CN106727964A - Composition of dibenzopyrans ketone and morphinane alkaloid and application thereof - Google Patents
Composition of dibenzopyrans ketone and morphinane alkaloid and application thereof Download PDFInfo
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- CN106727964A CN106727964A CN201611174510.6A CN201611174510A CN106727964A CN 106727964 A CN106727964 A CN 106727964A CN 201611174510 A CN201611174510 A CN 201611174510A CN 106727964 A CN106727964 A CN 106727964A
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- mangiferin
- rotundin
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- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
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- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
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Abstract
The composition of a kind of dibenzopyrans ketone and morphinane alkaloid, with mangiferin and rotundin as active component, the compatibility relationship of two kinds of compositions by weight is:Mangiferin 10%~90%, rotundin 10%~90%.Animal experiments prove that, the present composition can improve blood sugar and glycosylated hemoglobin, the DEVELOPMENT PROSPECT with medicine.
Description
Technical field
The present invention relates to a kind of composition for taking from plant, more particularly to a kind of dibenzopyrans ketone and morphinane alkaloid
Compatible composition, and the application of its extract and active component in prevention and treatment diabetic composition is produced.
Background technology
Diabetes (Diabetes Mellitus, DM) be it is a kind of because internal insulin is absolute or relative deficiency caused by
A series of clinical syndromes.The disease can also cause some complication in development process, such as:Hypoglycemia
(Hypoglycemia), DKA (Ketoacidosis), non-ketone hyperosmolar coma (Nonketotic
Hyperosmolar Coma), angiocardiopathy, chronic renal failure, PVR, DPN and microangiopathies etc..Sugar
The conventional medicine of urine disease treatment mainly has three major types:Biological medicament class, such as:Insulin (Insulin);Chemical drugs, such as:Sulfonylurea
(Sulfonylurea), biguanides (Biguanide), glitazone (Glitazone) and Chinese patent drug class.It is limited to not have still at present
More ripe insulin non-injection administration technology, it is used still based on injection, and injection process there is also security risks.
Though chemical classes medicine is with stronger hypoglycemic effect, big to toxic and side effects such as liver, kidneys, it is also easy to cause cardiovascular complication
Aggravate.Additionally, also have some medicines, such as:GLUCAGON LIKE PEPTIDE (Glucagon-like peptide 1, GLP-1), fat
Be acylated GLUCAGON LIKE PEPTIDE (NN2211, Novo Nordisk), Exendin-4 () and poly- second two Amylin
Exendin-4 (Chinese invention patent application 00809516.7) of alcohol modification etc., though blood sugar, drop can be effectively controlled after long term administration
Low-saccharification Hb H bA1c numerical value and improvement β islet cell functions, but because the also same purpose of these molecules is in nervous centralis
Acceptor, so the symptom of vomiting and dizziness is more difficult after administration avoid, and administering mode is still based on injection.Another kind of DPPIV enzymes
Inhibitor, though can be oral, it will produce inhibitory action to the big fermentoid in organism, so as to can be distributed body fat
Change, and the actual effect of administration is also relatively poor.
Chinese invention patent application 93100485.3 discloses a kind of health buckwheat foodstuff, auxiliary with tartary buckwheat powder as base-material
With soyabean protein powder, then the Chinese herbal medicine natural component such as matrimony vine, ginseng, the wind-weed, calcium activated is added, its formulation weight percentage composition
For:Duck wheat flour 60-80%, soyabean protein powder 15-30%, LBP-X 0.5-2.5%, timosaponin 0.2-0.5%, people
Gracilis polysaccharide 0.5-1.5%, calcium activated 1.2-4.3%.The food of composition has therapeutic action to diabetes.The health food is with buckwheat
Based on wheat, the diet of diabetic can be played a role, but effect in terms for the treatment of needs further experiment card
It is real.
