CN106562958A - A medicine containing Volvalerelactones A and used for protecting aging type immune organs - Google Patents
A medicine containing Volvalerelactones A and used for protecting aging type immune organs Download PDFInfo
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- CN106562958A CN106562958A CN201610923978.4A CN201610923978A CN106562958A CN 106562958 A CN106562958 A CN 106562958A CN 201610923978 A CN201610923978 A CN 201610923978A CN 106562958 A CN106562958 A CN 106562958A
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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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
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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
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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Abstract
A medicine containing Volvalerelactones A and used for protecting aging type immune organs is disclosed. Effective components include the Volvalerelactones A and tiliroside. Through combined application of the Volvalerelactones A and the tiliroside, experiment results prove that effects for protecting aging type immune organs are good when the ratio of the Volvalerelactones A to the tiliroside is 15:1-18:1.
Description
Technical field
The present invention relates to a kind of be used to protect the medicine of involution form immune organ comprising Volvalerelactones A, category
In pharmaceutical technology field.
Background technology
In recent years, international medical community shortens to telomere and telomere azymia is very active with the research of Senescence, it is believed that
When the normal somatic cell division number of times of people reaches boundary (Hay flick boundaries), fringes of chromosome contraction in length is to certain journey
Degree, mitosiss are just irreversibly blocked certain period between the G1 phases and G2/M phases of cell cycle, at this moment
Cell just enters aging period, subsequently dead.Research has shown that telomere is closely related with the control of cell survival.Mankind's telomere is long
Degree about 2～15kb, due to there are problems that end is replicated, DNA often replicates 1 time, and telomeric dna will lose 50～
200bp, with the increase of frequency dividing cell, telomeric dna progressively shortens, and after shortening to certain limit, just can not maintain
Chromosome is stablized, and cell just loses division growth ability and aging death, this shortening is exactly the mark of aging.Therefore,
Telomere is also referred to as " the life clock " of cell, and the aging of cell decides the aging of whole body.Telomerase has now been found that
The only ribonucleoprotein enzyme being made up of RNA and protein, with reverse transcription activity, can close by template of the RNA of itself
Into telomeric dna.The function of telomerase mainly has two：One is the progradation to telomeric dna；Two can repair fracture
End of chromosome, by repairing, can make chromosome keep complete, prevent mutual fusion, restructuring and other infringements of chromosome,
So as to keep the complete and stable of genome.It is now recognized that intracellular telomerase disappearance, causes telomere to shorten, when telomere contracting
Be short to one " critical length ", the stability of chromosome is just destroyed, its DNA double-strand may rupture and active cell itself
Checking system, at this moment cell just enter " phases of M 1 death state ", subsequent chromosome is further destroyed, such as dyeing body weight
Row, the abnormal conditions such as the formation of dicentric chromosome and aneuploidy change occur, and cell just enters " M2 phases death shape
State ", is finally dead arriving.If the relative shortage of telomerase activation causes the shortening of telomere length and induces thin
Born of the same parents' aging, can speculate by activating telomerase activation to maintain telomere length and stablize.Slow down the speed of telomere shortening and delay
Cell ageing.But if reactivating telomerase, these cells for regaining telomerase activation will likely become immortality cell,
Then cancer is developed into.Experiment in vitro confirms that the expression of telomerase and the maintenance of telomere integrity can not escape cell cycle
The control at the outpost of the tax office, so as to cause mrna instability to determine;Telomerase makes cellular immortalization also can prevent or reverses senile cell physiology work(
The forfeiture of energy, without causing other changes related to cancer.Rebuilding telomerase activation can make the cell life extension of people, and not
Change its feature sex expression.Therefore, all the time, the day about above-mentioned side effect, small toxicity, therapeutic effect can be overcome outstanding
So research and development of thing or new compound are constantly carried out.
Compound VolvalerelactonesA be one deliver within 2011 (Peng-Cheng Wang, et al.,
Volvalerelactones A and B, Two New Sesquiter penoid Lactones with an
Unprecedented Skeleton from Valeriana officinalis var. latifolia. Organic
Letters, 2011,13 (12), 3036-3039.) noval chemical compound, the compound possesses brand-new framework types, at present also not
See is being used to protect the application of involution form immune organ with regard to VolvalerelactonesA and silver forging glycosides.
The content of the invention
For the problem that above-mentioned prior art is present, the present invention provides one kind to be used for comprising Volvalerelactones A
The medicine of protection involution form immune organ.
To achieve these goals, the technical solution used in the present invention is：It is a kind of to use comprising Volvalerelactones A
In the medicine of protection involution form immune organ, effective ingredient includes VolvalerelactonesA, and structural formula is as follows：
Effective ingredient includes also including silver forging glycosides.
