CN107496427A - The purposes of rutaecarpin and mouthwash and preparation method thereof - Google Patents
The purposes of rutaecarpin and mouthwash and preparation method thereof Download PDFInfo
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- CN107496427A CN107496427A CN201710932784.5A CN201710932784A CN107496427A CN 107496427 A CN107496427 A CN 107496427A CN 201710932784 A CN201710932784 A CN 201710932784A CN 107496427 A CN107496427 A CN 107496427A
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- China
- Prior art keywords
- rutaecarpin
- mouthwash
- periodontitis
- purposes
- stem cell
- Prior art date
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- ACVGWSKVRYFWRP-UHFFFAOYSA-N Rutecarpine Chemical compound C1=CC=C2C(=O)N(CCC=3C4=CC=CC=C4NC=33)C3=NC2=C1 ACVGWSKVRYFWRP-UHFFFAOYSA-N 0.000 title claims abstract description 93
- 239000002324 mouth wash Substances 0.000 title claims abstract description 40
- 229940051866 mouthwash Drugs 0.000 title claims abstract description 40
- 238000002360 preparation method Methods 0.000 title claims abstract description 16
- 201000001245 periodontitis Diseases 0.000 claims abstract description 48
- 210000000130 stem cell Anatomy 0.000 claims abstract description 46
- 210000002379 periodontal ligament Anatomy 0.000 claims abstract description 44
- 210000002997 osteoclast Anatomy 0.000 claims abstract description 38
- 239000002270 dispersing agent Substances 0.000 claims abstract description 26
- 206010061218 Inflammation Diseases 0.000 claims abstract description 21
- 230000004054 inflammatory process Effects 0.000 claims abstract description 21
- 239000003112 inhibitor Substances 0.000 claims abstract description 14
- 230000002265 prevention Effects 0.000 claims abstract description 14
- 239000003814 drug Substances 0.000 claims abstract description 13
- 230000036541 health Effects 0.000 claims abstract description 12
- 239000002994 raw material Substances 0.000 claims abstract description 12
- 230000004069 differentiation Effects 0.000 claims abstract description 11
- 230000035800 maturation Effects 0.000 claims abstract description 11
- 239000004094 surface-active agent Substances 0.000 claims abstract description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 9
- 239000002158 endotoxin Substances 0.000 claims description 27
- 229920006008 lipopolysaccharide Polymers 0.000 claims description 27
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 18
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims description 14
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims description 14
- 230000003239 periodontal effect Effects 0.000 claims description 14
- 108090001005 Interleukin-6 Proteins 0.000 claims description 13
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- 229940100601 interleukin-6 Drugs 0.000 claims description 13
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N EtOH Substances CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims description 9
- 235000011187 glycerol Nutrition 0.000 claims description 9
- 229960004711 sodium monofluorophosphate Drugs 0.000 claims description 9
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 7
- 239000004359 castor oil Substances 0.000 claims description 7
- 235000019438 castor oil Nutrition 0.000 claims description 7
- 238000005660 chlorination reaction Methods 0.000 claims description 7
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 7
- -1 polyoxyethylene Polymers 0.000 claims description 7
- 229960003333 chlorhexidine gluconate Drugs 0.000 claims description 5
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 claims description 5
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- ZSBXGIUJOOQZMP-UHFFFAOYSA-N Isomatrine Natural products C1CCC2CN3C(=O)CCCC3C3C2N1CCC3 ZSBXGIUJOOQZMP-UHFFFAOYSA-N 0.000 description 5
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- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
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- HMXRXBIGGYUEAX-SFHVURJKSA-N Evodiamine Natural products CN1[C@H]2N(CCc3[nH]c4ccccc4c23)C(=O)c5ccccc15 HMXRXBIGGYUEAX-SFHVURJKSA-N 0.000 description 2
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- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
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- NAOLWIGVYRIGTP-UHFFFAOYSA-N 1,3,5-trihydroxyanthracene-9,10-dione Chemical compound C1=CC(O)=C2C(=O)C3=CC(O)=CC(O)=C3C(=O)C2=C1 NAOLWIGVYRIGTP-UHFFFAOYSA-N 0.000 description 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
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- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
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- TXDUTHBFYKGSAH-SFHVURJKSA-N Evodiamine Chemical compound C1=CC=C2N(C)[C@@H]3C(NC=4C5=CC=CC=4)=C5CCN3C(=O)C2=C1 TXDUTHBFYKGSAH-SFHVURJKSA-N 0.000 description 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-N Gluconic acid Natural products OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Birds (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
Abstract
The invention provides a kind of purposes of rutaecarpin and mouthwash and preparation method thereof, belong to drug field.The purposes of rutaecarpin includes：Purposes of the rutaecarpin in the medicine or health products for preparing prevention or treatment periodontitis；Purposes of the rutaecarpin in the inhibitor for preparing periodontal ligament stem cell inflammatory reaction；Purposes of the rutaecarpin in the inhibitor of osteoclast differentiation and maturation is prepared.The raw material of this mouthwash for treating periodontitis includes：Rutaecarpin, surfactant, Hydrophilic dispersant and lipophile dispersant.The preparation method of this mouthwash includes：By rutaecarpin, surfactant, Hydrophilic dispersant and lipophile dispersant and it is dispersed in water, and is stirred at 80~85 DEG C.The present invention provides new thinking for the prevention or treatment of periodontitis, while has also expanded the application of rutaecarpin.In addition, mouthwash can effectively prevent and administer periodontitis made of rutaecarpin.
