CN106038576A - Application of syringin in preparation of medicines for treating osteoporosis and medicine composition of syringin - Google Patents
Application of syringin in preparation of medicines for treating osteoporosis and medicine composition of syringin Download PDFInfo
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- CN106038576A CN106038576A CN201610474623.1A CN201610474623A CN106038576A CN 106038576 A CN106038576 A CN 106038576A CN 201610474623 A CN201610474623 A CN 201610474623A CN 106038576 A CN106038576 A CN 106038576A
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- syringoside
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
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Abstract
The invention provides application of syringin in preparation of medicines for treating osteoporosis. The structural formula of the syringin compound is as shown in the specification, and the syringin has a molecular formula of C17H24O9 and a molecular weight of 372.37. The invention further provides a medicine composition of the syringin for preventing and treating osteoporosis.
Description
Technical field
The present invention relates to the new application of syringoside, particularly to a kind of syringoside as preparation treatment osteoporosis
The application of medicine and pharmaceutical composition.
Background technology
Osteoporosis (osteoporosis, OP) is that a kind of minimizing with bone amount is characterized with bone micro-structure destruction, causes
Bone strength declines, and fragility increases and is prone to the metabolic osteopathy of fracture.Along with aged tendency of population, OP has become the whole world and has paid close attention to
One of infirmities of age.Epidemiological study finds, osteoporosis occurs in the white man postmenopausal women that there are about half.OP patient sends out
The risk of bone growth promoting folding is up to 40%, is mainly in vertebra, hipbone and carpal joint.China is the country that old people is most in the world, this
Sick incidence rate is in being gradually increasing trend.At present, there is sufferers of osteoporosis face 84,000,000 in China, accounts for the 6.6% of total population, 50 years old with
The average age of onset of upper old man's Hip Fracture is 67.2 years old, and this not only have impact on the physiology of patient, mental health, is substantially reduced
Quality of life, also bring serious commercial burden to society.Osteoporosis belongs to degenerative disease, there is no specific drug at present.City
On field, existing anti-osteoporotic is broadly divided into three major types: bone resorption inhibitor, bone mineralizer and bone formation-promoter.Cause
Chemicals is prevented and treated osteoporosis and is often needed drug combination, and toxic and side effects is big, finds and prevent and treat osteoporosis disease from natural plants
Sick and that side effect is little monomeric compound has become study hotspot.
Syringoside (syringin), has another name called ligustrin, Syringin, is extraction isolated from Radix Et Caulis Acanthopanacis Senticosi rhizome
A kind of typical phenolic glycoside compounds, be also the main component of the Chinese medicines such as Daphne giraldii Nitsche, Hex godajam (colebr) Wall, Magnolia sieboldii, Radix Syringae velutinae,
It it is one of index components of measuring of medical material and formulation content thereof.From its chemical structure analysis, the aglycon of syringoside is sinapinic alcohol,
Its derivant belongs to phenylpropyl alcohol alcohols material, has antioxidant activity.Research for syringoside at present focuses mostly on containing measuring
Determining in the foundation of method, bioactive research is the most less, and only several document report syringoside have stronger antiinflammatory town
Pain and immunoregulation effect, yet there are no relevant syringoside and can be used for preventing and treating osteoporotic research report.
Summary of the invention
The invention provides the new opplication of syringoside, i.e. syringoside answering as preparation treatment osteoporosis agents
With.
There is a need to provide a kind of osteoporotic pharmaceutical composition of the preventing and treating containing syringoside.
The embodiment of the present invention provides a kind of syringoside to treat the application of osteoporosis agents, wherein purple fourth as preparation
The structural formula of fragrant glycosides is:
And the molecular formula of syringoside is C17H24O9, molecular weight is 372.37.