Chinese invention patent ZL95116521.6 discloses a kind of tonic hypoglycemic capsule and preparation method thereof, using cultivated land,
The taste bulk drug of the Radix Astragali, the fruit of Chinese wolfberry, the red sage root, golden cypress, the wind-weed and Chinese cassia tree etc. 20, through special processing and processing.The Jiangtang capsule
It is made after being crushed by Chinese medicine, because the content of cellulose for containing is more, and sugared absorption can be slowed down, adds monkshood and the medicine of Chinese cassia tree two
Cause that medicine hypoglycemic effect is more notable after material, be the emphasis place of the invention.
Chinese invention patent application 99126988.8 discloses a kind of capsule for lowering sugar of diabetes, with the dried rhizome of rehmannia, root of Chinese trichosanthes,
The medicinal materials such as radix scrophulariae, the wind-weed, golden cypress, the coptis, pilose antler, Bian Gui, Chinese yam, gypsum and dry lotus root starch are key component, are treated by diabetes
Disappear on causing, in disappear, under disappear and the food illness such as diuresis more.
Chinese invention patent application 02107203.5 discloses a kind of Chinese traditional compound medicine for treating diabetes B, with Pueraria lobota
Root, root of Chinese trichosanthes, rhizoma atractylodis, radix scrophulariae, the raw Radix Astragali, Chinese yam, gypsum, Chinese cassia tree, RADIX ACONITILATERALIS PREPARATA, Ramulus euonymi, ground beetle, Ramulus Taxilli, silk cocoon,
The natural traditional Chinese medicines such as stir-baked SQUAMA MANITIS, leech, dragon's blood, chinaroot greenbrier, the wind-weed, gynostemma pentaphylla, the dried rhizome of rehmannia, the tuber of dwarf lilyturf, the radix paeoniae rubrathe, the root bark of Chinese wolf-berry, rhubarb are
Raw material, is made up, for the treatment of type ii diabetes and its complication of operations such as crushing, decoction, drying, sterilizings.
Chinese invention patent application 200310110332.7 disclose it is a kind of treat diabetes medicine ginseng stilbene Chinese yam cream and
Its preparation method, by " monarch " medicine:Chinese yam and ginseng;" minister " medicine:Sea otter, hippocampus, asafoetide, frankincense, myrrh, safflower, Chinese cassia tree, treasure
Pearl, muscone, root of Chinese trichosanthes, golden cypress, the Radix Astragali, mango leaf and Guava Leaf;And " making " medicine:The common compatibility of the medicinal materials such as borneol and
Into.By broken section of mixing of the medicinal materials such as Chinese yam, ginseng, root of Chinese trichosanthes, golden cypress, the Radix Astragali, mango leaf and Guava Leaf, sesame oil is soaked in
In, through heating after three days, filtering adds red lead in oil strain, then stirs evenly, and receives cream;By in ointment addition cold water, it is stirred continuously,
Water is changed in extruding;Cream slow fire of getting it filled melts, and adds nacreous layer powder, borneol powder, muscone, sea otter, hippocampus, asafoetide, frankincense, does not have
The fine powder of the medicinal materials such as medicine, safflower and Chinese cassia tree, stirs evenly, and is split in and plaster is made on non-woven fabrics.Obtained ointment supplementing qi and nourishing yin, life
Tianjin is quenched the thirst, and has functions that to treat type ii diabetes.
Mango leaf dries leaf for Anacardiaceae Zhi Wu Mango Mangifera indica L.'s.Major function is cured mainly to disappear
Stagnant, dispelling wind cough-relieving, tradition is usually used in treatment indigestion, cough and skin and itches.People not yet recognize it to what prevents
Treat the pharmacological action of diabetes.
Stephania sinica is the dried root of menispermaceous plants stephania sinica Stephania sinica Diels.With heat-clearing
Removing toxic substances, blood stasis removing analgesic effect, for the infection of the upper respiratory tract, sphagitis, stomachache, acute gastroenteritis, bacillary dysentery, malaria, wind
Wet pain, trauma pain etc.;Traumatic injury, venomous snake bite, sore swollen toxin etc. are controlled in external application.People also not yet recognize it to prevention
What treats the pharmacological action of diabetes.
