CN107041899A - A kind of medicine for treating insulin resistance, preparation method and application - Google Patents
A kind of medicine for treating insulin resistance, preparation method and application Download PDFInfo
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- CN107041899A CN107041899A CN201710126857.1A CN201710126857A CN107041899A CN 107041899 A CN107041899 A CN 107041899A CN 201710126857 A CN201710126857 A CN 201710126857A CN 107041899 A CN107041899 A CN 107041899A
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- 206010022489 Insulin Resistance Diseases 0.000 title claims abstract description 36
- 208000001072 type 2 diabetes mellitus Diseases 0.000 title claims abstract description 36
- 239000003814 drug Substances 0.000 title claims abstract description 30
- 238000002360 preparation method Methods 0.000 title claims abstract description 30
- 239000000284 extract Substances 0.000 claims abstract description 46
- 244000123593 Litsea glutinosa Species 0.000 claims abstract description 24
- 239000008103 glucose Substances 0.000 claims abstract description 19
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- 210000004369 blood Anatomy 0.000 claims abstract description 16
- 239000008280 blood Substances 0.000 claims abstract description 16
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 24
- 239000003795 chemical substances by application Substances 0.000 claims description 17
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Classifications
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- 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)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/54—Lauraceae (Laurel family), e.g. cinnamon or sassafras
-
- 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
- A61K2236/30—Extraction of the material
- A61K2236/39—Complex extraction schemes, e.g. fractionation or repeated extraction steps
-
- 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
- A61K2236/51—Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
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- 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
- A61K2236/53—Liquid-solid separation, e.g. centrifugation, sedimentation or crystallization
-
- 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
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- Biotechnology (AREA)
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- Medicinal Chemistry (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The present invention relates to a kind of medicine for treating insulin resistance, preparation method and application.The medicine for the treatment of insulin resistance disclosed by the invention contains the extract of the purling original text Litsea pungens of south of the Five Ridges medicinal plant.Meanwhile, the invention also discloses the preparation method of above-mentioned Litsea glutinosa extract.The Litsea glutinosa extract tool prepared using the present invention is significantly reduced the effect of blood glucose, can add corresponding auxiliary material, polytype medicine or health products is prepared into, for improving insulin resistance.
Description
Technical field
The present invention relates to technical field of traditional Chinese medicines, be specifically related to a kind of medicine for treating insulin resistance, preparation method and
Using.
Background technology
Insulin resistance (Insulin Resistance, IR) is to cause insulin to promote body to utilize Portugal by a variety of causes
The ability of grape sugar declines, and to maintain euglycemia, B cell compensatory hypersecretion insulin, and then causes hyperinsulinism
Mass formed by blood stasis.Insulin resistance is the main factor for causing 2 type insulin resistances and its complication to develop.As people live
The change of mode, the incidence of disease of insulin resistance substantially rises, and it is prevented and treated turns into the public health problem of social concerns.Medicine
It is the effective means of insulin resistance treatment, but can directly improve the medicine of insulin resistance only have melbine and thiazolidine
Diones, and long-term taking can produce drug resistance or different degrees of toxic side effect.Therefore, effective treatment of insulin resistance according to
It is so problem in science urgently to be resolved hurrily.
The Litsea glutinosa system purling withered tree (Litsea of Lauraceae (Lauraceae) Litsea (Litsea) plant
Glutinosa), main product is in the areas such as Hainan, Guangdong, Guangxi, Yunnan [15].Purling withered tree has clearing heat and detoxicating effect, in sea
Southern Li nationality area is used as multitude's medicine.Seminar finds that purling withered tree is mainly distributed Wenchang, hainan Bronze Drum Ridge area, resource in investigation
It is abundant.
By literature search, so far, there is not yet preventing and treating the research report of insulin resistance on Litsea glutinosa.
The content of the invention
First purpose of the present invention is to provide a kind of medicine for having and treating insulin resistance, is carried containing Litsea glutinosa
Take thing.
