CN105126066A - Composition for enhancing diabetes prevention and treatment functions of secoisolariciresinol diglucoside and application of composition - Google Patents

Composition for enhancing diabetes prevention and treatment functions of secoisolariciresinol diglucoside and application of composition Download PDF

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Publication number
CN105126066A
CN105126066A CN201510519238.XA CN201510519238A CN105126066A CN 105126066 A CN105126066 A CN 105126066A CN 201510519238 A CN201510519238 A CN 201510519238A CN 105126066 A CN105126066 A CN 105126066A
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secoisolariciresinol diglucoside
effect
application
combination
composition
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杨琼
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Xi'an Shan Fang Pharmaceutical Technology Co Ltd
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Xi'an Shan Fang Pharmaceutical Technology Co Ltd
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Abstract

The invention relates to a composition for enhancing diabetes prevention and treatment functions of secoisolariciresinol diglucoside and application of the composition. The composition comprises the secoisolariciresinol diglucoside and certain natural products. The natural products can cooperate with the secoisolariciresinol diglucoside to realize the functions, and effects of enhancing the functions can be realized. The composition and the application have the advantages that the composition has excellent functions in the aspects of lowering blood glucose, improving insulin sensitivity and the like and accordingly has an active significance on diabetes prevention and treatment.

Description

A kind of secoisolariciresinol diglucoside that strengthens is for the combination of diabetes control effect and application
Technical field
The present invention relates to medical health field, particularly a kind of secoisolariciresinol diglucoside that strengthens is for the combination of diabetes control effect and application.
Background technology
Diabetes are one of chronic diseases that human morbidity is the highest.In recent years, along with the raising of people's living standard, the absorption of heat constantly increases and physical exertion reduces relatively, and the sickness rate of diabetes also rises year by year.According to correlation report, the ill population in the whole world of diabetes in 2011 has reached 3.66 hundred million, and the year two thousand thirty expectation will reach 5.52 hundred million, prevalence about 7.7%.Diabetes are a kind of complex diseases that low or both defect causes simultaneously hyperglycemia are feature with hypoinsulinism, insulin action, appear in any period of life.Diabetes can cause a lot of complication, and long-term blood glucose increases has serious impact to blood vessel, kidney portion, eye and foot etc.
Secoisolariciresinol diglucoside (FlaxLignans), also known as SDG, is a kind of biological active substances be present in Semen Lini seed coat.There is antitumor nucleus formation, estrogen and estrogen antagonist effect, suppress aromatase activity, suppress the characteristics such as DNA and RNA synthesis, antiviral, fungus.
Some can work in coordination with secoisolariciresinol diglucoside generation effect, the natural product of castering action effect comprises in chimonin, Phaseolin, chlorogenic acid, 1-DNJ and phlorhizin one or more.
Chimonin (Mangiferin), also known as mangiferin, is a kind of carbon glycoside of tetrahydroxy pyrrone, belongs to two benzene pyrrones flavone compound.Chimonin uses mainly as a kind of natural product for the treatment of chronic bronchitis, and research confirms: chimonin has many-sided physiologically active and the pharmacological actions such as antioxidation, antibacterium, antiviral, immunomodulating and antitumor.Chimonin can suppress alpha-glucosidase active, and the conversion of glucose in muscle and adipose cell is increased, and a large amount of glucose enters tissue, reduces blood glucose, and it also can make alpha-glucosaccharase enzyme deactivation simultaneously, and glucosyl group cannot be hydrolyzed into free glucose and enter blood.
