CN108379495A - Galangal rhizome extract is preparing the purposes in preventing and/or treating nonalcoholic fatty liver preparation - Google Patents
Galangal rhizome extract is preparing the purposes in preventing and/or treating nonalcoholic fatty liver preparation Download PDFInfo
- Publication number
- CN108379495A CN108379495A CN201810501185.2A CN201810501185A CN108379495A CN 108379495 A CN108379495 A CN 108379495A CN 201810501185 A CN201810501185 A CN 201810501185A CN 108379495 A CN108379495 A CN 108379495A
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- CN
- China
- Prior art keywords
- galangal rhizome
- rhizome extract
- fatty liver
- nonalcoholic fatty
- galangal
- 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.)
- Granted
Links
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Classifications
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
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- A61K2236/30—Extraction of the material
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- A61K2236/55—Liquid-liquid separation; Phase separation
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Abstract
The invention belongs to biotechnologies, are related to galangal rhizome extract and are preparing the purposes in preventing and/or treating nonalcoholic fatty liver preparation.General flavone content is 99wt% or more in the galangal rhizome extract, the galangal rhizome extract contains Galangin 67wt% 85wt%, 3 O methyl ether 7wt% 21wt% of Galangin, 4 ' O methyl ether 2wt% 13wt% of Kaempferol, summation are no more than 100%.The triglycerides, cholesterol, ALT, AST that the galangal rhizome extract of the present invention can reduce nonalcoholic fatty liver mouse are horizontal, have the function of increasing high density lipoprotein, reduce low-density lipoprotein.
Description
Technical field
The invention belongs to biotechnologies, prevent and/or treat non-preparing more particularly, to galangal rhizome extract
Purposes in alcohol fatty hepar.
Background technology
Non-alcoholic fatty liver disease (Non-alcoholic fatty liverdisease, NAFLD) is worldwide
Diagnosis constantly rise, be considered as one of most common liver diseases in western countries, account for about the 20%- of total population
30%.It is increasingly becoming the increasingly severe chronic liver disease problem in China simultaneously, incidence is about 15%.Nonalcoholic fatty liver
Hepatopathy, heavy drinking is clearly damaged with other caused by the factor of liver except referring to becomes pathology with diffusivity liver cell fat
The clinical syndrome of feature, including simple fatty liver, nonalcoholic fatty liver disease and its relevant hepatic sclerosis and liver cell
Cancer.In recent years, due to the change of improvement of living standard, life style and dietary structure and relatively lagging behind for precautionary measures
Deng NAFLD incidence rises year by year, becomes worldwide health problem.The progress of NAFLD is one and inflammation, oxidative stress, from
It bites, er stress and the relevant complex process of insulin resistance, there is no the drug of effectively treatment nonalcoholic fatty liver at present,
Chinese medicine, natural drug are the rarities in China, and material base is natural products, for Western medicine, have structure-rich, activity
Unique, the features such as side effect is low, action target spot is various, be the important sources of China's original new drug, and selection exploitation is a kind of in Chinese medicine
The drug of the lower prevention nonalcoholic fatty liver of safe and effective and toxic side effect, has extremely vast market prospect,
And good social and economic benefit can be created.
Galangal (Alpinia officinarum Hance) is Zingiber (Zingiberaceae) Alpinia plants, alias
Small galingal, current chart ginger, are a kind of plant resources of dietotherapeutic, often cook seasoning use in Guangdong and country in Southeast Asia, are one
Kind medical and edible dual purpose plant, rhizome are used as medicine, and have warming stomach for dispelling cold, promoting qi circulation and relieving pain effect.Galangal has the cultivation of centuries in China
Training and medicinal history contain a large amount of chromocor compound and Diphenylheptane compound in galangal.Modern pharmacological studies have shown that
Galangal and extract have antitumor, antibacterial, antiviral, anti-obesity, anti-gastric-ulcer and a protective effects on gastric mucosa, but about
Galangal rhizome extract prevention nonalcoholic fatty liver there is no pertinent literature to report at present.
Invention content
The object of the present invention is to provide a kind of new application of galangal rhizome extract, specially galangal rhizome extract is being prepared in advance
Purposes in anti-and/or treatment nonalcoholic fatty liver preparation.
