CN104107182A - Application of astraisoflavan-7-O-beta-D-glucoside in preparation of immunity inhibitors and vasodilators - Google Patents
Application of astraisoflavan-7-O-beta-D-glucoside in preparation of immunity inhibitors and vasodilators Download PDFInfo
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- CN104107182A CN104107182A CN201310132350.9A CN201310132350A CN104107182A CN 104107182 A CN104107182 A CN 104107182A CN 201310132350 A CN201310132350 A CN 201310132350A CN 104107182 A CN104107182 A CN 104107182A
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- radix astragali
- glucoside
- astraisoflavan
- beta
- astragaloside
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Abstract
Through the researches and experiments on astraisoflavan-7-O-beta-D-glucoside, it has been found for the first time that astraisoflavan-7-O-beta-D-glucoside can prominently inhibit T lymphocyte proliferation induced by concanavalin A (Con A) and rat isolated arterial ring contracts induced by potassium chloride (KCl), has immunity inhibiting and vasodilative effects, and is advantageously used to prepare immunity inhibitors and vasodilators.
Description
Technical field
The present invention relates to field of medicaments, be specifically related to the purposes of Radix Astragali Astragaloside-Ⅳ aspect preparation immunosuppressant and vasodilator drug.
Background technology
The Radix Astragali is the Chinese medicine of invigorating the spleen and benefiting QI simply, there is the effect of invigorating QI to consolidate the body surface resistance, diuresis poison holding, evacuation of pus, expelling pus and promoting granulation, clinical weak for the deficiency of vital energy, anorexia and loose stool, sinking of QI of middle-JIAO, chronic diarrhea proctoptosis, the metrorrhagia of having blood in stool, exterior deficiency spontaneous perspiration, deficiency of vital energy edema, carbuncle is difficult bursts, burst and do not hold back for a long time, blood deficiency dull yellowish colored skin, interior-heat is quenched one's thirst, the disease such as chronic nephritis proteinuria and diabetes (referring to: Chinese Pharmacopoeia Commission. Pharmacopoeia of People's Republic of China () [z]. Beijing: Chemical Industry Press, 2005:212-213.).Modern pharmacology research is thought, the Radix Astragali can regulate body's immunity and have antivirus action (referring to Yan Hongbo, Liang Wen, Tu Yating. the immunomodulating of the Radix Astragali and antivirus action [J]. south China national defence medical journal, 2008,22 (6): 69-70); In addition, the Radix Astragali also has many-sided effects such as heart tonifying, arrhythmia, adjusting blood pressure (referring to Huang Mei, Qu Jing, Li Xiaotian, Deng. Radix Astragali chemical composition and to the progress of Cardiovascular System [J]. Aged in China is learned magazine, 2009,6 (29): 1451-1453).
The main chemical compositions of the Radix Astragali comprises: aminoacid and trace element in Radix Astragali flavone compounds, Radix Astragali saponin compounds, astragalus polysaccharides compounds and the Radix Astragali, wherein Radix Astragali flavone compounds is the important effective ingredient of the Radix Astragali.Radix Astragali Astragaloside-Ⅳ is one of important compound of gathering isoflavone apoplexy due to endogenous wind, and it there is no people's report at present in the purposes aspect immunosuppressant and vasodilation.
Summary of the invention
The object of this invention is to provide the purposes of Radix Astragali Astragaloside-Ⅳ aspect preparation immunosuppressant and vasodilator drug.
The chemical constitution of the Radix Astragali Astragaloside-Ⅳ that the present invention studies is as follows, by separation from Radix Astagali, prepares:
Radix Astragali isoflavan-7-O-β-D-Glucose glycosides (being called for short Radix Astragali Astragaloside-Ⅳ):
The present invention, by concanavalin A, Con A (Con A) inducing mouse T lymphocyte proliferation assay, finds that Radix Astragali Astragaloside-Ⅳ is inhibited to T lymphopoiesis first, can be for following preparation immunosuppressant.The present invention shrinks experiment by the rat artery ring of potassium chloride (KCl) induction, finds that first Radix Astragali Astragaloside-Ⅳ has vasorelaxation action, can be for preparing vasodilator drug future.
