CN102614205A - New application of stilbene glucoside to preparation of skin ageing-resistant medicaments - Google Patents
New application of stilbene glucoside to preparation of skin ageing-resistant medicaments Download PDFInfo
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- CN102614205A CN102614205A CN2012100623342A CN201210062334A CN102614205A CN 102614205 A CN102614205 A CN 102614205A CN 2012100623342 A CN2012100623342 A CN 2012100623342A CN 201210062334 A CN201210062334 A CN 201210062334A CN 102614205 A CN102614205 A CN 102614205A
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Abstract
The invention provides new application of stilbene glucoside to the preparation of skin ageing-resistant medicaments. The stilbene glucoside has the effect of clearing oxygen radicals, can also repair cells damaged because of the accumulation of the oxygen radicals in an ageing process, and overcomes the detects that a skin ageing-resistant medicament has one effect and cures the symptoms but not the disease. The stilbene glucoside can be applied to the preparation of the skin ageing-resistant medicaments. The stilbene glucoside and pharmaceutically acceptable salts, esters or sugars and excipients thereof and the like are applied to the preparation of the medicaments for preventing or treating skin ageing state. The stilbene glucoside and the pharmaceutically acceptable salts, esters or sugars and excipients thereof and the like can be prepared into pharmaceutically acceptable orally taken and externally used preparations and formulations, such as tablets, capsules, liniments, medicinal extracts, coating agents, emulsions, nanoparticle emulsions and the like. The stilbene glucoside has wide application prospect in aspects of medical healthcare and the like.
Description
Affiliated technical field
The invention belongs to medical technical field, exactly is the new purposes of stilbene glucoside in the resisting age of skin medicine.
Background technology
Stilbene glucoside is claimed the stilbene polyphenol again, belongs to polyhydroxy stilbene compound (polyhydrostilbenes), extensively is present in mosses and the senior plant.Stilbene glucoside is accredited as a kind of phytoalexin, is produced under unfavorable conditions such as fungal infection, ultraviolet radiation, mechanical damage by plant.Natural stilbene glucoside mainly combines the form of a monosaccharide groups to exist with stilbene aglycon side chain.Its chemistry is called 2,3,5,4 '-tetrahydroxy-stilbene-2-O-β-D-glucoside.The aqueous solution of stilbene glucoside is unstable down in hot conditions (80 ℃), and its content and temperature are the negative relation that becomes.Stilbene glucoside is very unstable in acid solution.In 4% sulfuric acid solution, room temperature is placed content behind the 12h and is reduced to originally 31.67%, then detects less than stilbene glucoside at 80 ℃ of held 4h.Its catabolite is the stilbene glucoside aglycon, and further is degraded to phenolic compound.Stilbene glucoside has very strong radioprotective stability.Under drying condition, warp
60The radiation of Co-gamma-rays, its content no significant difference.
Discover that stilbene glucoside has multiple physiologically active and medical value, demonstrate function at aspects such as blood fat reducing, defying age, antioxidation, inhibition tumors, this shows its important research and development especially and is worth in the society of current aging day by day.Chinese patent number: 99119853.0 disclose the patent of invention that name is called " a kind of Tetrahydroxydiphenylglycosides glycosides compounds of preventing and treating cardiovascular and cerebrovascular disease "; The patent No. is 201110196199.6 to disclose by name " a kind of stilbene glucoside injection and preparation technology thereof ", discloses the purposes that stilbene glucoside can be used for treating aspects such as dementia, apoplexy, coronary heart disease, angina pectoris.
Summary of the invention
The purpose of this invention is to provide the new purposes of stilbene glucoside in the resisting age of skin medicine.It not only has the effect of removing oxygen-derived free radicals, also can repair in the ager process and accumulate damaged cells because of free radical, has overcome the shortcoming that resisting age of skin drug effect commonly used is single, cure the symptoms, not the disease.Stilbene glucoside can be used in preparation resisting age of skin medicine.The medicine that stilbene glucoside and pharmaceutically acceptable salt thereof, ester or sugar and excipient etc. are used for preparing prevention or treating the resisting age of skin state is used.The dosage form that stilbene glucoside and pharmaceutically acceptable salt thereof, ester or sugar and excipient etc. can be prepared into is pharmaceutically acceptable for oral administration and external preparation and dosage form thereof such as tablet, capsule, liniment, unguentum, liniment, emulsion, nanoparticle emulsion.
