CN102188475B - Application of total flavonoids of astragalus in preparing pharmaceutical for preventing and treating acute radiation pneumonitis - Google Patents
Application of total flavonoids of astragalus in preparing pharmaceutical for preventing and treating acute radiation pneumonitis Download PDFInfo
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- CN102188475B CN102188475B CN2011101067683A CN201110106768A CN102188475B CN 102188475 B CN102188475 B CN 102188475B CN 2011101067683 A CN2011101067683 A CN 2011101067683A CN 201110106768 A CN201110106768 A CN 201110106768A CN 102188475 B CN102188475 B CN 102188475B
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Abstract
The invention discloses an application of total flavonoids of astragalus in preparing pharmaceutical for preventing and treating acute radiation pneumonitis. The total flavonoids of astragalus contains various medicinal compositions, has prevention and treatment effects on the acute radiation pneumonitis, and can obviously alleviate lung tissue inflammatory lesion, and relieve incrassation and hyperemia of alveolar wall and alveolus pulmonis clearances, and has obvious effects.
Description
Technical field
The present invention relates to a kind of medical usage of Radix Astragali extract, be specifically related to the application of a kind of Radix Astragali total flavones in preparation prevention and treatment acute radiation pneumonia medicine.
Background technology
The Radix Astragali, another name: Radix Astragali, continuous stilbene, the continuous Radix Astragali, the cotton Radix Astragali, Radix astragali, Radix Astragali, arrow stilbene, the arrow Radix Astragali, astragalus mongholicus Bge; The Rhizoma Paridis tetraphyllae wears stilbene, wears crushed grain, wears mulberry, only mulberry, and another name for Sichuan Province fat, hundred, hundred absorbent cotton, hundred medicines are continuous; Quick-fried the root in soil mountain, the only son and heir takes out greatly, and two people lift, and have much stilbene, cover stilbene, Radix Astragali, red blue stilbene, RADIX ASTRAGALI; The casting skin stilbene, Radix Astragali, astragalus membranaceus, Inner Mongolia Astragalis, towards positive stilbene, Wuchuan stilbene, the fort stilbene, the Huiyuan stilbene is the general designation of plant and Chinese crude drug.The plant Radix Astragali originates in ground such as the Inner Mongol, Shanxi, Gansu, Heilungkiang, is state three level protecting plant.The Chinese crude drug Radix Astragali is the root of leguminous herbaceous plant's Radix Astagali, Radix Astragali, has effects such as invigorating QI to consolidate the body surface resistance, diuretic detumescent, expelling pus and toxin by strengthening QI, granulation promoting.Cure mainly: the deficiency of vital energy is weak, anorexia and loose stool, and sinking of QI of middle-JIAO, the chronic diarrhea proctoptosis, the metrorrhagia of having blood in stool, the exterior deficiency spontaneous perspiration, deficiency of vital energy edema, carbuncle is difficult bursts, and burst for a long time and do not hold back, the blood deficiency dull yellowish colored skin, interior-heat is quenched one's thirst; Chronic nephritis proteinuria, diabetes.
The medicinal history in existing more than 2000 year so far of the Radix Astragali; Modern study; The Radix Astragali contains multiple compositions such as flavonoid, Saponin, sucrose, polysaccharide, several amino acids, folic acid and selenium, zinc, copper, the enhancing human body immunity function is arranged, protects the liver, diuresis, defying age, anti-stress, blood pressure lowering and antibacterial action more widely.Contained flavone compound mainly contains osajin in the Radix Astragali, and flavanone mainly contains kaempferide, Quercetin, isorhamnetin, rhamnocitrin, kumatakenin, sesame handle florigen, calycosin (calycosm); Formononetin (formononetm); 2,4-dihydroxy-5,6-dimethoxy-flavane (2; 4-dihydroxv-5,6-dimethoxvisoflavane) L-3-hydroxyl-9-methoxyl group Lignum pterocarpi indici alkane-(L-3-hydroxv-9-methoxypterocarpan) etc.Existing research shows that Radix Astragali flavone has following function: 1, the pair cell immunologic function has facilitation; 2, has function of resisting myocardial ischemia; 3, vascular endothelial cell had protective effect; 4, hepatic injury had protective action; 5, has antiinflammatory action; 6, have mutation and anti-damaging action; 7, remove the free radical effect; 8, has function of resisting osteoporosis.In recent years; The relevant patent application of adopting the medicine of Radix Astragali total flavones preparation treatment pneumonia is also arranged; For example, patent 03156284.1 discloses a kind of Radix codonopsis and Radix Astragali composition in prevention and the purposes of treating in the acute lung injury, but said composition is to be used for treatment by LPS (lipopolysaccharide; Lipopolysaccharide) the acute lung injury disease that causes does not relate to the acute radiation pneumonia.
