CN110327316A - Astaxanthin is in the purposes for preparing glucosidase inhibitor - Google Patents
Astaxanthin is in the purposes for preparing glucosidase inhibitor Download PDFInfo
- Publication number
- CN110327316A CN110327316A CN201910570277.0A CN201910570277A CN110327316A CN 110327316 A CN110327316 A CN 110327316A CN 201910570277 A CN201910570277 A CN 201910570277A CN 110327316 A CN110327316 A CN 110327316A
- Authority
- CN
- China
- Prior art keywords
- astaxanthin
- glucosidase
- purposes
- alpha
- crude extract
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 235000013793 astaxanthin Nutrition 0.000 title claims abstract description 100
- JEBFVOLFMLUKLF-IFPLVEIFSA-N Astaxanthin Natural products CC(=C/C=C/C(=C/C=C/C1=C(C)C(=O)C(O)CC1(C)C)/C)C=CC=C(/C)C=CC=C(/C)C=CC2=C(C)C(=O)C(O)CC2(C)C JEBFVOLFMLUKLF-IFPLVEIFSA-N 0.000 title claims abstract description 99
- 239000001168 astaxanthin Substances 0.000 title claims abstract description 99
- MQZIGYBFDRPAKN-ZWAPEEGVSA-N astaxanthin Chemical compound C([C@H](O)C(=O)C=1C)C(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC=C(C)C=CC1=C(C)C(=O)[C@@H](O)CC1(C)C MQZIGYBFDRPAKN-ZWAPEEGVSA-N 0.000 title claims abstract description 99
- 229940022405 astaxanthin Drugs 0.000 title claims abstract description 99
- 239000003112 inhibitor Substances 0.000 title claims abstract description 8
- 102000004366 Glucosidases Human genes 0.000 title claims abstract description 7
- 108010056771 Glucosidases Proteins 0.000 title claims abstract description 7
- 108010028144 alpha-Glucosidases Proteins 0.000 claims abstract description 32
- 102100024295 Maltase-glucoamylase Human genes 0.000 claims abstract description 30
- 239000003814 drug Substances 0.000 claims abstract description 18
- 229940079593 drug Drugs 0.000 claims abstract description 17
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract description 16
- 239000013543 active substance Substances 0.000 claims abstract description 5
- 239000000470 constituent Substances 0.000 claims abstract description 5
- 230000036541 health Effects 0.000 claims abstract description 5
- 239000000837 restrainer Substances 0.000 claims abstract description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 34
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 34
- 239000000243 solution Substances 0.000 claims description 34
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 27
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 26
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 24
- 239000000287 crude extract Substances 0.000 claims description 22
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 18
- 239000003208 petroleum Substances 0.000 claims description 17
- 241000081271 Phaffia rhodozyma Species 0.000 claims description 14
- 238000000605 extraction Methods 0.000 claims description 12
- 239000007788 liquid Substances 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- 239000000843 powder Substances 0.000 claims description 11
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical class [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 10
- 235000013305 food Nutrition 0.000 claims description 10
- 239000000284 extract Substances 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 8
- 235000021466 carotenoid Nutrition 0.000 claims description 7
- 150000001747 carotenoids Chemical class 0.000 claims description 7
- 238000002425 crystallisation Methods 0.000 claims description 7
- 230000008025 crystallization Effects 0.000 claims description 7
- 239000013078 crystal Substances 0.000 claims description 5
- 238000004090 dissolution Methods 0.000 claims description 5
- 230000002265 prevention Effects 0.000 claims description 5
- 239000002775 capsule Substances 0.000 claims description 3
- 238000005238 degreasing Methods 0.000 claims description 3
- -1 g/ml extract 2 times Chemical compound 0.000 claims description 3
- 238000002347 injection Methods 0.000 claims description 3
- 239000007924 injection Substances 0.000 claims description 3
- 239000003826 tablet Substances 0.000 claims description 3
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 239000008187 granular material Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 13
- 238000002360 preparation method Methods 0.000 abstract description 12
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract description 8
- 239000008103 glucose Substances 0.000 abstract description 8
- 239000008280 blood Substances 0.000 abstract description 7
- 210000004369 blood Anatomy 0.000 abstract description 7
- 150000002772 monosaccharides Chemical class 0.000 abstract description 7
- 150000001720 carbohydrates Chemical class 0.000 abstract description 6
- 230000023852 carbohydrate metabolic process Effects 0.000 abstract description 5
- 230000005764 inhibitory process Effects 0.000 abstract description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract description 4
- 235000021256 carbohydrate metabolism Nutrition 0.000 abstract description 3
- 238000009098 adjuvant therapy Methods 0.000 abstract description 2
- 201000001421 hyperglycemia Diseases 0.000 abstract description 2
- 230000031891 intestinal absorption Effects 0.000 abstract description 2
- 230000007062 hydrolysis Effects 0.000 abstract 1
- 238000006460 hydrolysis reaction Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 description 15
- 229960001760 dimethyl sulfoxide Drugs 0.000 description 13
- 102000004190 Enzymes Human genes 0.000 description 11
- 108090000790 Enzymes Proteins 0.000 description 11
