CN102727593A - New use of wild buckwheat rhizome and wild buckwheat rhizome extract in preparation of hypoglycemic medicine and healthcare food - Google Patents
New use of wild buckwheat rhizome and wild buckwheat rhizome extract in preparation of hypoglycemic medicine and healthcare food Download PDFInfo
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- CN102727593A CN102727593A CN2012102437451A CN201210243745A CN102727593A CN 102727593 A CN102727593 A CN 102727593A CN 2012102437451 A CN2012102437451 A CN 2012102437451A CN 201210243745 A CN201210243745 A CN 201210243745A CN 102727593 A CN102727593 A CN 102727593A
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Abstract
The invention discloses a new use of wild buckwheat rhizome and wild buckwheat rhizome extract in preparation of hypoglycemic medicine and healthcare food, wherein a technical scheme provided by the invention is as follows: extracting the wild buckwheat rhizome to respectively obtain an ethanol extract of the wild buckwheat rhizome and an ethyl acetate extract of the wild buckwheat rhizome, then detecting the activity of the ethanol extract of the wild buckwheat rhizome and the ethyl acetate extract of the wild buckwheat rhizome by a high-throughput screening alpha-amylase inhibitor, wherein a statistical processing result displays that the wild buckwheat rhizome and the wild buckwheat rhizome extract have a strong capability of inhibiting amylase and glucosidase and can reduce the blood sugar; and activity detection model analysis in vitro and preliminary clinical curative effect observation of 140 cases of patients with diabetes display that the wild buckwheat rhizome and the wild buckwheat rhizome extract have the capability of reducing the concentration of the blood sugar in vivo; therefore, the wild buckwheat rhizome and the wild buckwheat rhizome extract provided by the invention are applicable to preparing the hypoglycemic medicine and the healthcare food.
Description
Technical field
The present invention relates to the new purposes of a kind of medicinal plants, specifically is Rhizoma Fagopyri Dibotryis (Rhizoma Fagopyri Cymosi) and extract thereof the new purposes in preparation hypoglycemic drug and health food.
Prior art
Diabetes are four big one of the diseases that cause death that threaten human health.(Lancet) multinational joint study demonstration of magazine of online being published on June 25 " lancet " in 2011; Along with population growth and aging development; Whole world blood sugar level and onset diabetes rate raise year by year, and global diabetes number of patients has increased to 3.47 hundred million.The United Nations's diabetes day on November 14th, 2011; Diabetology branch of Chinese Medical Association (CDS), International Diabetes Federation (IDF) unite the result who has issued a Chinese diabetes socioeconomic impact research; Show that Chinese diabetics number has reached 9,240 ten thousand, China is the maximum country of diabetes number in the world.Meanwhile, inland of China year the treating diabetes expense reached 1,734 hundred million yuans, account for 13% of national medical total expenses.Seek the natural plants that can replace hypoglycemic drug from occurring in nature is the heat subject the research always.
Hypoglycemic drug is a lot of in the market, gets up to be divided into five types but summarize, i.e. sulphanylureas, biguanides, alpha-glucosidase inhibitor, non-sulphanylureas insulin promoter, euglycemic agent.
Wherein alpha-glucosidase inhibitor mainly comprises acarbose (acarbose), voglibose (doubly glad), and its blood sugar lowering principle is: the absorption of carbohydrate will be leaned on the alpha-glucosidase of small intestinal mucosa brush border, just can be decomposed into monosaccharide and is absorbed into blood.Alpha-glucosidase inhibitor class medicine promptly plays blood sugar reducing function through the absorption that delays carbohydrate.