Advantage of the present invention is: not only have the effect of removing oxygen-derived free radicals, also can repair in the ager process and accumulate damaged cells because of free radical, overcome the shortcoming that resisting age of skin drug effect commonly used is single, cure the symptoms, not the disease.Show that this chemical compound is used to prepare the resisting age of skin medicine and has wide application prospect.
The specific embodiment
Below in conjunction with embodiment the present invention is further specified.
Embodiment 1. stilbene glucosides are tested the protective effect of photoaging mouse skin:
Kunming mice, male, body constitution amount 20-30g, ad lib and drinking-water.During the experiment beginning, the mice random packet is respectively each dose groups of blank group, model control group and stilbene glucoside.All mouse back preserved skin 1 * 2cm, twice weekly.Solar simulator 15cm is apart from irradiation 50mJ/cm
2, the next day once, shone for 4 weeks.Each end of radiation is after 30 minutes, and blank and model control group give the distilled water of 1ml/kg, and each dose groups of stilbene glucoside is respectively 40mg/kg, 80mg/kg and 160mg/kg, and all medicines are to be smeared; 1h draws materials after the last administration, skin histology homogenate, and xanthine oxidase detects antioxidase SOD activity in the mouse skin, and it is active that the test kit method is measured GSH-px.
SOD active
in the table 1 photoaging mouse skin
aP＜0.05,
bCompare with the blank group P＜0.01
Photoaging is one of external environmental factor of skin aging; Sun exposure makes and produces a large amount of free radicals in the skin histology for a long time; The accumulation of free radical is the major reason that causes skin aging; And SOD, GSH-px are the important enzymes of body tissue inner equilibrium free radical level, can improve SOD, the active medicine of GSH-px, can alleviate the skin aging process to a certain extent.This experiment shows that stilbene glucoside has tangible anti-light aging effect.There were significant differences (P＜0.01) for the SOD of the stilbene glucoside group of 80mg/kg and 160mg/kg, the activity of GSH-px and model control group.
Embodiment 2. stilbene glucosides cause the mouse skin protective effect test that declines to medicine:
Male Kunming strain mice, body weight 50-60g, mice freely drinks water and takes food.Mice is divided into each dose groups of blank group, model control group and stilbene glucoside at random.Blank group, model control group give the normal saline of 1ml/kg; Each dose groups of stilbene glucoside is respectively 21mg/kg, 42mg/kg and 84mg/kg; All medicines are gastric infusion, once a day, and behind the administration 15min; All the other respectively organize mice cervical region subcutaneous injection D-galactose 150mg/kg/d, blank group injecting normal saline except that the blank group.Continuously injection is 60 days, since the 30th day by the such scheme administration, behind the last administration 24h, disconnected neck method is put to death mice, preserved skin is got skin of back 2 * 2cm, it is active to measure SOD with embodiment 1 method, it is active that the test kit method is measured GSH-px.
Table 2 medicine causes SOD active
in the mouse skin that declines
aP＜0.05,
bCompare with the blank group P＜0.01
Internal body is in the process of aging, and activity, the productive rate of SOD and GSH-px constantly reduce, the free radical level that can not reequilibrate body intracellular metabolite produces, and free radical begins accumulation, and skin begins to wear out.Can improve SOD, the active medicine of GSH-px, to a certain extent can the delay skin aging process.This experiment shows that stilbene glucoside has tangible resisting age of skin effect.The stilbene glucoside group SOD of 42mg/kg and 84mg/kg, GSH-px are active, and there were significant differences with model control group (P＜0.01).
