CN109223847A - Carlina acaulis extract is preparing the application in anti-fatigue medicament and biological products - Google Patents

Carlina acaulis extract is preparing the application in anti-fatigue medicament and biological products Download PDF

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CN109223847A
CN109223847A CN201811353774.7A CN201811353774A CN109223847A CN 109223847 A CN109223847 A CN 109223847A CN 201811353774 A CN201811353774 A CN 201811353774A CN 109223847 A CN109223847 A CN 109223847A
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carlina acaulis
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acaulis extract
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赵玉勤
陈荫
孙坤来
王斌
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Zhejiang Ocean University ZJOU
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/28Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/06Free radical scavengers or antioxidants

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Abstract

Plant extracts application field of the present invention, to solve the problems, such as that the present invention provides Carlina acaulis extracts to prepare the application in anti-fatigue medicament and biological products presently, there are there is no the technology vacancy being used for Carlina acaulis extract in antifatigue drug and biological products.Carlina acaulis extract can effectively delay Skeletal Muscle Fatigue for drug or biological products, additionally it is possible to the content of sarcolactic acid in skeletal muscle be effectively reduced.

Description

Carlina acaulis extract is preparing the application in anti-fatigue medicament and biological products
Technical field
Plant extracts application field of the present invention more particularly to Carlina acaulis extract are preparing anti-fatigue medicament and biology system Application in product.
Background technique
Energy substance is consumed totally during Skeletal Muscle Fatigue and Skeletal Muscle Contraction, the fatigue generated due to vital movement Substance is put aside in cell, and organismic internal environment imbalance generates free radicals and many reasons is waited to have close relationship.And with the modern times The rhythm of social life is getting faster, and pressure is also increasing, and fatigue starts to become like the shadow following the person.Probe into the foot of fatigue preparations Step is also advanced constantly.
In recent years, the research by researchers constantly to the anti-fatigue active of various natural extracts, It was found that sachalin rhodiola rhizome, ligustrazine, Blackfungus polyhexose, flammulina velutipes, aloe extract etc. are to toad gastrocnemius fatigue effect There is retarding action.Research shows that sachalin rhodiola rhizome, ligustrazine, the anti-fatigue active of Blackfungus polyhexose etc. may can be removed with it Free radical prevents lipid peroxidation, changes a variety of enzymatic activitys on cell membrane, adjusts cell Ca2+Concentration is to delay skeletal muscle tired Labor.First also have plurality of Chinese fatigue preparations and has entered market such as ginseng wheat injection, Hongjingtian instant tea etc..
Globe artichoke is the common food with certain health care functions, is frequently grown in Mediterranean littoral, due to its function Diversity, now in one band of China Jiangsu and Zhejiang Provinces, also there is a plantation for comparing large area on the ground such as Yunnan, and cultivation range is also increasingly wider It is wealthy.Globe artichoke is rich in Polyphenols, flavone compound, terpene, synanthrin, soluble sugar, minerals, vitamin and asparagine Equal substances.Some researches show that globe artichokes to hyperlipidemia, and hypertension, the diseases such as chronic hepatitis all have certain auxiliary curative effect.It is existing Have multiple research shows that it is with antioxidant activity, therefore it may have potential anti-fatigue active.
The polyphenol contained in Carlina acaulis extract include cynarin (cynarin), chlorogenic acid (chlorogenic acid), Caffeic acid (caffeic acid), 1- coffee quininic acid (1-caffeoylquinic acid), 3- coffee quininic acid (3- Caffeoylquinic acid), 4- coffee quininic acid (4-caffeoylquinic acid), 5- coffee quininic acid (5- Caffeoylquinic acid), bis- coffee quininic acid of 3,4- (3,4-di-O-caffeoylquinic acid), bis- coffee of 3,5- Coffee quininic acid (3,5-di-O-caffeoylquinic acid), bis- coffee quininic acid (1,5-di-O- of 1,5- Caffeoylquinic acid), bis- coffee quininic acid of 4,5- (4,5-di-O-caffeoylquinic acid) etc..It is wherein foreign Silibin content is most.Known phenolic hydroxyl group is present in polyphenol compound, can provide hydrogen or neutron in the reaction, can To remove intracorporal superoxide anion and hydroxy radical, therefore preliminary plant of the judgement with polyphenol compound has centainly Antioxidation.The flavone compound contained in Carlina acaulis extract includes naringenin rutin sophorin (narirutin), naringenin Glucoside (naringin glucoside), apiolin -7-O- rutinoside (apigenin-7-O-rutin Six kinds of flavone compounds such as glycoside).Flavone compound female ring chemical structure it is also seen that there is hydroxyl, hydroxyl With antioxidant activity, and flavone compound is also commonly used for treatment hyperlipidemia at medicinal aspect, and hypertension promotees gastrointestinal