CN104997787A - Application of glycyrrhetinic acid in preparation of anti-radiation product - Google Patents
Application of glycyrrhetinic acid in preparation of anti-radiation product Download PDFInfo
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- CN104997787A CN104997787A CN201510376808.4A CN201510376808A CN104997787A CN 104997787 A CN104997787 A CN 104997787A CN 201510376808 A CN201510376808 A CN 201510376808A CN 104997787 A CN104997787 A CN 104997787A
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Abstract
The invention relates to the technical fields of medicine, food and beverage, and provides application of glycyrrhetinic acid in preparation of anti-radiation products. Cell experiments and animal experiments confirm that glycyrrhetinic acid can increase the survival rate of cells and animals after gamma-ray radiation, reduce apoptosis induced by gamma-ray, and improve intestinal tissue lesions of the radiated mouse; therefore, it indicates that glycyrrhetinic acid has anti-radiation protective effects.
Description
Technical field
The present invention relates to the technical fields such as medicine, food, beverage, specifically relate to the novelty teabag of enoxolone, namely the new opplication in anti-radiation product prepared by enoxolone.
Background technology
Along with nuclear technology is widely used in military affairs, science and technology, medical treatment and production, the chance that people contact with various ray is increasing, suffers the probability of radiation damage also increasing.Radiation effects, when organism, causes and ionizes and produce free radical, and then a series of biochemical reaction occurs, and changes membrane passage, attacks DNA, RNA and protein macromolecule, causes the normal function of cell loss.Lymphocyte in human body is the most responsive to ionizing radiation, and other are followed successively by the medullary cell, enterocyte, epidermis cell, hepatocyte etc. of gonadal cell, propagation.Therefore, the damage of Radiation On Human body is mainly manifested in immune system, hemopoietic system and reproductive system.Although to the development of antiradiation drug through the unremitting effort of decades, found some active drugs, present spendable antiradiation drug is still less, comprise estrogen as nilestriol and sulfur-containing compound amifostine, but side effect is more.Sulfur-bearing radioprotectant shows good preventive effect, but its toxic and side effects is obvious, only just demonstrates radioprotective activity when reaching toxic dose.
Natural product contains the chemical composition of various structures, wherein many have the effects such as immunomodulating, antioxidation and scavenging free radicals, the damage of Radiation On Human body can be slowed down by Mutiple Targets, and there is the little advantage of toxic and side effects, become the focus of radioprotector research.Active component flavonoid, polysaccharide and saponins etc. in natural product have good protective action to the animal and human's cell being subject to radiation.(list of references: Zhao Lu etc., the progress of active skull cap components radiation resistance, pharmaceutical services and research, 2012; 12 (2): 86-89.)
Radix Glycyrrhizae (Glycyrrhiza) is herbaceos perennial, and belong to pulse family Glycyrrhiza, being used as medicine with root and rhizome, is China's Chinese traditional herbs, and property is put down, and sweet in the mouth, has effect of invigorating the spleen and replenishing QI, heat-clearing and toxic substances removing, expelling phlegm for arresting cough, relieving spasm to stop pain, coordinating the actions of various ingredients in a prescription; There is antioxidation, regulate the multiple pharmacological activities such as immunity of organisms.In Radix Glycyrrhizae, contained main pharmacological activity material is glycyrrhizic acid and salt (i.e. glycyrrhizin) thereof, and the composition such as hydrolysing activity composition enoxolone in vivo and licoflavone.Enoxolone (glycyrrhetinic acid, GA), belongs to pentacyclic triterpenoid, another name β-glycyrrhetinic acid; 3 beta-hydroxy-11-oxygen-12-oleanene-30 acid, relative molecular weight is 470.68, and have the various biological effects such as antiinflammatory, antihistamine, antitumor and blood sugar lowering, its chemical structural formula is as shown in formula I:
After Shen Jian etc. report the irradiation of glycyrol total extract various dose, gastric infusion all has significant protective effect (Shen Jian to the mice of different radiation dose; Deng, the research of Radix Glycyrrhizae extract antiradiation effect, University of the Inner Mongol's journal; 2015,46 (1): 75-80.).Wang Yanan etc. report that body function that monoammonium glycyrrhizinate salt pair microwave radiation causes is unbalance certain protective effect; its mechanism may with scavenging free radicals, improve the relevant (Wang Yanan of antioxidant ability of organism; Deng; the experimentation of monoammonium glycyrrhizinate salt pair microwave radiation rat blood injury protection effect; world's combination of Chinese and Western medicine magazine; 2013,8 (5): 445-447).