Summary of the invention
The present invention be directed to existing situation, the application of a kind of Radix Astragali total flavones in preparation prevention and treatment acute radiation pneumonia medicine is provided.
The invention provides a kind of Radix Astragali ethanol extract---a kind of new purposes of Radix Astragali total flavones.The only openly effect of Radix Astragali total flavones in background technology in the current material, but the inventor finds that under study for action Radix Astragali total flavones also has therapeutic effect for the acute pneumonia that the radioactivity situation causes, and its concrete technical scheme is following:
The application of a kind of Radix Astragali total flavones in preparation treatment acute radiation pneumonia medicine.
Further, the pharmaceutical dosage form that makes is an injection.
Further, the application mode of Radix Astragali total flavones is: Radix Astragali total flavones is adopted physiological saline solution, be mixed with the injection that concentration is 100-150mg/L.
Further, the concentration of Radix Astragali total flavones is 120-140 mg/L in the said injection.
Further, the concentration of Radix Astragali total flavones is 130 mg/L in the injection.
Mainly contain 6 kinds of chemical compounds in the Radix Astragali total flavones of the present invention; Wherein 4 kinds is isoflavonoid, and they are respectively: 13-sitosterol, formononetin, calycosin, cupreol-3-0-β-D-glucoside, formononetin-7-0-β-D pyranglucoside and calycosin-7-0-β-D pyranglucoside.
The method for preparing of the Radix Astragali total flavones that the present invention is used is:
(1) medicine pre-treatment: with the Radix Astragali dry to moisture below 10wt%, pulverize, cross 40 orders then and shine, sealing is preserved;
(2) Radix Astragali total flavones extracts
A, get Radix Astragali powder, using volume fraction is the soak with ethanol 72h of 90 %, and constantly stirs, and soaks after-filtration and gets lixiviating solution and preserve, and filtering residue gets into next step;
B, filtering residue is used volume fraction is 90% washing with alcohol, ultrasonic extraction 30min in 80 ℃ of water-baths then, and ultrasonic after-filtration is collected extracting solution;
C, the filtering residue after ultrasonic is put into percolation vat, the volume ratio of pressing 1:1 adds 90% ethanol, carries out diafiltration after stirring, and collects effluent;
D, with the lixiviating solution of step a, the effluent of the extracting solution of step b and step c mixes, room temperature leaves standstill, and collects upper strata liquid;
E, upper strata liquid is further filtered, is concentrated into dried, Radix Astragali total flavones.
In the method for preparing of above-mentioned Radix Astragali total flavones, the 1g Radix Astragali is with the soak with ethanol of 10-12ml among the step a.
In the method for preparing of above-mentioned Radix Astragali total flavones, among the step b, during washing, filtering residue and alcoholic acid volume ratio are 1:1.
In the method for preparing of above-mentioned Radix Astragali total flavones, during ultrasonic extraction, supersonic frequency is that 25kHz, power are 350W; During diafiltration, flow velocity is 2mL/min.
Contain multiple medicinal ingredient in the Radix Astragali total flavones, the acute radiation pneumonia is had the effect of prevention and treatment, it can obviously alleviate the lung tissue inflammatory lesion that is caused by the radiation factor, alleviates that alveolar wall and alveolar gap thicken, hyperemia, and effect is remarkable.