tract function Can, treat chronic hepatitis, treatment angina pectoris etc..It can be seen that Carlina acaulis extract has huge potential exploitation at medicinal aspect Meaning.Contain carbon-carbon double bond in the terpenoid female ring contained in Carlina acaulis extract, carbon-carbon double bond also has certain resist Oxidation activity.Globe artichoke also contains soluble polysaccharide, including sucrose, glucose, a small amount of ribose etc..Known carbohydrate is as machine Body carries out one of the main Energy supply material of vital movement, and body normal activities is being maintained to play an important role, and Skeletal muscle, which shrink, is needed energy substance.Also contain synanthrin, K+、Ca2+、Na+Equal inorganic ions, the contraction of skeletal muscle with Calcium ion is closely related, when Skeletal Muscle Cell is stimulated, Ca2+Interior stream enters endochylema outside film, to make the Ca in cell2 +Concentration increases.Ca intracellular2+It can have greatly changed in conjunction with troponin so as to cause the configuration of troponin, the change Change causes myosin to shift, so that the binding site of actin on cross-bridges be made to be exposed, actin it is in combination at Actomyosin, the activity of the ATP enzyme on cross-bridges increases at the same time, promotes ATP to be converted to ADP and energy, to make cross-bridges It twists, actin filament is slided to thick filament, contraction of muscle occurs.Also contain a certain amount of vitamin C, beta carotene etc..Dimension Also contain multiple hydroxyl groups in the molecular structure of raw element C, illustrates that vitamin C has certain antioxidation.And has and grind Study carefully and show that Carlina acaulis extract has preferable elimination effect to superoxide anion, also there is certain clearance rate to DPPH free radical.
Summary of the invention
To solve, presently, there are there is no the technology that Carlina acaulis extract is used in antifatigue drug and biological products empty Scarce problem, the present invention provides Carlina acaulis extracts to prepare the application in anti-fatigue medicament and biological products.It first has to Realize purpose Carlina acaulis extract being used in antifatigue drug and biological products.
To achieve the above object, the present invention uses following technical scheme.
A kind of Carlina acaulis extract is preparing the application in anti-fatigue medicament.
Preferably, the application mode of the Carlina acaulis extract is preparation, said preparation includes that the globe artichoke extracts Object and pharmaceutically acceptable auxiliary material.
Preferably, pharmaceutically acceptable auxiliary material is selected from diluent, adhesive, disintegrating agent, surfactant, coating material At least one of material, capsule material and filmogen.
Preferably, the Carlina acaulis extract is to extract selected from water extract, dehydrated alcohol extract, ethanol water Object, steam-volatile oil or supercritical extract extract.
A kind of Carlina acaulis extract is preparing the application in biological products.
Preferably, the Carlina acaulis extract is to extract selected from water extract, dehydrated alcohol extract, ethanol water Object, steam-volatile oil or supercritical extract extract.
Due to hyperkinesia, sleep insuffience, disease, pressure is excessive etc. to cause body not felt well and work efficiency drop Symptom can be defined as fatigue.Skeletal Muscle Fatigue as referred to herein is the Skeletal Muscle Contraction power due to caused by hyperkinesia The phenomenon that decline cannot maintain original exercise intensity.Number of free radical increases in sports fatigue and Skeletal Muscle Cell, and metabolism is produced The accumulation of the substances such as raw metabolite, the energy substances such as muscle glycogen exhaust that a variety of inorganic ions stable states such as calcium ion, potassium ion are lost It adjusts related.
Through studying, the polyphenol compound separated and extracted from globe artichoke there is excellent removing to imitate DPPH free radical Fruit is carrying out the Oxidation Resistance Test of rat hepatocytes in vitro rear, the results showed that the water-phase extract of 0.001mg/ml can drop The content of low MDA, while without influencing liver cell GSH-PX activity (GSH) level, the opposite loss and two for reducing glutathione Vulcanize the loss of glutathione (GSSG).
Above the experimental results showed that Carlina acaulis extract has antioxidant activity.Containing more in known polyphenol compound A phenolic hydroxyl group is the donor of excellent hydrogen or neutron, it is possible to reduce superoxide anion and hydroxy radical have certain anti-oxidant Activity.Also contain hydroxyl in the compounds such as flavone compound and vitamin and Carlina acaulis extract plays antioxidant activity Functional components.
The generation of MDA is since the resulting product of peroxidization occurs for oxygen radical and lipid.Oxygen radical can peroxide Change and destroy skeletal muscle cell membrane, so as to cause the Ca of sarcoplasmic reticulum, mitochondria and endochylema in Skeletal Muscle Cell2+What is be metabolized is unbalance, To inhibit the aerobic oxidation process of endocellular sugar, so that the generation content of ATP be caused to decline, skeletal muscle is caused certain journey occur The fatigue of degree.To sum up experiment, which can obtain Carlina acaulis extract, certain Scavenging activity to oxygen radical, to show that globe artichoke mentions Take object that can delay Skeletal Muscle Fatigue.
