CN106822599A - A kind of dendrobium loddigesii Rolfe extract and its anti-diabetes use - Google Patents
A kind of dendrobium loddigesii Rolfe extract and its anti-diabetes use Download PDFInfo
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- CN106822599A CN106822599A CN201710013103.5A CN201710013103A CN106822599A CN 106822599 A CN106822599 A CN 106822599A CN 201710013103 A CN201710013103 A CN 201710013103A CN 106822599 A CN106822599 A CN 106822599A
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- dendrobium loddigesii
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- 239000000284 extract Substances 0.000 title claims abstract description 63
- 241000229499 Dendrobium loddigesii Species 0.000 title claims abstract description 62
- 206010012601 diabetes mellitus Diseases 0.000 title claims abstract description 7
- 239000011347 resin Substances 0.000 claims abstract description 19
- 229920005989 resin Polymers 0.000 claims abstract description 19
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims abstract description 14
- 230000003178 anti-diabetic effect Effects 0.000 claims abstract description 8
- 239000003472 antidiabetic agent Substances 0.000 claims abstract description 8
- 239000000203 mixture Substances 0.000 claims abstract description 8
- 235000013402 health food Nutrition 0.000 claims abstract description 6
- 238000002791 soaking Methods 0.000 claims abstract description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 43
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 22
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- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/898—Orchidaceae (Orchid family)
- A61K36/8984—Dendrobium
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/55—Liquid-liquid separation; Phase separation
Abstract
The present invention relates to a kind of dendrobium loddigesii Rolfe extract and its anti-diabetes use.The dendrobium loddigesii Rolfe extract be the stem cold soaking by dendrobium loddigesii Rolfe in aqueous acetone solution, extract is obtained through resin separation purification.It is verified by experiments, dendrobium loddigesii Rolfe extract of the invention has significant hypoglycemic activity, can be used for the treatment of diabetes and health care.The present invention also provides antidiabetic compositions and health food comprising dendrobium loddigesii Rolfe extract of the invention.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, in particular it relates to a kind of dendrobium loddigesii Rolfe extract and its in antidiabetic
Application in product and food.
Background technology
Diabetes Mellitus Treated With Traditional Chinese Medicine has the long history of thousands of years in China, has compared with the less advantage of doctor trained in Western medicine toxicity.The stem of noble dendrobium
It is usually used in treatment pyreticosis Tianjin wound on tcm clinical practice, dry polydipsia, deficiency of stomach-Yin, deficiency of food is retched, and abnormal heat is not moved back after being ill, deficiency of Yin fire
Prosperous, hectic fever due to yin labor heat, mesh is secretly failed to understand, the disease such as muscles and bones impotence.Have been reported that the stem of noble dendrobium is decocted altogether with kinds of traditional Chinese medicines, to reducing type ii diabetes
The blood sugar of patient, blood fat, mitigation insulin resistance have definite curative effect.Dendrobium loddigesii Rolfe is also the small ring hairpin stem of noble dendrobium, Dendrobium loddigesii, powder
The flower stem of noble dendrobium, is distributed mainly on the province such as Guizhou, Guangxi, Yunnan and Guangdong, is recorded by Chinese Pharmacopoeia from 2000, is tcm clinical practice
The representative of upper wide variety of stem of noble dendrobium medicinal material.Existing document discloses and extracts from some monomers of dendrobium loddigesii Rolfe and have certain α
- glucosidase inhibitory active, but these monomers are not the main components of dendrobium loddigesii Rolfe, it is acquired unstable, and in vivo
Anti-diabetic effect also fails to be confirmed.
The content of the invention
It is an object of the invention to provide a kind of dendrobium loddigesii Rolfe extract, the extracting method of the extract includes：（a）Will
Dendrobium loddigesii Rolfe cold soaking after crushing 1-5 days in 50-80 v/v % aqueous acetone solutions, daily ultrasonic wave added 1-2 times, each 30-
40 minutes, repeat to extract 3-4 times；（b）By step（a）Gained acetone-water extract is concentrated, with reverse phase silica gel, macroporous absorption tree
Fat or MCI resin adsorptions, then eluted successively with water, 70%, 80%, 90%, 100% methyl alcohol or ethanol, each gradient solvent consumption is
2-4 column volume, collects 70% ~ 90% methyl alcohol or ethanol elution part, obtains dendrobium loddigesii Rolfe extract.