Description
Technical field
The present invention relates to medicines and health protection field, purposes and mouthwash in particular to a kind of rutaecarpin and its
Preparation method.
Background technology
Periodontitis is to invade the chronic inflammation of gum and periodontium, is a kind of destructive disease, it is mainly characterized by tooth
The formation of all bags and inflammation, absorption of alveolar bone and the tooth of bag wall gradually loosen, and it is cause adult's loss of tooth main
Reason.Its disease is more because bacterial plaque, dental calculus, food impaction, ill fitting prosthesis, stinging wound etc. and causing, and various focusing depths represented swelling, makes simultaneously
Bacterial plaque accumulation aggravates, and is prolonged by expanding under gingivally on gum.It is a large amount of due to the characteristics of micro-ecological environment, being grown under gum in subgingival plaque
The larger Periodontal Pathogens of virulence, such as gum bacteroid, middle bacteroid, conveyor screw, the increased inflammation and expansion for making gum prolong,
Cause periodontal bag formation and absorption of alveolar bone, cause periodontitis.
Periodontitis is after cancer, cardiovascular and cerebrovascular disease by medical field final conclusion, threatens the 3rd of human body health
Big killer, and " number one killer " of oral health.Some advanced symptoms that periodontitis occurs, also disliked as oral cavity " inferior health "
The principal character of change.
Most patients with periodontitis all along with the symptom of gingival atrophy, are investigated and found, the crowd more than 45 years old,
More than 90% has a different degrees of gingival atrophy phenomenon, and gingival atrophy, and also one is irreversible to being considered as by medical circle of oral cavity
Physiology degradation phenomena.It is appreciated that due to heredity, the influence of environment, food security aspect factor, gingival atrophy physiology
Degradation phenomena has the trend that becomes younger year by year, and minimus gingival atrophy patient is 18 years old.
The existing treatment method of periodontitis is more based on scaling and antibiosis extract for treating, and wherein antibiosis extract for treating is given including whole body
Medicine (oral and injection) and periodontal are locally administered, and side effect is greatly and unsatisfactory curative effect.Based on this, it is strong to be badly in need of a kind of universality now
Technology, the periodontitis of getting worse is prevented either to treat.
The content of the invention
The first object of the present invention is to provide a kind of new application of rutaecarpin, i.e. rutaecarpin is preparing prevention or controlled
Treat the purposes in the medicine or health products of periodontitis；Rutaecarpin is in the inhibitor for preparing periodontal ligament stem cell inflammatory reaction
Purposes；Purposes of the rutaecarpin in the inhibitor of osteoclast differentiation and maturation is prepared, is carried for the prevention or treatment of periodontitis
For new thinking, the application of rutaecarpin has also been expanded.
The second object of the present invention is to provide a kind of mouthwash extremely preparation method for being used to treat periodontitis, this to gargle
Saliva can effectively prevent and treat cementopathia using rutaecarpin as active ingredient, avoid tooth mobility, and therapeutic effect is good.
In order to realize the above-mentioned purpose of the present invention, spy uses following technical scheme：
Purposes of the rutaecarpin in the medicine or health products for preparing prevention or treatment periodontitis.
Purposes of the rutaecarpin in the inhibitor for preparing periodontal ligament stem cell inflammatory reaction.
Purposes of the rutaecarpin in the inhibitor of osteoclast differentiation and maturation is prepared.
A kind of mouthwash for being used to treat periodontitis, the raw material of mouthwash include：It is rutaecarpin, surfactant, hydrophilic
Property dispersant and lipophile dispersant.
A kind of preparation method for being used to treat the mouthwash of periodontitis, it includes：
By rutaecarpin, surfactant, Hydrophilic dispersant and lipophile dispersant and it is dispersed in water, and
20~30min is stirred at 80~85 DEG C.
