CN1506106A - Sinowilsonia henryi extract and its prepn process, composition and use - Google Patents
Sinowilsonia henryi extract and its prepn process, composition and use Download PDFInfo
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Abstract
The present invention discloses Sinowilsonia henryi extract for suppressing alpha-glucosidase, its preparation process and medicine composition, and the application of the extract and the medicine composition in preparing medicine, especially in preparing medicine for treating hyperglycemia and obesity.
Description
Technical field
The present invention relates to extract the extract that can suppress alpha-glucosidase from Rhizoma Melaleuca Viridiflora, this preparation method of extract, the pharmaceutical composition that contains this extract, and this extract and the purposes of its pharmaceutical composition, the especially application of preparation treatment hyperglycemia and obesity drug as medicine.
Background technology
Show that according to the WHO interrelated data according to the 3rd of uninfection, it has become after cardiovascular and cerebrovascular disease and tumor for the prevalence of diabetes, disability rate and mortality rate and the general health extent of injury, the third-largest disease of serious threat human health.There are diabetics 1.3 hundred million people the world today, wherein suffers from type 2 diabetes mellitus more than 90%, and annual with 1% speed increase, and the year two thousand twenty of expectation will increase sharply to 2.3 hundred million.The diabetics sum of China is existing more than 6,000 ten thousand, estimates that annual morbidity rate of increase surpasses 6%.This disease is not only brought great misery to the patient, and quality of life is subjected to very big influence, even threatens people's life, returns society and brings heavy financial burden.Clinician and patient wish to have more, more effective treatment means.The oral drugs for the treatment of diabetes at present clinically have sulfonylurea, biguanides, thiazolidinediones euglycemic agent, the agent of non-sulfonylurea insulin secretion and alpha-glucosidase inhibitor etc.
Sulfonylurea has tosyl urea, chlorpropamide, glibenclamide, glipizide and gliclazide.Secondary failure easily takes place in this class medicine except the mortality of treatment first is higher, have 10% patient that treatment is not subsequently replied approximately.Adverse reaction rate is higher, as irritated, dizzy, hepatic injury, mainly is that hypoglycemia shock and weight increase, especially chlorpropamide, glibenclamide are more common, should not use this type of medicine with overweight patient.
Biguanides has metformin, phenformin.Though this type of medicine has been used for the treatment of diabetes at the end of the fifties, adverse reaction rate is very high, mainly contains significantly digestive tract side effects and lactic acid type poisonings such as gastrointestinal irritation, and its application is restricted.Particularly phenformin is because of its serious adverse effects, and a lot of countries forbid.
The thiazolidinediones medicine can directly strengthen type 2 diabetes mellitus patient's liver, muscle and the muscular tissue sensitivity to insulin, the significant feature target spot is peroxidase paraphyte activated receptor γ (PPAR γ), type 2 diabetes mellitus patient's empty stomach and post-prandial glycemia are reduced, and low density lipoprotein, LDL and very low density lipoprotein (VLDL) are reduced, hyperinsulinemia is improved, and use does not cause hypoglycemia separately.Development in recent years is very fast, and troglitazone, rosiglitazone, pioglitazone listing are successively arranged, and troglitazone is withdrawn from market owing to serious liver toxicity (liver failure).
A kind of fugitive oral insulin secernent has repaglinide and Nateglinide, mainly acts on the potassium channel of ATP-sensitivity of the β cell membrane of pancreas, promotes β emiocytosis insulin.Take when patient eats, can make the type 2 diabetes mellitus patient obtain correcting, simulation physiology insulin secretion in the relevant unusual insulin secretion pattern of feed.It is rapid-action, acts on the weak point of holding time, and secretion of insulin has stronger stimulation during only to meal, makes the patient reach the good whole glycemic control.Serious hypoglycemia incidence rate significantly is lower than sulfonylureas.It is through defecate, and Liver and kidney toxicity is little, but to beta cell failure, diabetic ketoacidosis and serious hepatorenal damage person forbidding.
In a word, biguanides, euglycemic agent and Drugs Promoting Insulin Secretion pass through the Liver and kidney metabolism in vivo, use for the unusual patient of hepatic and renal function just to be restricted.
