CN110038004A - AE treats the application for improving diabetes drug and food and related preparations as preparation - Google Patents
AE treats the application for improving diabetes drug and food and related preparations as preparation Download PDFInfo
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- CN110038004A CN110038004A CN201910030716.9A CN201910030716A CN110038004A CN 110038004 A CN110038004 A CN 110038004A CN 201910030716 A CN201910030716 A CN 201910030716A CN 110038004 A CN110038004 A CN 110038004A
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- hypoglycemic
- asorbyl
- epigallocatechin
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- 239000003814 drug Substances 0.000 title claims abstract description 22
- 238000002360 preparation method Methods 0.000 title claims abstract description 17
- 229940079593 drug Drugs 0.000 title claims abstract description 10
- 206010012601 diabetes mellitus Diseases 0.000 title claims abstract description 9
- 235000013305 food Nutrition 0.000 title abstract description 8
- 102100024295 Maltase-glucoamylase Human genes 0.000 claims abstract description 23
- 108010028144 alpha-Glucosidases Proteins 0.000 claims abstract description 23
- 230000036541 health Effects 0.000 claims abstract description 15
- 239000000654 additive Substances 0.000 claims abstract description 10
- 230000000996 additive effect Effects 0.000 claims abstract description 10
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 8
- 239000003472 antidiabetic agent Substances 0.000 claims abstract description 5
- 230000002218 hypoglycaemic effect Effects 0.000 claims description 14
- 239000000837 restrainer Substances 0.000 claims description 12
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
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- 239000008103 glucose Substances 0.000 abstract description 31
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- XZKIHKMTEMTJQX-UHFFFAOYSA-N 4-Nitrophenyl Phosphate Chemical compound OP(O)(=O)OC1=CC=C([N+]([O-])=O)C=C1 XZKIHKMTEMTJQX-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 208000002249 Diabetes Complications Diseases 0.000 description 2
- 239000006144 Dulbecco’s modified Eagle's medium Substances 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- GXCLVBGFBYZDAG-UHFFFAOYSA-N N-[2-(1H-indol-3-yl)ethyl]-N-methylprop-2-en-1-amine Chemical compound CN(CCC1=CNC2=C1C=CC=C2)CC=C GXCLVBGFBYZDAG-UHFFFAOYSA-N 0.000 description 2
- 230000003178 anti-diabetic effect Effects 0.000 description 2
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- 238000007410 oral glucose tolerance test Methods 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- IFBHRQDFSNCLOZ-ZIQFBCGOSA-N 4-nitrophenyl alpha-D-glucoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC1=CC=C([N+]([O-])=O)C=C1 IFBHRQDFSNCLOZ-ZIQFBCGOSA-N 0.000 description 1
- GZSOSUNBTXMUFQ-NJGQXECBSA-N 5,7,3'-Trihydroxy-4'-methoxyflavone 7-O-rutinoside Natural products O(C[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@H](Oc2cc(O)c3C(=O)C=C(c4cc(O)c(OC)cc4)Oc3c2)O1)[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@H](C)O1 GZSOSUNBTXMUFQ-NJGQXECBSA-N 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
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- 206010022489 Insulin Resistance Diseases 0.000 description 1
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- 108050006759 Pancreatic lipases Proteins 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
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- GAMYVSCDDLXAQW-AOIWZFSPSA-N Thermopsosid Natural products O(C)c1c(O)ccc(C=2Oc3c(c(O)cc(O[C@H]4[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O4)c3)C(=O)C=2)c1 GAMYVSCDDLXAQW-AOIWZFSPSA-N 0.000 description 1
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- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000013361 beverage Nutrition 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 235000020279 black tea Nutrition 0.000 description 1
- PFTAWBLQPZVEMU-UHFFFAOYSA-N catechin Chemical compound OC1CC2=C(O)C=C(O)C=C2OC1C1=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-UHFFFAOYSA-N 0.000 description 1
- ADRVNXBAWSRFAJ-UHFFFAOYSA-N catechin Natural products OC1Cc2cc(O)cc(O)c2OC1c3ccc(O)c(O)c3 ADRVNXBAWSRFAJ-UHFFFAOYSA-N 0.000 description 1
- 235000005487 catechin Nutrition 0.000 description 1
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- 238000001514 detection method Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- GZSOSUNBTXMUFQ-YFAPSIMESA-N diosmin Chemical compound C1=C(O)C(OC)=CC=C1C(OC1=C2)=CC(=O)C1=C(O)C=C2O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@H]2[C@@H]([C@H](O)[C@@H](O)[C@H](C)O2)O)O1 GZSOSUNBTXMUFQ-YFAPSIMESA-N 0.000 description 1
- IGBKNLGEMMEWKD-UHFFFAOYSA-N diosmin Natural products COc1ccc(cc1)C2=C(O)C(=O)c3c(O)cc(OC4OC(COC5OC(C)C(O)C(O)C5O)C(O)C(O)C4O)cc3O2 IGBKNLGEMMEWKD-UHFFFAOYSA-N 0.000 description 1
- 229960004352 diosmin Drugs 0.000 description 1