The embodiment of the present invention also provides for a kind of osteoporotic pharmaceutical composition of the preventing and treating containing syringoside, including purple fourth
Any adjuvant on fragrant glycosides and medicament, the weight ratio of described syringoside and described adjuvant is 1:99～10:90, wherein utilizes purple fourth
Fragrant glycosides prevents and treats osteoporosis as active component, and wherein the structural formula of syringoside is:
And the molecular formula of syringoside is C17H24O9, molecular weight is 372.37.
Above-mentioned syringoside treats the application of osteoporosis agents and a kind of preventing and treating containing syringoside as preparation
Osteoporotic pharmaceutical composition, is that inventor causes mice osteoporosis animal experiment it was confirmed syringoside has through removal ovary
There is the osteoporotic effect of preventing and treating, and prepare the osteoporotic pharmaceutical composition of the preventing and treating containing syringoside.
Detailed description of the invention
Inventor causes mice osteoporosis animal experiment through removal ovary, it was demonstrated that it is osteoporotic that syringoside has preventing and treating
Effect.
The embodiment of the present invention provides a kind of syringoside to treat the application of osteoporosis agents, wherein purple fourth as preparation
The structural formula of fragrant glycosides is:
Syringoside (Syringin), has another name called ligustrin, Syringin, and molecular formula is C17H24O9, molecular weight is 372.37, is
The main component of the Chinese medicines such as Radix Et Caulis Acanthopanacis Senticosi.
Further, in the embodiment of the present invention, syringoside can make the osteoporotic pharmaceutical composition of preventing and treating, this medicine
Compositions includes that any adjuvant on syringoside and pharmaceutics, syringoside are 1:99～10 with the weight ratio of other adjuvant:
90, wherein utilize syringoside as active component to prevent and treat osteoporosis, other adjuvant is any acceptable on medicament
Excipient, such as starch, lactose, microcrystalline Cellulose, dextrin, hydroxypropylcellulose, polyvinylpolypyrrolidone, pregelatinized Starch, Pulvis Talci,
Magnesium stearate, micropowder silica gel, sodium lauryl sulphate, Tween 80, hydrogenated vegetable oil etc..
Causing mice osteoporosis animal experiment through removal ovary, confirmation syringoside has the effect of osteoporosis, tool
Body experiment sieving process is as follows:
(1) animal, reagent and instrument.
1, animal: 2 month female ICR mices 60, cleaning grade, body weight 25 ± 5g.
2, medicine and reagent: test medicine: syringoside, purity > 95%.Positive control drug: estradiol valerate (is mended good
Happy).
3, instrument: (analyze software is that Micview V2.1.2 three-dimensional reconstruction processes to eXplore Locus SP type Micro-CT scanning
Software；The special bone analysis software of ABA)；Dual-energy x-ray absorptiometry (Lunar company DPX type)；Analytical balance
(AL104, METTLER TOLEDO)；Table-type high-speed refrigerated centrifuge (1-15K type)；Ultra cold storage freezer (Forma-86C ULT
Freezer)。
(2) animal experiment method.
1, experiment packet and gastric infusion dosage: 2 month female ICR mices are randomly divided into 6 groups by body weight, often organize 10
Only, packet and dosage are as follows:
Sham operated rats (SHAM is orally administered to equal-volume 0.5%CMC-Na)；
Model control group (OVX is orally administered to equal-volume 0.5%CMC-Na)；
Positive drug group (EV is orally administered to estradiol valerate, 0.1mg/kg/d)；
Syringoside high dose (SYH, oral dose 40mg/kg/d respectively)；
Dosage (SYM, oral dose 20mg/kg/d respectively) in syringoside；
Syringoside low dosage (SYL, oral dose 10mg/kg/d respectively).
Above positive control drug and test medicine make solvent by 0.5% Sodium Tvlose (0.5%CMC-Na) respectively
It is made into the concentration of needs.
2, zoopery.