- 239000000047 product Substances 0.000 description 9
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 description 4
- 229960002632 acarbose Drugs 0.000 description 4
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 description 4
- 230000031700 light absorption Effects 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 239000013641 positive control Substances 0.000 description 4
- 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 3
- 239000007853 buffer solution Substances 0.000 description 3
- 150000002632 lipids Chemical class 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 229960002668 sodium chloride Drugs 0.000 description 3
- 235000002639 sodium chloride Nutrition 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 2
- 241000238557 Decapoda Species 0.000 description 2
- 230000006838 adverse reaction Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000012153 distilled water Substances 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 239000012535 impurity Substances 0.000 description 2
- 230000000670 limiting effect Effects 0.000 description 2
- 239000012452 mother liquor Substances 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 210000000813 small intestine Anatomy 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 206010000060 Abdominal distension Diseases 0.000 description 1
- 241000143060 Americamysis bahia Species 0.000 description 1
- HDLNSTQYXPTXMC-UHFFFAOYSA-N Astaxanthin-diacetat Natural products O=C1C(OC(=O)C)CC(C)(C)C(C=CC(C)=CC=CC(C)=CC=CC=C(C)C=CC=C(C)C=CC=2C(CC(C(=O)C=2C)OC(C)=O)(C)C)=C1C HDLNSTQYXPTXMC-UHFFFAOYSA-N 0.000 description 1
- 241000195493 Cryptophyta Species 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 229940122069 Glycosidase inhibitor Drugs 0.000 description 1
- 102000005744 Glycoside Hydrolases Human genes 0.000 description 1
- 108010031186 Glycoside Hydrolases Proteins 0.000 description 1
- 206010018473 Glycosuria Diseases 0.000 description 1
- 239000007836 KH2PO4 Substances 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 206010063837 Reperfusion injury Diseases 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000003035 anti-peroxidant effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 150000001514 astaxanthins Chemical class 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 102000006995 beta-Glucosidase Human genes 0.000 description 1
- 108010047754 beta-Glucosidase Proteins 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- NEHMKBQYUWJMIP-UHFFFAOYSA-N chloromethane Chemical class ClC NEHMKBQYUWJMIP-UHFFFAOYSA-N 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 1
- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 description 1
- 229910000396 dipotassium phosphate Inorganic materials 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 238000004821 distillation Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000000855 fermentation Methods 0.000 description 1
- 230000004151 fermentation Effects 0.000 description 1
- 206010016766 flatulence Diseases 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 229930182478 glucoside Natural products 0.000 description 1
- 239000003316 glycosidase inhibitor Substances 0.000 description 1
- 229930182470 glycoside Natural products 0.000 description 1
- 150000002338 glycosides Chemical class 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 description 1
- 238000004321 preservation Methods 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000003252 repetitive effect Effects 0.000 description 1
- 238000002390 rotary evaporation Methods 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 150000003457 sulfones Chemical class 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 235000007586 terpenes Nutrition 0.000 description 1
- 150000003505 terpenes Chemical class 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000004809 thin layer chromatography Methods 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
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
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/14—Yeasts or derivatives thereof
- A23L33/145—Extracts
-
- 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
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- 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)
- Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Mycology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Polymers & Plastics (AREA)
- Food Science & Technology (AREA)
- Nutrition Science (AREA)
- Microbiology (AREA)
- Epidemiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses a kind of new application of astaxanthin, for specially astaxanthin in the purposes for preparing glucosidase inhibitor, the purposes is to be used to prepare alpha-glucosidase restrainer using astaxanthin as one of active constituent or sole active agent.Inventor has found that astaxanthin significantly inhibits alpha-glucosidase, and alpha-glucosidase can by the intracorporal carbohydrate catalyzing hydrolysis of people at monosaccharide by intestinal absorption, cause type II diabetes so as to cause hyperglycemia or because of carbohydrate metabolism disturbance, the activity that astaxanthin passes through inhibition alpha-glucosidase, it is possible to reduce the content of internal monosaccharide is to achieve the purpose that reduce blood glucose；And the astaxanthin will not generate side effect, can apply in the drug that preparation treats or prevents diabetes, can also apply in the health care product of preparation adjuvant treatment diabetes.