Sugar is the main energy sources substance that skeletal muscle carries out long-time contraction movement, and the generation of sarcolactic acid is since skeletal muscle exists Carry out motion process in, due to hyperkinesia, the circulatory system can not provide enough oxygen, and sugared aerobic breakdown is obstructed, sugar into Row anaerobic decomposition provides energy for the contraction of skeletal muscle, and the resulting product of sugared anaerobic decomposition is lactic acid.The anaerobic decomposition of sugar Speed is greater than the aerobic breakdown of sugar, but resulting energy is much smaller than the aerobic breakdown of sugar.The H that lactic acid ionization generates+It is skeletal muscle One of pH value decrease reason of cell, pH value decline will affect the dense of a variety of enzymatic activitys and a variety of inorganic ions in Skeletal Muscle Cell Degree, to will affect the synthesis of Skeletal Muscle Contraction, nerve conduction and ATP, to cause Skeletal Muscle Fatigue.But when the lactic acid of accumulation Into blood, subsequently into liver, when then generating glucose by gluconeogenesis approach in liver, lactic acid is recycled through lactic acid and is given birth to At glucose again can continue to provide energy for the contraction of skeletal muscle, this process ensure that the utilization rate of lactic acid also avoids The acid poisoning due to caused by lactic acid accumulation.Experiment shows that Carlina acaulis extract can reduce the content of sarcolactic acid in skeletal muscle, can Delay Skeletal Muscle Fatigue.
The beneficial effects of the present invention are:
1) Carlina acaulis extract effectively and efficiently utilize by the present invention;
2) Carlina acaulis extract can effectively delay Skeletal Muscle Fatigue for drug or biological products;
3) Carlina acaulis extract can be effectively reduced the content of sarcolactic acid in skeletal muscle for drug or biological products.
Detailed description of the invention
Fig. 1 is high performance liquid chromatography testing result figure;
Fig. 2 is the HPLC map of ten kinds of common monosaccharides;
Fig. 3 is the infared spectrum of Carlina acaulis extract;
Fig. 4 is the influence diagram that globe artichoke is gone for an outing in early spring to toad gastrocnemius convergent force.
Specific embodiment
Further clear detailed description explanation is made to the present invention below in conjunction with specific embodiment and Figure of description.This Field those of ordinary skill will realize the present invention based on these explanations.In addition, being related in following the description The embodiment of the present invention be generally only an of the invention branch embodiment, instead of all the embodiments.Therefore, it is based on this hair Embodiment in bright, those of ordinary skill in the art's every other reality obtained without making creative work Example is applied, should fall within the scope of the present invention.
Unless otherwise specified, raw materials used in the embodiment of the present invention is commercially available or those skilled in the art pass through conventional hand Raw material obtained by section;Unless otherwise specified, method therefor is the normal of those skilled in the art's grasp in the embodiment of the present invention Rule method.
Embodiment
S1. the extraction, configuration and detection of Carlina acaulis extract:
20% NaCl solution 32.5ml, 10% KCl solution 1.4ml, 5% NaHCO are poured into 1000ml large beaker3It is molten Liquid 4ml, 10% CaCl2Solution 1.2ml, 1% sodium dihydrogen phosphate 1.0ml, glucose 2g, finally plus distilled water arrives 1000ml is made into ringer solution.Then Carlina acaulis extract 10mg, 50mg, 250mg, then plus ringer solution are weighed respectively with electronic balance 100ml ultrasonic dissolution is made into the Carlina acaulis extract solution of 0.1mg/ml, 0.5mg/ml, 2.5mg/ml respectively;Using infrared light Spectrometry, high performance liquid chromatography etc. detect Carlina acaulis extract, wherein high performance liquid chromatography testing result such as Fig. 1 institute Show, and be compared with the HPLC map of ten kinds of common monosaccharides of Fig. 2, it is found that 44min or so occurs one apparent strong in Fig. 1 Peak shows it for glucose with Fig. 2 standard diagram comparison result;Fig. 3 is the infared spectrum of Carlina acaulis extract, can be bright from figure It is aobvious to find out in 3302cm-1There is not sharp absorption peak at place, and globe artichoke is rich in polyphenol compound, illustrates to be hydroxyl Absorption peak caused by stretching vibration.In 2925cm-1There is absorption, illustrate that C-H may be contained in Carlina acaulis extract, which may It is the absorption peak as caused by the stretching vibration of C-H bond.In 1640cm-1There is absorption peak, which may be the presence by carbonyl The absorption peak occurred illustrates that carbonyl may be contained in Carlina acaulis extract.In 1427cm-1,1368cm-1There is absorption peak at place, It may be the stretching vibration of phenyl ring or the covert vibration of methyl, illustrate that there may be phenyl ring in Carlina acaulis extract.And 1154cm-1, 1027cm-1The strong sharp absorption peak at place illustrates the stretching vibration there are cyclic ethers, illustrates to contain in Carlina acaulis extract There is the composition of saccharide ring or glucosides;