By above 60 female mices temperature be 24 ± 0.5 DEG C, humidity be 45-50%, well-ventilated in the environment of suitable
After Ying Yizhou, carry out removal ovary experimental study.It is grouped according to above animal, takes mice, lumbar injection 7% chloral hydrate
(0.3ml/100g) anaesthetize.After confirming animal holonarcosis, aseptically, cut off about 1cm in bilateral back rapidly
Otch: sham operated rats mice only take out back bilateral fat a little after sew up the incision, other is respectively organized mice and all takes out bilateral ovaries
Tighten fallopian tube rear cutout and remove ovary, sew up the incision.Each group mice prevents wound sense in the postoperative penicillin of lumbar injection for three days on end
Dye.
Each treated animal starts to be administered after performing the operation 3 days.Often group mice is by body weight 10ml/kg gastric infusion, sham operated rats
SHAM group and model OVX group give same volume 0.5%CMC-Na, and other each administration group presses above each administration group dosage gavage every day
It is administered once, 6 times a week.Successive administration 12 weeks.Claim 1 body weight every two weeks, adjust dosage.
After last 1 time is administered, being respectively placed in metabolic cage by every mice, water is can't help in fasting, collects urine, and in anesthesia
Rear right common femoral artery takes blood and collects serum, peels off rapidly femur and tibia masking foil on the right side of hind leg and wraps；The most each sample standard deviation
It is placed in-80 DEG C of Refrigerator stores standby.
3, bone index determining.
Dual-energy x-ray borne densitometers is utilized to measure total bone density (t-BMD) of every right side of mice femur.
4, femur osseous tissue Senile Mouse.
Take right side femur, reject muscle and soft tissue, will hang down at femur about 1 cm between near end of thighbone tuberosity with cutting machine
Vertical cut cuts, and puts in micro-CT and is scanned.After having scanned, use Micview V2.1.2 three-dimensional reconstruction to process software and carry out
The reconstruction of each sample 3-D view；The special bone analysis software of ABA carries out Data Analysis Services.
5, data analysis.
Experimental data is all usedRepresent, statistical analysis spss 16.0 software carries out one factor analysis of variance, with p <
0.05 for having significant difference.
6, interpretation of result.
Each group mouse femur total bone density t-BMD testing result is shown in Table 1.After mice is administered 12 weeks, model OVX group Mouse Bone
Density is compared with sham operated rats SHAM, and bone density significantly reduces (p < 0.01), and modeling success is described.With model group mice phase
Ratio, syringoside high, medium and low dosage group (SYH, SYM and SYL) can significantly improve the Mouse Bone density reduction that removal ovary causes
(p<0.01).Therefore, bone density result shows, mice removal ovary causes osteoporosis modeling success, and syringoside can be notable
Improve the bone density of ovariectomized mouse.
The total bone density of mouse femur (n=8) respectively organized by table 1
Note: compared with model group OVX,**p<0.01。
Microscopic CT scanning gained bone mineral content and each parametric results of bone trabecula of the osseous tissue form of each group mouse femur are shown in
Shown in table 2 and table 3.
Mouse femur bone mineral content parameter (n=4) respectively organized by table 2
Note: compared with model group OVX,*p<0.05,**p<0.01。
The each parameter of Mouse Bone girder (n=4) respectively organized by table 3
Note: compared with model group OVX,*p<0.05,**p<0.01。
Can be found out intuitively by table 2 and table 3: after (1) mice removal ovary, compared with SHAM group, OVX group rat bone mineral content
(Bone Mineral Content, BMC), organizes mineral content (Tissue Mineral Content, TMC) bone volume mark
(Bone Volume Fraction, BVF), tissue bone density (Tissue Mineral Density, TMD), bone trabecula quantity
(Trabecular Number, Tb.N) and bone trabecula Connection Density (Connectivity Density, CD) substantially reduce (p <
0.05)；Bone trabecula separating degree (Trabecular Separation, Tb.Sp) significantly increases (p < 0.05)；(2) each administration group,
Positive drug, syringoside high, medium and low dosage group all can significantly improve osseous tissue and loosen situation, wherein BMC, TMC, BVF, Tb.N
Dramatically increasing (p < 0.05), Tb.Sp is substantially reduced (p < 0.05)；(3) bone trabecula thickness (Trabecular Thickness,
Tb.Th) aspect, though each group of trend having increase, but no difference of science of statistics.