Calculate according to weight, VolvalerelactonesA and silver forging glycosides ratio are 15:1-20:1.
Calculate according to weight, VolvalerelactonesA and silver forging glycosides ratio are 20:1.
The preferred solid orally ingestible of the pharmaceutical composition；Further, described oral formulations be tablet, capsule,
Granule, dry suspension or drop pill.
It should be noted that available adjuvant on pharmaceuticss of the present invention, refers to and be included in addition to the active ingredient (s agent
Inert matter in type, includes but are not limited to filler (diluent), lubricant (fluidizer or antitack agent), dispersion
Agent, wetting agent, binding agent, solubilizing agent, antioxidant, antibacterial, emulsifying agent, disintegrating agent etc..Binding agent includes syrup, Arab
Glue, gelatin, Sorbitol, tragacanth, cellulose and its derivates are (such as Microcrystalline Cellulose, sodium carboxymethyl cellulose, ethyl cellulose
Or hydroxypropyl methylcellulose etc.), gelatine size, syrup, starch slurry or polyvinylpyrrolidone etc.；Filler comprising Lactose, Icing Sugar,
Dextrin, starch and its derivant, cellulose and its derivates, inorganic calcium salt are (such as calcium sulfate, calcium phosphate, calcium hydrogen phosphate, sedimentation carbon
Sour calcium etc.), Sorbitol or glycine etc.；Lubricant includes micropowder silica gel, magnesium stearate, Pulvis Talci, aluminium hydroxide, boric acid, hydrogen
Change vegetable oil, Polyethylene Glycol etc.；Disintegrating agent is comprising starch and its derivant (such as carboxymethyl starch sodium, Explotab, pre- glue
Change starch, modified starch, hydroxypropyl starch, corn starch etc.), polyvinylpyrrolidone or Microcrystalline Cellulose etc.；Wetting agent bag
Containing sodium lauryl sulphate, water or alcohol etc.；Antioxidant packages contain sodium sulfite, sodium sulfite, sodium pyrosulfite, dibutyl benzoic acid
Deng；Antibacterial includes 0.5% phenol, 0.3% cresol, 0.5% chlorobutanol etc.；Emulsifying agent includes Tween-80, does not have acid
Pyrusussuriensiss are smooth, lecithin, fabaceous lecithin etc.；Solubilizing agent includes tween 80, bile, glycerol etc.
The a kind of of present invention offer is used to protect the medicine of involution form immune organ comprising Volvalerelactones A, passes through
VolvalerelactonesA and silver forging glycosides use in conjunction, test result indicate that, VolvalerelactonesA and silver forging glycosides exist
15:1-18:In 1 ratio, for protection immune organ hepatic tissue has good cooperative effect.
Specific embodiment
Described above is only the general introduction of technical solution of the present invention, in order to better understand the technological means of the present invention,
And can be practiced according to the content of description and ordinary skill in the art means, the animal experiment example of the present invention is done below
It is described in further detail.
Chinese:Silver forging glycosides CAS：20316-62-5.Chengdu Zhi Biaohuachun Bioisystech Co., Ltd is on sale.
The preparation method of compound VolvalerelactonesA involved in the present invention is referring to document：(Peng-
ChengWang,etal.,VolvalerelactonesAandB,TwoNewSesquiterpenoidLactoneswith
AnUnprecedentedSkeletonfromValerianaofficinalisvar.latif olia.Organic Letters,
2011,13(12),3036–3039.)
Checking test：
Modeling：Two grades of male ablactation rats, the g of body weight 40～60,25 DEG C～28 DEG C of animal housing's ambient temperature, humidity 35%
～45%.Two grades of male ablactation rats 210.21 groups are randomly divided into, one group is blank group.D- gal Aging rat models
Modeling, continuous 8 weeks daily nape part ih D- galactose solution 500mg/kg of remaining group group of normal group nape part ih normal saline.
Experimental technique
Murine liver tissue Biochemical Indexes are determined：Hepatic tissue is taken, 100ml is cut and is placed in homogenizer, add PBS solution 1ml
, it is homogenized on ice, 10% liver homogenate liquid is made, 3500r/min centrifugation 10min take supernatant and are stored in -20 DEG C illustratively
Book determines GSH-ps enzymatic activitys, MAO activity and MDA contents, and determines protein content using BCA methods.