The content of the invention
It is it is an object of the present invention to provide a kind of composition, mango leaf and stephania sinica is compatible, with improvement
The pharmacological action of blood sugar and glycosylated hemoglobin.
It is another object of the present invention to provide a kind of composition, the extract of mango leaf and stephania sinica has to be improved
The pharmacological action of blood sugar and glycosylated hemoglobin.
It is yet a further object of the present invention to provide a kind of composition, it has with mangiferin and rotundin as active component
There is the pharmacological action for improving blood sugar and glycosylated hemoglobin.
A further object of the present invention is to provide a kind of composition, and mango leaf and stephania sinica is compatible, and its is carried
Take thing isoreactivity composition and be made medicine, food and health products, for the prevention and treatment of diabetes.
A further object of the present invention is to provide a kind of composition, its so that mango leaf and stephania sinica is compatible, and
Its extract isoreactivity composition, the also prevention and treatment for diabetes combined with other materials.
" mangiferin " alleged by the present invention, also known as asphonin, chemical name is 2- β-D- glucopyranosyl -1,3,6,7-
TetrahydroxyKetone, is a kind of flavone compound.It is slightly soluble in methyl alcohol, ethanol, water, dissolves in hot dilute methanol, hot Diluted Alcohol, no
It is dissolved in non-polar solven.Can be directly synthesized chemically it is prepared, typically from the plant containing mangiferin or Chinese medicine
(such as:The wind-weed) middle extraction.This kind of medicinal material through solvent, such as:Water, ethanol, methyl alcohol, propyl alcohol, butanol or the pure aqueous solution, high temperature are carried
Take, concentrate after separate etc. step obtain purity more than 60% mangiferin (Chinese invention patent application
200710066354.6).This kind of medicinal material successively through alcohol extracting, decolourize, go solvent, dilute alcohol dissolving and go what the steps such as solvent obtained to carry
Mangiferin purity is more than 90% (Chinese invention patent application 200610079234.5) in taking thing.These contain the medicinal material of mangiferin
Such as:But it is not limited only to, mango leaf, myrica rubra leaf, the wind-weed and pyrrosia lingua etc..
" rotundin " alleged by the present invention is CAS No.:The compound of 10097-84-4, white or yellowish crystallization;
Odorless, it is tasteless;Chance light is heated and easily turn yellow.Dissolved in chloroform, it is slightly molten in ethanol or ether, it is insoluble in water;In dilute sulfuric acid
In it is readily soluble.Fusing point is 141 DEG C~144 DEG C.
Composition alleged by the present invention, also including the various excipient substances being adapted with contained compound or composition, with
The formulation beneficial to administration (drug delivery) is formed with, such as:But be not limited only to aqueous solution injection, powder-injection, pill, dissipate
Agent, tablet, patch, suppository, emulsion, creme, gel, granule, capsule, aerosol, spray, powder spray, sustained release agent
With controlled release agent etc..These pharmaceutic adjuvants both can be it is conventional use of in various preparations, such as:But it is not limited only to isotonic agent, buffering
Liquid, flavouring, excipient, filler, adhesive, disintegrant and lubricant etc.;Can also be to be adapted with the material
And select what is used, such as:Emulsifying agent, solubilizer, bacteriostatic agent, anodyne and antioxidant etc., this kind of auxiliary material can effectively improve combination
The stability and dissolubility of compound contained by thing change rate of release and absorption rate of compound etc., so as to improve variousization
Compound metabolism in vivo, and then strengthen the administering effect of composition.Further, it is also possible to realize specific administration purpose
Or mode, such as:Sustained-release administration, controlled release drug administration and pulsatile administration etc., and the auxiliary material for using, such as:But it is not limited only to gelatin, white egg
In vain, shitosan, polyethers and polyester-based polymer material, such as:But be not limited only to, polyethylene glycol, polyurethane, makrolon and its altogether
Polymers etc..Alleged the main of " being conducive to administration " is presented with:But be not limited only to improve therapeutic effect, improve bioavilability,
Reduce toxic and side effect and improve patient's compliance etc..