To achieve the goals above, a kind of galangal rhizome extract of present invention offer is preparing prevention and/or is treating non-alcohol
Property fat hepar in purposes, general flavone content is 99wt% or more in the galangal rhizome extract, the galangal extraction
Object contains Galangin 67wt%-85wt%, Galangin -3-O- methyl ether the 7wt%-21wt%,-O- methyl ethers of Kaempferol -4 '
2wt%-13wt%, summation are no more than 100%.
In the present invention, each component content is preferably measured using high-efficient liquid phase technique, specifically, is surveyed with reference to following documents
It is fixed:Zhao Xiao Di, Chen Xiaohui, Geng Lulu etc., HPLC methods measure the content of 3 kinds of flavones ingredients in galangal simultaneously.Pharmaceutical Analysis
Magazine, 2009,29 (12):2036-2039.
Galangal rhizome extract of the present invention is preferably made by method comprising the following steps:By galangal rhizome powder
It is broken, methyl tertiary butyl ether(MTBE) is added and carries out homogenate extraction, filters to obtain the dregs of a decoction, the dregs of a decoction add ethyl acetate to extract, and recycle acetic acid second
Ester extract obtains galangal rhizome extract medicinal extract, and medicinal extract is by column chromatography for separation, petroleum ether-ethyl acetate gradient elution, thin layer
Chromatography monitoring, merging contain Galangin, Galangin -3-O- methyl ether %, and the fraction of-O- methyl ethers of Kaempferol -4 ' removes fraction
In petroleum ether-ethyl acetate solvent, then through ethyl alcohol recrystallization, the galangal rhizome extract is made.
Specifically, homogenate extraction can carry out twice.Ethyl acetate is added to extract and can carry out at normal temperatures.The methyl
The dosage of tertbutyl ether and ethyl acetate can be the 4-6 mass times of object to be extracted.
According to the present invention, petroleum ether-ethyl acetate gradient elution preferably uses volume ratio 10: 1,8: 1,5: 1,3: 1,1: 1
Petroleum ether-ethyl acetate gradient eluent.
According to the present invention, the column chromatography is preferably polyamide column chromatography.
According to a kind of specific implementation mode of the present invention, the galangal rhizome extract is made by following steps:By galangal
Rhizome crushes, and adds 4-6 times of methyl tert-butyl ether solvent, flash extracter to extract 2 times, filters to obtain the dregs of a decoction.The dregs of a decoction add 4-6 times again
Ethyl acetate extracts 2 times, obtains acetic acid ethyl acetate extract, and recycling ethyl acetate obtains galangal rhizome extract medicinal extract, and medicinal extract passes through polyamides
Amine column chromatography for separation, the petroleum ether-ethyl acetate gradient elution for being 10: 1,8: 1,5: 1,3: 1,1: 1 with volume ratio, thin-layer chromatography
Monitoring, merging contain Galangin, Galangin -3-O- methyl ether %, the fraction of-O- methyl ethers of Kaempferol -4 ', fraction recycling oil
Ether-ethyl acetate solvent, then can be obtained with ethyl alcohol recrystallization.
In the present invention, the preparation both can be drug, or food, such as health food.
The drug may include one or more pharmaceutically acceptable carriers.As used herein, term " pharmaceutically may be used
The carrier of receiving " refers to the excipient and/or adjuvant for promoting the active component of the present invention to be processed into preparation that can be medicinal.For
The suitable excipient of the present invention includes the filler of such as carbohydrate (for example, lactose, sucrose, mannitol, D-sorbite);Fiber
Plain derivative;Magnesium sulfate;Calcium phosphate (for example, tricalcium phosphate, calcium monohydrogen phosphate);Such as gelatinized corn starch is (for example, cornstarch, wheat
Starch, rice starch, potato starch), the adhesive of gel, tragacanth or polyvinylpyrrolidone.It can be used for the present invention
Suitable adjuvant include throttling agent and lubricant, such as talcum, silica, stearic acid or derivatives thereof (for example, magnesium stearate),
And/or polyethylene glycol.