Rhizoma Fagopyri Dibotryis is dry rhizome [1] (1 one of the Chinese Pharmacopoeia: 203) of Chinese medicine polygonaceae plant Rhizoma Fagopyri Dibotryis Fagopyrum dibotrys (D. Don) Hara.Rhizoma Fagopyri Dibotryis also claim (" Chinese Plants will ": volume: 25 (1), the page number: 111.Science Press publishes) day Semen Fagopyri Esculenti, Radix Et Rhizoma Fagopyri Tatarici, Radix seu Folium Gaultheriae Forrestii is a kind in the buckwheat (Poygonum), most wild border at height above sea level 250-3200m, bushes, the limit, field, by the road, and dark and damp mountain region.It is the widest a kind of that it is that Chinese Fagopyrum wild species apoplexy due to endogenous wind distributes, and in China, all there is distribution in Shaanxi, East China, Central China, south China and the west and south, and Thailand, India, Nepal is ubiquity also.Tuber is used as medicine, but heat-clearing and toxic substances removing, evacuation of pus blood stasis removing.Be used for the lung abscess vomiting pus, dyspnea and cough due to lung-heat, tonsillitis is swollen and ache.
At present; From Rhizoma Fagopyri Dibotryis, isolated multiple chemical compound; Comprise the former cyanidin of double focusing (dimeric Procyanidin); Hecogenin (hecogenin), contains left-handed epicatechin (epicatechin) at the glycoside of cupreol (β-sitosterol), can right-coumaric acid (p-coumaric acid) after tannin (tannin) and a kind of hydrolysis, ferulic acid ferulic acid) and glucose (glucose); 3-galloylepicatechin (3-galloyl epicatechin); 3,3 of former cyanidin (procyanidin) B-2, B-4 and former cyanidin B-2 '-digallic acid ester (3,3 '-digalloylprocyanidin); Alnusenone, isorhamnetin, Quercetin, Quercetin-3-O-rhamnoside, eriodictyol, catechin, 3,5-dimethoxybenzoic acid-4-O-glucoside, daucosterol etc.(" China's book on Chinese herbal medicine " 26 volumes: 629. Shanghai science tech publishing house).
From the patent documentation and non-patent literature retrieved, Rhizoma Fagopyri Dibotryis and extract thereof are mainly used in preparation treatment dysentery, enteritis, treatment pulmonary abscess, chronic bronchitis, treatment pulmonary carcinoma and are used for medicine such as heat-clearing and toxic substances removing cough-relieving.And the application facet in the preparation hypoglycemic drug, Shang Weijian has disclosed report.
Summary of the invention
The object of the invention is studied aspect the effect of lowering blood sugar Rhizoma Fagopyri Dibotryis and extract thereof exactly; Rhizoma Fagopyri Dibotryis and extract thereof the new purposes in preparation hypoglycemic drug and health food is provided; For the application in the preparation hypoglycemic drug of Chinese medicine Rhizoma Fagopyri Dibotryis and extract thereof provides theoretical and experiment is supported, also open up a new approach as hypoglycemic drug for seeking natural plants from occurring in nature.
Technical scheme of the present invention is earlier Rhizoma Fagopyri Dibotryis to be extracted; Obtain Rhizoma Fagopyri Dibotryis ethanol extraction and Rhizoma Fagopyri Dibotryis ethyl acetate extract respectively, adopt the high flux screening alpha-amylase inhibitor to detect the activity of Rhizoma Fagopyri Dibotryis ethanol extraction and Rhizoma Fagopyri Dibotryis ethyl acetate extract again; The external activity detection model is analyzed and the preliminary clinical observation on the therapeutic effect of 140 routine type people, and the statistical disposition result shows stronger inhibition amylase, glucosidase ability, can reduce the absorption of carbohydrate and plays blood sugar reducing function.
Below be concrete experimental procedure:
1, the preparation of Rhizoma Fagopyri Dibotryis ethanol extraction
Depletion Semen Fagopyri Esculenti dry root is suitably pulverized the back and is extracted 1-3 time with the 50%-90% ethanol room temperature of 5 ~ 12 times of weight, and its extracting solution is evaporated to does not have the alcohol flavor, promptly gets the Rhizoma Fagopyri Dibotryis ethanol extraction.