Alpha-glucosidase inhibitor is representational 3 kinds of acarbose, Fu Gelibo sugar and miglitols.Along with Bayer acarbose (Acarbose) listing at the beginning of the nineties, be acknowledged as the new way of treatment diabetes at home and abroad, its main action target spot is not subjected to the influence of hepatic and renal function at small intestinal, and the scope of application is wider.Thereby acarbose become a line medicine of treatment diabetes, and further enlarges indication.Therefore, it is very necessary researching and developing new alpha-glucosidase inhibitor, and significant.
Rhizoma Melaleuca Viridiflora, Latin is called suregade glomerulata (BL.), belongs to the Euphorbiaceae Suregada.Arbor, high 2-13 rice; Sprig band grey black or brown.The blade keratin, wide or long and narrow ellipse, or how many obovate or the lanceolar that falls, long 5-12 centimetre, wide 3-6 centimetre, full edge, the top is anxious sharp blunt or round, and rare notch, base portion are gradually narrow, and middle arteries and veins is in the two sides projection, the every limit of lateral vein 5-10 bar; Stipule is near the wide triangle of inflorescence, and is thicker, is about 1 millimeter, and wide 2 millimeters, the top is blunt, and the stipule of bottom is caducous; The long 3-8 millimeter of petiole (Hainan flora, Chen Huanyong chief editor second volume, front page nineteen sixty-five, PP177).About the chemical constituent and the pharmacological action of Rhizoma Melaleuca Viridiflora there is no report.
Summary of the invention
The present invention the object of the present invention is to provide a kind of extract that extracts in order to overcome the deficiencies in the prior art from Rhizoma Melaleuca Viridiflora.
Another object of the present invention is to provide a kind of method for preparing this extract.
Another purpose of the present invention is to provide a kind of pharmaceutical composition, comprises as carrier commonly used in the Rhizoma Melaleuca Viridiflora extract of the present invention of active component and the pharmaceutical field.
Another purpose of the present invention is to provide a kind of Rhizoma Melaleuca Viridiflora and/or extract, or contains the application of compositions in the preparation alpha-glucosidase inhibitor of Rhizoma Melaleuca Viridiflora and/or extract.
A further object of the present invention is to provide a kind of Rhizoma Melaleuca Viridiflora and/or extract, or contains the application of compositions in preparation treatment hyperglycemia and obesity drug of Rhizoma Melaleuca Viridiflora and/or extract.
In order to finish the object of the invention, the present invention takes following technical scheme:
Rhizoma Melaleuca Viridiflora crude drug drying and suitable pulverizing in order to the contact area of increase with solvent, are raised the efficiency.
The extraction solvent of crude drug makes the mixture of water, alcohols or water and alcohols.Preferred alcohols comprises methanol, ethanol, isopropyl alcohol, butanols etc.The mixture of water and alcohols for example contains the water of pure 40-80% (volume ratio).During extraction quantity of solvent be former medicine weight 4-14 doubly.Extraction can be static or down dynamic, preferably under dynamic condition.In order to improve the efficient of extraction, can use ultrasound wave etc.The temperature of extracting be from room temperature (for example 20 ℃) to the scope of solvent refluxing temperature in, preferably under the temperature of backflow.Extraction can be carried out continuously or intermittently, can repeat 1-4 time during intermittent extraction.
Behind the last EOS, merging filtrate, elimination medicinal residues.Filtrate is cooled off when normal pressure or decompression heating are concentrated into doubly volume of medical material weight 1-5 under dynamical state.If with water extraction then add alcohol and make its alcohol that contains reach the concentration of 40-80% (volume ratio), the alcohol of use comprises methanol, ethanol, isopropyl alcohol, butanols etc., or its mixture; Ethanol preferably.Staticly settle, filter or the centrifugal insoluble matter of removing, insoluble matter washes with water, general 1-3 time.Filtrate merging further is condensed into paste.