There is no bibliographical information enoxolone at present relevant to radiation protection.
Summary of the invention
The object of the present invention is to provide the novelty teabag of enoxolone, specifically the application in anti-radiation product prepared by enoxolone.
The present invention is by the plant extract of a large amount of screening radiation resistance and monomer, find that enoxolone has radiation resistance, and found that the radiation resistance of enoxolone is better than the effect of glycyrol total extract, liquorice beverage total extract, glycyrrhizic acid (glycyrrhizin) and licoflavone.Enoxolone is given cell or the animal that will accept radiation by the present invention's display in advance, cell survival rate can be improved and reduce apoptosis, increase the survival rate of mice and improve the damage of radiation murine small intestine, showing that enoxolone has Antiradiation injury effect.
The invention provides enoxolone and prepare the application in anti-radiation product.
Anti-radiation product of the present invention is prevention or the medicine, health food, health beverage etc. for the treatment of radiation damage.
Medicine of the present invention, for enoxolone is as sole active composition or the pharmaceutical composition comprising enoxolone.
In medicine of the present invention, the content of enoxolone is >50%wt%, and optimum is >=98%wt%.
In medicine of the present invention; enoxolone routinely pharmaceutics can make various dosage form; described dosage form comprise in tablet, capsule, granule, suspensoid, Emulsion, solution, syrup, unguentum, patch or injection etc. one or more, take one or more route of administration in oral, external, injection (comprise in intravenous injection, intravenous drip, intramuscular injection or subcutaneous injection etc. one or more) etc. to carry out the prevention of radiation and directly related disease thereof, protection or treatment.
Radiation of the present invention is radioprotective, ionizing radiation etc.
The present invention confirms through cell experiment, zoopery; enoxolone can improve the survival rate of cell and animal after gamma Rays; reduce the apoptosis that gamma-rays causes, improve the pathological changes of radiation murine small intestine, illustrate that enoxolone has Radiological Defense effect.
The invention provides a kind of new natural product can slow down Radiation On Human body damage by Mutiple Targets, and there is the little advantage of toxic and side effects; Enoxolone will become a kind of novel radioprotector.The present invention is also for prevention or treatment radiation damage provide new means.
Accompanying drawing explanation
Fig. 1. enoxolone pair
60the impact of survival rate after Co radiation C57 mice.
Fig. 2. enoxolone pair
60the pathologic examination of Co radiation C57 mice rear intestinal damage, wherein A is 0Gy, B be 4Gy, C is 4Gy+ enoxolone.
Detailed description of the invention
Now in conjunction with the embodiments and accompanying drawing, the present invention is described in detail, but enforcement of the present invention is not limited only to this.
Agents useful for same of the present invention and raw material all commercially maybe can be prepared by literature method.
Unless otherwise indicated, otherwise percentage ratio and number calculate by weight.
Embodiment 1. enoxolone causes the protective effect of cell injury to radiation
1.1 experiment material
Enoxolone, purchased from Dalian Mei Lun Bioisystech Co., Ltd.
Human umbilical vein endothelial (HUVEC) is purchased from Chinese Academy of Sciences's Shanghai cell bank.
1.2 experimental technique
1.2.1MTT method detects the protective effect of enoxolone to cell injury caused by radiation
Experiment is divided into matched group (not accepting radiation, non-administration), model group (accepting radiation, non-administration), administration group (accepting radiation, administration).
Take the logarithm the HUVEC cell of trophophase with 1.0 × 10
5the density of/ml is inoculated in 96 orifice plates, every hole 100 μ L, treat that cell is all adherent after inoculation 24h, the DMEM culture medium changing serum-free into continues to hatch 8h and balances, after balance, DMEM culture medium in each hole is removed, matched group and model group change normal cell culture fluid into, administration group adds the cell culture fluid that 100 μ L contain the compound (enoxolone, glycyrrhizic acid, licoflavone) of final concentration 10 μMs, after jointly hatching 24h, disposablely give 20Gy
60co-gamma Rays, continue to cultivate 24h, mtt assay detects cell survival rate.