Another aspect of the present invention provides a kind of antidiabetic compositions, and it includes the of the present invention of therapeutically effective amount
Dendrobium loddigesii Rolfe extract and pharmaceutically acceptable carrier.
Further aspect of the present invention provides a kind of anti-diabetic health food, the ring of the present invention grass that it includes effective dose
Herba Dendrobii extract and food additives.
Further aspect of the present invention provides a kind of method for preparing dendrobium loddigesii Rolfe extract, and it includes（a）By the ring after crushing
Careless stem of noble dendrobium cold soaking is 1-5 days in 50-80% aqueous acetone solutions, and daily ultrasonic wave added 1-2 times is each 30-40 minutes, repeats to extract
3-4 times；（b）By step（a）Gained acetone-water extract is concentrated, with reverse phase silica gel, macroporous absorbent resin or MCI resin adsorptions,
Eluted successively with 70%, 80%, 90%, 100% methyl alcohol or ethanol again, each gradient solvent consumption be 2-4 column volume, collection 70% ~
90% methanol-eluted fractions, obtain dendrobium loddigesii Rolfe extract.
Further aspect of the present invention provides dendrobium loddigesii Rolfe extract of the present invention and is preparing treatment diabetes medicament or guarantor
Application in health food.
Pharmaceutical composition of the invention or health food can be prepared into appropriate formulation, including but not limited to, tablet, capsule
The solid pharmaceutical preparations such as agent, oral liquid, soft capsule, granule or liquid preparation.Pharmaceutical composition of the invention is taken with per weight
The form of amount is used.Usage amount can carry out one according to the change such as patient age, body weight, the type and the order of severity for the treatment of disease
It is secondary or be used for multiple times.
In some embodiments, the step of dendrobium loddigesii Rolfe extract of the invention（a）The addition of middle acetone-water solution
It is 10 ~ 15 times of dendrobium loddigesii Rolfe quality of medicinal material（Mass ratio）.In some embodiments, dendrobium loddigesii Rolfe extract of the invention
Step（a）After extraction, filtering takes filtrate, reclaims acetone-water solution, is concentrated to give medicinal extract.
In some embodiments, the step of dendrobium loddigesii Rolfe extract of the invention（b）Middle reverse phase silica gel is adsorbed, then with
Water, 70%, 80%, 90%, 100% methyl alcohol are eluted successively.Reverse phase silica gel is in purification on normal-phase silica gel（Common silica gel, functional group is OH）Base
Chemically reacted on plinth and OH is substituted by OR（R is hydrocarbon chain or makees carbochain, CH）Silica gel, such as C18 reverse phase silica gels are commercially available
From Japanese fuji.
In some embodiments, the step of dendrobium loddigesii Rolfe extract of the invention（b）Middle macroporous absorbent resin is adsorbed,
Eluted successively with water, 70%, 80%, 90%, 100% ethanol again.Macroporous absorbent resin is a class without cation exchange groups and has macropore knot
The preparation of structure, with good macroreticular structure and larger specific surface area, can be optionally through thing
Organic matter in reason adsorption aqueous solution, may be selected from D101, D201, D301, HPD100, HPD400, HPD500, HPD600, AB-8
And NKA-9.
In some embodiments, the step of dendrobium loddigesii Rolfe extract of the invention（b）It is middle to use MCI resin adsorptions, then with
Water, 70%, 80%, 90%, 100% methyl alcohol are eluted successively.MCI resins be selected from CHP20/P20, CHP20/P30, CHP20/P50,
CHP20/P70、CHP20/P120、CHP50/P30、CHP50/P20、CHP50/P30、CSP50/P10、CHP07/P120、
CMG20/P10, CMG20/P30 and CMG20/P150.Preferably, the MCI resins be selected from CHP20/P20, CHP20/P30,
CHP20/P50, CHP20/P70, CHP20/P120, CHP50/P30, CHP50/P20, CHP50/P30, CSP50/P10 and
CHP07/P120.It is highly preferred that the MCI resins be CHP20/P20, CHP20/P30, CHP20/P50, CHP20/P70,
One kind in CHP20/P120.The MCI resins are purchased from such as Mitsubishi chemical Co., Ltd（Japan, Tokyo）.