- 150000002016 disaccharides Chemical class 0.000 description 1
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
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- 230000002255 enzymatic effect Effects 0.000 description 1
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- 238000000855 fermentation Methods 0.000 description 1
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- 239000012894 fetal calf serum Substances 0.000 description 1
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- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 239000006481 glucose medium Substances 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 235000009569 green tea Nutrition 0.000 description 1
- VUYDGVRIQRPHFX-UHFFFAOYSA-N hesperidin Natural products COc1cc(ccc1O)C2CC(=O)c3c(O)cc(OC4OC(COC5OC(O)C(O)C(O)C5O)C(O)C(O)C4O)cc3O2 VUYDGVRIQRPHFX-UHFFFAOYSA-N 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 230000003345 hyperglycaemic effect Effects 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 231100001231 less toxic Toxicity 0.000 description 1
- 239000011344 liquid material Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 150000002772 monosaccharides Chemical class 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 230000000050 nutritive effect Effects 0.000 description 1
- 239000003538 oral antidiabetic agent Substances 0.000 description 1
- 229940127209 oral hypoglycaemic agent Drugs 0.000 description 1
- 230000010355 oscillation Effects 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 150000008442 polyphenolic compounds Chemical class 0.000 description 1
- 235000013824 polyphenols Nutrition 0.000 description 1
- -1 polypropylene Polymers 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
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- 238000011160 research Methods 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Diabetes (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Mycology (AREA)
- Nutrition Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Epidemiology (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Treating the invention discloses AE as preparation improves diabetes in the application of drug and food and related preparations, AE is able to suppress alpha-glucosidase activity, also there is facilitation to the glucose consumption of HepG2 cell, and the hyperglycemia and Maltose tolerant of type-II diabetes mouse can be alleviated.Therefore, 8-C-Asorbyl- (-)-Epigallocatechin may be used as antihypelipidemic foodstuff and products and health products additive agent, can be also used for preparing hypoglycemic drug or health care product.
Description
Technical field
The invention belongs to food and medicine fields, are related to AE (8-C-Asorbyl- (-)-Epigallocatechin) conduct
Alpha-glucosidase restrainer, the application in antihypelipidemic foodstuff, in terms of drug and health care product.
Technical background
Tea is beverage most popular in the world, there is long history in China, has unique flavor and abundant
Nutritive value and health-care efficacy mainly have green tea (azymic), oolong tea (semi-fermented) and black tea (fermentation), mainly live in tea
Property ingredient includes tea polysaccharide and tea polyphenols etc..
AE (8-C-Asorbyl- (-)-Epigallocatechin) (formula 1), earliest by Itsuo Nishioka seminar
It was extracted from oolong tea in 1989 isolated.2013, Yang Zhen seminar was obtained with catechin and ascorbic acid biosynthesis for the first time
It arrives.Studies have shown that 8-C-Asorbyl- (-)-Epigallocatechin has various health cares and pharmacological action to human body,
Such as inhibit pancreatic lipases, AntiHIV1 RT activity, it is antitumor the effects of.
The chemical structure of 1 AE of formula (8-C-Asorbyl- (-)-Epigallocatechin)
Alpha-glucosidase restrainer is a kind of effective oral hypoglycemic agents, can be with the alpha-glucosidase in small intestine
Central active position combine, suppress the performance of enzymatic activity, retardance disaccharide is hydrolyzed to monosaccharide, prolongs after soak time to drop
Low postprandial hyperglycemia plays beneficial effect.Alpha-glucosidase restrainer is in addition to the pre- of diabetes and diabetic complication
Anti- and treatment has outside good effect, moreover it is possible to albumen and lipid be inhibited to glycosylate.China natural resources are abundant, but most of have
Hypoglycemic drug is not developed also, therefore, new less toxic, efficient alpha-glucosidase restrainer is screened from natural products
Increasingly it is valued by people.
It there is no at present and inhibit alpha-glucosidase and anti-sugar about 8-C-Asorbyl- (-)-Epigallocatechin
Urinate the report of disease.Therefore, 8-C-Asorbyl- (-)-Epigallocatechin is used as alpha-glucosidase restrainer, is dropping
The application of confectionery, health care product and pharmaceutical preparations has certain research significance and novelty.