Compared with prior art, beneficial effects of the present invention for example including：
The new application for this rutaecarpin that present disclosure provides, i.e. rutaecarpin are preparing prevention or treatment periodontitis
Medicine or health products in purposes, prevention for periodontitis or treatment provide new thinking.Inventor, which studies, to be found, evodia rutaecarpa
Alkali preventing and treating periodontitis is mainly realized by following two aspects：First, rutaecarpin can effectively suppress periodontal ligament stem cell
The generation of inflammatory reaction, so as to suppress interleukin-6, interleukin 1 and the expression of tumor necrosis factor-alpha, thus
Prompting rutaecarpin can be used in the inhibitor for preparing periodontal ligament stem cell inflammatory reaction；Second, rutaecarpin can be effective
Suppress osteoclast differentiation and maturation, so as to significantly inhibit the symptom of the alveolar bone excessive consumption as caused by osteoclast activation,
Thus prompting rutaecarpin can be used in the inhibitor of osteoclast differentiation and maturation is prepared.
Present disclosure provides this for treating mouthwash of periodontitis and preparation method thereof, using rutaecarpin as medicine
Composition is imitated, dispersed mouthwash, Neng Gouyou is made in its using surfactant, Hydrophilic dispersant and lipophile dispersant
Effect prevention and improvement periodontitis.
Brief description of the drawings
In order to illustrate more clearly about the embodiment of the present invention or technical scheme of the prior art, below will be to embodiment or existing
There is the required accompanying drawing used in technology description to be briefly described.
Fig. 1 is the experimental result picture of the suppression osteoclast formation of rutaecarpin concentration dependant；
Fig. 2 is the statistical chart of the quantity of osteoclast in Fig. 1；
Fig. 3 is the area coverage statistical chart of osteoclast in Fig. 1；
Fig. 4, which is that rutaecarpin is time dependent, suppresses osteoclast formation experimental result picture；
Fig. 5 is the statistical chart of the quantity of osteoclast in Fig. 2；
Fig. 6 is the area coverage statistical chart of osteoclast in Fig. 2.
Embodiment
Embodiment of the present invention is described in detail below in conjunction with embodiment, but those skilled in the art will
Understand, the following example is merely to illustrate the present invention, and is not construed as limiting the scope of the present invention.It is unreceipted specific in embodiment
Condition person, the condition suggested according to normal condition or manufacturer are carried out.Agents useful for same or the unreceipted production firm person of instrument, it is
The conventional products that can be obtained by commercially available purchase.
Present embodiment provides a kind of use of rutaecarpin in the medicine or health products for preparing prevention or treatment periodontitis
On the way.
Stem cell periodontium in periodontium healing, regenerative process is mainly by gum, periodontal ligament, cementum and tooth
Groove bone form, this complicated tissue, after making periodontium injury, can by it is a kind of it is special in a manner of heal.Periodontal ligament
Important mission is born in regenerative process, the mesenchyma that research shows to have a group to have repair near periodontal ligament is done thin
Born of the same parents, there is extensive propagation and differentiation potential, new tooth grain bone and parodontium can be divided into.But current research is found, this
Group's cell is called periodontal ligament stem cell (PDSC), is a healthy double-edged sword.Periodontal can be divided under normal physiological conditions
Tissue carries out periodontal reparation, can also largely secrete inflammatory factor under pathological conditions, activates periodontal mononuclear macrophage, promotes
Excessive osteoclast formation, causes the formation of tooth grain bone information and oral pocket, causes and deteriorate periodontitis.
Based on this, the key of prevention or treatment periodontitis is exactly how effectively to avoid periodontal ligament stem cell in pathological conditions
Lower excessive secretion inflammatory factor.Inventor has found in long-term research work, this natural monomers compound energy of rutaecarpin
Enough effectively preventions or treatment periodontitis, therefore rutaecarpin can be used in medicine or the health care for preparing prevention or treatment periodontitis
In product.
Rutaecarpin (Evodiamine, EVO) is a kind of indoles alkaloid, is colourless or light yellow crystal.Evodia rutaecarpa
The molecular formula of alkali is C19H17N3O, molecular weight 303.36, CAS No.518-17-25.Document report rutaecarpin has anti-swollen
The activity of knurl and antiangiogenic.Its structural formula is as follows：
Inventor, which studies, to be found, rutaecarpin preventing and treating periodontitis is mainly realized by following two aspects：
In a first aspect, rutaecarpin can effectively suppress the generation of periodontal ligament stem cell inflammatory reaction.