Description of drawings
Fig. 1 organizes the lung tissue light microscopic figure (200 times) after mice HE-dyes for A;
Fig. 2 organizes the lung tissue light microscopic figure (200 times) after mice HE-dyes for B;
Fig. 3 organizes the lung tissue light microscopic figure (200 times) after mice HE-dyes for C;
Fig. 4 organizes the lung tissue light microscopic figure (200 times) after mice HE-dyes for H.
The specific embodiment
Through specific embodiment the present invention is further set forth below, should be understood that, following explanation only is in order to explain the present invention, its content not to be limited.
Embodiment 1
Extract Radix Astragali total flavones
One, medicine pre-treatment:
The Radix Astragali is put into baking oven, dry by the fire to moisture below 10%, pulverize, cross 40 mesh sieves, sealing is preserved;
Two, the alcohol extraction of Radix Astragali total flavones:
1, accurately take by weighing Radix Astragali powder 1000g after oven dry is pulverized, pour in the round-bottomed flask, by the ratio of 1g: 10-12ml with 90% soak with ethanol 72 hours, stirring frequently therebetween;
2, after the stirring solution is filtered, collects lixiviating solution; Filtering residue uses the alcoholic solution with concentration to wash by 1: 1 volume ratio; Clean the back with numerical control supersonic washer ultrasonic in 80 ℃ of water-baths (supersonic frequency is that 25kHz, power are 350W) extraction 30 minutes, filter, collect extracting solution;
3, will in the Radix Astragali powder of supersound extraction is evenly packed percolation vat into, add 90% ethanol by 1: 1 volume ratio, effluent is collected in the back diafiltration (flow velocity is 2mL/min) that stirs;
4, last, the ethanol extract mixing with collecting leaves standstill under room temperature; Collect upper strata liquid, remove bottom precipitate, use the filter paper filtering alcohol extract; To filtrate obtains concentrated solution with Rotary Evaporators is concentrated, and the latter continues to be concentrated into dried, gets the Radix Astragali total flavones extract.
Through measuring, mainly comprise 6 kinds of chemical compounds in the Radix Astragali total flavones, wherein 4 kinds is isoflavonoid.They are respectively: 13-sitosterol, formononetin, calycosin, cupreol-3-0-β-D-glucoside, formononetin-7-0-β-D pyranglucoside and calycosin-7-0-β-D pyranglucoside, content of total flavone is more than 70%.
Preparation Radix Astragali total flavones injection
Embodiment 2
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 100mg/L.
Embodiment 3
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 110mg/L.
Embodiment 4
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 120mg/L.
Embodiment 5
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 125mg/L.
Embodiment 6
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 130mg/L.
Embodiment 7
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 132mg/L.
Embodiment 8
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 135mg/L.
Embodiment 9
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 140mg/L.
Embodiment 10
Method according to embodiment 1 makes Radix Astragali total flavones, then it is adopted physiological saline solution, is mixed with the injection that Radix Astragali total flavones concentration is 150mg/L.
Zoopery
In order to verify the pharmacy effect of flavone in the Radix Astragali, the inventor is that example has been carried out a series of zoopery with embodiment 2,4,6,9,10, and experimental technique and process are following:
1, experimental drug
The Radix Astragali total flavones that adopts alcohol extracting method to make is used physiological saline solution; Be made into and be configured to the injection that concentration is 100 mg/L (embodiment 2), 120 mg/L (embodiment 4), 130 mg/L (embodiment 6), 140 mg/L (embodiment 9), 150mg/L (embodiment 10), adopt disposable sterilized filter filtration sterilization.
2, experimental technique
2.1,96 healthy BALC/c mices are divided into 8 groups of A, B, C, D, E, F, G, H at random, wherein the A group is simple administration group, the B group is simple irradiation group, C, D, E, F, G group are medication therapy groups, the H group is the normal control group.