In aqueous solution injection, auxiliary material generally comprises isotonic agent and buffer solution, and necessary emulsifying agent is (such as:
Tweeen-80, Pluronic and Poloxamer etc.), solubilizer and bacteriostatic agent etc..Additionally, also including containing pharmaceutically acceptable
Other pharmaceutic adjuvants, such as:Antioxidant, pH adjusting agent and anodyne etc..
Auxiliary material for producing oral liquid generally comprises solvent, and necessary flavouring, bacteriostatic agent, emulsifying agent
With colouring agent etc..
Auxiliary material for producing tablet generally comprises filler (such as:It is starch, Icing Sugar, dextrin, lactose, amylum pregelatinisatum, micro-
Crystalline cellulose, calcium sulfate, calcium monohydrogen phosphate and mannitol etc.), adhesive (such as:Ethanol, starch slurry, sodium carboxymethylcellulose, hydroxypropyl
Base cellulose, methylcellulose, ethyl cellulose, hydroxypropyl methyl cellulose, gelatin solution, sucrose solution and polyvinyl pyrrole
Aqueous solution or alcoholic solution of alkanone etc.), disintegrant (such as:Dried starch, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, crosslinking
Polyvinylpyrrolidone and Ac-Di-Sol) and lubricant is (such as:Magnesium stearate, superfine silica gel powder, talcum powder, hydrogenation
Vegetable oil, polyethylene glycol 4,000, polyethylene glycol 6,000 and magnesium laurylsulfate etc.) etc..
For produce emulsion auxiliary material generally water, oil (such as:Aliphatic acid), emulsifying agent, and necessary preservative and rectify
Taste agent etc..
Auxiliary material for preparing granular agent is similar with tablet, but granulation process is different.As needed, by obtained granule
Load capsule after mixing with glidant and obtain final product capsule.
" organism ", " animal " or " patient " alleged by the present invention refers to people, wild animal and domestic animal (Livestock).
Wild animal is the animal without domestication under nature.Domestic animal be to provide for food source and artificial feeding it is dynamic
Thing, such as:But it is not limited only to dog, cat, mouse, rat, hamster, pig, rabbit, milk cow, buffalo, bull, sheep, goat, goose and chicken etc..Give
" patient " or " organism " prioritizing selection mammal for the treatment of is given, especially people.
" prevention " alleged by the present invention refer to not by clinical criteria assert disease before, it is various for preventing disease from occurring
Or means or the measure of development, including medical science, method physically or chemically, with prevent and reduce disease various symptoms generation or
Development.
" prevention diabetes " alleged by the present invention refer to refer to the present composition for not meeting " diabetes " clinic also
Target, continuity over time will slowly develop into the potential patient for being clinically defined as " diabetes ", so as to improve these
Tolerance of the patient to glucose, promotes human body to the ability of glycometabolism, increases sensitiveness of the human body to insulin.It is this kind of potential
Patient often suffers from " metabolic syndrome (Metabolic Syndrome) " (Annnu.Rev.Nutri., 2005,25,391-
406;Annnu.Rev.Med., 2005,56,45-62;Nat.Rev.Drug.Disc., 2006,5,295-309;
Nat.Rev.Endocri., 2006,2,335-348), such as:Obesity, insulin resistance, glucose intolerance, hypertension, artery
Hardening card (antherosclerosis), dyslipidemia (dyslipidemia) (triglyceride levels i.e. in blood are higher,
HDL is simultaneously relatively low) etc..
" treatment " alleged by the present invention refers to prevent and reducing the generation or development of disease, make the development of disease course
Or exacerbation is able to suppress, contain, mitigate, improve, slow down, stop, postponing or invert, when described holding and/or medication
The various indexs of disease, disorderly or pathologic state include mitigating or reducing symptom or complication, or cure or eliminate disease
Disease, disorderly or situation.