Summary of the invention
The purpose of the present invention is to provide a kind of natural small molecule 8-C-Asorbyl- (-)-Epigallocatechin works
Application for alpha-glucosidase restrainer, in antihypelipidemic foodstuff, in terms of drug and health care product.Above-mentioned purpose of the invention is logical
What the technical solution below crossing was achieved:
A kind of AE treats the application of improvement diabetes drug, its structure of the AE as preparation are as follows:
A kind of AE is as the application for preparing hypoglycemic drug and food additives, its structure of the AE are as follows:
A kind of application of AE as preparation hypoglycemic health-care product additive, pharmaceutically acceptable carrier or excipient,
Pharmaceutically acceptable dosage form is made.
A kind of application of AE as preparation hypoglycemic health-care product additive.
A kind of application of AE as preparation products and health products additive agent.
A kind of AE is as the application for preparing alpha-glucosidase restrainer
A kind of hypoglycemic medicine, containing AE, its structure of the AE are as follows:
Moreover, further including the carrier or excipient that hypoglycemic medicine receives.
Moreover, the excipient that the drug receives include tablet, capsule, granule, injection, pill, syrup,
Powder, paste or liquid preparation.
The advantages and positive effects of the present invention are as follows:
Present invention discover that 8-C-Asorbyl- (-)-Epigallocatechin is alpha-glucosidase restrainer, Ke Yiyong
Make antihypelipidemic foodstuff and products and health products additive agent, can be also used for preparing hypoglycemic medicine or health care product.
Detailed description of the invention
Fig. 1 is that 8-C-Asorbyl- (-)-Epigallocatechin promotes HepG2 grape cell sugar consumption (GC), with
500 μM of melbine (Met) is object of reference, * P < 0.05 and * * P < 0.01, compared with control group.
Fig. 2 is blood glucose level after diabetic mice administration.Mouse fasting plasma glucose concentration (Fig. 2A) and corresponding after being administered 4 weeks
AUC (Fig. 2 B), take orally malt glucose load after mouse blood sugar concentration (Fig. 2 C) and corresponding AUC (Fig. 2 D), oral glucose
The blood sugar concentration (Fig. 2 E) and corresponding AUC (Fig. 2 F) of mouse afterwards.AE is 8-C-Asorbyl- (-)-
Epigallocatechin.Data are expressed as average value ± SD (n=10).* P < 0.05 and * * P < 0.01 are in contrast to model
Group.
Specific embodiment
Essentiality content of the invention is specifically introduced below with reference to embodiment, but protection of the invention is not limited with this
Range.
Embodiment 1
8-C-Asorbyl- (-)-Epigallocatechin is used as alpha-glucosidase restrainer, in antihypelipidemic foodstuff, medicine
Application in terms of product and health care product
One, experimental material
Yeast α-glucosidase, p-nitrophenyl α-D- glucopyranoside (pN α GP), 4- nitrophenylphosphate two
Sodium salt (pNPP), HepG2 cell are obtained from Shanghai Inst. of Life Science, CAS (Chinese Shanghai).
Male mouse of kunming (18-22g) is provided by Chinese People's Liberation Army's Academy of Medical Sciences Experimental Animal Center, through ground
Square animal protection office approval strictly observes local and country the code of ethics.Mouse is maintained in polypropylene cage (every cage 5
) and (18-23 DEG C, 55-60% humidity, 12 hours Dark-light cycles) raising in laboratory conditions, all free diet of mouse
Drinking-water.
Two, experimental method
1. external alpha-glucosaccharase enzyme inhibition activity test method
Blank group, control group and experimental group are set, and reaction system is 200 μ L, and test buffer is pH 6.8,50mM's
Kaliumphosphate buffer.Test compound of the experimental group comprising 10 μ L, the alpha-glucosidase (0.04U/mL) of 20 μ L, 30 μ L,
4- nitrobenzophenone-α-D- the glucopyranoside (pN α GP) of 0.5mM is used as substrate；Do not include enzyme and compound in blank group,
(250 μM) of acarbose are used as positive control.Temperature incubates 5min under the conditions of 37 DEG C of compound of enzyme and test, and substrate is then added, after
Continuous temperature incubates 30min, and absorbance value is read at 405nm using microplate reader, calculates test compound and inhibits to alpha-glucosidase
Rate.