In some embodiments, dendrobium loddigesii Rolfe of the invention is orchid dendrobium loddigesii Rolfe（Dendrobium
loddigesii Rolfe）Stem, be distributed in Guangdong, Guangxi, Yunnan, Guizhou, Hainan, preferably Dendrobium is produced in Yunnan
Loddigesii Rolfe plants.
Dendrobium loddigesii Rolfe extract of the present invention individually can be applied directly, can be mutually combined application, it is also possible to other medicines
Thing includes that the form of plant extracts composition compound is used.Through animal pharmacodynamics it is experimentally confirmed that dendrobium loddigesii Rolfe of the invention is extracted
Thing with clear and definite hypoglycemic drug effect, its notable insulin secretion accelerating, mitigate insulin resistance.
Specific embodiment
Essentiality content of the invention is further illustrated with embodiments of the invention below, but this is not limited with this
Invention, substance of the invention belongs to the scope of protection of present invention to the simple modifications that the present invention is carried out.
The preparation of embodiment 1-dendrobium loddigesii Rolfe extract of the present invention
Take dry dendrobium loddigesii Rolfe（Dendrobium loddigesii Rolfe）, crush, weigh 1000g and be placed in container, use
VAcetone：VWater=8：1 acetone-water solution cold soaking 3 times, first time immersion 5 days is respectively soaked 1 day, during immersion for the second time, for the third time
Using ultrasound assisted extraction, every time using 10 times of acetone-water solution, filtering takes filtrate, reclaims acetone, and be concentrated under reduced pressure
Powdered extract 55g.Dendrobium loddigesii Rolfe powdered extract proper amount of methanol is dissolved, is 10cm ' 40cm by sample upper prop volume
（i.d.）C-18 reverse phase silica gel posts, then with water, 70%, 80%, 90%, 100% methyl alcohol is eluted successively, and each gradient consumption is 5
Column volume, collects 70%, 80% meoh eluate, and decompression is spin-dried for obtaining the dry g of dendrobium loddigesii Rolfe extract 18.
The preparation of embodiment 2-dendrobium loddigesii Rolfe extract of the present invention
Dendrobium loddigesii Rolfe powdered extract is prepared with embodiment 1.Dendrobium loddigesii Rolfe powdered extract ethanol in proper amount is dissolved, by sample up to
Column volume is 10cm ' 100cm（i.d.）D101 macroporous absorbent resin adsorption columns, then with water, 70%, 80%, 90%, 100% ethanol
Elute successively, each gradient solvent consumption is 3 column volumes, collects 70% ~ 90% ethanol elution part, obtain dendrobium loddigesii Rolfe extraction
Thing.
The preparation of embodiment 3-dendrobium loddigesii Rolfe extract of the present invention
Dendrobium loddigesii Rolfe powdered extract is prepared with embodiment 1.Dendrobium loddigesii Rolfe powdered extract proper amount of methanol is dissolved, by sample up to
Column volume is 10cm ' 80cm（i.d.）MCI GEL resin absorbing columns, then with water, 70%, 80%, 90%, 100% methyl alcohol is washed successively
De-, each gradient solvent consumption is 3 column volumes, collects 70% ~ 90% methanol-eluted fractions, obtains dendrobium loddigesii Rolfe extract.
The preparation of 4-pharmaceutical composition of embodiment（Tablet）
The mg of dendrobium loddigesii Rolfe extract 60, lactose 130mg, starch 55mg, magnesium stearate 5mg obtained in the method for Example 1,
Dendrobium loddigesii Rolfe extract, lactose, starch are mixed, is moistened with water, the mixture after moistening is sieved and dried, re-sieving, plus
Enter magnesium stearate, then by mixture compressing tablet, every weight 250mg, dendrobium loddigesii Rolfe extractive content 60mg.
The preparation of 5-health food of embodiment（Capsule）
The mg of dendrobium loddigesii Rolfe extract 60, lactose 137mg, magnesium stearate 3mg obtained in the method for Example 2.By dendrobium loddigesii Rolfe
Extract mixes with auxiliary agent, sieving, uniform mixing, the mixture loading hard gelatin capsule that will be obtained, each capsule weight 200mg,
Dendrobium loddigesii Rolfe extractive content is 60mg.