" treatment diabetes " alleged by the present invention refer to that the present composition is used for into the trouble that clinical diagnosis is " diabetes "
Person, improves tolerance of these patients to glucose, promotes human body to the ability of glycometabolism, increases sensitivity of the human body to insulin
Property.And then cause being controlled in normal level with fasting blood-glucose after the meal for patient.Because the ability to glucose metabolism is obtained
To improve, so as to slow down the various angiocardiopathies, chronic renal failure, PVR, the god that are produced by long term hyperglycemia
Through lesion and the occurrence and development of microangiopathies.
" food " alleged by the present invention refers to that the various compounds of present invention offer, composition or extract are made can
Edible single compound or composition.The production and manufacture of this kind of single compound or composition should meet relevant food peace
Full standard, but these food security standards must not limit the present invention.
" health products " alleged by the present invention refer to various compounds, composition or the extract system that will include present invention offer
Into edible single compound or composition to impose on patient, the purpose prevented and treated to disease is played.It belongs to
Food alleged by the present invention, but its production, manufacture should also meet various related requirements, standards and norms to sale.
" medicine " alleged by the present invention refers to that can be used for preventing or treating the single compound of certain disease, various chemical combination
Composition, Chinese medicine and its extract that thing is formed, or refer to the composition or preparation with single compound as main active
(formulation), also refer to that by multiple compounds be the composition or preparation of active component." medicine " should be interpreted to refer to root
According to the legal provisions of a state, examined by its administrative organization for setting up and grant the product of production, also referred in order to be passed through
During examination & approval and permission production, it is all kinds of physical forms of active component containing single compound to be formed." formation " should
It is interpreted as being obtained by approach such as chemical synthesis, bioconversion or purchases.
A kind of composition that the present invention is provided, mango leaf and stephania sinica is compatible, the two kinds by weight compatibilities of composition
Relation is:0.3 part~7 parts of mango leaf, 0.1~5 part of stephania sinica.So that composition can play improvement blood sugar and saccharification blood
The pharmacological action of Lactoferrin.
Another composition that the present invention is provided, mango leaf and stephania sinica is compatible, and two kinds by weight compositions are matched somebody with somebody
5 relations are:1~3 part of mango leaf, 0.2~2 part of stephania sinica.So that composition can play improvement blood sugar and HbAle
The pharmacological action of albumen.
Another composition that the present invention is provided, mango leaf and stephania sinica is compatible, and two kinds by weight compositions are matched somebody with somebody
5 relations are:1~3 part of mango leaf, 0.5~1 part of stephania sinica.So that composition can play improvement blood sugar and HbAle
The pharmacological action of albumen.
It has also been found that, mango leaf and Radix Stephaniae Japonicae extract also have the pharmacology for improving blood sugar and glycosylated hemoglobin to make
With.
Another composition that the present invention is provided, takes 0.3 part~7 parts of mango leaf by weight, 0.1~5 part of stephania sinica,
Plus 50v/v%~90v/v% alcohol refluxs are extracted 2 times, wherein, the 1st time is 8 times of amount 50v/v%~90v/v% ethanol, 1~3
Hour, the 2nd time is 6 times of amount 50v/v%~90v/v% ethanol, 1~2 hour, after filtration, merges 2 filtrates, and second is recovered under reduced pressure
To without alcohol taste, relative density is 1.20~1.34 to alcohol when continuing to be concentrated under reduced pressure into 50 DEG C ± 5 DEG C, obtains extract.
Another composition that the present invention is provided, takes 1~3 part of mango leaf by weight, 0.2~2 part of stephania sinica, plus
50v/v%~80v/v% alcohol refluxs are extracted 2 times, wherein, the 1st time is 8 times of amount 50v/v%~90v/v% ethanol, and 1~3 is small
When, the 2nd time is 6 times of amount 50v/v%~90v/v% ethanol, 1~2 hour, after filtration, merges 2 filtrates, and ethanol is recovered under reduced pressure
To without alcohol taste, relative density is 1.20~1.34 when continuing to be concentrated under reduced pressure into 50 DEG C ± 5 DEG C, obtains extract.