The lipopolysaccharides (lipopolysaccharide, LPS) of periodontal dominant bacteria is the weight for causing periodontosis generally acknowledged at present
Influence factor is wanted, it can not only trigger periodontium damage and the generation of periodontitis, additionally it is possible to periodontal tissue is produced thin
Cytotoxicity.Studies have found that LPS can trigger the synthesis and release of a variety of inflammatory mediators and cell factor, as leucocyte is situated between
Element -1 (IL-1), interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α) etc..Work as Periodontal ligament stem cell
When (human periodontal ligament stem cell, hPDLSCs) is stimulated by LPS, it can pass through secretion
The cell factor such as TNF-α, IL-6, IL-1 is participated in local immunity reaction as immune auxiliary cell, and in the hair of periodontitis
Played a significant role in raw, development.
Inventor, which studies, to be found, rutaecarpin can suppress IL-6, IL-1 caused by LPS, TNF-α mRNA expression and rise, and say
To suppress periodontal ligament stem cell inflammatory reaction, thus bright rutaecarpin can produce inflammatory factor by suppressing periodontal ligament stem cell
Prompting rutaecarpin can be used in the inhibitor for preparing periodontal ligament stem cell inflammatory reaction.
Second aspect, rutaecarpin can effectively suppress osteoclast differentiation and maturation.
Periodontal ligament stem cell is stimulated by periodontal bacteria, and a large amount of inflammatory factors that produce can't cause serious periodontosis
Become, only after its caused inflammatory factor largely activates osteoclast, can just produce the symptom of alveolar bone excessive consumption, draw
Play serious periodontosis and tooth mobility.
Inventor, which studies, to be found, after the rutaecarpin of various dose is added, the quantity of mature osteoclast has bright
Aobvious decline, show that rutaecarpin can significantly inhibit the symptom that alveolar bone caused by osteoclast activation crosses absorption, thus prompt
Rutaecarpin can be used in the inhibitor of osteoclast differentiation and maturation is prepared.
Present embodiment also provides a kind of mouthwash for being used to treat periodontitis, and the raw material of the mouthwash includes：Evodia rutaecarpa
Alkali, surfactant, Hydrophilic dispersant and lipophile dispersant.
Further, Hydrophilic dispersant includes：Double de- ethanol, sodium monofluorophosphate, chlorhexidine gluconate.
Further, lipophile dispersant includes：Glycerine, polyoxyethylene chlorination castor oil, polyethylene glycol hydrogenated castor-oil plant
Oil.
Further, surfactant includes：Lauryl sodium sulfate, neopelex, polysorbate, fat
Sour sorb is smooth, fatty glyceride, lecithin.
Optionally, the raw material of the mouthwash includes by weight：4~6 parts of rutaecarpin, surfactant 0.5~1.5
Part, 8.1~12.4 parts of Hydrophilic dispersant, 3.5~8.5 parts of lipophile dispersant.
Optionally, the raw material of the mouthwash includes by weight：4~6 parts of rutaecarpin, lauryl sodium sulfate 0.5~
1.5 parts, double de- 8~12 parts of ethanol, sodium monofluorophosphate 0.03~0.07,0.1~0.3 part of chlorhexidine gluconate, glycerine 3~
7 parts and 0.5~1.5 part of polyoxyethylene chlorination castor oil.
Or the raw material of the mouthwash includes by weight：5 parts of rutaecarpin, 1 part of lauryl sodium sulfate, double de- second
10 parts of alcohol, 0.05 part of sodium monofluorophosphate, 0.2 part of chlorhexidine gluconate, 5 parts of glycerine and polyoxyethylene chlorination castor oil 1
Part.
This preparation method for being used to treat the mouthwash of periodontitis, it includes：
By rutaecarpin, surfactant, Hydrophilic dispersant and lipophile dispersant and it is dispersed in water, and
20~30min is stirred at 80~85 DEG C.
Optionally, it is additionally included in after the completion of reaction and adjusts the pH value of reaction solution between 5.5~6.5.It is more preferable, use
Sodium bicarbonate or ammoniacal liquor adjust pH.
It is this to be used to treat mouthwash of periodontitis and preparation method thereof, using rutaecarpin as effective component, utilize surface
Activating agent, Hydrophilic dispersant and lipophile dispersant by its it is dispersed mouthwash is made, can effectively prevent and administer tooth
Zhou Yan.
The feature and performance of the present invention are described in further detail with reference to embodiments：
Embodiment 1
The present embodiment provides a kind of mouthwash for being used to treat periodontitis, and its preparation method includes：
A. stock up：Rutaecarpin 5g, lauryl sodium sulfate 1g, double de- ethanol 10g, sodium monofluorophosphate 0.05g, glucose
Sour Chlorhexidine 0.2g, glycerine 5g and polyoxyethylene chlorination castor oil 1g.
B. emulsion reaction：Each component in above-mentioned raw materials is mixed and dispersed in 80g purified water, and stirred at 82 DEG C
25min is mixed, pH to 6.0 is adjusted with alkali, remembers mouthwash after filtering.
