CN101518597A - Application of thearubigins to pharmacy - Google Patents
Application of thearubigins to pharmacy Download PDFInfo
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- CN101518597A CN101518597A CN200910094072A CN200910094072A CN101518597A CN 101518597 A CN101518597 A CN 101518597A CN 200910094072 A CN200910094072 A CN 200910094072A CN 200910094072 A CN200910094072 A CN 200910094072A CN 101518597 A CN101518597 A CN 101518597A
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Abstract
The invention discloses a new purpose of thearubigins in the field of pharmacy. The thearubigins is a natural product extracted from Pu'er tea which is used as raw material. The result of pharmacological experiments shows that the thearubigins can remarkably restrain the activity of protein tyrosine phosphatase, and can be used for treating or preventing II type diabetes, lipogenous diabetes and adiposis. Being a pure natural substance extracted from the Pu'er tea, the thearubigins has no toxic side effect and is safe and reliable to take.
Description
Technical field
The present invention relates to the purposes of thearubigins, relate in particular to the purposes in pharmaceutical field.
Background technology
Diabetes are the common and major diseases that influence human health, and by the end of the year ends 2007, the whole world has diabetics 2.5 hundred million people, expect whole world trouble diabetes in 2025 and will reach 300,000,000 people.At present, China has 6,500 ten thousand diabeticss approximately, and sickness rate is 5%, and sickness rate accounts for second in the world.Have 80% to be type ii diabetes in diabetics, it is sugared anti-receptors that 5,000 ten thousand people are still arranged, and they further develop also will become diabetics.At present, insulin and part chemical synthetic drug (example hydrochloric acid metformin, rosiglitazone etc.) extensive use clinically, but side effect is puzzlement patient's a big problem always.Especially for insulin resistant and chemicals opposing diabetics, exploitation safety, side effect is little, be easy to the emphasis that oral natural drug is world today's Remedies for diabetes research and development.
1992, E.H.Fisher and E.G.Krebs obtained Nobel's physiology and medical science prize jointly because of finding protein phosphatase and kinases.Discover that for many years protein phosphatase and kinases and numerous disease are in close relations.The PTP1B that studies have shown that in recent years is the drug targets of a treatment type ii diabetes and obesity.PTP1B is earlier with Insulin receptor INSR (IR) dephosphorylation that is activated, and makes the IRS that it can not the phosphorylation downstream, and then stoped the signal transduction pathway of insulin, further influenced the performed physiological function of insulin, caused the generation of diabetic symptom.Therefore, any PTP1B expression relevant with IR and the variation of vigor all may influence the insulin signaling transduction, and may cause the generation of insulin impedance, and then cause the generation of type ii diabetes.Leptin is a kind of secreted protein by the OB gene code, with the effect that can bring into play adjusting body weight and energy expenditure after the leptin receptors bind.Many obesities are principal character with the leptin opposing.Lacking the leptin gene knockout (ob/ob) of PTP1B rat shows as body weight does not increase, and fatty tissue reduces and resting metabolic rate improves, and to the leptin mediation lose weight and appetite inhibiting has enhancement effect.Reply the neuron accumulation regions at the rat hypothalamus leptin and express, experiment shows that PTP1B can cause the leptin opposing by the dephosphorylation to leptin receptor-associated kinase JAK2.
In recent years, a lot of research worker both domestic and external are all being sought optionally PTP1B inhibitor always, though special, effective and safe non-peptide inhibitor does not find that also the research of PTP1B inhibitor has obtained certain progress.Most of PTP1B inhibitor of having found at present are peptide class or the stronger material of toxicity, and for example nonselective PTP inhibitor vanadate and pervanadate etc. can't be developed as medicine.Other is as Chinese patent application CN1794989A; the PTP1B inhibitor of being mentioned is N-(((((1; the 3-thiazol-2-yl) sulfonyl phenyl carbonyl amino)))) phenylalanine derivative and related compound need obtain complex manufacturing by the multistep chemosynthesis.Screening PTP1B inhibitor is one of most promising method from the Chinese medicine resource, the now existing PTP1B inhibitor that separation and Extraction obtains from natural plants such as Chinese medicine, as Chinese patent application CN1521157A, in plant Herba Ardisiae Japonicae and Herba Hyperici Erecti, separate having obtained a series of PTP1B mortifier 1,4-benzoquinone compounds and derivant thereof.Also has the patent application (200710055256.2) that suppresses PTP1B at the Chinese medicine magnolia bark preparation.But do not find as yet that so far the tea pigment of clear and definite structure in the Folium Camelliae sinensis suppresses the relevant report of PTP1B.