2, the preparation of Rhizoma Fagopyri Dibotryis ethyl acetate extract
Depletion Semen Fagopyri Esculenti ethanol extraction is scattered in and forms suspension in the water, press the suspension volume respectively 1 times, 1/2 times; 1/3 extraordinarily goes into ethyl acetate extraction 3 times; 3 extracts of combined ethyl acetate after vacuum decompression concentrates the recovery solvent, promptly obtain Rhizoma Fagopyri Dibotryis ethyl acetate extractum; Promptly get the Rhizoma Fagopyri Dibotryis ethyl acetate extract through vacuum drying below 50 ℃ or frozen drying.
3, testing in vitro method: this method is used 96 orifice plates; Change with the absorption value of a plurality of samples of the disposable detection of Bioteck Synergy2 instrument at 660nm; Identify α-amylase and α-glucosidase decomposition rate, thereby definite sample is to the inhibition degree of α-amylase and α-glucosidase action effect to substrate corn starch etc.
The testing sample of negative control group (buffer solution blank), positive controls (being standard inhibitor--acarbose) and 6 variable concentrations of Rhizoma Fagopyri Dibotryis ethanol extraction is established in experiment, each concentration establish 2 parallel; The testing sample of 6 variable concentrations of Rhizoma Fagopyri Dibotryis ethyl acetate extract, each concentration establish 2 parallel; Sample concentration to be measured is seen form
1) adds each testing sample 20 μ L in the micropore of 96 orifice plates respectively; Secondly, adding concentration in each testing sample is α-amylase solution 20 μ L of 0.2mg/mL, place 37 ℃ of the multi-functional ELIASAs of synergy2 to vibrate incubation 15min after; Take out; Adding configuration concentration rapidly is 20mg/mL corn starch solution 60 μ L, puts into ELIASA rapidly, begins rapidly to measure at 660nm after the quick oscillation;
2) add each testing sample 20 μ L in the micropore of 96 orifice plates respectively; Be incorporated as α-glucosidase solution 20 μ L of 0.15U/mL again in each testing sample; After placing 37 ℃ of vibrations of the multi-functional ELIASA of synergy2 incubation 15min, take out, adding the configuration concentration that just from magnetic stirring apparatus, takes out rapidly is 20mg/mL corn starch solution 60 μ L; Put into ELIASA rapidly, begin rapidly to measure at 660nm after the quick oscillation;
Utilize ELIASA to be equipped with software records absorbance OD; The initial absorbance value is designated as f1, measures a point later at set intervals, and absorbance is designated as f1 respectively; F2 ... Integral area under the inhibitor effect under the attenuation curve, the blank TG-AUC of deduction unrestraint agent draws net area (Net AUC) under the curve of inhibitor.
Area AUC can be similar to and regard each trapezoidal area sum as under the decline curve, can be expressed as:
AUC=0.5×(f1+f2)×ΔT+0.5×(f2+f3)×ΔT+...+0.5×(fx+fx+1)×ΔT+...+0.5×(fn-1?+fn)×ΔT=0.5×[2×(f1?+f2?+...+?fn-1?+fn)-f1?-fn]×ΔT
Absorbance when wherein fn represents n measuring point, Δ T are the interval between adjacent two measuring points, and because of Δ T in this measuring method is set at 2min, one has 61 measuring points, so this formula can be reduced to:
AUC=2×(f2+f3+...+f60)+?f1?+?f61
Ask suppression ratio by formula:
Inhibition%=(AUC appearance AUC is blank)/AUC appearance * 100
With the sample concentration is abscissa, is vertical coordinate with the suppression ratio, maps and obtains the concentration that suppression ratio is 50% o'clock sample (IC50), and sample is active result promptly represent with half-inhibition concentration (IC50).
Measure the result referring to table 1
From table, can find out that Rhizoma Fagopyri Dibotryis ethanol extraction and Rhizoma Fagopyri Dibotryis ethyl acetate extract all have stronger alphalise starch enzyme inhibition activity and alpha-glucosidase activity, can reach hypoglycemic effect.