Description
Technical field
The present invention relates to the new applications of astaxanthin, and in particular to a kind of astaxanthin is in the use for preparing glucosidase inhibitor
On the way.
Background technique
Glucuroide is the big fermentoid in glycoside hydrolase large family, and major function is hydrolyzation of glucose glycosidic bond, is released
Glucose is released as product, is class of enzymes indispensable in organism glycometabolism approach.According to the bonding of glucoside bond
Glucuroide can be divided into alpha-glucosidase and beta-glucosidase by mode.During alpha-glucosidase is glycometabolism
Key enzyme, main function are to be absorbed the carbohydrate in food and carbohydrate inversion by human small intestine at monosaccharide.
But excessive monosaccharide can cause blood glucose rise after being absorbed by the body, and lead to carbohydrate metabolism disturbance and then cause type-2 diabetes mellitus.Institute
It can effectively prevent in food carbohydrate and carbohydrate to be converted to monosaccharide to control alpha-glucosidase and be absorbed, in turn
Blood glucose level and type-2 diabetes mellitus disease incidence can be reduced.
Occurs the drug inhibited for alpha-glucosidase activity currently on the market, principle is inhibited using inhibitor
The activity of alpha-glucosidase, the absorption of delay glucose in vivo, to achieve the purpose that reduce blood glucose.But many α-grapes
There are side effects, such as acarbose for glycosidase inhibitor, some adverse reactions can be generated to stomach, such as flatulence, diarrhea, abdominal distension
Deng.Therefore, the natural alpha-glucosidase restrainer of new type of safe is developed from natural algae or plant becomes research hotspot.
Astaxanthin is a kind of non-V of the terpenes for being prevalent in natureAThe carotenoid in source has and delays to decline
Always, inhibit tumour, strengthen immunity, protection nerve, anti peroxidation of lipid, the bioactivity such as anti-inflammatory, but astaxanthin as drop blood
There are no pertinent literature reports for the development and utilization of sugared health care product and drug.
Summary of the invention
The present invention is directed to solve one of above-mentioned technical problem at least to a certain extent.For this purpose, one object of the present invention
It is to provide a kind of astaxanthin in the purposes for preparing glucosidase inhibitor.
In one aspect of the invention, the invention proposes a kind of astaxanthins in the use for preparing glucosidase inhibitor
It on the way, is to be used to prepare alpha-glucosidase restrainer using astaxanthin as one of active constituent or sole active agent.
According to an embodiment of the invention, inventor is surprised to find during studying the mechanism of action of astaxanthin ester
Astaxanthin significantly inhibits alpha-glucosidase, and alpha-glucosidase can be by the intracorporal carbohydrate catalytic water of people
Solution, by intestinal absorption, causes type-2 diabetes mellitus so as to cause hyperglycemia or because of carbohydrate metabolism disturbance, astaxanthin passes through inhibition at monosaccharide
The activity of alpha-glucosidase, it is possible to reduce the content of internal monosaccharide is to achieve the purpose that reduce blood glucose；And the astaxanthin is not
Side effect can be generated, can be applied in the drug that preparation treats or prevents diabetes, it also can be in preparation adjuvant treatment diabetes
It is applied in health care product.
In inhibiting rate measurement experiment of the astaxanthin to alpha-glucosidase activity, astaxanthin is to alpha-glucosidase activity
There is certain inhibiting effect, and with the increase of astaxanthin concentration, astaxanthin also increases with it alpha-glucosaccharase enzyme inhibition rate,
When astaxanthin concentration is 0.08mmol/L, the inhibiting rate for alpha-glucosidase is 76.11%.Also, astaxanthin pair
The inhibitory activity of alpha-glucosidase is better than positive control (acarbose), has good inhibiting effect to alpha-glucosidase.