1.2.2 Apoptosis by Flow Cytometry
Take the logarithm the HUVEC cell of trophophase with 1.0 × 10
5the density of/ml is inoculated in 6 orifice plates, and after the growth of every hole 2ml, 24h cell attachment, balance 8h, remove DMEM, administration group adds the cell culture fluid that 2ml contains final concentration 10 μMs of enoxolone, after jointly hatching 24h, disposablely gives 20Gy
60co-gamma Rays, continues to cultivate after 24h, peptic cell collected by centrifugation, operate by Annexin V-PI apoptosis detection kit description, add Annexin V-FITC and PI Staining Solution respectively to mix, with flow cytomery, obtain apoptosis rate.
1.3 statistical procedures
Experimental data is all with mean ± standard deviation
represent, between each group, data compare with SPSS 17.0 software kit, adopt one factor analysis of variance (ANOVA) to carry out significance analysis.
1.4 experimental result
1.4.1MTT method detects the protective effect of enoxolone to cell injury caused by radiation
As shown in table 1, accept 20Gy
60after Co-gamma Rays, the cell survival rate of model group is 79.12 ± 2.52%, enoxolone administration group (10 μ Μ) survival rate is 92.50 ± 4.55%, and difference has statistical significance (P<0.05) compared with model group.And the cell survival rate of glycyrrhizic acid, licoflavone group is respectively 88.24 ± 5.17%, survival rate is 84.36 ± 4.29%.
Table 1MTT method detect enoxolone to the protective effect of cell injury caused by radiation (
n=3)
*p<0.05vs model group
1.4.2 Flow cytometry respectively organizes apoptosis situation
As shown in table 2, accept 20Gy
60after Co-gamma Rays, model group apoptosis rate significance increases (P<0.01); Compared with model group, the apoptosis rate of administration group (10 μMs) is starkly lower than model group (P<0.05).
Table 2 enoxolone on radiation cause apoptotic impact (
n=3)
##p<0.05 model group vs normal group;
*p<0.05 enoxolone group vs model group
The protective effect that embodiment 2. enoxolone causes mice to damage to radiation
2.1 experiment material
Enoxolone, purchased from Dalian Mei Lun Bioisystech Co., Ltd.
C57 mice purchased from Shanghai Slac Experimental Animal Co., Ltd., ticket number SCXK (Shanghai) 2012-0002.
2.2 experimental technique
2.2.1 enoxolone causes the impact of mouse survival rate on radiation
C57 mouse stomach gives the enoxolone (30,60mg/kg/d) two weeks of various dose, then with 8Gy
60co-gamma Rays, after radiation, mice continues gastric infusion, observes the survival rate of mice in 30 days after radiation.
2.2.2 enoxolone causes the impact of mouse small intestine tissue injury on radiation
C57 mouse stomach gave enoxolone (60mg/kg/d) after two weeks, accepted 4Gy
60co-gamma Rays, after radiation, mice continues gastric infusion, and radiation used chloral hydrate anesthesia mice after 7 days, get mouse small intestine tissue, use normal saline flushing blood, be placed on ice, put into glutaraldehyde fixative immediately and fix 4h, osmic acid is adopted to fix 2h after PBS wash buffer, gradient alcohol dehydration, each 10min, uses Epon812 epoxy resin embedding after dehydration, microtome is adopted, by the Change of Ultrastructure of transmission electron microscope observing Ge Zu small intestine after embedding.
2.3 statistical procedures
Experimental data is all with mean ± standard deviation
represent, between each group, data compare with SPSS 17.0 software kit, adopt one factor analysis of variance (ANOVA) to carry out significance analysis.
2.4 experimental result
2.4.1 enoxolone pair
60the impact of Co radiation C57 mouse survival rate
As shown in Figure 1, the life cycle of radiation patterns group mice is not all more than 11 days; Compare with model group, the survival rate of enoxolone low dosage, high dose group is significantly improved.The mice of high dose group is lived forever and live by the 18th day most.Enoxolone significantly improves the survival rate of mice after the radiation of 8Gy fatal dose.
2.4.2 enoxolone pair
60the pathologic examination of Co radiation C57 mice rear intestinal damage
As shown in Figure 2, transmission electron microscope results display: 4Gy
60co-gamma Rays can cause mouse intestinal tissue injury, and small intestine epithelial cells nuclear chromatin is assembled, and has the more cavity differed in size, Cuticle of cell microvillus arrangement disorder, portion fractures (Fig. 2 B) in endochylema; Enoxolone (60mg/kg/d) administration group injury of small intestine degree is lower than model group, and intestinal villi arrangement is sparse, but has no fracture, has a small amount of cavity structure (Fig. 2 C) in endochylema.