A is VolvalerelactonesA, and B is silver forging glycosides
The GSH-ps enzymatic activitys of each group rat, MAO activity and MDA comparision contents (g/ L, x ± s)
| Group | Dosage g/kg.bw | MAD(U/mg) | GSH-px（u/mg） | MAO (U/mg) |
| A:B(20:1) | 0.2 | 2.5+0.02 | 433.4+60.7 | 61.7 +4.3 |
| A:B(20:1) | 0.1 | 2.6+0.3 | 421.7+73.5 | 62.5+4.2 |
| A:B(18:1) | 0.2 | 1.1+0.3 | 551.6+70.2 | 50.4+4.2 |
| A:B(18:1) | 0.1 | 1.3+0.3 | 541.2+75.6 | 49.1.4+4.2 |
| A:B(15:1) | 0.2 | 1.0+0.3 | 568.6+51.3 | 48.4+4.2 |
| A:B(15:1) | 0.1 | 1.2+0.2 | 561.3.5+86.3 | 49.9+4.1 |
| A:B(10:1) | 0.2 | 2.6 +0.2 | 432.7+74.5 | 61.6+4.2 |
| A:B(10:1) | 0.1 | 2.8 +0.2 | 427.5+60.3 | 64.7+4.1 |
| A:B(2:1) | 0.2 | 2.9 +0.4 | 412.4+62.3 | 65.3+4.2 |
| A:B(2:1) | 0.1 | 3.0+0.2 | 403.2+70.5 | 68.6+4. |
| A:B(1:1) | 0.2 | 2.8+0.4 | 413.6+75.8 | 63.1+4.0 |
| A:B(1:1) | 0.1 | 2.9 +0.4 | 401.4+70.2 | 62.6+4.2 |
| A:B(1:5) | 0.2 | 3.1 +0.3 | 409.2+69.6 | 63.1+4.4 |
| A:B(1:5) | 0.1 | 3.2 +0.3 | 404.4+61.3 | 66.7+4.2 |
| A:B(1:10) | 0.2 | 3.1 +0.2 | 421.2+60.3 | 68.5.4+4.2 |
| A:B(1:10) | 0.1 | 3.2+0.2 | 412.8+59.6 | 70.3+4.1 |
| A | 0.2 | 3.2+0.1 | 412.3+70.4 | 77.3+4.0 |
| A | 0.1 | 3.5+0.1 | 404.5+51.5 | 80.2+4.2 |
| B | 0.2 | 3.3+0.1 | 422.4+48.4 | 78.2+4.3 |
| B | 0.1 | 3.6+0.1 | 406.1+45.3 | 81.4+4.2 |
| Blank control group | 0.2 | 0.9+0.1 | 578.5+81.2 | 47.4+4.1 |
P<0.05
Test result indicate that：Each group rat GSH-ps enzymatic activitys, the comparison of MAO activity and MDA contents, are administered after experiment
VolvalerelactonesA and silver forging glycosides are 18:1-15:The GSH-ps enzymatic activitys of 1 two groups of rats, MAO activity and MDA contents
All very close to the visible medicine VolvalerelactonesA of blank group and silver forging glycosides 18:1-15:For protection immune organ between 1
Hepatic tissue has good cooperative effect.
Claims (4)
1. it is a kind of to be used to protect the medicine of involution form immune organ comprising Volvalerelactones A, it is characterised in that effectively
Composition includes VolvalerelactonesA, and structural formula is as follows：
。
2. it is according to claim 1 it is a kind of comprising Volvalerelactones A be used for protect involution form immune organ
Medicine, it is characterised in that effective ingredient also includes silver forging glycosides.
3. it is according to claim 2 it is a kind of comprising Volvalerelactones A be used for protect involution form immune organ
Medicine, it is characterised in that calculate according to weight, VolvalerelactonesA and silver forging glycosides ratio are 1:1-20:1.
4. it is a kind of according to any one of claim 1-3 to be used to protect involution form immunity comprising Volvalerelactones A
The medicine of organ, it is characterised in that：Described pharmaceutical composition is oral formulations.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610923978.4A CN106562958A (en) | 2016-10-23 | 2016-10-23 | A medicine containing Volvalerelactones A and used for protecting aging type immune organs |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610923978.4A CN106562958A (en) | 2016-10-23 | 2016-10-23 | A medicine containing Volvalerelactones A and used for protecting aging type immune organs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106562958A true CN106562958A (en) | 2017-04-19 |
Family
ID=58534215
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610923978.4A Pending CN106562958A (en) | 2016-10-23 | 2016-10-23 | A medicine containing Volvalerelactones A and used for protecting aging type immune organs |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106562958A (en) |
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2016
- 2016-10-23 CN CN201610923978.4A patent/CN106562958A/en active Pending
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| PB01 | Publication | ||
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Application publication date: 20170419 |