2. cellular level hypoglycemic activity evaluation method
The experiment of 2.1HepG2 grape cell sugar consumption
HepG2 cell is containing 10% fetal calf serum, the DMEM high sugar training of 10U/mL penicillin and 10mg/mL streptomysin
It supports in base, in 37 DEG C, 5%CO2Under the conditions of cultivate.The cell in logarithmic growth phase is taken, is inoculated on 96 orifice plates, is inoculated with close
Degree is 5 × 104Cells/mL, every hole 100, while blank well and control wells are set, in 37 DEG C, 5%CO2It is cultivated in incubator
24h；Culture medium is discarded, 1 × PBS is washed 2 times, changes the DMEM high glucose medium of serum-free into, continues culture for 24 hours；By culture medium
It discards, 1 × PBS is washed 2 times, changes 1640 culture mediums containing 0.2%BSA into, and test compound or DMSO, melbine is added
(500 μM) are used as positive control, and effect is for 24 hours；Each instrument connection glucose content is measured with glucose kit.
After glucose consumption experiment, using MTT colorimetric method for determining cell activity, each hole glucose consumption value is corrected.It will
MTT (20 μ L, 5mg/mL are dissolved in PBS) is added in each hole, after 4h, DMSO (100 μ L) is added to dissolve crystal and is placed in oscillation
10min on device measures OD value with microplate reader under the wavelength of 492nm.By the ratio (GC/MTT=for calculating GC and MTT
mmol·L-1/ OD) glucose consumption due to caused by cell Proliferation can be reduced.
3. anti-diabetic activity is studied in animal body
The foundation of 3.1 type-II diabetes mouse models
After mouse adaptive feeding 1 week, high lipid food is raised 4 weeks, and 6h is deprived of food but not water, small with the dosage of 100mg/kg
STZ is injected intraperitoneally in mouse, continues high lipid food and feeds.Blood glucose value is measured again after 1 week, and mouse successful for non-modeling is again
The dosage for giving intraperitoneal injection STZ 60mg/kg, measures mouse blood sugar value, fasting blood sugar is greater than 11.0mM again after 1 week
Modeling success.It is arranged 5 groups, i.e., normal group, model group, positive controls, drug high and low dose group.
The detection of 3.2 postprandial plasma glucose levels and glucose tolerance (OGTT)
After being deprived of food but not water 3h, isometric physiological saline is given in normal group and model group stomach-filling, and positive controls are given
Acarbose (50mg/kg), administration group give diosmin (50mg/kg) and (100mg/kg), fill up feed, after 2h is administered,
Mouse tail vein takes blood, and blood glucose meter measures postprandial plasma glucose level, and records weight, is administered once daily, successive administration 4 weeks.
The 3rd week survey Mouse oral glucose tolerance (OGTT) is administered, records each group mouse fasting blood sugar and weight, gives
After medicine 1h, the dosage of each group mouse glucose 2g/kg is given, measures blood glucose in 30,60,90,120min tail vein blood respectively
Value calculates change of blood sugar area under the curve (AUC).
4th week measurement Mouse oral Maltose tolerant records each group mouse fasting blood sugar and weight, after 1h is administered, gives
The dosage of each group mouse maltose 2g/kg is given, blood glucose value is measured in 30,60,90,120min tail vein blood respectively, calculates blood
Area (AUC) under sugared change curve.
Three, experimental result
1, inhibiting effect of 8-C-Asorbyl- (-)-Epigallocatechin to alpha-glucosidase
The alpha-glucosaccharase enzyme inhibition activity of 8-C-Asorbyl- (-)-Epigallocatechin is studied.Face
Alpha-glucosidase restrainer acarbose on bed is as reference compound.As shown in table 1,8-C-Asorbyl- (-)-
Epigallocatechin has apparent inhibiting effect, IC to alpha-glucosidase50Value is 142.8 μM, and inhibiting effect is better than
Acarbose (IC50=250.2 μM).
Inhibiting effect of 1. 8-C-Asorbyl- (-)-Epigallocatechind of table to alpha-glucosidase
aThe result is that the average value of independent experiment three times,bReference compound.
2,8-C-Asorbyl- (-)-Epigallocatechin promotes HepG2 grape cell sugar consumption
For the anti-diabetic activity for studying 8-C-Asorbyl- (-)-Epigallocatechin, HepG2 cell is had rated
Glucose consumption activity, and glucose utilization (GC) result is corrected with MTT experiment result.As shown in Figure 1,8-
C-Asorbyl- (-)-Epigallocatechin can promote the consumption of glucose under 0.1-10 μM of dosage, and deposit
In dose-dependant.
3. 8-C-Asorbyl- (-)-Epigallocatechin reduces intracorporal blood glucose level.