Embodiment 3 stilbene glucosides are to people's keratinocyte injury repairing effect experiment of ultraviolet induction
People's keratinocyte (HaCaT) is with being divided into five groups exponential phase of growth at random, blank group, model group, administration group (0.001mmol/L, 0.01mmmol/L, 0.1mmol/L); The UVA radiation added drug incubation in preceding 12 hours; The PBS flushing is three times before the radiation, UVA radiation, intensity 18mJ/cm
2, continued was with pastille culture medium culturing 12 hours.Trypsinization, 1000r/min abandons supernatant behind the centrifugal 5min, and distilled water is regulated cell concentration to 2.0 * 10
10/ L, test kit detects the activity of SOD, GSH-px.
Table 3 stilbene glucoside is to SOD activity influence
in the damage of uv induction people keratinocyte
aP＜0.05,
bCompare with the blank group P＜0.01
Keratinocyte is to constitute the most important cell of epidermal area, and most ultraviolet all absorbs at this, is the umbrella of skin, about the power of its oxidation resistance the ager process of skin.The importance of SOD, GSH-px is existing enumeration in embodiment 2, improves the activity of SOD and GSH-px, can improve keratinocyte antagonism ultra-vioket radiation and cause the free radical accumulation.This experiment shows that stilbene glucoside has the effect of tangible raising keratinocyte oxidation resistance.
To sum up experimental study confirms that stilbene glucoside has good improvement effect to the experimental animal skin aging, points out it to have the prospect that significantly is used to develop prevention and treatment skin aging.
Claims (3)
1. the new purposes of stilbene glucoside in the resisting age of skin medicine is characterized in that stilbene glucoside can use in preparation resisting age of skin medicine.
2. the new purposes of stilbene glucoside according to claim 1 in the resisting age of skin medicine is characterized in that the medicine that stilbene glucoside and pharmaceutically acceptable salt thereof, ester or sugar are used for preparing prevention or treatment resisting age of skin uses.
3. the new purposes of stilbene glucoside according to claim 1 in the resisting age of skin medicine is characterized in that the dosage form that stilbene glucoside and pharmaceutically acceptable salt thereof, ester or sugar and excipient etc. can be prepared into is pharmaceutically acceptable for oral administration and external preparation and dosage form thereof such as tablet, capsule, liniment, unguentum, liniment, emulsion, nanoparticle emulsion.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116751237A (en) * | 2023-05-17 | 2023-09-15 | 遵义医科大学第五附属(珠海)医院 | Mitochondrial targeting stilbene glucoside derivative and preparation method and application thereof |
Citations (3)
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| CN101289479A (en) * | 2007-04-17 | 2008-10-22 | 上海医药工业研究院 | Process for abstracting fleece-flower root total stilbene glucoside |
| CN101991590A (en) * | 2009-08-17 | 2011-03-30 | 南京正大天晴制药有限公司 | Stilbene glucoside medical composite and preparation method thereof |
| CN102321129A (en) * | 2011-07-14 | 2012-01-18 | 中国人民解放军第四军医大学 | Stilbene glycoside injection and preparation process thereof |
-
2012
- 2012-03-12 CN CN2012100623342A patent/CN102614205A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101289479A (en) * | 2007-04-17 | 2008-10-22 | 上海医药工业研究院 | Process for abstracting fleece-flower root total stilbene glucoside |
| CN101991590A (en) * | 2009-08-17 | 2011-03-30 | 南京正大天晴制药有限公司 | Stilbene glucoside medical composite and preparation method thereof |
| CN102321129A (en) * | 2011-07-14 | 2012-01-18 | 中国人民解放军第四军医大学 | Stilbene glycoside injection and preparation process thereof |
Non-Patent Citations (2)
| Title |
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| 吕丽爽: "何首乌中二苯乙烯苷的研究进展", 《食品科学》 * |
| 王春英，等: "何首乌中有效成分二苯乙烯苷的研究进展", 《河北医科大学学报》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116751237A (en) * | 2023-05-17 | 2023-09-15 | 遵义医科大学第五附属(珠海)医院 | Mitochondrial targeting stilbene glucoside derivative and preparation method and application thereof |
| CN116751237B (en) * | 2023-05-17 | 2023-12-05 | 遵义医科大学第五附属(珠海)医院 | Mitochondrial targeting stilbene glucoside derivative and preparation method and application thereof |
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Application publication date: 20120801 |