The inventor is to Folium Camelliae sinensis, especially systematic research has been carried out in the application of Folium camelliae assamicae in pharmacy, Chinese invention patent (number of patent application: 200810233620.4) has been applied in the application in the medicine of preparation treatment or prevent diabetes to Folium camelliae assamicae and preparation thereof on November 21st, 2008.On this basis, the inventor has done more intensive test and research to several active ingredients in the Folium Camelliae sinensis, obtains multinomial progress of making us feeling inspired.
Summary of the invention
The object of the present invention is to provide the new purposes of thearubigins, i.e. the new application of thearubigins in pharmacy.
In fact, the present invention relates to the application of thearubigins in the medicine of preparation treatment or prevention type ii diabetes.
Relate to the application of thearubigins in the medicine of preparation treatment or prevention of obesity diabetes.
Relate to the application of thearubigins in the medicine of preparation treatment or prevention of obesity disease.
Relate to the application of thearubigins in the medicine of preparation Profilin matter tyrosine phosphatase.
Purpose of the present invention is achieved by following technical proposals.
Thearubigins is a kind of polyphenol compound that Folium Camelliae sinensis forms during the fermentation, and its content is determining the quality of tea.The technical problem to be solved in the present invention is, extracts thearubigins from Folium Camelliae sinensis, is used for the treatment of type ii diabetes and obesity, or is the various preparations that feedstock production is used for the treatment of type ii diabetes and obesity with the thearubigins.
Thearubigins of the present invention is to be raw material with the Folium camelliae assamicae, extracts the natural product that obtains by method of extraction from Folium Camelliae sinensis, in the activity of external significantly Profilin matter tyrosine phosphatase 1B (PTP1B).
Thearubigins preparation of the present invention can be by being the prepared a kind of preparation that arrives of one of raw material or raw material with the thearubigins, comprises thearubigins electuary, thearubigins powder, thearubigins extractum, thearubigins pill, thearubigins oral liquid or thearubigins capsule.This thearubigins preparation can be used as treatment and food, medicine or the food of Protein Tyrosine Phosphatases 1B relevant disease and the composition of medicine in the activity of external energy Profilin matter tyrosine phosphatase 1B; And can be used as a series of and one of food, medicine or the medicine of PTP1B relevant disease and compositions of food such as treatment type ii diabetes, obesity.
The preparation method of thearubigins of the present invention, adopt following steps:
1. exsiccant Folium Camelliae sinensis: water=1:10～20 (W/V), under 100 ℃, boiled 10～30 minutes, filter with 120 mesh sieves and remove residue, collect the water extract.Repeat this step 2～4 time, merge each extracting solution.Total extracting solution is filtered with 200 mesh sieves and 0.45 μ M filter respectively, obtain the tea powder agent through high temperature spray-drying;
2. with tea powder: water=1:25 (W/V) obtains the tea powder hydrotrope;
3. the tea powder hydrotrope is added isopyknic chloroform, extract three times, keep water;
4. add isopyknic ethyl acetate to aqueous phase, extract three times, keep the ethyl acetate phase;
5. be added to equal-volume 2.5%NaHCO to ethyl acetate
3, extraction keeps water;
6. with the water evaporative removal of aqueous phase, obtain thearubigins extractum;
7. thearubigins extractum is heated to 80 ℃～150 ℃ and carries out drying, obtain thearubigins dry powder to remove remaining water.
In order to understand essence of the present invention better, will the new purposes of thearubigins in pharmaceutical field be described with corresponding pharmacological testing and result below.
Thearubigins is to the mensuration of PTP1B activity inhibition---
A. the measuring principle of inhibition
PTP1B is a kind of phosphorylase, and it can make the albumen dephosphorylation of phosphorylation.P-nitrophenyl disodic alkaliine (pNPP) can be become paranitrophenol by the PTP1B dephosphorylation, and it is yellow that color is.The variation that detects 410nm place absorbance value comes the situation of change of indirect detection enzymatic activity.The mensuration system is as follows: 25mM morpholino propane sulfonic acid (MOPS), 1mM bovine serum albumin (BSA), 1mM dithiothreitol, DTT (DTT), 0.1mM disodium EDTA (EDTA), 20mM is right-Nitrobenzol phosphoric acid (p-NPP), 5nM PTP1B at 37 ℃ of reaction 30min, adds 100 μ l 0.2M NaHCO
3Cessation reaction is at the changing value of 410nm place mensuration light absorption.