The specific embodiment
Below in conjunction with embodiment, the invention will be further described:
Embodiment 1: the impact of Radix Astragali Astragaloside-Ⅳ on the proliferation of mouse T lymphocytes of concanavalin A, Con A (ConA) induction
1 material
1.1 animal
BALB/c mouse, body weight 18～20g, male; By laboratory animal portion of Peking University, provide (credit number: SCXK11-00-0008).Animal feeding is in standard environment: temperature (23 ± 1) ℃, relative humidity (55 ± 5) %, light and shade cycle 12h/12h, standard particle forage feed.
1.2 reagent
Concanavalin A, Con A (Con A), tetrazolium bromide (MTT) is purchased from U.S. Sigma company; Hyclone (FBS), purchased from U.S. GIBCO company; Erythrocyte cracked liquid, RPMI-1640, phosphate (PBS) buffer is all purchased from Beijing Mai Chen biotechnology company; DMSO (dimethyl sulfoxide, lot number 20101008), purchased from Beijing Chemical Plant.Radix Astragali Astragaloside-Ⅳ sample is prepared with DMSO.
1.3 instrument
Bro-Rad iMark microplate reader (Bio Rad Laboratories), Sigma3K-15 centrifuge (German Sigma company), CO
2incubator (U.S. Thermal Technology LLC company), superclean bench (Beijing Dong Lianhaer instrument manufacturing company limited) etc.
2 methods
Mice is plucked eyeball blood-letting, and asepticly get spleen homogenate and filter, centrifugal 5min (4 ℃, 1000rmin
-1), abandon supernatant, with washing 2 times with PBS after erythrocyte cracked liquid splitting erythrocyte; With RPMI-1640 (containing 10%FBS) suspension splenocyte, cell counting is also used the survival rate of the blue Determination Staining cell of platform dish, survival rate=not painted cell number/total cellular score * 100%, survival rate > is for test, and cell is adjusted to 2 * 10
6individual/mL.
With mitogen canavaline (ConA, 2.5 μ gmL
-1) stimulate T cell to make its propagation.Grouping: cell matched group (containing isocyatic DMSO), Con A stimulating group, (concentration is decided to be 30 μ molL according to trial test result to Radix Astragali Astragaloside-Ⅳ sample sets
-1), respectively establish 3 multiple holes, repeat 3 times.Cultivation 44h (37 ℃, 5%CO
2, saturated humidity) after add MTT20 μ L (0.5mgmL
-1), cultivate 4h, centrifugal 6min (1500rmin
-1), abandoning after supernatant each Kong Jun and add the DMSO100 μ L 10min that slightly vibrates, microplate reader 570nm surveys absorbance (A value).
Suppression ratio (%)=(Con A group A average-sample sets A average)/Con A group A average * 100%
3 experimental results
Con A can obviously promote mouse T lymphocyte propagation (p < 0.01), find that first Radix Astragali Astragaloside-Ⅳ can obviously suppress the T cell proliferation (p < 0.01) of ConA induction, suppression ratio is: 50.97%, the medicine that can be used for following preparation immunosuppressant aspect, concrete outcome sees the following form:
Table 1: the T lymphopoietic impact of Radix Astragali Astragaloside-Ⅳ on ConA induction
(n＝3，mean±SD)
Compare with DMSO matched group,
##p < 0.01, compares * * P < 0.01 with ConA group.
Experimental example 2: the impact that Calycosin-7-O-BETA-D-glucoside shrinks the rat serum pipe ring of potassium chloride (KCl) induction
1 material
1.1 animal
SD rat, body weight 180～200g, male and female half and half, provide (credit number: SCXK11-00-0008) by laboratory animal portion of Peking University.Animal feeding is in standard environment: temperature (23 ± 1) ℃, relative humidity (55 ± 5) %, light and shade cycle 12h/12h, standard particle forage feed.