According to an embodiment of the invention, such use can also have following additional technical feature:
According to one embodiment of present invention, which is using astaxanthin as one of active constituent or sole active agent
It is used to prepare prevention or treats the product of diabetes.The type of the product of the prevention or treatment diabetes is not particularly limited.
According to one embodiment of present invention, the product of the prevention or treatment diabetes is for preventing or treating glycosuria
Drug, health care product or the food of disease.
According to one embodiment of present invention, the drug is at least the one of tablet, capsule, granule or injection
Kind.
According to one embodiment of present invention, the astaxanthin is isolated and purified from phaffia rhodozyma and is obtained.
According to one embodiment of present invention, the method for astaxanthin is isolated and purified in phaffia rhodozyma, comprising the following steps:
Step 1: phaffia rhodozyma thallus broken wall: using dimethyl sulfoxide to phaffia rhodozyma thallus broken wall, broken wall condition are as follows:
Thallus and dimethyl sulfoxide press mass volume ratio, i.e. g/ml, ratio 1/2, at a temperature of 55 DEG C, broken wall 5min；
Step 2: acetone slightly mentions astaxanthin: being extracted with acetone by solid-liquid ratio 1:15 after broken wall, the solid-liquid ratio is Fife's ferment
The mass volume ratio of female thallus and acetone, i.e. g/ml extract 2 times, combined extract, low-temperature rotary evaporative removal acetone, residual
Group be divided into the astaxanthin crude extract of dmso solution, residual component is crude extract of astaxanthin；
Step 3: degreasing and the low polarity carotenoid of removal: using crude extract of petroleum ether extraction astaxanthin, extract ratio
Example is crude extract of astaxanthin: petroleum ether volume ratio 1:2, and extraction times are 2 times, discards upper layer petroleum ether, it is molten to collect lower layer
Liquid, lower layer's solution are the secondary crude extract of astaxanthin；
Step 4: removal dimethyl sulfoxide: the secondary crude extract of astaxanthin be pre-chilled to 4 DEG C of saturated sodium-chloride water solution by
Volume ratio 1:3.5 mixing, mixed liquor are extracted with ethyl acetate, and the dosage of ethyl acetate is the 3 of the secondary crude extract of astaxanthin
Times volume；Ethyl acetate phase is collected, low-temperature rotary is evaporated to dryness, and the higher astaxanthin powder of purity is made；
Step 5: crystallization: by astaxanthin powder made from step 4, methylene chloride dissolution is added, to have dissolved astaxanthin
Until powder, then into solution be added methanol to have crystallization be precipitated until, stand, methylene chloride volatilizees naturally, so that astaxanthin
Crystal is precipitated；Under 4 DEG C, 9961 × g centrifugal condition, it is centrifuged 10min, collecting bottom crystal is astaxanthin.
The present invention proposes a kind of drug in second aspect, and the drug is for preventing or treating diabetes, the medicine
Object includes astaxanthin and pharmaceutically acceptable excipient.Wherein, drug can be treatment diabetes drug either it is auxiliary
Help the drug for the treatment of diabetes.Drug can be ejection preparation or oral preparation.Oral agent can for tablet, capsule or
Granula etc..Ejection preparation can be freeze drying powder injection.
The present invention proposes a kind of food in the third aspect, and the food is for preventing or treating diabetes, the food
Product include acceptable additive in astaxanthin and bromatology.
Additional aspect and advantage of the invention will be set forth in part in the description, and will partially become from the following description
Obviously, or practice through the invention is recognized.
Detailed description of the invention
Fig. 1 is according to astaxanthin of the present invention to the inhibiting effect of alpha-glucosidase.
Specific embodiment
Below by way of specific specific example and Detailed description of the invention technical solution of the present invention.It should be understood that the present invention mentioned
One or more method and steps do not repel clearly to be mentioned there is also other methods step or at these before and after the combination step
To the step of between can also be inserted into other methods step；It should also be understood that these embodiments are merely to illustrate the present invention and do not have to
In limiting the scope of the invention.Moreover, unless otherwise indicated, the number of various method steps is only to identify the convenience of various method steps
Tool, rather than for the arrangement order of limitation various method steps or limit the scope of the invention, the change of relativeness
Or adjustment, without material changes in technical content, when being also considered as the enforceable scope of the present invention.