It can be by any ideal administration route, including in oral, local, intramuscular, intraperitoneal, subcutaneous, tumor or vein
Approach gives the preparation of the drug.In the present invention, the dosage form of the drug can be the dosage form of the various conventional suitables in this field,
Including but not limited to tablet, capsule, granule, pill, oral solution.
Other features and advantages of the present invention will be described in detail in subsequent specific embodiment part.
Description of the drawings
Exemplary embodiment of the invention is described in more detail in conjunction with the accompanying drawings, it is of the invention above-mentioned and its
Its purpose, feature and advantage will be apparent.
Fig. 1 shows the Normal group liver structure observed under light microscopic.
Fig. 2 shows the model group liver structures observed under light microscopic.
Fig. 3-5 shows the galangal rhizome extract low dose group, galangal rhizome extract middle dose group, height observed under light microscopic
Rhizoma Alpiniae Officinarum extract high dose group liver structure.
Fig. 6 shows the positive drug group liver structure observed under light microscopic.
Specific implementation mode
The preferred embodiment of the present invention is described in more detail below.Although the following describe the preferred implementations of the present invention
Mode, however, it is to be appreciated that may be realized in various forms the present invention without should be limited by embodiments set forth herein.
The galangal rhizome extract further illustrated the present invention below by way of specific effect experiment is small to nonalcoholic fatty liver
The intervention and therapeutic effect of mouse.
1, drug
Given the test agent:The galangal rhizome extract of the present invention is made by following preparation method:Galangal rhizome is crushed,
Add 5 times of methyl tert-butyl ether solvent, flash extracter to extract 2 times, filters to obtain the dregs of a decoction.The dregs of a decoction add 5 times of ethyl acetate extractions 2 again
It is secondary, acetic acid ethyl acetate extract is obtained, recycling ethyl acetate obtains galangal rhizome extract medicinal extract, and medicinal extract is detached by polyamide column chromatography,
The petroleum ether-ethyl acetate gradient elution for being 10: 1,8: 1,5: 1,3: 1,1: 1 with volume ratio, thin-layer chromatography monitoring, merging contain
Galangin, Galangin -3-O- methyl ether %, the fraction of-O- methyl ethers of Kaempferol -4 ', it is molten that fraction recycles petroleum ether-ethyl acetate
Agent, then can be obtained with ethyl alcohol recrystallization.
Positive control drug:Fenofibrate, French Li Bofuni drugmakers production.
2, animal:SPF grades of Kunming mouse models, 8 week old, weight 20-22g, male;In being tested by the Central China University of Science and Technology
The heart provides.
3, experimental method
60 SPF grades of male mouse of kunming are randomly divided into 6 groups, respectively:1. Normal group, 2. positive drug group is (non-
Nobert 10mg/kg), 3. galangal rhizome extract high dose group (200mg/kg), 4. galangal rhizome extract middle dose group (100mg/
Kg) 5. galangal rhizome extract low dose group (50mg/kg), 6. model group, every group 10.After adaptable fed 1 week, except normal right
Outer according to group, remaining 5 groups with high lipid food (autogamy:Basal feed 73%, lard 25%, cholesterol 2%), continuously it is fed with 16
Week recorded weekly mouse food ration and mouse weight from feeding high lipid food first week, and mouse is raised in clean animal room
It supports, room temperature:22 ± 2 DEG C, humidity:Ventilation in 30~70%, 20 minutes is primary, each 12 hours of light and shade.Galangal rhizome extract, fenofibrate
Spy dissolved with 0.5%CMC-Na, the high, medium and low dose concentration of galangal rhizome extract be respectively 50mg/kg, 100mg/kg,
200mg/kg, gavage, once a day, continuous 16 weeks;Blank control group and the corresponding 0.5%CMC- of hyperlipidemia model group intragastric administration on mice
Na solution.It is deprived of food but not water 12h after the last administration, weighs in, eye socket takes blood, and liver is won in rapid dissection.From left lobe of liver phase
The hepatic tissue that one piece of about 1.5cm × 1.5cm × 1.5cm sizes are taken with position is completely soaked and is fixed in 10% paraformaldehyde liquid,
It is dyed for subsequent slice HE.HE stained slices are in 200 times of light microscopic observations.