Second object of the present invention is to provide the preparation method of the above-mentioned medicine with treatment insulin resistance,
Its step is：
a：Litsea glutinosa after drying is taken, plus 10~30 times of amount extractants decoct or refluxing extraction 2~4 times, every time 1~3
Individual hour, merge extract solution, filtration, the filtrate that is concentrated under reduced pressure is concentrated and dried；
b：The extract obtained by step a is taken, it is soluble in water, the aqueous solution is obtained, purifying is produced.
Further, described extractant is the ethanol of volume fraction 70%；The operating procedure purified in the step b is such as
Under：The aqueous solution of gained in b is taken, petroleum ether is sequentially added, ethyl acetate, n-butanol is extracted, after extract is concentrated and dried,
Obtain the extract in the present invention.
Further, in described step b, the operating procedure of purifying is as follows：The aqueous solution of gained is added and loaded in step b
In good large pore resin absorption column, distilled water flushing resin column is used, it is colourless to eluent；Then elution is added into resin column
Agent, collects eluent, is concentrated and dried, the final extract obtained in the present invention.
Further, in the step b, chromatographic column filler used is D series, HPD series, HP series, XAD series or AB-8
Macroporous absorbent resin；Eluant, eluent methanol used, ethanol, acetone, 50-95v% ethanol or 50-95v% aqueous acetone solution.
Third object of the present invention is to provide the above-described medicine with treatment insulin resistance and is preparing treatment
Application on the preparation of insulin resistance.
Fourth object of the present invention is to provide the above-described medicine with treatment insulin resistance and is preparing reduction
Application on the preparation of blood glucose.
The fifth aspect of the invention is to provide a kind of preparation of anti-diabetic, containing described in claim any one of 1-5
Treatment insulin resistance medicine.
Preparation suitable for the anti-diabetic of the present invention can be any pharmaceutically useful formulation, and these formulations include：Tablet,
Sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, mouth containing agent, granule,
Electuary, pill, powder, paste, sublimed preparation, supensoid agent, pulvis, solution, injection, suppository, ointment, emplastrum, creme, spray
Mist agent, drops, patch；It is preferred that peroral dosage form, such as：Capsule, tablet, oral liquid, granule, pill, powder, sublimed preparation, paste
Deng.Described peroral dosage form such as adhesive, filler, diluent, tablet agent, lubricant, can be collapsed containing conventional excipient
Agent, colouring agent, flavor enhancement and wetting agent are solved, tablet can be coated if necessary.Suitable filler includes cellulose, sweet dew
Sugar alcohol, lactose and other similar fillers；Suitable disintegrant includes starch, polyvinylpyrrolidone and starch derivatives,
Such as sodium starch glycollate；Suitable lubricant includes, for example magnesium stearate.Suitable pharmaceutically acceptable wetting agent includes
Lauryl sodium sulfate.
Health products, e.g. beverage, capsule, effervesce can also be made suitable for the preparation of the anti-diabetic of the present invention
Piece, tea bag, oral liquid, granule etc..
Beneficial effects of the present invention and meaning are：Extract in the present invention be from Litsea glutinosa extract, purifying and
, the resource very abundant, we have discovered that can be used as preparing improves the active drug or health products of insulin resistance, simultaneously
For further comprehensive utilization medicinal material, drive the local medicinal material expanding economy in Hainan that there is critically important realistic meaning.
The present invention carries out pharmacodynamic experiment using insulin resistant mice, and experimental demonstration Litsea glutinosa extract has non-
The effect of blood glucose is often significantly decreased, is purling withered in the preparation for being expected to be used for the pharmaceutical preparation of insulin resistance and health products
A kind of new medicinal and health value of Litsea pungens extract developing.
Brief description of the drawings
Fig. 1 is influence (n=6) of the purling withered tree extract (CG) to blood glucose, and wherein A is fasting blood-glucose performance graph；B be to
Fasting blood glucose level of the medicine after 6 weeks；Variable quantities of the C for 6 weeks blood glucose of administration compared with initial blood sugar level.
Fig. 2 is influence (n=6) of the purling withered tree extract (CG) to serum insulin level.