S2. the preparation of toad sura sample:
Toad 18 are selected, is dissociated the gastrocnemius of toad, and general with the brain and spinal cord for ruining broach and smashing up toad, then with glass minute hand Cotton thread is fixed at the heel string of toad, then cuts the heel string of toad with operating scissors again, then washed with configured ringer solution Except the blood stains being attached on toad gastrocnemius.2 pieces of specimen-gastrocnemius muscles of every toad are randomly divided into control group and experimental group again, Experimental group is divided into low concentration group, middle concentration group and high concentration group at random again.Control group toad gastrocnemius is placed in ringer solution again Low concentration group toad gastrocnemius is placed in the Carlina acaulis extract solution of 0.1mg/ml and impregnates 15min by middle immersion 15min, will Middle concentration group toad gastrocnemius, which is placed in the Carlina acaulis extract solution of 0.5mg/ml, impregnates 15min, by high concentration group toad calf Myenteron, which is placed in the Carlina acaulis extract of 2.5mg/ml, impregnates 15min;
S3. instrument is arranged:
The cotton thread that will be connected to soaked toad gastrocnemius is fixed on tonotransducer, and stimulating electrode is fixed on toad sura Flesh, setup parameter are intensity 10V, wave wide 0.3ms, frequency 1Hz, continuous list electro photoluminescence.Rubber head was used every 1 minute in the process Dropper, which is drawn, impregnates drop in the activity on toad gastrocnemius, keeping toad gastrocnemius;
S4. it records shrinkage curve and carries out processing analysis:
Curve is changed over time with RM6240 System of organism signal record gastrocnemius shrinkage amplitude, observes the song of generation The maximum shrinkage amplitude of line, and record the time.Then record reaches required for 90%, 50%, the 10% of maximum shrinkage amplitude Time t0.9、t0.5、t0.1, then seek the average of the required time of each group and standard deviation and record;
It is as shown in table 1 on toad gastrocnemius convergent force influence table to obtain Carlina acaulis extract;
Influence of 1 Carlina acaulis extract of table to toad gastrocnemius convergent force (it is 6 that single group, which tests quantity)
Group t0.9/s t0.5/s t0.1/s
Control group 131.25±15.50A 234.25±14.24A 1654.64±84.21A
Low concentration group (0.1mg/ml) 234.64±11.24B 394.64±13.54B 2156.56±163.47B
Middle concentration group (0.5mg/ml) 275.21±8.24C 412.94±17.34C 2965.74±123.54C
High concentration group (2.5mg/ml) 295.25±19.42D 564.54±19.40D 3152.61±148.24D
In table: different capitalizations indicate that comparing difference is significant (P < 0.05) between same perpendicular column and control group
And the influence diagram that Fig. 4 globe artichoke is gone for an outing in early spring to toad gastrocnemius convergent force is converted by above-mentioned table data, from by table 1 and Fig. 4 Slow down it will be evident that the speed of each concentration group toad gastrocnemius convergent force decline of globe artichoke is more significant than blank control group, And as the speed for improving the decline of toad gastrocnemius convergent force of globe artichoke concentration is slower, initial guess Carlina acaulis extract is to bone The decline of bone myotility slows down effect with certain, it may also be said to which Carlina acaulis extract, which has Skeletal Muscle Fatigue, centainly to be delayed Effect;
S5. in skeletal muscle sarcolactic acid and MDA content measurement:
With the same a part for the toad gastrocnemius that scissors clip has been tested, 0.1g is weighed, and is cleaned with 15% Klorvess Liquid Gastrocnemius, then suck remaining blood stains with qualitative filter paper, then 0.1g cut into thin gastrocnemius be transferred to EP and manage and added with pipette EP pipe is placed on ice bath with same dynamics, same direction by 15% Klorvess Liquid for entering 0.1ml, and grinding 10min is made even Slurry.The EP pipe is finally placed in 4 degrees Celsius, is centrifuged in the centrifuge of 3000r/min, completion to be centrifuged takes supernatant, freezing.To Biochemistry detection is carried out together after the completion of each group experiment, and biochemical indicator is as shown in following table table 2:
2 toad gastrocnemius biochemical indicator of table
Group Sarcolactic acid (mmol/g tissue) MDA (nmol/mg tissue)
Control group 24.67 11.67
Low concentration group (0.1mg/ml) 24.12 10.25
Middle concentration group (0.5mg/ml) 17.24 9.24
High concentration group (2.5mg/ml) 13.52 7.96
By table 2 it will be evident that compared with the control group, sarcolactic acid content and MDA content in the skeletal muscle of each concentration group of globe artichoke It is in apparent decreasing trend, and increasing with Carlina acaulis extract concentration, sarcolactic acid and MDA concentration reduce.Therefore speculate court The sarcolactic acid and MDA that fresh Ji extract generates skeletal muscle in contraction process have inhibiting effect, may be to Skeletal Muscle Fatigue With certain inhibiting effect.