Paste carries out purification, by macroporous resin, ion exchange resin or adsorpting column chromatography, and the effective site that chromatography obtains.Preferred ion exchange resin is a cationic resin, can comprise-SO3
-H
+,-COO
-H
+Preferred sulfonic resin in the cationic resin.Cross-linkage of resin 2-20%, preferred 2-6%.Adsorpting column chromatography comprises silica gel, aluminium oxide, cellulose, polyamide.The consumption of adsorbent is 30-200 a times of sample size, and preferred 80-100 times, more preferably 90-100 doubly.Elution system can be sieved with thin layer chromatography, selects to make the solvent system of the Rf value of separated component at 0.2-0.3.Add suitable alkali in the eluant, for example ammonia, diethylamine, pyridine, 2-picoline, trimethylpyridine, N-ethylmorpholine are in case the anti-avulsion tail, promote to separate.Activated carbon can be admixed an amount of kieselguhr and make diluent, to increase the flow velocity of solution.
Extracting solution also can be directly with exchange column and membrane technology make with extra care concentrate after, become extractum or dry powder again.Operable exchange column comprises macroporous resin, ion exchange resin, active carbon, polydextran gel etc.; Preferred macroporous resin and active carbon.
Extract can become dry powder through lyophilization or vacuum drying, also can directly be spray dried to dry powder to concentrated liquid and carry out various preparations shapings.
The invention still further relates to and contain as the extract of the present invention of active ingredient and the pharmaceutical composition of conventional medicine excipient or adjuvant.Usually pharmaceutical composition of the present invention contains the extract of the present invention of 0.1-95% weight.
The present invention also provides a kind of pharmaceutical composition, and it comprises medicine effective dose, as the Rhizoma Melaleuca Viridiflora extract and/or the Rhizoma Melaleuca Viridiflora and the pharmaceutically acceptable carrier that extract as the inventive method of active component.
The pharmaceutical composition of extract of the present invention can be according to method preparation well known in the art.When being used for this purpose, if desired, extract of the present invention and one or more solids or liquid medicine excipient and/or adjuvant can be combined, make and can be used as suitable administration form or the dosage form that people's medicine or veterinary drug use.
Extract of the present invention or contain its pharmaceutical composition can the unit dosage form administration, route of administration can be intestinal or non-intestinal, as oral, muscle, subcutaneous, nasal cavity, oral mucosa, skin, peritoneum or rectum etc., preferably overcomes administration.
Extract of the present invention or the route of administration that contains its pharmaceutical composition can be drug administration by injection.Injection comprises intravenous injection, intramuscular injection, subcutaneous injection, intradermal injection etc.
Form of administration can be liquid dosage form, solid dosage forms.As liquid dosage form can be true solution class, colloidal type, particulate formulations, emulsion dosage form, mixed suspension form.Other dosage forms are tablet, capsule, drop pill, aerosol, pill, powder, solution, suspensoid, Emulsion, granule, suppository, lyophilized injectable powder etc. for example.
Extract of the present invention can be made ordinary preparation, also can be slow releasing preparation, controlled release preparation, targeting preparation and various particulate delivery system.
For the unit form of administration is made tablet, can be extensive use of various carrier well known in the art.Example about carrier is, for example diluent and absorbent are as starch, dextrin, calcium sulfate, lactose, mannitol, sucrose, sodium chloride, glucose, carbamide, calcium carbonate, kaolin, microcrystalline Cellulose, aluminium silicate etc.; Wetting agent and binding agent are as water, glycerol, Polyethylene Glycol, ethanol, propanol, starch slurry, dextrin, syrup, Mel, glucose solution, mucialga of arabic gummy, gelatine size, sodium carboxymethyl cellulose, lac, methylcellulose, potassium phosphate, polyvinylpyrrolidone etc.; Disintegrating agent, for example dry starch, alginate, agar powder, laminaran, sodium bicarbonate and citric acid, calcium carbonate, polyoxyethylene sorbitol fatty acid ester, dodecyl sodium sulfate, methylcellulose, ethyl cellulose etc.; Disintegrate inhibitor, for example sucrose, glyceryl tristearate, cocoa butter, hydrogenation wet goods; Absorption enhancer, for example quaternary ammonium salt, sodium lauryl sulphate etc.; Lubricant, for example Pulvis Talci, silicon dioxide, corn starch, stearate, boric acid, liquid paraffin, Polyethylene Glycol etc.Tablet further can also be made coated tablet, for example sugar coated tablet, thin membrane coated tablet, ECT, or double-layer tablet and multilayer tablet.