Embodiment 2
The present embodiment provides a kind of mouthwash for being used to treat periodontitis, and its preparation method includes：
A. stock up：Rutaecarpin 4g, polysorbate 1.5g, double de- ethanol 8g, sodium monofluorophosphate 0.03, gluconic acid chlorine oneself
Determine 0.3g, glycerine 3g and polyoxyethylene chlorination castor oil 0.5g.
B. emulsion reaction：Each component in above-mentioned raw materials is mixed and dispersed in 80g purified water, and stirred at 80 DEG C
30min is mixed, between adjusting pH to 6.5 with alkali, mouthwash is produced after filtering.
Embodiment 3
The present embodiment provides a kind of mouthwash for being used to treat periodontitis, and its preparation method includes：
A. stock up：Rutaecarpin 6g, fatty acid sorbitan 1.5g, double de- ethanol 12g, sodium monofluorophosphate 0.03, glucose
Sour Chlorhexidine 0.1g, glycerine 7g and polyoxyethylene chlorination castor oil 1.5g.
B. emulsion reaction：Each component in above-mentioned raw materials is mixed and dispersed in 80g purified water, and stirred at 85 DEG C
20min is mixed, between adjusting pH to 5.5 with alkali, mouthwash is produced after filtering.
Embodiment 4
The present embodiment provides a kind of mouthwash for being used to treat periodontitis, and its preparation method includes：
A. stock up：Rutaecarpin 5g, neopelex 1g, double de- ethanol 12g, sodium monofluorophosphate 0.03, grape
Saccharic acid Chlorhexidine 0.36g, glycerine 5g and Crodaret 1g.
B. emulsion reaction：Each component in above-mentioned raw materials is mixed and dispersed in 80g purified water, and stirred at 82 DEG C
25min is mixed, pH to 6.0 is adjusted with alkali, remembers mouthwash after filtering.
Embodiment 5
The present embodiment provides a kind of mouthwash for being used to treat periodontitis, and its preparation method includes：
A. stock up：Rutaecarpin 5g, polysorbate 1g, double de- ethanol 8g, sodium monofluorophosphate 0.03, chlorhexidine gluconate
0.07g, glycerine 3g and Crodaret 1g.
B. emulsion reaction：Each component in above-mentioned raw materials is mixed and dispersed in 80g purified water, and stirred at 82 DEG C
25min is mixed, pH to 6.0 is adjusted with alkali, remembers mouthwash after filtering.
Effect of the rutaecarpin in terms of preventing or treating periodontitis is evaluated with reference to experimental data.
Experimental example 1
Effect of the rutaecarpin to periodontitis：
First, experimentation：
1.1 main agents and instrument
250g/L trypsase, clostridiopetidase A, α-MEM culture mediums (GibcoBRL, the U.S.)；Porphyromonas gingivalis LPS
(Sigma, the U.S.)；RT-polymerase chain reaction (RT-PCR) kit, cell total rna extracts kit, reverse transcription reagents
Box (Takara, Japan)；Enzyme-linked immunosorbent assay instrument (BIO-TEK, the U.S.)；Inverted microscope and photographic system (Olympus,
Japan)；RT-PCR instrument (Applied Biosystems, the U.S.)
The separation method of 1.2 periodontal ligament stem cells
Collect 12~15 years old and ground before volunteer (patient and its equal informed consent of parent) health for being pulled out by correction subtrahend
Tooth 18, after being rinsed repeatedly with PBS immediately, in root 1/3 periodontal membrane tissue is scraped, and transferred them to added with appropriate
In the sterile petri dish of α-MEM nutrient solutions；Then again α-MEM nutrient solutions infiltration under by parodontium tissue be cut into 1mm × 1mm ×
1mm tissue block, and with 250g/L Trypsin Induced 15min.
After terminating digestion, supernatant is abandoned in centrifugation, then the tissue block of separation is evenly laid out in 6 orifice plates；Use sterile cover slips
After covering tissue block is allowed to adherent, the α-MEM nutrient solutions containing 100mL/L hyclones in right amount are added per hole, are placed in 50mL/L
CO2, cultivated in 37 DEG C of incubator.Change liquid 1 time per 3d, when cell growth is up to 80%, use STRO-1 for label with
Immuno magnetic cell separation screens Periodontal ligament stem cell, and carries out routine passage culture.