In Fig. 1-2,###Represent p<0.001, model group vs. normal groups；*Represent p<0.05 experimental group vs. model groups,**Table
Show p<0.01 experimental group vs. model groups,***Represent p<0.01 experimental group vs. model groups.
Embodiment
Following examples are that the present invention is further illustrated, but are never limited the scope of the present invention.Referring to
Embodiment is further elaborated on the present invention, it should be appreciated to those skilled in the art that the present invention is not limited to these implementations
Example and the preparation method used.Moreover, those skilled in the art can be equal according to description of the invention to the present invention
Replace, combine, improve or modify, but these are intended to be included in the scope of the present invention.
Embodiment 1：The preparation of Litsea glutinosa extract
Litsea glutinosa medicinal material 1Kg is taken, is crushed after being dried 24 hours in 60 DEG C of baking ovens.Added into grinding medicinal materials
1000ml volume fraction is 70% ethanol water, is soaked at room temperature after 2h, heating water bath to backflow, each refluxing extraction
2h, is total to refluxing extraction 3 times；Collect ethanol extract and reclaim ethanol to without alcohol taste, dry crude extract, crude extract is soluble in water,
The aqueous solution is obtained, with petroleum ether extraction, petroleum ether layer and water layer is obtained；It is extracted with ethyl acetate, obtains ethyl acetate layer and water layer；Plus
Extracting n-butyl alcohol, obtains n-butanol extracting liquid, and n-butanol extracting liquid is carried out into solvent recovery, drying, produces the extraction in the present invention
Thing.
Crude extract obtained as above can also be purified using macroreticular resin.Concrete operation step is：Obtained as above
After crude extract is soluble in water, adds in the large pore resin absorption column that has loaded, use distilled water flushing resin column, to eluent without
Color；Then eluant, eluent is added into resin column, eluent is collected, is concentrated and dried, the final extract obtained in the present invention.Institute
It is D series, HPD series, HP series, XAD series or AB-8 macroporous absorbent resins with chromatographic column filler；Eluant, eluent water used, first
Alcohol, ethanol, acetone, 50-95v% ethanol or 50-95v% aqueous acetone solution.
Embodiment 2：Litsea glutinosa extract hypoglycemic effect experimental study
9 week old male ob/ob mouse 50 are bought from Beijing Vital River Experimental Animals Technology Co., Ltd., are normally being raised
Support and environment is adapted under condition (normal mouse chow, 23 DEG C of room temperature, humidity 70%, 12h/12h day/nights) 1 week, subsequent fasting
6h simultaneously measures tail vein sugar level, takes fasting blood-glucose to include this research in more than 10mmol/L 30 animals.By 30 heros
Property mouse is randomly divided into 5 groups, every group of 6 animals：Model group, melbine group and extract high (200mg/Kg), in (100mg/
Kg) and low (50mg/Kg) dosage group, it is Normal group separately to take 6 wild type C57BL/6J mouse.Normal group and model
Group gives distilled water, and positive drug group gives Rosiglitazone (10mg/kg), and the high, medium and low dosage group of extract gives corresponding agent respectively
The extract of amount, is administered 6 weeks altogether.Periodic detection fasting blood-glucose, oral glucose tolerance is carried out on the 8th week in experiment weekly
(OGTT), terminate rear sacrificed by decapitation animal in experiment, take animal's whole blood, liver and adipose tissue to be weighed and biochemical indicator inspection
Survey, investigating extract improves the effect of insulin resistance.
(1) purling withered tree extract effectively reduces animal fasting blood glucose level
Model group is compared with Normal group, and fasting blood glucose level is all remarkably higher than control group within whole experimental period
(Figure 1A), and have gradually increase tendency (Fig. 1 C), the diabetic symptom of display model group animal is gradually aggravated.Daily gavage is given
Purling withered tree extract 50,100,200mg/kg is given, after administration 4 weeks, the fasting blood glucose level of administration group animal is substantially less than mould
Type control group (Figure 1A), and 200mg/kg hypoglycemic effect and positive drug Rosiglitazone (10mg/kg) quite, show substantially
Blood sugar reducing function (Figure 1A-C).Under 50mg/kg dosage, although be not significantly different with the blood glucose of model control group, still
During whole experiment, the fasting blood glucose level of animal is more steady always, significantly rise trend (Figure 1A and C) does not occur.