Another composition that the present invention is provided, takes 1~3 part of mango leaf by weight, 0.5~1 part of stephania sinica, plus
50v/v%~90v/v% alcohol refluxs are extracted 2 times, wherein, the 1st time is 8 times of amount 50v/v%~90v/v% ethanol, and 1~3 is small
When, the 2nd time is 6 times of amount 50v/v%~90v/v% ethanol, 1~2 hour, after filtration, merges 2 filtrates, and ethanol is recovered under reduced pressure
To without alcohol taste, relative density is 1.20~1.34 when continuing to be concentrated under reduced pressure into 50 DEG C ± 5 DEG C, obtains extract.
Further study show that, mangiferin and its pharmaceutically acceptable salt are (such as:Mangiferin sodium salt and mangiferin sylvite)
With rotundin and its pharmaceutically acceptable salt (such as:Rotundin hydrochloride and rotundin sulfate) it is active component, also show
Go out to improve the pharmacological action of blood sugar and glycosylated hemoglobin.
Another composition that the present invention is provided, it is with mangiferin and its pharmaceutically acceptable salt and rotundin and its medicine
Acceptable salt is active component on, and the compatibility relationship of two kinds of compositions by weight is:Mangiferin and its pharmaceutically acceptable
Salt 10%~90%, rotundin and its pharmaceutically acceptable salt 10%~90%.
Another composition that the present invention is provided, it is with mangiferin and its pharmaceutically acceptable salt and rotundin and its medicine
Acceptable salt is active component on, and the compatibility relationship of two kinds of compositions by weight is:Mangiferin and its pharmaceutically acceptable
Salt 51%~90%, rotundin and its pharmaceutically acceptable salt 10%~49%.
Another composition that the present invention is provided, it is with mangiferin and its pharmaceutically acceptable salt and rotundin and its medicine
Acceptable salt is active component on, and the compatibility relationship of two kinds of compositions by weight is:Mangiferin and its pharmaceutically acceptable
Salt 61%~90%, rotundin and its pharmaceutically acceptable salt 10%~39%.
The various compositions that the present invention is provided, with the pharmacological action for improving blood sugar, can be as unique or main
Active component and being applied to produces medicines, food and the health products of various prevention and treatment diabetes, or a kind of or many with other
Planting, there is the chemical substance or medicine that improve diabetes to give organism in the lump.These chemical substances are such as:But it is not limited only to mango
Leaf extract, Radix Stephaniae Japonicae extract, mangiferin and rotundin etc..Alleged " giving organism in the lump " refers to that the present invention is various
Compound has individually or with other one or more and improves after the compound of diabetes, extract or medicine mix through single
Method of administration, such as:But it is not limited only to, oral (Oral), nasal cavity (Nasal), (face) cheek (Buccal), transdermal
(Transdermal), lung (Pulmonal), vagina (Vaginal), subcutaneous (Subcutaneous) or vein
(Intravenous) organism is given;Or with other one or more there is the chemical substance or medicine that improve diabetes to distinguish
Organism is given through various methods of administration.
A kind of pharmaceutical composition that the present invention is provided, is active component with the composition that the present invention is provided.
Another food that the present invention is provided, is active component with the composition that the present invention is provided.
Another health products that the present invention is provided, are active component with the composition that the present invention is provided.
The beneficial effect that technical solution of the present invention is realized:
The composition that the present invention is provided, it is mango leaf and stephania sinica is compatible so that having after both compatibilities improves blood
The pharmacological action of sugar and glycosylated hemoglobin, the DEVELOPMENT PROSPECT with medicine.
The composition that the present invention is provided, it is mango leaf and Radix Stephaniae Japonicae extract is compatible so that both have after compatibility
Improve the pharmacological action of blood sugar and glycosylated hemoglobin, the DEVELOPMENT PROSPECT with food, health products and medicine.
The composition that the present invention is provided, with mangiferin and rotundin as active component, also shows to improve blood sugar and saccharification
The pharmacological action of hemoglobin.
Specific embodiment
Technical scheme described in detail below.The embodiment of the present invention be merely illustrative of the technical solution of the present invention and
It is unrestricted, although being described in detail to the present invention with reference to preferred embodiment, it will be understood by those within the art that,
The technical scheme invented can be modified or equivalent, without deviating from the spirit and scope of technical solution of the present invention,
It all should cover in scope of the presently claimed invention.