2.2, divide into groups after, B, C, D, E, F, G group mice are accepted the irradiation of 10Gy chest, A, two groups of mices of D are simulated irradiation.After the irradiation; The Radix Astragali total flavones injection of A group mouse tail vein injection concentration 150mg/L; The Radix Astragali total flavones injection of C group mouse tail vein injection concentration 100mg/L, the Radix Astragali total flavones injection of D group mouse tail vein injection concentration 120mg/L, the Radix Astragali total flavones injection of E group mouse tail vein injection concentration 130mg/L; The Radix Astragali total flavones injection of F group mouse tail vein injection concentration 140mg/L; The Radix Astragali total flavones injection of G group mouse tail vein injection concentration 150mg/L is 2 times/w, per injection 0.1ml; H group injected in mice normal saline is as contrast.
2.3, anesthesia 1-2 mice of execution down, exoculation ball method is got blood to each group after above-mentioned processing, 4 ℃ of centrifugal acquisition serum during respectively at 1w (week), 2w, 3w, 4w, 5w, 6w, 8w.The formalin fixed lung tissue.
3, experimental result
3.1, lung tissue pathology
HE-dyeing: irradiation back one all mices the lung tissue inflammatory promptly occurs and change.Wherein, See that alveolar wall and alveolar gap thicken, hyperemia under simple irradiation group (B group) and medication therapy groups (C, D, E, F, G group) the mice light microscopic, the locking of part alveolar, the high power lens visual field is macrophage, the neutrophil infiltration of visible more amount down; Interstitial edema; pathological changes is main to ooze out, simple administration group (A group) does not have above-mentioned variation with normal control group (H group), specifically sees Fig. 1-4.
In the above-mentioned lung tissue inflammatory lesion, simple irradiation group is obviously seriously in medication therapy groups, and wherein, a little less than the variation of medication therapy groups E group, D, F group are taken second place.
3.2, the SABC result:
TGF-β: B group 5w after irradiation, the swelling broadening at interval of visible lung, promptly visible a large amount of TGF-β positive cells in the pulmonary parenchyma.A large amount of fibrocytes are arranged in addition, especially in blood vessel side and paratracheal zone.Protein positive is expressed main in the endochylema of alveolar epithelial cells, macrophage, bronchial mucosa epithelial cell, Interstitial cell etc., and it is blue that most nucleus are.Medication therapy groups and B group is compared a little less than the expression, and wherein, E group effect is best, express a little less than, D, F group are taken second place.
TNF-α: B group 3w after irradiation, visible TNF-α expresses around alveolar septum, bronchioles smooth muscle, vascular smooth muscle, blood vessel endothelium, blood vessel, and positive area is big.Protein positive is expressed main in the endochylema of alveolar epithelial cells, interstitial lung macrophage, and it is blue that most nucleus are.Medication therapy groups and B group is compared a little less than the expression, and wherein, E group effect is best, express a little less than, D, F group are taken second place.
3.3, the serum anti oxidation index
Measure and respectively organize SOD in serum content in the mice, the result sees the following form 1:
Can find out that from last table the SOD in serum content of simple administration group A is apparently higher than normal control group H (statistics index
P=0.031, difference has statistical significance), simple irradiation group B (statistics index
P<0. 01, difference has the height statistical significance) and medication therapy groups C, D, E, F, G (statistics index
P<0.01 difference has the height statistical significance), have significant difference, and normal control group SOD in serum content is apparently higher than simple irradiation group B (statistics index
P<0. 01, difference has the height statistical significance) and medication therapy groups C, D, E, F, G (statistics index
P<0.038 difference has statistical significance).Thus can, Radix Astragali total flavones can improve animal body SOD in serum content, and body is played a protective role, and simultaneously, can play preventive effect to radiolesion.
4, experimental summary
Can find out that through above experiment the pulmonary lesion that Radix Astragali total flavones causes for the radioactivity reason has the good curing effect, it can alleviate the lung tissue pathological changes, and rising SOD in serum content obviously improves the state of an illness of radioactivity acute pneumonia, and is respond well.