2nd, test method
The influence that 2.1MTT methods measure rutaecarpin is bred to periodontal ligament stem cell
The 4th generation Periodontal ligament stem cell that growth conditions are good is taken, through Trypsin Induced and density is made with α-MEM is
5×107After/L cell suspension, 96 orifice plates are inoculated in per hole with 200 μ L；After cultivating 24h under standard environment, original fluid is abandoned simultaneously
Cell is randomly divided into totally 5 groups of A, B, C, D and E；A groups add the α-MEM of the μ g/mL+LPS 10ng/mL containing rutaecarpin 1, B groups
Add the α-MEM of the μ g/mL+LPS 10ng/mL containing rutaecarpin 3, C groups add the μ g/mL+LPS 10ng/mL's containing rutaecarpin 6
α-MEM, D groups add the α-MEM of the 10ng/mL containing LPS, E groups add the α-MEM without LPS and continue to cultivate (per the μ L of hole 200).
Each group cell (every group of each time point each 4 hole) is taken respectively at culture 12,24,48,72h each time points, is added per hole
After entering 20 μ L MTT solution continuation quiescent culture 4h, supernatant in hole is carefully sucked, 150 μ L DMSO are respectively added in every hole,
And 15min is vibrated at room temperature；Then detect absorbance (A490) value at each hole 490nm wavelength respectively with ELIASA, and take 4
The average value in hole carries out statistical analysis.
The inhibition for the periodontal ligament stem cell inflammatory reaction that 2.2 rutaecarpins are induced LPS
The 4th good generation Periodontal ligament stem cell of growth conditions is taken, and packet transaction and training are carried out by 2.1 same methods
Support.After continuous culture 72h, cell RNA is extracted with Trizol kits one-step method, and according to Reverse Transcriptase kit specification, use
Random priming is by RNA reverse transcriptions into cDNA.According to GenBank databases, with the computer software design primers of Primer 5.0,
And primer is carried out by Shanghai Sheng Gong companies and synthesized, each primer sequence is shown in Table 1.
The primer sequence of table 1.
Then using cDNA as template, β-actin are internal reference, enter performing PCR with RT-PCR instrument and react, reaction condition is：94
DEG C pre-degeneration 4min, 94 DEG C of denaturation 20s, 60 DEG C of annealing 30s, 72 DEG C of extension 30s, totally 35 circulations；Last 72 DEG C of detection signals.
PCR reactions obtain threshold values Ct directly in PCR instrument after terminating, and using 2-△△ctMethod calculates each group IL-6, IL-1 β, TNF-α
MRNA relative expression levels.Every group is respectively provided with 5 parallel multiple holes, averages.
Osteoclast is broken up 2.3 rutaecarpins and the influence of maturation.
Find that periodontal mononuclear macrophage is in nuclear factor receptor activation factor ligand RANKL and people's macrophage according to research
It can break up under the stimulation induction of colony-stimulating factor to osteoclast.Osteoporosis is often led by excessive bone information
Cause, be the result of osteoclast overactivity.
Therefore selection mononuclear macrophage studies the osteoclast generation that Sophoridine is induced RANKL as cell model
Influence is very suitable for.Whether observation Sophoridine can suppress the expression of the special related gene of osteoclast and its osteoclast is bitten
The influence of bone ability, so as to illustrate that Sophoridine is being prepared for preventing and treating application and mechanism in the medicine of osteoporosis.
Osteoclast is divided into show that Sophoridine of the present invention can suppress Bone Marrow Macrophage, now by mouse bone marrow cells
Macrophage is with 1 × 104Individual/cell is inoculated in 96 orifice plates, and culture medium is discarded after cell covers with, (empty with final concentration of 0 respectively
White control group), 5 μ g/mL, 10 μ g/mL, 15 μ g/mL rutaecarpin is added in each fresh culture, then add 96 orifice plates
In, while RANKL (50ng/mL), M-CSF (50ng/mL) inducing mouse bone marrow macrophages break up to osteoclast.Then,
TRAP dyeing (Fig. 1) is carried out to mouse macrophage, and quantitative statisticses (Fig. 2 and Fig. 3) are carried out to result, is found with Sophoridine
The increase of concentration can substantially suppress Bone Marrow Macrophage and be divided into osteoclast.
From above-mentioned experiment and Fig. 1~Fig. 3, rutaecarpin of the present invention can be with the suppression monokaryon macrophage of concentration dependant
Cell breaks up to osteoclast, suppresses bone information, suppresses tooth mobility caused by periodontitis from source.
The formation of osteoclast can preferably be suppressed to determine that period adds rutaecarpin, now by mouse bone marrow cells
Macrophage is with 1 × 104Individual/cell is inoculated in 96 orifice plates, at the same RANKL (50ng/mL) inducing mouse bone marrow macrophages to
Osteoclast breaks up, and then discards culture medium at the 0th day, the 2nd day, the 4th day and the 5th day respectively, adds final concentration of 60 μ g/mL
Rutaecarpin culture medium.Then, TRAP dyeing (Fig. 4) is carried out to mouse macrophage, and quantitative analysis is carried out to result
(Fig. 5 and Fig. 6).As a result show, need to appear in early stage and whole to effectively suppress the formation rutaecarpin of osteoclast
In individual RANKL inductions atomization.