If the reagent used by the present invention is not known indicating, it is purchased from Sigma-Aldrich (Sigma-
Aldrich)。
The mango leaf of embodiment 1 and stephania sinica are compatible
0.1~5 part of mixing of 0.3 part~7 parts of mango leaf and stephania sinica, test sample is obtained by way of powder processed or decocting
1。
The mango leaf of embodiment 2 and Radix Stephaniae Japonicae extract are produced
0.3 part~7 parts of mango leaf, 0.1~5 part of stephania sinica, plus 90% alcohol reflux are taken by weight extracts 2 times, the 1st
Secondary ethanol is 8 times of amounts, and 3 hours, the 2nd ethanol was 6 times of amounts, and 1 hour, double gauze filtration merged 2 filtrates, is recovered under reduced pressure
To without alcohol taste, relative density is 1.30 to ethanol when continuing to be concentrated under reduced pressure into 55 DEG C, obtains extract, is designated as test sample 2.
Embodiment 3 mangiferin is produced
With reference to《Chinese patent drug》The 1st phase content of page 161 of volume 34 in 2012, produces mangiferin monomeric compound, goes forward side by side
Row Structural Identification, data are as follows:
ESIMS(m/z)421[M-H]-。
1H-NMR (400MHz, Pyridine-d5) δ 14.62 (s, 1H), 8.11 (s, 1H), 7.18 (s, 1H), 6.64 (s,
1H), 5.88 (d, J=10.0Hz, 1H), 5.28-5.23 (m, 1H), 4.60 (d, J=10.4Hz, 1H), 4.53-4.44 (m,
3H), 4.25-4.23 (m, 1H).
13C-NMR (100MHz, Pyridine-d5) δ 182.4,167.3,165.2,159.6,158.1,154.1,147.5,
115.2,111.3,110.9,105.4,104.8,96.3,85.0,82.7,77.6,74.8,74.0,64.9.
The compound commodity can also be obtained, such as:Wuhan Hong Xinkang fine chemistry industries company.
Embodiment 4 rotundin is produced
With reference to《Guangxi Chemical Industry》The 2nd phase content of page 4 of volume 25 in 1996, produces rotundin monomeric compound, goes forward side by side
Row Structural Identification, data are as follows:
HR-MS, m/z:356.1856[M+H]+。
1H-NMR (600MHz, CD3OD), δ:6.91 (d, 1H, J=8.4Hz), 6.87 (d, 1H, J=8.4Hz), 6.84 (s,
1H), 6.69 (s, 1H), 4.17 (d, 1H, J=15.6Hz), 3.81 (s, 9H), 3.78 (s, 3H), 3.48 (d, 1H, J=
11.4Hz), 3.46 (d, 1H, J=15.6Hz), 3.40 (dd, 1H, J=16.2,3.6Hz), 3.17 (dd, 1H, J=11.4,
3.6Hz), 3.07 (td, 1H, J=16.2), 2.66~3.04 (m, 2H), 2.59 (td, 1H, J=11.4,3.6Hz).
13C-NMR (150MHz, CD3OD)δ:151.7,149.2,149.1,146.2,130.6,128.9,128.6,
127.8,125.2,112.9,112.6,110.4,60.8,60.5,56.7,56.4,56.3,54.8,52.7,36.5,29.3.
The compound commodity can also be obtained, such as:Wuhan Xing Zhongcheng Science and Technology Ltd.s.
Embodiment 5 with mangiferin and rotundin be active component compatibility
By weight, by mangiferin that is obtained or buying and rotundin consumption:Mangiferin 10%~90%, rotundin 10%
~90% compatibility, is obtained 2 groups of compositions, is designated as test sample 3 and test sample 4.
Influence of the embodiment 6 to Spontaneous Diabetic GK rat blood sugars
35 GK male rats of glucostasis value > 9.0mmol/L are taken, 5 groups, respectively every group 7, mould are randomly divided into
The pharmaceutical composition group of the present invention of type control group, 1~test sample of test sample 4, separately with 7 with week old Wistar rats as normal right
According to group.Gastric infusion.