1.2 reagent
Ke-Heng Shi (K-H) liquid preparation: NaCl118.0, KCl5.4, NaH
2pO
341.0, MgSO
47H
2o1.2, CaCl
21.9, NaHCO
325.0 and glucose 11.1 (mmolL
-1), adjusting pH is 7.4.Water solublity sample is prepared with PBS, and fat-soluble sample is prepared with DMSO.
1.3 instrument
Constant temperature water bath, tonotransducer, biological acquisition system etc.
2 methods
Stunning rat, speed is got thoracic aorta and is made the wide vascular ring of 3～4mm and hang on bath and (containing K-H liquid 15mL, 37 ℃, continue to pass to 95%O
2+ 5%CO
2mist), in, connect tonotransducer, balance 1h, rest tension 1g, every 15min changes K-H liquid 1 time.After balance, adding final concentration is 60mmolL
-1kCl, after vascular ring shrinks, observe Radix Astragali Astragaloside-Ⅳ (cumulative concentration 2.5 * 10
-4～10 * 10
-4molL
-1) on vasoconstrictive impact, matched group adds isopyknic DMSO (solvent of Radix Astragali Astragaloside-Ⅳ), record respectively vascular ring basis tension force, add the tension force after KCl and add the tension variation after compound, diastolic rate is the ratio that the antiotasis that causes after dosing changes the maximum vasoconstriction amplitude causing with KCl.
3 results
Find that first Radix Astragali Astragaloside-Ⅳ can resist the isolated rat thoracic aortic ring contraction that KCl causes, there is vasodilator effect (p < 0.01, p < 0.05), maximum diastolic rate is 65.22%, can be used for preparing vasodilator drug future, concrete outcome sees the following form:
Table 2: the impact that Radix Astragali Astragaloside-Ⅳ shrinks the rat serum pipe ring of KCl induction
(n＝3，mean±SD)
#compare P < 0.05 with DMSO matched group,
##compare P < 0.01 with DMSO matched group.
Claims (2)
- Radix Astragali isoflavan-7-O-β-D-Glucose glycosides in preparation the purposes in immunosuppressant, its structural formula is as follows:
- 2. the purposes of Radix Astragali isoflavan-7-O-β-D-Glucose glycosides in preparing vasodilator drug, its structural formula is as follows:
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108610387A (en) * | 2018-03-19 | 2018-10-02 | 沈阳化工大学 | One kind having active four isoflavan glycosides compounds of neurocyte protection and preparation method thereof |
| CN110487646A (en) * | 2019-07-26 | 2019-11-22 | 西安医学院 | A kind of method of vitro detection vessel retraction function |
Citations (1)
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|---|---|---|---|---|
| CN101766678A (en) * | 2008-12-26 | 2010-07-07 | 广州康臣药物研究有限公司 | Application of total flavonoid in astragalus to preparing medicaments for preventing and controlling diabetes and nephropathy |
-
2013
- 2013-04-17 CN CN201310132350.9A patent/CN104107182A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101766678A (en) * | 2008-12-26 | 2010-07-07 | 广州康臣药物研究有限公司 | Application of total flavonoid in astragalus to preparing medicaments for preventing and controlling diabetes and nephropathy |
Non-Patent Citations (3)
| Title |
|---|
| 李秀丽等: "四种黄芪黄酮类化合物单体对血管内皮细胞功能的保护作用", 《兰州大学学报》 * |
| 毛平等: "不同药性补气中药对小鼠脾淋巴细胞增殖及细胞因子分泌的影响", 《上海中医药大学学报》 * |
| 焦艳等: "膜荚黄芪茎叶总黄酮对小鼠细胞免疫功能的影响", 《中国中西医结合杂志》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108610387A (en) * | 2018-03-19 | 2018-10-02 | 沈阳化工大学 | One kind having active four isoflavan glycosides compounds of neurocyte protection and preparation method thereof |
| CN108610387B (en) * | 2018-03-19 | 2021-03-12 | 沈阳化工大学 | Four isoflavan glycosides compounds with nerve cell protection activity and preparation method thereof |
| CN110487646A (en) * | 2019-07-26 | 2019-11-22 | 西安医学院 | A kind of method of vitro detection vessel retraction function |
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