The antidiabetic effect of experimental example 1-dendrobium loddigesii Rolfe extract
Experimental principle：Dbdb mouse are the animal models that typical single gene mutation causes 2 patients with type Ⅰ DM（BKS.Cg-
Dock7m +/+Leprdb/Nju）, this is mouse by No. 4 Janus albumen junket ammonia of autosome leptin receptor (LEPR)
Acid kinase (JAK) gene loci is undergone mutation and is derived.Dbdb mouse tool is fat, hyperglycaemia, height insulin resistance
Spontaneous II patients with type Ⅰ DM characteristic, under C57BLKS backgrounds, is able to observe that many features, such as the uncontrolled increasing of blood sugar
Height, produces the beta Cells Depletions of insulin, the uncontrollable blood sugar concentration of exogenous insulin and the rising of gluconeogenesis enzymatic activity.
Peripheral neuropathy and Myocardial damage are observed that in C57BLKS-Leprdb homozygotes, recovery speed slows down, metabolism increases
Plus etc., it is the animal model of conventional research II patients with type Ⅰ DM medicine and mechanism.
Experimental technique：Db/db mouse, 5 week old after adaptability is raised one week, are randomly divided into 3 groups：Model control group, ring
Careless Herba Dendrobii extract group（It is prepared by embodiment 1-3）(100m g/kg), melbine group (130 mg/kg), every group 8,
Separately C57 mouse are taken as Normal group.Daily gastric infusion, administration time 9:00~10:00 am, Per-Hop behavior 7
My god, successive administration 7 weeks, every 7 days detection Mouse Weights and blood glucose value 1 time.Mouse ad lib, drinking-water during experiment.
Sugar tolerance method of testing：In administration the 6th week, on an empty stomach after 12 hours, gavage was to glucose solution for each group mouse（2g/
kg）, respectively test mouse to sugar after 0.5,1,1.5,2h blood glucose values.Blood sugar test method：Using test paper method.Blood glucose meter model：
ACCU-CHEK Performa.Blood sugar test paper model：ACCU-CHEK Performa.
The hypoglycemic experimental result of dendrobium loddigesii Rolfe extract is shown in Table 1, and experimental result is expressed as the mouse blood sugar value for detecting weekly
Average value, wherein administration group are dendrobium loddigesii Rolfe extract group, and positive drug group is melbine group, model group and Normal group.
Dendrobium loddigesii Rolfe extract is shown in Table 2 on dbdb glucose tolerance in mice influence experimental result, and experimental result is expressed as mouse 12 hours on an empty stomach
Blood glucose value average value and oral glucose liquid（2g/kg）0.5,1,1.5,2 hours blood glucose value average value afterwards, wherein administration group are ring
Careless Herba Dendrobii extract group, positive drug group is melbine group, model group and Normal group.
Can be drawn from table 1, the experimental result of table 2, dendrobium loddigesii Rolfe extract has preferably internal hypoglycemic effect, internal hypoglycemic
The close clinic antidiabetic drug melbine of drug effect.
Hypoglycemic experiment in table 1-dendrobium loddigesii Rolfe extract dbdb Mice Bodies
2-dendrobium loddigesii Rolfe of table extract influences to test on dbdb Mice Bodies sugar tolerancea
a:Each experimental mice oral glucose dosage is 2 g/kg.
Claims (9)
1. a kind of dendrobium loddigesii Rolfe extract, the extracting method of the extract includes：
（a）By the dendrobium loddigesii Rolfe cold soaking after crushing 1-5 days in 50-80 v/v % aqueous acetone solutions, daily ultrasonic wave added 1-2
It is secondary, it is each 30-40 minutes, repeat to extract 3-4 times；
（b）By step（a）Gained acetone-water extract is concentrated, with reverse phase silica gel, macroporous absorbent resin or MCI resin adsorptions, then
Eluted successively with water, 70%, 80%, 90%, 100% methyl alcohol or ethanol, each gradient solvent consumption is 2-4 column volume, collects 70%
~ 90% methyl alcohol or ethanol elution part, obtain dendrobium loddigesii Rolfe extract.