(2) purling withered tree extract significantly improves hyperinsulinemia and oral glucose tolerance
Ob/ob animal patterns are in addition to fasting blood-glucose is dramatically increased, and also pole is significantly increased serum insulin level, performance
Go out serious symptoms of insulin resistance (Fig. 1).Give purling withered tree extract (CG) 50,100,200mg/kg can significantly reduce it is dynamic
The serum insulin level of thing, wherein 200mg/kg CG effect is even better than positive drug Rosiglitazone, makes the serum pancreas of animal
Island element level is returned to close to intact animal level (Fig. 2).This result shows that purling withered tree extract (CG) has excellent change
The pharmacological activity of kind insulin resistance.Meanwhile, tied as the oral glucose tolerance test (OGTT) for characterizing insulin response degree
Fruit displays that purling withered tree extract (CG) can significantly improve the glucose tolerance of animal, and the Postprandial insulin of enhancing animal rings
Answering property (Fig. 2), the ability that CG improves insulin resistance is proved from another angle.
Litsea glutinosa extract powder preparation example in the present invention of embodiment 3
Obtained Litsea glutinosa extract is ground into fine powder, sieving, takes 1 part of the Chinese medical extract fine powder sieved,
Add 3.5 parts of starch, 6.5 parts of lactose progressively increases by equivalent, and mixing method is well mixed, powder is made in method divided dose by measure.
The preparation example of the Litsea glutinosa extract hard capsule of the present invention of embodiment 4
By obtained by embodiment 1 or 2 Litsea glutinosa extract crush, cross 60-100 mesh sieves, take sieved this in
1 part of medicament extract fine powder, adds 1.1 parts of dried starch as filler, adds 1-3% talcum powder and make glidant, with sky after mixing
Hard capsule is made in heart-soothing capsule filling.
The preparation example of Litsea glutinosa extract tablet in the present invention of embodiment 5
Litsea glutinosa extract obtained by embodiment 1 or 2 was crushed into 60-100 mesh sieves, the Chinese medicine sieved is taken
1 part of extract fine powder, adds 1.1 parts of hydroxypropyl cellulose and cooks disintegrant, adds 0.4 part of medicinal dextrin and makees adhesive, adds suitable
The mix lubricant that amount 50-95% ethanol is addition 1-3% after lubricant, wet granulation, drying, whole grain is uniform, is pressed into
Tablet.
The preparation example of Litsea glutinosa extract dispersible tablets in the present invention of embodiment 6
4 parts of 1 part of Litsea glutinosa extract and carrier material obtained by embodiment 1 or 2 are dissolved in 50-95%'s jointly
In ethanol, after being dried with spray drying process, sieving, the microcrystalline cellulose for adding 2.0 parts cooks disintegrant, adds appropriate superfine silica gel powder
Glidant is done, by powder direct pressing piece agent after being well mixed, dispersible tablet is produced.
The preparation example of Litsea glutinosa extract health beverage in the present invention of embodiment 7
By the Litsea glutinosa extract obtained by embodiment 1 or 2 is a and 0.001 part of co-dissolve of sugar-free sweetener in
In food grade water, add flavor enhancement and be prepared into the beverages of various tastes, it is filling after produce health drink.
Litsea glutinosa bulk drug and its extract of the present invention also can be as needed, add corresponding auxiliary material and prepare
Into other formulations, for example, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, soft capsule, oral liquid, mouth containing
Agent, granule, electuary, pill, paste, sublimed preparation, supensoid agent, pulvis, solution, injection, suppository, ointment, emplastrum, frost
Agent, spray, drops, patch etc., are not limited to formulation cited in embodiment 3-7.