In order to better understand the above technical scheme, the exemplary reality that the present invention will be described in more detail below with reference to accompanying drawings
Apply example.Although showing exemplary embodiment of the present invention in attached drawing, it being understood, however, that may be realized in various forms this hair
It is bright and should not be limited by the embodiments set forth herein.It is to be able to thoroughly understand this on the contrary, providing these embodiments
Invention, and the scope of the present invention can be fully disclosed to those skilled in the art.
The test material that the present invention uses is all common commercially available product, can all be bought in market.
Below with reference to embodiment, the present invention is further explained:
The preparation of 1 astaxanthin of embodiment
Phaffia rhodozyma 5534 × g of fermentation liquid is centrifuged 8min, abandons supernatant, is centrifuged again after being washed with distillation, repetitive operation 2
It is secondary, phaffia rhodozyma thallus is made.
Phaffia rhodozyma thallus broken wall: using dimethyl sulfoxide to phaffia rhodozyma thallus broken wall, broken wall condition are as follows: thallus and two
Methyl sulfoxide press mass volume ratio, i.e. g/ml, ratio 1/2, at a temperature of 55 DEG C, broken wall 5min；It is broken using dimethyl sulfoxide
Wall rate is high, and extraction effect is good；The processing short time is short (5min), and treatment temperature low (55 DEG C) is conducive to the stabilization of astaxanthin structure.
Acetone slightly mentions astaxanthin: being extracted with acetone by solid-liquid ratio 1:15 after broken wall, the solid-liquid ratio is phaffia rhodozyma thallus
With the mass volume ratio of acetone, i.e. g/ml, extract 2 times, combined extract, low-temperature rotary evaporative removal acetone, remaining component
For the astaxanthin crude extract of dmso solution, residual component is crude extract of astaxanthin.
Degreasing and the low polarity carotenoid of removal: using crude extract of petroleum ether extraction astaxanthin, and extraction ratio is shrimp
Crude extract of green element: petroleum ether volume ratio 1:2, extraction times are 2 times, discard upper layer petroleum ether, collect lower layer's solution, lower layer
Solution is the secondary crude extract of astaxanthin.
It is sub- to the lower phase dimethyl of extracting solution (crude extract of astaxanthin), petroleum ether extraction system after petroleum ether extraction
Sulfone, the upper phase petroleum ether of petroleum ether extraction system and astaxanthin standard items carry out thin-layer chromatographic analysis, the solvent of thin-layer chromatography
For acetone/petroleum ether volume ratio=1/5, wherein low polar carotenoid is extracted to petroleum ether phase, dimethyl sulfoxide phase
Predominantly astaxanthin, the reason is that there are two hydroxyl in astaxanthin molecule, polarity is bigger than other carotenoid.Extract through petroleum ether
After taking, the low polar impurity such as lipid, which is substantially all, to be extracted into petroleum ether phase, and it is low that dimethyl sulfoxide is mutually substantially free of lipid etc.
Polar impurity.
Removal dimethyl sulfoxide: the secondary crude extract of astaxanthin and it is pre-chilled to 4 DEG C of saturated sodium-chloride water solution by volume
1:3.5 mixing, mixed liquor are extracted with ethyl acetate, and the dosage of ethyl acetate is 3 times of volumes of the secondary crude extract of astaxanthin；
Ethyl acetate phase is collected, low-temperature rotary is evaporated to dryness, and the higher recrystallized product astaxanthin powder of purity is made；The purpose of this step
It is to recycle astaxanthin from dimethyl sulfoxide, because the boiling point of dimethyl sulfoxide is very high (189 DEG C), rotary evaporation cannot be passed through
Method removes, in addition, dimethyl sulfoxide and water mixing heat release, saturated sodium-chloride water solution mixed with dimethyl sulfoxide it is preceding prior
It is cooling；Sodium chloride can help system layering, avoid the generation of emulsion, form clearly two-phase；Sodium chloride system is not added not
Layering, therefore sodium chloride is indispensable in this operating process.
Crystallization: by astaxanthin powder obtained above, methylene chloride dissolution, the dissolution of astaxanthin in methylene chloride is added
Degree is 30mg/ml, and methanol is added until having crystallization to be precipitated until having dissolved astaxanthin powder, then into solution, stands, two
Chloromethanes volatilizees naturally, so that astaxanthin crystal is precipitated；Under 4 DEG C, 9961 × g centrifugal condition, it is centrifuged 10min, collects bottom
Crystallization is astaxanthin, spare.