For example, can be extensive use of various carrier well known in the art for pill is made in the administration unit.Example about carrier is, for example diluent and absorbent are as glucose, lactose, starch, cocoa butter, hydrogenated vegetable oil, polyvinylpyrrolidone, Gelucire, Kaolin, Pulvis Talci etc.; Binding agent is as arabic gum, Tragacanth, gelatin, ethanol, Mel, liquid sugar, rice paste or batter etc.; Disintegrating agent is as agar powder, dry starch, alginate, dodecyl sodium sulfate, methylcellulose, ethyl cellulose etc.
For example for capsule is made in the administration unit, effective ingredient extract of the present invention is mixed with above-mentioned various carriers, and the mixture that will obtain thus places hard gelatine capsule or soft capsule.Also effective ingredient extract of the present invention can be made microcapsule, be suspended in and form suspensoid in the aqueous medium, in the hard capsule of also can packing into or make injection and use.
For example, extract of the present invention is made injection preparation, as solution, suspensoid solution, Emulsion, lyophilized injectable powder, this preparation can be moisture or non-water, can contain acceptable carrier, diluent, binding agent, lubricant, antiseptic, surfactant or dispersant on a kind of and/or multiple pharmacodynamics.Can be selected from water, ethanol, Polyethylene Glycol, 1 as diluent, the isooctadecanol of ammediol, ethoxylation, the isooctadecanol of polyoxyization, Polyoxyethylene Sorbitol Fatty Acid Esters etc.In addition, ooze injection, can in injection preparation, add proper amount of sodium chloride, glucose or glycerol, in addition, can also add conventional cosolvent, buffer agent, pH regulator agent etc. in order to prepare etc.These adjuvants are that this area is commonly used
In addition, as needs, also can in pharmaceutical preparation, add coloring agent, antiseptic, spice, correctives, sweeting agent or other material.
For reaching the medication purpose, strengthen therapeutic effect, medicine of the present invention or pharmaceutical composition can be with any known medication administrations.
The dosage of extract pharmaceutical composition of the present invention depends on many factors, for example to prevent or treat the character and the order of severity of disease, the sex of patient or animal, age, body weight, personality and individual reaction, route of administration, administration number of times, therapeutic purposes, therefore therapeutic dose of the present invention can have large-scale variation.In general, the using dosage of Chinese materia medica composition of the present invention is well known to a person skilled in the art.The actual drug quantity that can be according to the present invention be contained in the last preparation in the extractive composition, in addition suitable adjustment to reach the requirement of its treatment effective dose, is finished prevention of the present invention or therapeutic purposes.The consumption of the suitable dose scope extract of the present invention of the every day of extract of the present invention is the 0.001-100mg/Kg body weight, is preferably the 0.1-60mg/Kg body weight, and more preferably the 1-30mg/Kg body weight most preferably is the 2-15mg/Kg body weight.Above-mentioned dosage can the single dose form or be divided into several, for example two, three or four dosage form administrations this be subject to administration doctor's clinical experience and comprise the dosage regimen of using other treatment means.Each treats that required accumulated dose can be divided into repeatedly or by the dose administration.Extract of the present invention or compositions can be taken separately, or merge use and adjust dosage with other treatment medicine or symptomatic drugs.
Alpha-glucosidase can make carbohydrate breakdown become the absorbent monosaccharide of small intestinal.Test of many times result shows, extract of the present invention to the IC50 of enzymatic activity in 5 μ g-10 μ g/ml crude drug scopes.Illustrate that this extract has very strong α glucoside enzyme inhibition.In the experiment to blood sugar increasing behind the normal mouse glucose load, single blank group of giving glucose (2.0g/kg), glucose and Acarbose (BAITANGPING, 10mg/kg) the extract of the present invention of positive control drug group and glucose and various dose (35mg/kg, 70mg/kg, 140mg/kg) experimental group is at the blood glucose value zero difference of different time points.Further specifying this medicine treatment diabetes action target spot is to suppress the α glucosidase activity.