To understand the mechanism that 8-C-Asorbyl- (-)-Epigallocatechin inhibits alpha-glucosidase, Wo Menjin
One step internal Maltose tolerant experimental study influence of the flavone compound 2 to blood glucose level.Alpha-glucosidase handle
Maltose hydrolysis is glucose, and therefore, the blood glucose level after oral maltose reflects the activity of alpha-glucosidase indirectly.
As shown in Figure 2 C, after treating 2h with 8-C-Asorbyl- (-)-Epigallocatechin (50 and 100mg/kg), with diabetes
Model group is compared, and level of postprandial blood sugar significantly improves.When dosage is 50mg/kg and 100mg/kg, 2 groups of diabetic mices
Glucose AUC reduces by 11.2% and 13.5% (Fig. 2 D) respectively.8-C-Asorbyl- (-)-Epigallocatechin can be shown
Writing reduces internal fasting blood glucose level and improves malt sugared tolerance, suitable with acarbose activity.
In order to which the glucose for assessing the diabetic mice for using 8-C-Asorbyl- (-)-Epigallocatechin treatment is steady
State and insulin sensitivity, we have also carried out dextrose tolerance test.Oral 8-C-Asorbyl- (-)-
Epigallocatechin causes fasting blood glucose level to significantly reduce (Fig. 2A and Fig. 2 B), while glucose tolerance significantly improves
(Fig. 2 E and Fig. 2 F).
Embodiment 2
The application of 8-C-Asorbyl- (-)-Epigallocatechin
As food additives, suitable 8-C-Asorbyl- (-)-Epigallocatechin system is such as added in biscuit
At hypoglycemic biscuit.
As products and health products additive agent, suitable 8-C-Asorbyl- (-)-Epigallocatechin is such as added in honey
Hyperglycemic health care honey is made.
It is used to prepare hypoglycemic drug, active constituent 8-C-Asorbyl- (-)-Epigallocatechin, further includes medicine
Pharmaceutically acceptable dosage form pharmaceutically acceptable carrier or tax is made in acceptable carrier or excipient on
Shape agent includes one or more solids, semisolid or Auxiliary Liquid Material；Pharmaceutically acceptable dosage form include tablet, capsule,
Granule, injection, pill, syrup, powder, paste, liquid preparation etc..
Above-described embodiment shows that 8-C-Asorbyl- (-)-Epigallocatechin is that alpha-glucosidase restrainer can
For use as antihypelipidemic foodstuff and products and health products additive agent, can be also used for preparing hypoglycemic medicine or health care product.
Claims (9)
1. a kind of AE treats the application for improving diabetes drug, its structure of the AE as preparation are as follows:
2. a kind of AE is as the application for preparing hypoglycemic drug and food additives, its structure of the AE are as follows:
3. a kind of application of AE as preparation hypoglycemic health-care product additive, pharmaceutically acceptable carrier or excipient, make
At pharmaceutically acceptable dosage form.
4. a kind of application of AE as preparation hypoglycemic health-care product additive.
5. a kind of application of AE as preparation products and health products additive agent.
6. a kind of AE is as the application for preparing alpha-glucosidase restrainer.
7. a kind of hypoglycemic medicine, it is characterised in that: containing AE, its structure of the AE are as follows:
8. hypoglycemic medicine according to claim 7, it is characterised in that: further include the carrier or figuration that hypoglycemic medicine receives
Agent.
9. hypoglycemic medicine according to claim 7, it is characterised in that: the excipient that the drug receives includes tablet, glue
Wafer, granule, injection, pill, syrup, powder, paste or liquid preparation.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910030716.9A CN110038004A (en) | 2019-01-14 | 2019-01-14 | AE treats the application for improving diabetes drug and food and related preparations as preparation |
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ID=67274120
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000226329A (en) * | 1998-12-04 | 2000-08-15 | Meiji Milk Prod Co Ltd | Mmp inhibitor |
-
2019
- 2019-01-14 CN CN201910030716.9A patent/CN110038004A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000226329A (en) * | 1998-12-04 | 2000-08-15 | Meiji Milk Prod Co Ltd | Mmp inhibitor |
Non-Patent Citations (2)
| Title |
|---|
| SATABDEE MOHAPATRA等: "In silico investigation of black tea components on α-amylase, α-glucosidase and lipase", 《JOURNAL OF APPLIED PHARMACEUTICAL SCIENCE》 * |
| YINGDONG ZHU等: "Tea Flavanols Block Advanced Glycation of Lens Crystallins Induced by Dehydroascorbic Acid", 《CHEMICAL RESEARCH IN TOXICOLOGY》 * |
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