The foregoing is merely illustrative of the preferred embodiments of the present invention, is not intended to limit the invention, all essences in the present invention
God is with principle, and any modification, equivalent substitution and improvements made etc. should be included in the scope of the protection.
Claims (9)
1. a kind of have the medicine for treating insulin resistance, it is characterised in that contains Litsea glutinosa Litsea glutinosa extract.
2. a kind of preparation method of medicine with treatment insulin resistance according to claim 1, it is characterised in that bag
Include following steps：
a：Litsea glutinosa after drying is taken, plus 10~30 times of amount extractants decoct or refluxing extraction 2~4 times, 1~3 small every time
When, merge extract solution, filtration, the filtrate that is concentrated under reduced pressure is concentrated and dried；
b：The extract obtained by step a is taken, it is soluble in water, the aqueous solution is obtained, purifying is produced.
3. a kind of preparation method of medicine with treatment insulin resistance according to claim 2, it is characterised in that institute
The extractant stated is the ethanol of volume fraction 70%；The operating procedure purified in the step b is as follows：It is water-soluble obtained by taking in b
Liquid, sequentially adds petroleum ether, and ethyl acetate, n-butanol is extracted, and after extract is concentrated and dried, obtains the extraction in the present invention
Thing.
4. a kind of preparation method of medicine with treatment insulin resistance according to claim 2, it is characterised in that institute
In the step b stated, the operating procedure of purifying is as follows：The aqueous solution of gained adds the macroporous absorbent resin loaded in step b
In post, distilled water flushing resin column is used, it is colourless to eluent；Then eluant, eluent is added into resin column, eluent, concentration is collected
And dry, the final extract obtained in the present invention.
5. a kind of preparation method of medicine with treatment insulin resistance according to claim 4, it is characterised in that：Institute
State in step b, chromatographic column filler used is D series, HPD series, HP series, XAD series or AB-8 macroporous absorbent resins；It is used
Eluant, eluent methanol, ethanol, acetone, 50-95v% ethanol or 50-95v% aqueous acetone solution.
6. the medicine with treatment insulin resistance described in claim any one of 1-5 is preparing the system for the treatment of insulin resistance
Application in agent.
7. there is the medicine for the treatment of insulin resistance on the preparation for preparing reduction blood glucose described in claim any one of 1-5
Using.
8. a kind of preparation of anti-diabetic, it is characterised in that：Contain the treatment insulin resistance described in claim any one of 1-5
Medicine.
9. the preparation of anti-diabetic according to claim 8, it is characterised in that：Described formulation be tablet, sugar coated tablet,
Film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, mouth containing agent, granule, electuary, ball
Agent, powder, paste, sublimed preparation, supensoid agent, pulvis, solution, injection, suppository, ointment, emplastrum, creme, spray, drop
Agent, patch.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN111285766A (en) * | 2020-03-16 | 2020-06-16 | 海南医学院 | Two labdanum diterpenoid compounds, and extraction method and application thereof |
| CN114948956A (en) * | 2021-02-19 | 2022-08-30 | 海南医学院 | Application of neolitorine in preparing medicine for preventing and treating diabetic complication |
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| CN104186181A (en) * | 2014-09-12 | 2014-12-10 | 南京通泽农业科技有限公司 | Litsea glutinosa cuttage method |
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| CN104186181A (en) * | 2014-09-12 | 2014-12-10 | 南京通泽农业科技有限公司 | Litsea glutinosa cuttage method |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111285766A (en) * | 2020-03-16 | 2020-06-16 | 海南医学院 | Two labdanum diterpenoid compounds, and extraction method and application thereof |
| CN111285766B (en) * | 2020-03-16 | 2022-06-28 | 海南医学院 | Two labdanum diterpenoid compounds, and extraction method and application thereof |
| CN114948956A (en) * | 2021-02-19 | 2022-08-30 | 海南医学院 | Application of neolitorine in preparing medicine for preventing and treating diabetic complication |
| CN114948956B (en) * | 2021-02-19 | 2024-01-19 | 海南医学院 | Application of Xinmu Jiang Zijian in preparing medicine for preventing and treating diabetic complications |
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