Above-mentionedly just list the zoopery of having lifted the indivedual embodiment of the present invention, the injection of other drug concentration also can alleviate the lung tissue pathological changes, and rising SOD in serum content obviously improves the state of an illness of radioactivity acute pneumonia.
Claims (9)
1. the application of Radix Astragali total flavones in preparation treatment acute radiation pneumonia medicine is characterized in that the method for preparing of Radix Astragali total flavones is:
(1) medicine pre-treatment: with the Radix Astragali dry to moisture below 10wt%, pulverize, cross 40 orders then and shine, sealing is preserved;
(2) Radix Astragali total flavones extracts
A. get Radix Astragali powder, using volume fraction is the soak with ethanol 72h of 90 %, and constantly stirs, and soaks after-filtration and gets the lixiviating solution preservation, and filtering residue gets into next step;
B. filtering residue being used volume fraction is 90% washing with alcohol, ultrasonic extraction 30min in 80 ℃ of water-baths then, and ultrasonic after-filtration is collected extracting solution;
C. the filtering residue after ultrasonic is put into percolation vat, the volume ratio of pressing 1:1 adds 90% ethanol, carries out diafiltration after stirring, and collects effluent;
D. with the lixiviating solution of step a, the effluent of the extracting solution of step b and step c mixes, room temperature leaves standstill, and collects upper strata liquid;
E. upper strata liquid is further filtered, is concentrated into dried, Radix Astragali total flavones.
2. application according to claim 1 is characterized in that: the pharmaceutical dosage form that makes is an injection.
3. application according to claim 2 is characterized in that: Radix Astragali total flavones is adopted physiological saline solution, be mixed with the injection that concentration is 100-150mg/L.
4. application according to claim 3 is characterized in that: the concentration of Radix Astragali total flavones is 120-140 mg/L in the injection.
5. application according to claim 4 is characterized in that: the concentration of Radix Astragali total flavones is 130 mg/L in the injection.
6. application according to claim 1 is characterized in that main component is in the said Radix Astragali total flavones: 13-sitosterol, formononetin, calycosin, cupreol-3-0-β-D-glucoside, formononetin-7-0-β-D pyranglucoside and calycosin-7-0-β-D pyranglucoside.
7. application according to claim 1 is characterized in that: in the method for preparing of Radix Astragali total flavones, the 1g Radix Astragali is with the soak with ethanol of 10-12ml among the step a.
8. application according to claim 1 is characterized in that: in the method for preparing of Radix Astragali total flavones, among the step b, during washing, filtering residue and alcoholic acid volume ratio are 1:1.
9. application according to claim 1 is characterized in that: during ultrasonic extraction, supersonic frequency is that 25kHz, power are 350W; During diafiltration, flow velocity is 2mL/min.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1560069A (en) * | 2004-03-11 | 2005-01-05 | 南开大学 | Process for extracting total flavone and total oside of astragalus from astragalus |
| CN101040896A (en) * | 2007-04-18 | 2007-09-26 | 中国药科大学 | Flavone of astragalus extract, the medicine use and the compound thereof |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1560069A (en) * | 2004-03-11 | 2005-01-05 | 南开大学 | Process for extracting total flavone and total oside of astragalus from astragalus |
| CN101040896A (en) * | 2007-04-18 | 2007-09-26 | 中国药科大学 | Flavone of astragalus extract, the medicine use and the compound thereof |
Non-Patent Citations (5)
| Title |
|---|
| .参芪扶正注射液辅助治疗放射性肺炎22例.《中国中西医结合杂志》.2005,(第3期),274－275. |
| 刘明伟.黄芪合并抗生素、激素治疗放射性肺炎16例临床分析.《中原医刊》.2005,第32卷(第05期),8. * |
| 周朝娟 |
| 王刚 |
| 王刚;周朝娟;.参芪扶正注射液辅助治疗放射性肺炎22例.《中国中西医结合杂志》.2005,(第3期),274-275. * |
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