Measurement of 2 astaxanthin of embodiment to the inhibiting rate of alpha-glucosidase activity
The preparation of reagent:
The preparation of phosphate buffer (PBS): precise 6.8g KH2PO4, add distilled water to dissolve, be transferred to 250mL appearance
Constant volume obtains a liquid in measuring bottle；Separately take 8.7g K2HPO4, add distilled water to dissolve, be transferred to constant volume in 250mL volumetric flask and obtain b liquid；It connects
, two solution of a, b is pipetted respectively to 500mL volumetric flask constant volume, make its pH to making phosphate buffer carry out calibration using pH meter
=6.8.
The preparation of alpha-glucosaccharase enzyme solution: take the alpha-glucosaccharase enzyme powder of 75U that the PBS of 1mL, i.e. alpha-glucosidase is added
Enzyme activity be 75U/mL.The 75U/mL alpha-glucosaccharase enzyme solution of 10 μ L is taken, the PBS of 990 μ L, i.e. alpha-glucosaccharase enzyme concentration is added
For 0.75U/mL, alpha-glucosaccharase enzyme solution is answered ready-to-use.
The preparation of substrate 4- nitrobenzene-β-D- glucopyranoside solution (p-NPG solution): precise 7.9mg p-
NPG is added the dissolution of 10mL PBS buffer solution, is made into the p-NPG solution of 2.5mmol/L, is kept in dark place under the conditions of -20 DEG C standby
With.
Measurement of the astaxanthin to the inhibiting rate of alpha-glucosidase
The astaxanthin that astaxanthin uses embodiment 1 to obtain.
In 5 centrifuge tubes, it is separately added into the alpha-glucosidase enzyme solution of 112 μ L PBS buffer solution and 20 μ L, is then divided
It Jia Ru not 0.01, astaxanthin methanol solution 20 μ L (the astaxanthin methanol solution herein of 0.02,0.04,0.06,0.08mmol/L
It is to be obtained after being diluted by mother liquor, mother liquor is precisely to weigh 0.01mmol astaxanthin, is dissolved in 10mL methanol, and 1mmol/L mother is obtained
Liquid), it is added 20 μ L substrate p-NPG solution after 37 DEG C of heat preservation 15min, after 37 DEG C of the reaction was continued 15min, is surveyed at wavelength 405nm
Determine light absorption value A1。
Enzyme solution is replaced with 20 μ L PBS buffer solution, measures its light absorption value A under the same conditions2.Shrimp is replaced with 20 μ L methanol
Green element solution, measures its light absorption value A3, alpha-glucosidase enzyme solution and shrimp are replaced respectively with 20 μ L PBS and 20 μ L methanol solutions
Green element solution, measures light absorption value A4。
Using acarbose as positive control, every group of experiment measures parallel three times.
The inhibiting rate of alpha-glucosidase is calculated as follows:
As a result as shown in Figure 1, abscissa indicates astaxanthin concentration, ordinate indicates inhibiting rate.From figure 1 it appears that
Astaxanthin has certain inhibiting effect to alpha-glucosidase, and with the increase of astaxanthin concentration, astaxanthin is to phlorose
Glycosides enzyme inhibition rate also increases with it, and when astaxanthin concentration is 0.08mmol/L, the inhibiting rate for alpha-glucosidase is
76.11%.Positive control, acarbose have inhibitory activity, IC to alpha-glucosidase50Value is 1.648mmol/L, is one
The common alpha-glucosidase restrainer of kind.By regression curve calculate astaxanthin to the IC of alpha-glucosidase50Value are as follows:
0.029mmol/L.As it can be seen that astaxanthin is better than positive control to the inhibitory activity of alpha-glucosidase, have to alpha-glucosidase
Good inhibiting effect.
In addition, astaxanthin is a kind of main carotenoid, it is novel antioxidant that be otherwise known as supper vitamin E
One of.U.S. FDA ratifies its feed addictive as culture fishery within 1987；Ratify it as meal supplement within 1999
Agent, it is seen that it is with certain safety.There is existing Research of Animal Model for Study report astaxanthin protection liver, brain, kidney, small intestine to lack
The effect of blood reperfusion injury, therefore astaxanthin not will lead to some adverse reactions of stomach.