Phaseolin (Phaseolin) is the extract deriving from Semen Phaseoli Vulgaris seed, is a kind of alpha-amylase inhibitor, effectively can suppresses amylolysis, have effect of fat-reducing.
Chlorogenic acid (ChlorogenicAcid), also known as chlorogenic acid, the carboxylic phenolic acid be made up of caffeic acid and quinic acid.There is multiple biological activity, as: cardiovascular protective effect, antioxidation, uvioresistant and radiation resistance, antimutagenic and antitumaous effect, antibacterial action, antivirus action, blood lipid-reducing blood sugar-decreasing effect, immunoregulation effect etc.
1-DNJ (1-deoxynojirimycin) is a kind of potent alpha-glucosidase inhibitor, has the effect suppressing sugar transition, reduce sugared content in blood.
Phlorhizin (Phloridzin), also known as phlorhizin, is the glucoside of phloretin, belongs to the dihydrochalcone-type material in flavonoid.Have and reduce blood glucose, Improving memory power, antioxidation, the multiple important biological activity such as anticancer.
Summary of the invention
The invention provides the combination of a kind of new natural product, and its purposes in the diabetes that cause of control a variety of causes.This by secoisolariciresinol diglucoside, and some can work in coordination with the natural product combination of its generation effect, castering action effect, can be used as medicine, functional food, health product, bread and cheese main component for the control of diabetes.
The invention provides secoisolariciresinol diglucoside, its generation effect can be worked in coordination with some, the natural product of castering action effect coordinates for the method for diabetes control, the two coupling has played the effect of Synergistic, there is obvious effect preventing and treating in diabetes, providing a kind of new means and selection for preventing and treating diabetes.
The invention provides secoisolariciresinol diglucoside, and some can work in coordination with the composition of natural products of its generation effect, castering action effect, said composition using secoisolariciresinol diglucoside with can work in coordination with its generation effect, castering action effect natural product as effective ingredient.Particularly, secoisolariciresinol diglucoside and the natural product that its generation effect, castering action effect can be worked in coordination with in compositions of the present invention, calculate with physical presence gauge, its weight ratio is between 1:0.05-0.05:1, preferred between 1:0.5-0.5:1, most preferred is 1:0.8.
Natural products component of the present invention can be commercially available prod, also can extract by plant material the content product or synthetic succedaneum that are prepared from routinely.
Natural product combination of the present invention, can use as the raw material of medicine, functional food, health product, bread and cheese.
Detailed description of the invention
Further illustrate the present invention by the following examples, but not as limitation of the present invention.Simultaneously example sets forth beneficial effect invent described compositions further by experiment, and these experimental examples comprise the present composition and stablize the experiment of the preliminary crowd fact for the experiment in vitro on glycosidase inhibition, post-prandial glycemia, test the impact of blood glucose/Heart quality index/left ventricular mass index caused by diabetes, test the impact of diabetic nephropathy rats.
Embodiment 1:
Get content be 95% secoisolariciresinol diglucoside 10g and 15g Phaseolin content be 50% Semen Phaseoli Vulgaris extract is mixed homogeneously, to obtain final product.
Embodiment 2:
Get content be 95% secoisolariciresinol diglucoside 10g and 8g content be 95% chimonin is mixed homogeneously, to obtain final product.
Embodiment 3:
Get content be 95% secoisolariciresinol diglucoside 10g and 8g content be 95% phlorhizin is mixed homogeneously, to obtain final product.
Embodiment 4:
Get content be 95% secoisolariciresinol diglucoside 10g and 8g content be 95% chlorogenic acid is mixed homogeneously, to obtain final product.
Embodiment 5:
Get content be 95% secoisolariciresinol diglucoside 10g and 8g content be 95% 1-DNJ is mixed homogeneously, to obtain final product.
Embodiment 6:
Get content be 95% secoisolariciresinol diglucoside 10g and 1g content be 95% 1-DNJ, the 2g content chlorogenic acid that is 95%, the 2g content phlorhizin that is 95%, 2g content be 95% chimonin, 1g content be 95% Phaseolin, mix homogeneously, to obtain final product.
Embodiment 7:
Get content be 95% secoisolariciresinol diglucoside 10g and 4g content be 95% chlorogenic acid, 4g content be 95% Phaseolin, mix homogeneously, to obtain final product.
Embodiment 8:
Get content be 95% secoisolariciresinol diglucoside 10g and 8g content be 50% chlorogenic acid, 8g content be 50% Phaseolin, mix homogeneously, to obtain final product.
Embodiment 9:
Get content be 50% secoisolariciresinol diglucoside 20g and 16g content be 50% Phaseolin, mix homogeneously, to obtain final product.
Embodiment 10:
Get content be 20% secoisolariciresinol diglucoside 10g and 8g content be 20% Phaseolin, mix homogeneously, to obtain final product.
Embodiment 1: to the experiment in vitro of glycosidase inhibition
The measuring inhibit activities of secoisolariciresinol diglucoside and embodiment 1-10 pairs of alpha-glucosidases and rat small intestine glycosidase.Whole detection is carried out on 96 orifice plates, if 3 groups, often organizes 4 multiple holes, is respectively: matched group (buffer+substrate+enzyme liquid), blank group (buffer), sample determination group (sample+substrate+enzyme liquid).Operational approach is: in plate hole, add 80 μ L sample solutions in advance (use 0.1molL -1pH7.0 phosphate buffer is diluted to 6 Concentraton gradient (20 ~ 1000gmL respectively -1)), then add 20 × 10 of 40 μ L -3molL -1substrate PNPG, 37 DEG C of insulation 5min, add enzymatic solution 40 μ L, and 37 DEG C of insulation 15min, add the 0.2molL of 160 μ L -1na 2cO 3stop enzyme reaction.Finally in microplate reader, 405nm place measures absorbance, calculates suppression ratio, suppression ratio (%)=[(a-b)-(c-b)/(a-b)] × 100%, and calculate corresponding IC by following method 50.Measurement data represents with x ± s, application t test evaluation result of the test.Experimental result and data statistics are in table 1.
Table 1: secoisolariciresinol diglucoside and embodiment 1-10 are to alpha-glucosidase and rat small intestine glucoside inhibiting activity
Experimental result shows: secoisolariciresinol diglucoside and all have good inhibit activities to alpha-glucosidase and rat small intestine glycosidase by the sample that embodiment 1-10 method is made, and embodiment 1-10 group is all better than secoisolariciresinol diglucoside group.
Experimental example 2: post-prandial glycemia stablizes the experiment of the preliminary crowd fact
Stochastic choice 30 patients with diabetes mellitus.Patient all meets WHO type 2 diabetes mellitus in 1997 diagnostic criteria, 40 to 70 years old ages, the course of disease 1 to 15 year, stable disease.At duration of test, do not change original Drug therapy, get rid of the patients such as cerebral apoplexy, acute myocardial infarction, operation, infection, tumor.All selected objects in the 1st day breakfast feed bean milk 1 bowl (300 milliliters), tea egg 1,2, highland barley bread (50 grams), heat is about 399.8kca; Use by the made sample of embodiment 6 method while within 2nd day, giving same diet.Fasting glucose is before the meal measured early respectively at the 1st day and the 2nd day, and the blood glucose value of feed early 30min, 60min, 90min, 120min, 180min after the meal, the results are shown in Table 2.
The routine diabetics of table 230 the 1st day and the 2nd day feed front and back change of blood sugar situation
Note: " * ", for before Vs feed after feed in group, wherein " * " is P<0.05, and " * * " is P<0.01; " Δ " is that after within the 1st day and the 2nd day, taking food, same time point compares, and wherein " Δ " is P<0.05, and " Δ Δ " is P<0.01.
Experimental result shows: 30 routine patients all obviously raise the 1st day and the 2nd day blood glucose after having eaten, reach summit on the feed, decline to some extent again when 120min during 60min.Blood glucose value wherein during the 1st day 60min is about 1.89 times of fasting blood sugar on the same day, and before and after feed, blood glucose fluctuation scope is about 6.37mmol/L; Blood glucose value during the 2nd day 60min is about 1.65 times of fasting blood sugar on the same day, and before and after feed, blood glucose fluctuation scope is 4.59mmol/L.Show that the made sample of embodiment 6 effectively can control the blood sugar level of diabetics.