As shown in Figure 1, light is under the microscope, Normal group liver structural integrity, liver cell arrangement is radial, and liver cell is big
Small form is normal, has no the abnormalities such as hepatic steatosis, oedema.As shown in Fig. 2, most of liver cell under model group hepatic tissue mirror
There is apparent fat to become, cell becomes larger, and fat drips are larger.As in Figure 3-5, galangal rhizome extract is from low dosage to high low dosage
Group, liver cell fat become degree and mitigate successively, and apparent dosage correlation is presented.It is thin that Fig. 5 can be seen that galangal high dose group liver
Born of the same parents' fat becomes quantity and significantly reduces, and almost uniform in size, form is normal.As shown in fig. 6, fenofibrate group murine liver tissue pathology
Histology is similar to Normal group, no abnormality seen lesion.To sum up, it can be seen that galangal rhizome extract is to nonalcoholic fatty liver
With significant improvement.
The blood biochemistry index such as blood fat, transaminase are detected according to biochemistry detection kit operating instruction.
Experimental data is tentatively arranged with office excel, with mean+SD/standard error (mean ± SD/SEM)
It indicates, analyzed using 17.0 statistical softwares of SPSS, experimental result is all made ofIt indicates, comparison among groups use single factor test variance
Analysis.
The results are shown in Table 1.
Influence of 1 galangal rhizome extract of table to nonalcoholic fatty liver mouse liver function
As it can be seen from table 1 the galangal rhizome extract of the present invention can reduce the glycerine three of nonalcoholic fatty liver mouse
Ester, cholesterol, ALT, AST are horizontal, have the function of increasing high density lipoprotein, reduce low-density lipoprotein.And galangal
High dose group has and the comparable effect of positive drug.
Various embodiments of the present invention are described above, above description is exemplary, and non-exclusive, and
It is not limited to disclosed each embodiment.Without departing from the scope and spirit of illustrated each embodiment, for this skill
Many modifications and changes will be apparent from for the those of ordinary skill in art field.
Claims (9)
1. galangal rhizome extract is preparing the purposes in preventing and/or treating nonalcoholic fatty liver preparation, which is characterized in that institute
It is 99wt% or more to state general flavone content in galangal rhizome extract, and the galangal rhizome extract contains Galangin 67wt%-
85wt%, Galangin -3-O- methyl ether the 7wt%-21wt%,-O- methyl ether 2wt%-13wt% of Kaempferol -4 ', summation do not surpass
Cross 100%.
2. galangal rhizome extract according to claim 1 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that each component content is measured using high-efficient liquid phase technique.
3. galangal rhizome extract according to claim 1 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that the galangal rhizome extract by method comprising the following steps be made:By galangal rhizome powder
It is broken, methyl tertiary butyl ether(MTBE) is added and carries out homogenate extraction, filters to obtain the dregs of a decoction, the dregs of a decoction add ethyl acetate to extract, and recycle acetic acid second
Ester extract obtains galangal rhizome extract medicinal extract, and medicinal extract is by column chromatography for separation, petroleum ether-ethyl acetate gradient elution, thin layer
Chromatography monitoring, merging contain Galangin, Galangin -3-O- methyl ether %, and the fraction of-O- methyl ethers of Kaempferol -4 ' removes fraction
In petroleum ether-ethyl acetate solvent, then through ethyl alcohol recrystallization, the galangal rhizome extract is made.
4. galangal rhizome extract according to claim 3 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that homogenate extraction carry out twice.
5. galangal rhizome extract according to claim 3 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that petroleum ether-ethyl acetate gradient elution use volume ratio 10: 1,8: 1,5: 1,3: 1,1: 1 oil
Ether-ethyl acetate gradient liquid.
6. galangal rhizome extract according to claim 3 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that the column chromatography be polyamide column chromatography.
7. galangal rhizome extract according to claim 1 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that the preparation includes drug and/or health food.
8. galangal rhizome extract according to claim 7 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that the drug includes one or more pharmaceutically acceptable carriers.
9. galangal rhizome extract according to claim 7 is in preparing prevention and/or treatment nonalcoholic fatty liver preparation
Purposes, which is characterized in that the dosage form of the drug be selected from tablet, capsule, granule, pill, oral solution.
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