In the description of this specification, reference term " one embodiment ", " some embodiments ", " example ", " specifically show
The description of example " or " some examples " etc. means specific features, structure, material or spy described in conjunction with this embodiment or example
Point is included at least one embodiment or example of the invention.In the present specification, schematic expression of the above terms are not
It is interpreted as that identical embodiment or example must be directed to.Moreover, particular features, structures, materials, or characteristics described
It can be combined in any suitable manner in any one or more of the embodiments or examples.In addition, those skilled in the art can
Different embodiments or examples described in this specification are engaged and be combined.
Although the embodiments of the present invention has been shown and described above, it is to be understood that above-described embodiment is example
Property, it is not considered as limiting the invention, those skilled in the art within the scope of the invention can be to above-mentioned
Embodiment is changed, modifies, replacement and variant.
Claims (8)
1. astaxanthin is in the purposes for preparing glucosidase inhibitor, which is characterized in that using astaxanthin as one of active constituent
Or sole active agent is used to prepare alpha-glucosidase restrainer.
2. purposes as described in claim 1, which is characterized in that using astaxanthin as one of active constituent or sole active agent
It is used to prepare prevention or treats the product of diabetes.
3. purposes as claimed in claim 2, which is characterized in that it is described prevention or treatment diabetes product be for prevent or
The drug, health care product or food for treating diabetes.
4. purposes as claimed in claim 3, which is characterized in that the drug is in tablet, capsule, granule or injection
It is at least one.
5. purposes as described in claim 1, which is characterized in that the astaxanthin is isolated and purified from phaffia rhodozyma and obtained.
6. purposes as claimed in claim 5, which is characterized in that the method that astaxanthin is isolated and purified in phaffia rhodozyma, including with
Lower step:
Step 1: phaffia rhodozyma thallus broken wall: using dimethyl sulfoxide to phaffia rhodozyma thallus broken wall, broken wall condition are as follows: thallus
With dimethyl sulfoxide press mass volume ratio, i.e. g/ml, ratio 1/2, at a temperature of 55 DEG C, broken wall 5min；
Step 2: acetone slightly mentions astaxanthin: being extracted with acetone by solid-liquid ratio 1:15 after broken wall, the solid-liquid ratio is Phaffia Rhodozyma
The mass volume ratio of body and acetone, i.e. g/ml extract 2 times, combined extract, low-temperature rotary evaporative removal acetone, remaining group
It is divided into the astaxanthin crude extract of dmso solution, residual component is crude extract of astaxanthin；
Step 3: degreasing and the low polarity carotenoid of removal: using crude extract of petroleum ether extraction astaxanthin, extraction ratio is
Crude extract of astaxanthin: petroleum ether volume ratio 1:2, extraction times are 2 times, discard upper layer petroleum ether, collect lower layer's solution, under
Layer solution is the secondary crude extract of astaxanthin；
Step 4: removal dimethyl sulfoxide: the secondary crude extract of astaxanthin and being pre-chilled to 4 DEG C of saturated sodium-chloride water solution by volume
It is mixed than 1:3.5, mixed liquor is extracted with ethyl acetate, and the dosage of ethyl acetate is 3 times of bodies of the secondary crude extract of astaxanthin
Product；Ethyl acetate phase is collected, low-temperature rotary is evaporated to dryness, and the higher astaxanthin powder of purity is made；
Step 5: crystallization: by astaxanthin powder made from step 4, methylene chloride dissolution is added, to have dissolved astaxanthin powder
Until, then into solution be added methanol to have crystallization be precipitated until, stand, methylene chloride volatilizees naturally, so that astaxanthin crystal
It is precipitated；Under 4 DEG C, 9961 × g centrifugal condition, it is centrifuged 10min, collecting bottom crystal is astaxanthin.
7. a kind of drug, which is characterized in that the drug includes astaxanthin for preventing or treating diabetes, the drug,
And pharmaceutically acceptable excipient.
