NANJING, JIANGSU PROVINCE TO: 213351 CHANGZHOU, JIANGSU PROVINCE |
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Effective date of registration: 20131209 Address after: 213351 Jiangsu city of Changzhou province Liyang Liyang Town of Wuhu Shanghai Road No. 168 Patentee after: Jiangsu Neolith Basalt Fiber Co., Ltd. Address before: 210009 No. 22, Hankou Road, Gulou District, Jiangsu, Nanjing Patentee before: Wu Junhua |
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| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20130828 Termination date: 20151026 |
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