The specific embodiment
Embodiment 1
The preparation of Rhizoma Fagopyri Dibotryis ethanol extraction capsule
Depletion Semen Fagopyri Esculenti dry root 2.0 kg suitably pulverize the back with 20kg 70% ethanol room temperature lixiviate 3 times, lixiviate for the first time 48 hours; For the second time, equal for the third time lixiviate is 24 hours; Merge three times lixiviating solution, the leaching liquid concentrating under reduced pressure is reclaimed ethanol, promptly get the Rhizoma Fagopyri Dibotryis ethanol extraction; The extract drying is obtained extract powder, and it is an amount of that extract powder adds starch etc., is mixed, granulates, dry, granulate, incapsulates, and contains Rhizoma Fagopyri Dibotryis dry product 0.20g by every capsules and process 1000.2 of each consumptions, were taken at every day 3 times in 10 minutes before the meal.
Embodiment 2
The preparation of Rhizoma Fagopyri Dibotryis ethyl acetate extract tablet
Prepare the Rhizoma Fagopyri Dibotryis ethanol extraction by embodiment 1 described method; Extract is scattered in formation suspension 10L in the water; Press the suspension volume respectively 1 times, 1/2 times, 1/3 extraordinarily goes into ethyl acetate extraction 3 times, 3 extracts of combined ethyl acetate; After vacuum decompression concentrates the recovery solvent, promptly obtain Rhizoma Fagopyri Dibotryis ethyl acetate extractum; Promptly get the Rhizoma Fagopyri Dibotryis ethyl acetate extract through vacuum drying below 50 ℃ or frozen drying; Contain Rhizoma Fagopyri Dibotryis ethyl acetate extract 0.1 g by every, add appropriate amount of auxiliary materials such as starch again, be mixed, granulate, drying, be pressed into 1000.2 of each consumptions, were taken at every day 3 times in 10 minutes before the meal.
Embodiment 3
Prepare the Rhizoma Fagopyri Dibotryis ethanol extraction by embodiment 1 described method, contain Rhizoma Fagopyri Dibotryis ethanol extraction 0.1 g by every again, add appropriate amount of auxiliary materials such as starch, be mixed, granulate, drying, compacting in flakes.2 of each consumptions, were taken at every day 3 times in 10 minutes before the meal.
Embodiment 4
Prepare the Rhizoma Fagopyri Dibotryis ethyl acetate extract by embodiment 2 described methods; The extract drying is obtained extract powder, and it is an amount of that extract powder adds starch etc., is mixed, granulates, dry, granulate; Incapsulate, contain Rhizoma Fagopyri Dibotryis dry product 0.20g by every capsules and process capsule.2 of each consumptions, were taken at every day 3 times in 10 minutes before the meal.
Embodiment 5
The preparation of Rhizoma Fagopyri Dibotryis cake
Get the Rhizoma Fagopyri Dibotryis ethanol extraction powdered extract powder of embodiment 1 preparation or the Rhizoma Fagopyri Dibotryis ethyl acetate extract dry powder 25g of embodiment 2 preparations, be added into 500g and fry in Fagopyrum esculentum Moench powder or the cooked maize starch, be made into the Semen Fagopyri Esculenti cake according to the cake drawing method.Advise that each 100 ~ 200g uses for canteen.