Claims (6)

1. a kind of Carlina acaulis extract is preparing the application in anti-fatigue medicament.
2. Carlina acaulis extract according to claim 1 is preparing the application in anti-fatigue medicament, which is characterized in that described The application mode of Carlina acaulis extract be preparation, said preparation includes the Carlina acaulis extract and pharmaceutically acceptable auxiliary Material.
3. the Carlina acaulis extract according to claim 2 exists preparing the application in anti-fatigue medicament, feature In, pharmaceutically acceptable auxiliary material be selected from diluent, adhesive, disintegrating agent, surfactant, coating material, capsule material and At least one of filmogen.
4. Carlina acaulis extract according to claim 1 or 2 or 3 exists preparing the application in anti-fatigue medicament, feature In the Carlina acaulis extract is selected from water extract, dehydrated alcohol extract, ethanol water solution extract, steam distillation Volatile oil or supercritical extract extract.
5. a kind of Carlina acaulis extract is preparing the application in biological products.
6. Carlina acaulis extract according to claim 5 is preparing the application in biological products, which is characterized in that described Carlina acaulis extract is selected from water extract, dehydrated alcohol extract, ethanol water solution extract, steam-volatile oil or to surpass Critical extraction extract.
CN201811353774.7A 2018-11-14 2018-11-14 Carlina acaulis extract is preparing the application in anti-fatigue medicament and biological products Pending CN109223847A (en)

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107853700A (en) * 2017-11-28 2018-03-30 爱可道生物科技有限公司 A kind of globe artichoke liver protection fatigue-resistant drug composition
CN108497496A (en) * 2018-04-19 2018-09-07 牡丹江师范学院 A kind of functional exercise nutriment and preparation method thereof
JP2020040884A (en) * 2018-09-06 2020-03-19 三基商事株式会社 Anti-fatigue composition by activation of energy metabolism in muscle cell containing artichoke leaf extract or cynaropicrin

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107853700A (en) * 2017-11-28 2018-03-30 爱可道生物科技有限公司 A kind of globe artichoke liver protection fatigue-resistant drug composition
CN108497496A (en) * 2018-04-19 2018-09-07 牡丹江师范学院 A kind of functional exercise nutriment and preparation method thereof
JP2020040884A (en) * 2018-09-06 2020-03-19 三基商事株式会社 Anti-fatigue composition by activation of energy metabolism in muscle cell containing artichoke leaf extract or cynaropicrin

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
秦桂芝等: "朝鲜蓟化学成分及药理活性的研究进展", 《食品与药品》 *

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