2.4 statistical analysis
Variance analysis is carried out to data with the softwares of SPSS 19.0, compares examined with t two-by-two, inspection level α=0.01.
3rd, experimental result
Influence of the 3.1 various concentrations rutaecarpins to periodontal ligament stem cell appreciation rate
After various concentrations rutaecarpin and 10ng/mL LPS act on Periodontal ligament stem cell 12,24,48,72h, MTT
Testing result is shown：The A490 values at each group each time point are minimum with negative control group (E groups)；A, B, C and D group in each time point
With the A490 values between E groups two-by-two compared with have significant difference (P ＜ 0.05).But compare between A, B, C and D group, evodia rutaecarpa
The cell proliferation rate of alkali group declines slightly, but not statistically significant, shows rutaecarpin below 6 μ g/mL concentration to periodontal
Film stem cell proliferation is without influence.
The effect that rutaecarpin is bred to periodontal ligament stem cell in the different time points of table 2
This experimental example is respectively adopted 10ng/mL LPS and Periodontal ligament stem cell is stimulated, and makes periodontal ligament stem cell inflammation
Disease model.Co-cultured simultaneously using rutaecarpin, influence of the observation rutaecarpin to periodontal ligament stem cell proliferation rate.
As a result show, compared with control group, A490 value significantly rise of the 10ng/mL LPS groups in each time, and add
A490 values after rutaecarpin at each time point change without conspicuousness；Prompting, the LPS (10ng/mL) of low concentration is to people's parodontium
The propagation of stem cell has facilitation, and rutaecarpin is acted on without conspicuousness the propagation of periodontal ligament stem cell.
3.2 rutaecarpins suppress the periodontal ligament stem cell inflammatory reaction of LPS inductions
The rutaecarpin (1,3,6 μ g/mL) of various concentrations acts on Periodontal ligament stem cell, RT- with 10ng/mL LPS
PCR testing results are shown：Compared with E groups, IL-6, IL-1 β, the TNF-α mRNA expressions of A, B, C and D group are lifted, and are represented
Model successfully.Compared with D groups, IL-6, IL-1 β, the TNF-α mRNA expressions of A, B and C group decline, and with high dose group C
Group becomes apparent from, C groups between D groups two-by-two compared with have significant difference (P ＜ 0.01) (table 3).
Inhibitory action of the rutaecarpin of table 3. to periodontal ligament stem cell inflammatory Cytokines Expression
This experimental example is respectively adopted 10ng/mL LPS and Periodontal ligament stem cell is stimulated, and makes periodontal ligament stem cell inflammation
Disease model.Co-cultured simultaneously using rutaecarpin, inhibition of the observation rutaecarpin to periodontal ligament stem cell inflammation.
TNF-α, IL-6 are monocyte, lymphocyte and multifunctional cytokine caused by fibroblast, and it is given birth to
Thing activity is relatively broad.Studies have found that the LPS of bacterium actinomycetem comitans and porphyromonas gingivalis can promote hPDLSCs to close
Into IL, TNF-α, and raise its mRNA expression.Wherein, the LPS of porphyromonas gingivalis mainly by with people's tooth
The acceptor of all film stem cell surfaces combines, and then stimulates Periodontal ligament stem cell to discharge inflammatory factor, thus in the hair of periodontitis
Played a significant role during life.The LPS for having studies have shown that porphyromonas gingivalis can promote the life of monocyte and liver cell
Long factor release interleukin, TNF-α and Prostaglandin E2, and IL-1 the and IL-6 secretion levels of stem cell factor can be made notable
Rise.
This result is shown, is contrasted with control group (D groups), A, B and C group (being respectively the basic, normal, high dosage group of rutaecarpin)
IL-6, IL-1 β, TNF-α mRNA expressions are remarkably decreased, and are declined with C groups (high dose group) and become apparent from；Between C groups and D groups
Comparing two-by-two has significant difference (P ＜ 0.05).Thus illustrate, rutaecarpin can suppress IL-6, IL-1 caused by LPS, TNF-α
MRNA expression rises.
From the above results, it is dry thin effectively to suppress parodontium caused by the LPS of porphyromonas gingivalis for rutaecarpin
Born of the same parents' inflammation, the inhibitor of periodontal ligament stem cell inflammatory reaction can be prepared with rutaecarpin.