These results suggest that, causing trabecular bone structure to loosen after mice removal ovary, bone mineral content etc. significantly reduces；Syringa oblata Lindl.
Glycosides can significantly inhibit bone density caused by removal ovary, bone mineral content reduces, and increases bone trabecula number and Connection Density.
7, conclusion.
Cause mice osteoporosis animal pattern result of the test by removal ovary and can show that syringoside has preventing and treating sclerotin
Loose drug action.
Claims (3)
1. syringoside is as an application for preparation treatment osteoporosis agents, wherein, the compound structure of syringoside
Formula is:
And the molecular formula of syringoside is C17H24O9, molecular weight is 372.37.
2. the osteoporotic pharmaceutical composition for the treatment of containing syringoside, it is characterised in that include syringoside and auxiliary
Material, described syringoside is 1:99～10:90 with the weight ratio of described adjuvant, wherein utilizes syringoside to come as active component
Preventing and treating osteoporosis, wherein the structural formula of syringoside is:
And the molecular formula of syringoside is C17H24O9, molecular weight is 372.37.
3. the osteoporotic pharmaceutical composition for the treatment of containing syringoside as claimed in claim 2, it is characterised in that described
Adjuvant is excipient, and described excipient includes starch, lactose, microcrystalline Cellulose, dextrin, hydroxypropylcellulose, polyvinylpolypyrrolidone, pre-
In gelling starch, Pulvis Talci, magnesium stearate, micropowder silica gel, sodium lauryl sulphate, Tween 80, hydrogenated vegetable oil any one.
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| CN201610474623.1A CN106038576A (en) | 2016-06-27 | 2016-06-27 | Application of syringin in preparation of medicines for treating osteoporosis and medicine composition of syringin |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100842785B1 (en) * | 2007-04-25 | 2008-07-01 | 주식회사 동원에프앤비 | A pharmaceutical composition comprising eleutheroside b for treating and preventing bone disease |
| KR20080095700A (en) * | 2007-04-25 | 2008-10-29 | 주식회사 동원에프앤비 | A health care composition comprising eleutheroside b for the prevention and alleviation of bone disease |
| CN101596203A (en) * | 2009-07-24 | 2009-12-09 | 李超生 | The application of syringoside in preparation treatment cardiovascular and cerebrovascular diseases medicament |
| CN103622980A (en) * | 2013-12-12 | 2014-03-12 | 宁夏医科大学 | Application of cistanche phenylethanoid glycoside compound to preparation of drugs for treating osteoporosis and drug composition containing cistanche phenylethanoid glycoside compound |
-
2016
- 2016-06-27 CN CN201610474623.1A patent/CN106038576A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100842785B1 (en) * | 2007-04-25 | 2008-07-01 | 주식회사 동원에프앤비 | A pharmaceutical composition comprising eleutheroside b for treating and preventing bone disease |
| KR20080095700A (en) * | 2007-04-25 | 2008-10-29 | 주식회사 동원에프앤비 | A health care composition comprising eleutheroside b for the prevention and alleviation of bone disease |
| CN101596203A (en) * | 2009-07-24 | 2009-12-09 | 李超生 | The application of syringoside in preparation treatment cardiovascular and cerebrovascular diseases medicament |
| CN103622980A (en) * | 2013-12-12 | 2014-03-12 | 宁夏医科大学 | Application of cistanche phenylethanoid glycoside compound to preparation of drugs for treating osteoporosis and drug composition containing cistanche phenylethanoid glycoside compound |
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Application publication date: 20161026 |