Can draw the following conclusions from above experiment:
60when Co-gamma Rays, can cause cell survival rate reduce and there is apoptosis in cell, the survival rate of mice shortens and occurs pathological changes with small intestine, and the survival rate of cell increases and the minimizing of apoptosis significance after giving enoxolone before radiation, animal survival rate obviously extends core small intestine pathological changes and alleviates.Result shows, enoxolone has anti-gamma Rays damaging action.
Above experimental result illustrates, enoxolone has radiation resistance to organism, enoxolone can be made the agent of organism Radiological Defense, and intervene organism with feasible dosage and dosage form, to reach the object of the organism under protection gamma Rays.These all belong to protection scope of the present invention.
Below the preferred embodiment of the invention is illustrated, but the invention is not limited to described embodiment, those of ordinary skill in the art also can make all equivalent modification or replacement under the prerequisite without prejudice to the invention spirit, and these equivalent modification or replacement are all included in the application's claim limited range.
Claims (8)
1. the application in anti-radiation product prepared by enoxolone.
2. enoxolone according to claim 1 is preparing the application in anti-radiation product, it is characterized in that, described anti-radiation product is medicine, the health food of prevention or treatment radiation damage, or health beverage.
3. enoxolone according to claim 2 is preparing the application in anti-radiation product, it is characterized in that, described medicine is that enoxolone is as sole active composition or the pharmaceutical composition comprising enoxolone.
4. enoxolone according to claim 3 is preparing the application in anti-radiation product, it is characterized in that, in described medicine, the content of enoxolone is >50%.
5. enoxolone according to claim 3 is preparing the application in anti-radiation product, it is characterized in that, in described medicine, various pharmaceutical dosage form made by enoxolone routinely pharmaceutics.
6. enoxolone according to claim 5 is preparing the application in anti-radiation product, it is characterized in that, described dosage form is tablet, capsule, granule, suspensoid, Emulsion, solution, syrup, unguentum, patch or injection.
7. according to the arbitrary described enoxolone of claim 1 to 6 preparing the application in anti-radiation product, it is characterized in that, described radiation is radioprotective, ionizing radiation.
8. according to the arbitrary described enoxolone of claim 1 to 6 preparing the application in anti-radiation product, it is characterized in that, described radiation is gamma Rays.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111758963A (en) * | 2020-05-14 | 2020-10-13 | 宁波荷仁健康科技有限公司 | Application of glycyrrhetinic acid in preventing and treating stem cell aging |
| CN112245436A (en) * | 2020-11-25 | 2021-01-22 | 中国农业大学 | Application of 18 beta-glycyrrhetinic acid in preparation of product for enhancing anti-fatigue capability of organism |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103908458A (en) * | 2013-01-04 | 2014-07-09 | 厦门鹭佳生物科技有限公司 | Application of glycyrrhetinic acid and glycyrrhizic acid in preparation of medicines for preventing or treating radioactive soft tissue injury |
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2015
- 2015-07-01 CN CN201510376808.4A patent/CN104997787A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103908458A (en) * | 2013-01-04 | 2014-07-09 | 厦门鹭佳生物科技有限公司 | Application of glycyrrhetinic acid and glycyrrhizic acid in preparation of medicines for preventing or treating radioactive soft tissue injury |
Non-Patent Citations (1)
| Title |
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| 杨梅春: "《甘草次酸抗急性放射性肺损伤的作用研究》", 31 May 2014 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111758963A (en) * | 2020-05-14 | 2020-10-13 | 宁波荷仁健康科技有限公司 | Application of glycyrrhetinic acid in preventing and treating stem cell aging |
| CN112245436A (en) * | 2020-11-25 | 2021-01-22 | 中国农业大学 | Application of 18 beta-glycyrrhetinic acid in preparation of product for enhancing anti-fatigue capability of organism |
| CN112245436B (en) * | 2020-11-25 | 2021-08-31 | 中国农业大学 | Application of 18 beta-glycyrrhetinic acid in preparation of product for enhancing anti-fatigue capability of organism |
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Application publication date: 20151028 |