2. dendrobium loddigesii Rolfe extract according to claim 1, wherein step（a）The addition of middle acetone-water solution is ring
10 ~ 15 times of careless stem of noble dendrobium quality of medicinal material.
3. dendrobium loddigesii Rolfe extract according to claim 1, wherein step（b）It is middle with reverse phase silica gel adsorb, then with water,
70%th, 80%, 90%, 100% methyl alcohol is eluted successively.
4. dendrobium loddigesii Rolfe extract according to claim 1, wherein step（b）Middle macroporous absorbent resin is adsorbed, then with
Water, 70%, 80%, 90%, 100% ethanol are eluted successively.
5. dendrobium loddigesii Rolfe extract according to claim 1, wherein step（b）It is middle to use MCI resin adsorptions, then with water,
70%th, 80%, 90%, 100% methyl alcohol is eluted successively.
6. a kind of antidiabetic compositions, the ring grass stone described in its claim any one of 1-5 for including therapeutically effective amount
Dry measure used in former times extract and pharmaceutically acceptable carrier.
7. a kind of anti-diabetic health food, the dendrobium loddigesii Rolfe described in its claim any one of 1-5 for including effective dose is extracted
Thing and food additives.
8. a kind of method for preparing dendrobium loddigesii Rolfe extract, it includes：
（a）By the dendrobium loddigesii Rolfe cold soaking after crushing 1-5 days in 50-80% aqueous acetone solutions, daily ultrasonic wave added 1-2 times, every time
30-40 minutes；Repeat to extract 3-4 times；
（b）By step（a）Gained acetone-water extract is concentrated, with reverse phase silica gel, macroporous absorbent resin or MCI resin adsorptions, then
Eluted successively with 70%, 80%, 90%, 100% methyl alcohol or ethanol, each gradient solvent consumption be 2-4 column volume, collection 70% ~
90% methanol-eluted fractions, obtain dendrobium loddigesii Rolfe extract.
9. the dendrobium loddigesii Rolfe extract described in any one of claim 1-5 is in treatment diabetes medicament or health food is prepared
Using.
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| CN108042458A (en) * | 2018-01-10 | 2018-05-18 | 中国科学院昆明植物研究所 | Dendrobium loddigesii extract and its application in cosmetics are prepared |
| CN108066244A (en) * | 2018-02-02 | 2018-05-25 | 广州赛莱拉干细胞科技股份有限公司 | A kind of composition containing brown algae polyphenols |
| CN110302312A (en) * | 2018-03-27 | 2019-10-08 | 中山大学 | A kind of dendrobium loddigesii Rolfe alkaloid valid target and its preparation method and application |
| CN110354205A (en) * | 2018-03-26 | 2019-10-22 | 中山大学 | A kind of Pale Ephemerantha active component and its preparation method and application |
| CN110478437A (en) * | 2019-08-21 | 2019-11-22 | 西华大学 | A kind of golden hairpin dendrobium extract and preparation method |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108042458A (en) * | 2018-01-10 | 2018-05-18 | 中国科学院昆明植物研究所 | Dendrobium loddigesii extract and its application in cosmetics are prepared |
| CN108066244A (en) * | 2018-02-02 | 2018-05-25 | 广州赛莱拉干细胞科技股份有限公司 | A kind of composition containing brown algae polyphenols |
| CN110354205A (en) * | 2018-03-26 | 2019-10-22 | 中山大学 | A kind of Pale Ephemerantha active component and its preparation method and application |
| CN110354205B (en) * | 2018-03-26 | 2021-11-16 | 中山大学 | Dendrobium candidum effective part and preparation method and application thereof |
| CN110302312A (en) * | 2018-03-27 | 2019-10-08 | 中山大学 | A kind of dendrobium loddigesii Rolfe alkaloid valid target and its preparation method and application |
| CN110302312B (en) * | 2018-03-27 | 2021-11-12 | 中山大学 | Dendrobium loddigesii alkaloid effective part and preparation method and application thereof |
| CN110478437A (en) * | 2019-08-21 | 2019-11-22 | 西华大学 | A kind of golden hairpin dendrobium extract and preparation method |
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