Embodiment 3: on the impact experiment of blood glucose, Heart quality index, left ventricular mass index caused by diabetes
70 male rats, body weight 220-280g, after adaptability raises 1 week, random selecting 60 rats disposable tail vein injection streptozotocin (STZ) 45mg/kg causes diabetes model, other 10 is blank group, only injects isopyknic citrate buffer solution.After 3 days, survey rat fasting blood-glucose, blood glucose >=16.7mmol/L is diabetes model.Successful for modeling rat is divided at random model group, secoisolariciresinol diglucoside group, embodiment 1-5 group, often organizes each 10.Blank group gives to distill 8ml/kg every day; Model control group gives distilled water 8ml/kg every day; Secoisolariciresinol diglucoside administration group gives 10mg/kg using secoisolariciresinol diglucoside as trial drug every day; 20mg/kg is given every day as trial drug by the made sample of embodiment 1-5 prescription method.Administration 2 weeks altogether.Tail venous blood sampling, measures rat fasting blood-glucose with blood-sugar detecting instrument; General utility balance claims rat body weight, and electronic balance claims rat heart quality, left ventricular mass, calculates rat heart performance figure and left ventricular mass index, the results are shown in Table 3.
The impact (X ± S) of fraction on rat blood glucose, Heart quality index and left ventricular mass index respectively tested by table 3
Experimental result shows: compared with normal group, and the blood glucose value of model group, Heart quality index, left ventricular mass index obviously rise; Compared with diabetic model group, secoisolariciresinol diglucoside group, embodiment group blood glucose, Heart quality index, left ventricular mass index all have decline, and in dose dependent, and embodiment group is all better than secoisolariciresinol diglucoside group and matched group, conbined usage successful both proving.
Embodiment 4: the impact of diabetic nephropathy rats is tested
After rat adaptability raises 14 days, be divided into blank group (10) and modeling group at random.After water 12h is can't help in the fasting of modeling group, through abdominal cavity shot streptozotocin (STZ) 45mg/kg, survey fasting glucose with tail venous blood sampling after three days and be greater than 16.7mmol/L for modeling success, blank group injects isopyknic normal saline in contrast.60 diabetes rats that blood glucose is still not less than this level after one week are divided into medicine-feeding test group and model group at random and start administration.Test is divided into six groups, and administration group gastric infusion every day once.Blank group gives distilled water 8ml/kg every day; Model control group gives distilled water 8ml/kg every day; Secoisolariciresinol diglucoside administration group gives 10mg/kg using secoisolariciresinol diglucoside as trial drug every day; Cooperativing medicine-feeding group gives 8mg/kg using cooperative drug as trial drug every day; By the made sample of embodiment 7-10 prescription method as trial drug every day to giving 20mg/kg respectively, administration 4 weeks altogether.Before last administration, all rat metabolic cages of 24h collect urine, are stored in-18 DEG C of refrigerators, for measuring urinaryalbumin; 1h after last administration, rats by intraperitoneal injection chloral hydrate 300mg/kg anaesthetize, abdomen venous blood collection, separation of serum, detect serum creatinine, urine creatine, calculate endogenous creatinine clearance rate (Ccr).The results are shown in Table 4.
Table 4 respectively tests composition to the impact (X ± S) of diabetes rat urinaryalbumin, Ccr
Experimental result shows: compared with normal group, and the urinaryalbumin value of model group obviously rises, and Ccr declines to some extent; Compared with model group, secoisolariciresinol diglucoside group, matched group and embodiment group urinaryalbumin significantly decline, and Ccr rises to some extent, and embodiment group is all better than secoisolariciresinol diglucoside group and matched group, conbined usage successful both proving.