In order to verify that further the present invention is in the effect aspect the diabetics blood sugar lowering; The made tablet of Rhizoma Fagopyri Dibotryis ethyl acetate extract that the existing capsule that embodiment 1 Rhizoma Fagopyri Dibotryis ethanol extraction is processed and embodiment 2 are prepared; " auxiliary hyperglycemic function evaluation methodology " human experiment experiment according to State Food and Drug Administration prints and distributes is carried out; It is oral to give 140 routine type patients, and observes its curative effect, and concrete condition is following:
1, case is selected
Be diagnosed as patient's 140 examples of diabetes, wherein male 64 examples, women 76 examples, age reckling 34 years old, the maximum 65 years old by the diagnosis and treatment standard of diabetics;
2, instructions of taking:
Take capsule or the made tablet of Rhizoma Fagopyri Dibotryis ethyl acetate extract that the Rhizoma Fagopyri Dibotryis ethanol extraction is processed, take 2 or 2 at every turn, every day 3 times, took in 10 minutes before the meal.
Effect criterion:
Effectively:
test back fasting glucose is recovered normal (≤5.6 mmol/L), or fasting glucose fall>=10%
2 hours after the meal blood sugar recoveries normal (≤7.8 mmol/L) after
test, or 2 hours after the meal blood glucose fall>=10%
Invalid: as not reach effective standard
140 routine observed results are as shown in the table
Can find out from above-mentioned 140 routine type people blood sugar lowering experiments; The made tablet of capsule that Rhizoma Fagopyri Dibotryis ethanol extraction of the present invention is processed and Rhizoma Fagopyri Dibotryis ethyl acetate extract has hydrolysis and the digestion that hinders carbohydrate in the food really; Reduce the absorption of sugar, reduce the ability of blood sugar concentration in the body.Also can further specify, Rhizoma Fagopyri Dibotryis ethanol extraction of the present invention and Rhizoma Fagopyri Dibotryis ethyl acetate extract can be used for preparing hypoglycemic drug and health food.Simultaneously, because used raw material Rhizoma Fagopyri Dibotryis is pure natural plant, be widely used in clinically, low to human toxicity, side effect is little, and raw material is easy to get, and cost is low; Can expect, in case process hypoglycemic drug and health food listing, with having very big market potential.
Claims (5)
1. Rhizoma Fagopyri Dibotryis has the medicine of hypoglycemic activity or the application in the health food in preparation.
2. the Rhizoma Fagopyri Dibotryis ethanol extraction has the medicine of hypoglycemic activity or the application in the health food in preparation.
3. the Rhizoma Fagopyri Dibotryis ethyl acetate extract has the medicine of hypoglycemic activity or the application in the health food in preparation.
4. the Rhizoma Fagopyri Dibotryis ethanol extraction has the tablet of hypoglycemic activity or the application in the capsule in preparation.
5. the Rhizoma Fagopyri Dibotryis ethyl acetate extract has the tablet of hypoglycemic activity or the application in the capsule in preparation.
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Cited By (3)
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| CN103966206A (en) * | 2013-01-25 | 2014-08-06 | 中国农业科学院植物保护研究所 | Preparation and application of recombinant alpha-amylase inhibitor protein |
| CN105560208A (en) * | 2016-01-21 | 2016-05-11 | 中国中药公司 | Wild buckwheat rhizome preparation and preparation method thereof |
| CN116813459A (en) * | 2023-06-28 | 2023-09-29 | 河南中医药大学 | Extraction method and application of wild buckwheat rhizome terpenoid |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103966206A (en) * | 2013-01-25 | 2014-08-06 | 中国农业科学院植物保护研究所 | Preparation and application of recombinant alpha-amylase inhibitor protein |
| CN105560208A (en) * | 2016-01-21 | 2016-05-11 | 中国中药公司 | Wild buckwheat rhizome preparation and preparation method thereof |
| CN105560208B (en) * | 2016-01-21 | 2018-10-26 | 中国中药公司 | A kind of Cymose buckwheat rhizome preparation and preparation method thereof |
| CN116813459A (en) * | 2023-06-28 | 2023-09-29 | 河南中医药大学 | Extraction method and application of wild buckwheat rhizome terpenoid |
| CN116813459B (en) * | 2023-06-28 | 2024-05-31 | 河南中医药大学 | Extraction method and application of wild buckwheat rhizome terpenoid |
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Application publication date: 20121017 |