3.3 rutaecarpins can significantly inhibit osteoclast differentiation and maturation
Periodontal ligament stem cell is stimulated by periodontal bacteria, and a large amount of inflammatory factors that produce can't cause serious periodontosis
Become, only after its caused inflammatory factor largely activates osteoclast, can just produce the symptom of alveolar bone excessive consumption, draw
Play serious periodontosis and tooth mobility.It is ripe osteoclastic after the rutaecarpin of various dose is added as shown in Fig. 1~Fig. 6
The quantity of cell decreases drastically (red for mature osteoclast).Show that rutaecarpin can significantly inhibit osteoclast
Alveolar bone caused by activation crosses absorption, and the inhibitor of osteoclast differentiation and maturation can be prepared with rutaecarpin.
In summary, rutaecarpin can effectively suppress periodontal ligament stem cell inflammation caused by the LPS of porphyromonas gingivalis,
And alveolar bone caused by suppressing osteoclast activation crosses absorption, it can be used for preparing medicine or the guarantor of prevention or treatment periodontitis
Strong product.
Experimental example 2
Therapeutic action of the rutaecarpin mouthwash to tooth mobility
User of 76 age distributions 46-59 year is randomly selected, men and women half and half, divides according to tooth mobility indices P TV
Into healthy group (19 people, PTV-8-9), slight loosening group (20 people, PTV10-19), loosening group (17 people, PTV20-29) and serious
(30) 20 people, PTV are more than loosening group.The user of all groups is carried out using the mouthwash provided in the embodiment of the present invention 1
The treatment of half a year, the tooth mobility situation of user is recorded after treatment according to tooth mobility indices P TV, as a result as shown in table 4：
The tooth mobility situation of the user of table 4.
| Before treatment (PTV ± SD) | After treatment (PTV ± SD) | |
| Healthy group | 3±4 | 1±4 |
| Slight loosening group | 16±5 | 12±2* |
| Loosening group | 25±3 | 15±4** |
| Serious loosening group | 37±5 | 28±3 |
*P≤0.05,**p≦0.01
Test result indicates that mouthwash on healthy group of crowd's tooth mobility situation without influence, in terms of showing no tooth
Side effect.To slight loosening group and loosening group, the therapeutic effect with conspicuousness, but the patient outcomes to seriously loosening
Typically.
In addition, the mouthwash that other embodiments are provided is used to carry out above-mentioned experiment, it is as a result basically identical with embodiment 1,
Therefore do not repeat one by one.
Although illustrate and describing the present invention with specific embodiment, but will be appreciated that without departing substantially from the present invention's
Many other change and modification can be made in the case of spirit and scope.It is, therefore, intended that in the following claims
Including belonging to all such changes and modifications in the scope of the invention.
Claims (10)
1. purposes of the rutaecarpin in the medicine or health products for preparing prevention or treatment periodontitis.
2. purposes of the rutaecarpin in the inhibitor for preparing periodontal ligament stem cell inflammatory reaction.
3. purposes according to claim 2, it is characterised in that the rutaecarpin is produced by suppressing periodontal ligament stem cell
Inflammatory factor suppresses periodontal ligament stem cell inflammatory reaction.
4. purposes according to claim 3, it is characterised in that the inflammatory factor includes interleukin-6, leucocyte
Interleukin -1, tumor necrosis factor-alpha.
5. purposes according to claim 2, it is characterised in that the periodontal ligament stem cell inflammatory reaction is by periodontal dominant bacteria
Lipopolysaccharide-induced generation.
6. purposes of the rutaecarpin in the inhibitor of osteoclast differentiation and maturation is prepared.
7. a kind of mouthwash for being used to treat periodontitis, it is characterised in that the raw material of the mouthwash includes：Rutaecarpin, table
Face activating agent, Hydrophilic dispersant and lipophile dispersant.
8. the mouthwash according to claim 7 for being used to treat periodontitis, it is characterised in that the Hydrophilic dispersant bag
Include：Double de- ethanol, sodium monofluorophosphate, chlorhexidine gluconate.
9. the mouthwash according to claim 7 for being used to treat periodontitis, it is characterised in that the lipophile dispersant bag
Include：Glycerine, polyoxyethylene chlorination castor oil, Crodaret.
10. the preparation method for being used to treat the mouthwash of periodontitis according to any one of claim 7~9, its feature exist
In it includes：
By the rutaecarpin, the surfactant, the Hydrophilic dispersant and the lipophile dispersant simultaneously
It is dispersed in water, and 20~30min is stirred at 80~85 DEG C.
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| CN108904504A (en) * | 2018-06-20 | 2018-11-30 | 暨南大学 | Application of the rutaecarpin in the drug of preparation enhancing NLRP3 inflammation corpusculum activation |
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