Claims (12)

1. can strengthen secoisolariciresinol diglucoside for the combination of diabetes control effect and an application, it is characterized in that: in combination, comprise secoisolariciresinol diglucoside, and some can work in coordination with the natural product of its generation effect, castering action effect.
2. the worked in coordination with secoisolariciresinol diglucoside generation effect as described in right 1, the natural product of castering action effect, is characterized in that: described natural product comprise in chimonin, Phaseolin, chlorogenic acid, 1-DNJ and phlorhizin one or more.
3. one kind can strengthen secoisolariciresinol diglucoside for the combination of diabetes control effect and application, it is characterized in that: in described natural product combination, calculate with physical presence gauge, secoisolariciresinol diglucoside and can work in coordination with its generation effect, castering action effect the consumption ratio of natural product between 1:0.05-0.05:1; Preferred secoisolariciresinol diglucoside and can work in coordination with its generation effect, castering action effect the consumption ratio of natural product between 1:0.5-0.5:1; Most preferred secoisolariciresinol diglucoside with can work in coordination with its generation effect, the consumption ratio of natural product of castering action effect is 1:0.8.
4. the strengthened secoisolariciresinol diglucoside as described in right 1-3, for the combination of diabetes control effect and application, is characterized in that: described secoisolariciresinol diglucoside derives from flax family (Linaceae) plant Caulis et Folium Lini, or synthetic succedaneum.
5. the strengthened secoisolariciresinol diglucoside as described in right 1-3 is for the combination of diabetes control effect and application, it is characterized in that: described chimonin derives from Anacardiaceae plant mango, or the liliaceous plant Rhizoma Anemarrhenae, or Salacia prinoides (Willd.) DC. platymiscium, or synthetic succedaneum.
6. the strengthened secoisolariciresinol diglucoside as described in right 1-3, for the combination of diabetes control effect and application, is characterized in that: described Phaseolin derives from leguminous plant scarlet runner bean, or synthetic succedaneum.
7. the strengthened secoisolariciresinol diglucoside as described in right 1-3 is for the combination of diabetes control effect and application, it is characterized in that: described chlorogenic acid derives from caprifoliaceae plant Flos Lonicerae, Flos Lonicerae, or Maguireothamnus speciosus Coffea arabica, middle fruit coffee, large fruit coffee, or the Eucommiaceae plant Cortex Eucommiae, or synthetic succedaneum.
8. the strengthened secoisolariciresinol diglucoside as described in right 1-3, for the combination of diabetes control effect and application, is characterized in that: described 1-DNJ derives from moraceae plants, Commelianaceae plant, liliaceous plant, or synthetic succedaneum.
9. the strengthened secoisolariciresinol diglucoside as described in right 1-3, for the combination of diabetes control effect and application, is characterized in that: described phlorhizin derives from Fagaceae Lithocarpus plant, Rosaceae Malus, or synthetic succedaneum.
10. the composition of natural products as described in any one of right 1-3, it is characterized in that: described strengthened secoisolariciresinol diglucoside is combined as diabetes control effect the various dosage forms that principle active component develops, and includes but not limited to tablet, capsule, oral liquid, syrup, granule, drop pill, oral cavity disintegration tablet, slow releasing tablet, slow releasing capsule, controlled release tablet, controlled release capsule, liquid drugs injection, freeze-dried powder, aseptic powder injection, transfusion.
The purposes of the composition of natural products described in 11. any one of claim 1-3, it is characterized in that: described strengthened secoisolariciresinol diglucoside is combined as principle active component for diabetes control effect, be prepared into the medicine of various form, functional food, health product or food.
The purposes of the composition of natural products described in 12. any one of claim 1-3, is characterized in that: described medicine is used for prevention and therapy diabetes.
CN201510519238.XA 2015-08-24 2015-08-24 Composition for enhancing diabetes prevention and treatment functions of secoisolariciresinol diglucoside and application of composition Pending CN105126066A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114796247A (en) * 2022-05-24 2022-07-29 广东医科大学 Application of secoisolariciresinol diglucoside in preparing anti-rotavirus medicines

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CN103961395A (en) * 2014-05-21 2014-08-06 吕健军 Composition of plant extract and method for regulating and controlling blood sugar by using same

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114796247A (en) * 2022-05-24 2022-07-29 广东医科大学 Application of secoisolariciresinol diglucoside in preparing anti-rotavirus medicines
CN114796247B (en) * 2022-05-24 2023-08-08 广东医科大学 Application of secoisolariciresinol diglucoside in preparation of rotavirus resistant medicine

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Application publication date: 20151209