Using the steady person of outstanding talent's type blood glucose meter of Johnson & Johnson, tail measuring blood sugar of blood extracting is cut.Determined during the random blood sugar morning 9~10;Fasting blood
Sugar (is determined) during the morning 9 for the hours blood glucose of fasting 6 during fasting afternoon 3.
Tail is cut before off-test and takes blood, glycosylated hemoglobin (HbA1c) is determined using Bio-Rad companies HbA1c analyzers.
Result is referring to table 1, table 2 and table 3.
Influence of the present composition of table 1 to GK rat fasting blood-glucoses
In table 1, * p < 0.05, * * p < 0.01 compares with model control group.
Table 1 is visible, and each test sample of each composition of the invention is respectively provided with reduction GK rat fasting blood-glucoses (p < 0.05, p <
0.01), and effect is significant, the drug effect of monomeric compound combination is combined better than medicinal material.
Influence of the present composition of table 2 to GK rat random blood sugars
In table 2, * p < 0.05, * * p < 0.01 compares with model control group.
Table 2 is visible, and each test sample of each composition of the invention can significantly reduce GK rats random blood sugar (p < 0.05, p
< 0.01), and effect is significant, the drug effect of monomeric compound combination is better than medicinal material combination.
Influence of the present composition of table 3 to GK rats glycosylated hemoglobin (HbA1c)
In table 3, * p < 0.05, * * p < 0.01 compares with model control group.
Table 3 is visible, and compared with model group, glycosylated hemoglobin (HbA1c) declines after each composition of the invention is administered 4 weeks
Significantly (p < 0.05, p < 0.01), the long term hyperglycemia state for pointing out each composition of the invention effectively to reduce GK rats.
Claims (9)
1. a kind of composition, it is characterised in that with mangiferin and its pharmaceutically acceptable salt and rotundin and its can pharmaceutically connect
The salt received is active component, and the compatibility relationship of two kinds of compositions by weight is:Mangiferin and its pharmaceutically acceptable salt 10%~
90%, rotundin and its pharmaceutically acceptable salt 10%~90%.
2. a kind of composition, it is characterised in that with mangiferin and its pharmaceutically acceptable salt and rotundin and its can pharmaceutically connect
The salt received is active component, and the compatibility relationship of two kinds of compositions by weight is:Mangiferin and its pharmaceutically acceptable salt 51%~
90%, rotundin and its pharmaceutically acceptable salt 10%~49%.
3. a kind of composition, it is characterised in that with mangiferin and its pharmaceutically acceptable salt and rotundin and its can pharmaceutically connect
The salt received is active component, and the compatibility relationship of two kinds of compositions by weight is:Mangiferin 61%~90%, rotundin 10%~
39%.
4. composition according to claims 1 to 3 is in the medicine of prevention and treatment diabetes, food or health products are prepared
Application.
5. composition according to claims 1 to 3 is in the medicine for improving glycosylated hemoglobin, food or health products are prepared
Application.
6. a kind of composition for preventing and treating diabetes, with the described composition of one of claims 1 to 3 as activity into
Point.
7. the composition for preventing and treating diabetes according to claim 6, it is characterised in that described composition
It is medicine.
8. the composition for preventing and treating diabetes according to claim 6, it is characterised in that described composition
It is food.
9. the composition for preventing and treating diabetes according to claim 6, it is characterised in that described composition
It is health products.
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CN201611174510.6A CN106727964A (en) | 2016-12-16 | 2016-12-16 | Composition of dibenzopyrans ketone and morphinane alkaloid and application thereof |
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CN103768112A (en) * | 2012-10-26 | 2014-05-07 | 昆明制药集团股份有限公司 | Mango leaf extract and application thereof |
CN103169743A (en) * | 2013-04-24 | 2013-06-26 | 天津中医药大学 | Mango leaf extractive as well as preparation method and application thereof |
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