The assay method of B.PTP1B inhibition
Various materials are by measuring half-inhibition concentration (IC to the investigation of the inhibition of PTP1B
50) weigh.Constituents for suppressing is diluted by gradient, each gradient after the dilution is added as in the top said reaction system, measure 37 ℃, after the changing value of the interior light absorption of 30min, with the absorption value of each gradient with do not add being divided by of constituents for suppressing, the numerical value that draws is for suppressing percent, and when reaching 50%, the multiple of pairing dilution gradient is as IC
50
The investigation standard and the result of the test of C.PTP1B inhibition
Thearubigins is mixed with the storage liquid of 25mg/ml with distilled water.By 2 times of gradient distilled water dilutings, measure the inhibition ability of each diluted concentration to PTP1B, record IC
50, with the concentration (mg/ml) of tea formulation IC as tea formulation
50Unit.After measured, the IC of thearubigins
50Be 0.027mg/ml.
The present invention compared with prior art has following beneficial effect:
Result of the test clearly illustrates that the thearubigins that the present invention extracts proves the significantly activity of Profilin matter tyrosine phosphatase 1B through in vitro study, can be used as food, medicine or drug regimen composition with Protein Tyrosine Phosphatases 1B relevant disease; And can be used as food, medicine or the drug regimen of a series of and PTP1B relevant disease such as treatment type ii diabetes, obesity.And because the present invention extracts the natural product obtain from Folium Camelliae sinensis, human body is had no side effect, to take safe and reliablely, this point is that prior art can't realize.
Description of drawings
Fig. 1 is a process flow diagram of the present invention.
The specific embodiment:
Embodiment 1
Boiled under 100 ℃ 10～30 minutes exsiccant Folium camelliae assamicae: water=1:10～20 (W/V), filters with 120 mesh sieves and remove residue, collects the water extract.Repeat this step 2～4 time, merge each extracting solution.Total extracting solution is filtered with 200 mesh sieves and 0.45 μ M filter respectively, obtain the Folium camelliae assamicae powder through high temperature spray-drying.
Embodiment 2
(W/V) obtains the tea powder hydrotrope with Pu'er tea powder: water=1:20～30.The tea powder hydrotrope is added isopyknic chloroform, extract three times, keep water.Add isopyknic ethyl acetate to aqueous phase, extract three times, keep the ethyl acetate phase.Be added to equal-volume 2.5%NaHCO to ethyl acetate
3, extraction keeps water and ethyl acetate respectively mutually.Water evaporative removal with aqueous phase obtains thearubigins extractum.Thearubigins extractum is heated to 80-150 ℃ of dryings to remove remaining water, obtains thearubigins dry powder.
Embodiment 3
Thearubigins dry powder is mixed with the storage liquid of 25mg/ml with distilled water.By 2 times of gradient distilled water dilutings, measure the inhibition ability of each diluted concentration to PTP1B, record IC
50, with the concentration (mg/ml) of tea formulation IC as thearubigins
50Unit.After measured, the IC of thearubigins
50Be 0.027mg/ml.
It is pointed out that also that at last above what enumerate only is specific embodiments of the invention.Obviously, the invention is not restricted to above embodiment, many distortion can also be arranged.Protection scope of the present invention is all thought in all distortion that those of ordinary skill in the art can directly derive or associate from content disclosed by the invention.
Claims (6)
1. thearubigins and preparation thereof the application in the medicine of preparation treatment or prevention type ii diabetes.
2. thearubigins and preparation thereof the application in the medicine of preparation treatment or prevention of obesity diabetes.
3. thearubigins and preparation thereof the application in the medicine of preparation treatment or prevention of obesity disease.
4. thearubigins and preparation thereof the application in the medicine of preparation Profilin matter tyrosine phosphatase.
5. according to the described application of claim 1～4, wherein said thearubigins is raw material with the Folium camelliae assamicae, extracts the natural product that obtains by method of extraction from Folium Camelliae sinensis.
6. according to the described application of claim 1～4, wherein said thearubigins preparation is by being the prepared a kind of preparation that arrives of one of raw material or raw material with the thearubigins, comprises thearubigins electuary, thearubigins powder, thearubigins extractum, thearubigins pill, thearubigins oral liquid or thearubigins capsule.
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| CN200910094072A CN101518597A (en) | 2009-02-02 | 2009-02-02 | Application of thearubigins to pharmacy |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101974248A (en) * | 2010-09-10 | 2011-02-16 | 云南农业大学 | Method for separating tea pigment components |
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2009
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101974248A (en) * | 2010-09-10 | 2011-02-16 | 云南农业大学 | Method for separating tea pigment components |
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Open date: 20090902 |