8. a kind of food, which is characterized in that the food includes astaxanthin for preventing or treating diabetes, the food,
And acceptable additive in bromatology.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910570277.0A CN110327316A (en) | 2019-06-27 | 2019-06-27 | Astaxanthin is in the purposes for preparing glucosidase inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910570277.0A CN110327316A (en) | 2019-06-27 | 2019-06-27 | Astaxanthin is in the purposes for preparing glucosidase inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110327316A true CN110327316A (en) | 2019-10-15 |
Family
ID=68143508
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910570277.0A Pending CN110327316A (en) | 2019-06-27 | 2019-06-27 | Astaxanthin is in the purposes for preparing glucosidase inhibitor |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN110327316A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007037438A1 (en) * | 2005-09-30 | 2007-04-05 | Fuji Chemical Industry Co., Ltd. | Ameliorating agent for metabolic syndrome |
| CN103848769A (en) * | 2014-02-21 | 2014-06-11 | 集美大学 | Method of separating and purifying astaxanthin from Phaffia rhodozyma |
-
2019
- 2019-06-27 CN CN201910570277.0A patent/CN110327316A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007037438A1 (en) * | 2005-09-30 | 2007-04-05 | Fuji Chemical Industry Co., Ltd. | Ameliorating agent for metabolic syndrome |
| CN103848769A (en) * | 2014-02-21 | 2014-06-11 | 集美大学 | Method of separating and purifying astaxanthin from Phaffia rhodozyma |
Non-Patent Citations (1)
| Title |
|---|
| 进口虾青素: "虾青素治疗糖尿病的作用机理，高血糖、糖尿病的朋友开来看看", 《HTTPS://WWW.SOHU.COM/A/236264521_100010409》 * |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Inthongkaew et al. | α-Glucosidase and pancreatic lipase inhibitory activities and glucose uptake stimulatory effect of phenolic compounds from Dendrobium formosum | |
| Sun et al. | Bioactivity-guided isolation and purification of α-glucosidase inhibitor, 6-OD-glycosides, from Tinta Cão grape pomace | |
| US6376682B1 (en) | Compound with α-glucosidase inhibiting action and method for producing the same | |
| CN101007017B (en) | Extract of traditional Chinese medicine having alpha-glucosidase inhibitor activity and its application | |
| CN103142720A (en) | Application of black raspberry extract in preparing anti-diabetic medicine | |
| CN105287511B (en) | The application of native Radix Glycyrrhizae A | |
| CN106220701B (en) | triterpene compound and preparation method and application thereof | |
| CN110787197A (en) | Quinoa bran extract and extraction method and application thereof | |
| CN101564405B (en) | Application of total aglycone of himalayan teasel roots and single-component hederagenin in medicaments preparing Alpha-glucosidase inhibitor | |
| CN101307090B (en) | Method for preparing timosaponin BIII and uses thereof | |
| EP3120847B1 (en) | Glechoma longituba extract for the treatment of kidney diseases or diabetes mellitus | |
| CN102000097B (en) | Bunge auriculate root C21 total steroidal glycoside degradation product and antitumor effect thereof | |
| CN110327316A (en) | Astaxanthin is in the purposes for preparing glucosidase inhibitor | |
| KR101676297B1 (en) | Composition for supressing of blood sugar level | |
| CN107349210B (en) | Compositions having synergistic alpha-amylase inhibitory activity | |
| CN109303799A (en) | It is a kind of to have ɑ-Glucosidase inhibitor effect lotus seeds shell extract and preparation method thereof | |
| KR20030025200A (en) | Substances extracted from corn which can inhibit the activities of amylase, pharmaceutical compositions and food additives containing the same extracts for treatment or prevention of obesity and diabetes mellitus, and processes for their preparation | |
| CN105963307B (en) | A kind of purposes of momordica grosvenori alcohol derivatives monomer and combinations thereof | |
| KR20090091615A (en) | Tetracera scandens extracts and 4h-chromen-4-one derivatives isolated therefrom increasing glucose uptake in differentiated l6 muscle cells | |
| CN110090243B (en) | Gorgon fruit extract for controlling postprandial blood sugar, preparation method and application | |
| Li et al. | The Active Ingredient Catalpol in Rehmannia glutinosa Reduces Blood Glucose in Diabetic Rats via the AMPK Pathway | |
| CN101797312B (en) | Method for preparing Alisma extract capable of inhibiting alpha-glucuroide activity | |
| KR20190142672A (en) | Pharmaceutical composition for preventing or treating liver damage comprising Curcuma longa extract | |
| CN106265699B (en) | Three galla turcica acidic group of the β -1,6- hexahydroxy biphenyl diformyl -2,3,4--application of D-Glucose compound in medicine preparation | |
| CN110066218B (en) | Bromophenol compound containing isoprene, and preparation method and application thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20191015 |