CN103027918A - Application of Houttuynoid E in preparation of drug for treating or preventing oral ulcer - Google Patents

Application of Houttuynoid E in preparation of drug for treating or preventing oral ulcer Download PDF

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Publication number
CN103027918A
CN103027918A CN2012104705750A CN201210470575A CN103027918A CN 103027918 A CN103027918 A CN 103027918A CN 2012104705750 A CN2012104705750 A CN 2012104705750A CN 201210470575 A CN201210470575 A CN 201210470575A CN 103027918 A CN103027918 A CN 103027918A
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houttuynoid
preparation
oral ulcer
drug
treating
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何晓涛
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Abstract

The invention relates to application of Houttuynoid E in preparation of a drug for treating or preventing oral ulcer. The use of the Houttuynoid E disclosed by the invention in the preparation of the drug for treating or preventing oral ulcer is firstly disclosed. The framework type is a brand-new framework type and has an unexpected strong effect of restraining the bacterial activity, and so the Houttuynoid E is impossibly reveled by other compounds, and has outstanding substantial characteristics. Meanwhile, the Houttuynoid E has significant progress in preparing the drug for treating or preventing oral ulcer.

Description

The application of Houttuynoid E in preparation treatment or preventing canker sore medicine
Technical field
The present invention relates to the application of Houttuynoid E in preparation treatment or preventing canker sore 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 of recurrent oral ulceration is complicated, and is 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, because the topical therapeutic toxic and side effects is lower, the people who has therefore obtained people can.Although the buccal tablets that use the part that occurs in recent years carries, easy to use, mouthfeel and compliance are better, and such 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 H outtuynoid E that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Houttuynoid E, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to DEF(Cai, J. Y. et al., 2012. Houttuynoid E, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Houttuynoid E 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 simultaneously oral ulcer and obviously have significant progress.
Summary of the invention
The invention provides the application of Houttuynoid E in preparation treatment or preventing canker sore medicine.
Described compound H outtuynoid E structure is shown in formula I:
Figure BDA0000242602201
The purposes of the Houttuynoid E 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 simultaneously oral ulcer and obviously have significant progress.
The specific embodiment
The preparation method of compound H outtuynoid E involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Houttuynoid E, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 compound H outtuynoid E tablet involved in the present invention:
Get 20 and digest compound Houttuynoid E, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid E capsule involved in the present invention:
Get 20 and digest compound Houttuynoid E, 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.
Test example 1 Houttuynoid E anti-oral ulcer experimental study
1, test objective: whether make the oral ulcer model with phenol, give the Houttuynoid E of the certain number of times of oral ulcer rat model every day, observing Houttuynoid E 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 ~ 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.Immediately grouping after 24 hours, divides 5 groups, i.e. model group (4 times/days of adjuvants do not contain medicine) by 10 every group; Houttuynoid E high dose group (4 times/days, 0.5mg/ time); Dosage among the Houttuynoid E (4 times/days, 0.1mg/ time); Houttuynoid E low dose group (4 times/days, 0.02mg/ time); Positive controls: cydiodine group (4 times/days, 0.5mg/ time).Houttuynoid E and cydiodine buccal tablet be pulverize before use, and administration is take flap coverage as degree.Observe ulcer area size (in the diameter of ulcer) and ulcer healing situation (being considered as healing without macroscopic ulcer) next day after reaching each administration before the successive administration 5 days, 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, ulcer healing rate X 2Check.
4, result of the test
Ulcer area is (table 1) relatively: Houttuynoid E 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 Houttuynoid E, and significant difference is relatively arranged corresponding every day; Houttuynoid E 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 Houttuynoid E, and significant difference is relatively arranged corresponding every day.
Table 1 is on the impact of rat ulcer area
Annotate: compare * p<0.05, * p<0.01 with model group.
Healing rate (table 2): adjuvant group and Houttuynoid E low dose group played off-test on the 1st day from administration, and ulcer is healing not; And Houttuynoid E high dose group just had ulcer healing from administration the 4th day, to off-test, reached 90%; The cydiodine group has ulcer healing from administration the 4th day, to off-test, reach 60%; The dosage group had ulcer healing among the Houttuynoid E from administration the 5th day, to off-test, reached 40%.
Table 2 is on the impact of rat ulcer healing time
Figure BDA0000242602203
Annotate: compare * p<0.05, * p<0.01 with model group.
5, conclusion
Houttuynoid E has the effect of obvious promotion oral ulcer healing.

Claims (1)

1.Houttuynoid the application of E in preparation treatment or preventing canker sore medicine, described compound H outtuynoid E structure as Formula IShown in:
Figure 667089DEST_PATH_IMAGE001
Formula I.
CN2012104705750A 2012-11-19 2012-11-19 Application of Houttuynoid E in preparation of drug for treating or preventing oral ulcer Withdrawn CN103027918A (en)

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
20120313: "Houttuynoids A-E,anti-herpes simplex virus active flavonoids with novel skeletons from houttuynia cordata", 《ORGANIC LETTERS》 *
克里木等: "鱼腥草治疗复发性口腔溃疡64例", 《新疆中医药》 *

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Application publication date: 20130410