The mice starch-bearing result of extract of the present invention shows, extract of the present invention can obviously suppress the rising of blood glucose behind the normal mouse starch-bearing under 35mg/kg, 70mg/kg, 140mg/kg dosage, move after the glycemic peaks, area reduces under the blood glucose curve, and presents certain dose-effect relationship.Extract mice sucrose load experimental result of the present invention shows, under 10mg/kg, 20mg/kg, 40mg/kg dosage, obviously suppress the rising of normal mouse sucrose load back blood glucose, move after the glycemic peaks, area reduces under the blood glucose curve, and presents dose-effect relationship preferably.
Pharmacological evaluation shows that extract of the present invention is an alpha-glucosidase inhibitor, can in small intestinal, combine with enzyme with carbohydrate is emulative, alpha-glucosidase hydrolytic enzyme in the nearly chamber epithelial cell of reversible inhibition mucous membrane of small intestine brush border, saccharides 1 such as blocking-up starch, sucrose, the cracking of 4-glycosidic bond reaches the effect of digesting and assimilating that delays carbohydrate.By delaying the digest and decompose process of carbohydrate, thereby reduce glucose absorption, reduce level of postprandial blood sugar, the amplitude that post-prandial glycemia is raise descends.
With the carbohydrate is China of staple food, and what this sugar absorbed delays, and the reduction of blood glucose, and then the sugared conversion to fat of influence reduce fat accumulation in vivo, the performance antiobesity action, and therefore, extract of the present invention also can be used as appetrol.
Description of drawings
Fig. 1. to the influence of blood glucose curve behind the normal mouse starch-bearing.
Fig. 2. to the influence of normal mouse sucrose load back blood glucose curve.
The specific embodiment
Extract experiment
Embodiment 1. water are carried extract
Rhizoma Melaleuca Viridiflora branch and leaf 100g with distilled water 500g hot reflux, extracts three times in (500g water/time), extracts one hour at every turn, must water extract 15.5g behind the extracting solution concentrating under reduced pressure.Extract 15.5g is dissolved in the 100ml water dissolution, adds ethanol to containing alcohol 70% (volume ratio), precipitation, filtration, concentrated filtrate to do yellow paste 13.6g.
Filtrate is partly gone up macroporous resin column and is separated:
Filtrate part 13.6g 50ml water dissolution is added on the 100g macroporous resin column (D-101), and it is colourless to be washed till effluent with distilled water, and the distilled water eluent is concentrated into dried 11g eluate.
Reuse ethanol elution macroporous resin is colourless to effluent, and the ethanol elution partial concentration gets 2.2g.Macroporous resin is washed to effluent does not have alcohol (macroporous resin regeneration).
Macroporous resin eluting partial cation resin column separates:
11g macroporous resin eluting is partly used the 50ml water dissolution, last 100g sulfonic acid cation resin post (003*7 styrene-2VB), and elder generation is washed till colourless with distilled water, be eluted to the inanimate object alkali reaction with the 0.5N aqua ammonia then.0.5N aqua ammonia eluent concentrating under reduced pressure gets total alkali eluate 2.4g.
Embodiment 2. water are carried extract
1 kilogram in Rhizoma Melaleuca Viridiflora branch with distilled water 14 kilograms of heating and refluxing extraction, extracts three times (14 kg of water/time), extracts one hour at every turn, must water extract 155g behind the extracting solution concentrating under reduced pressure.Extract 155g is dissolved in the 1550ml water dissolution, adds ethanol to containing alcohol 70% (volume ratio), precipitation, filtration, concentrated filtrate to do yellow paste 136g.
Filtrate is partly gone up macroporous resin column and is separated:
Filtrate part 136g 500ml water dissolution is added on the 1000g macroporous resin column (D-101), and it is colourless to be washed till effluent with distilled water, and the distilled water eluent is concentrated into dried 110g eluate.
Reuse ethanol elution macroporous resin is colourless to effluent, and the ethanol elution partial concentration gets 22g.Macroporous resin is washed to effluent does not have alcohol (macroporous resin regeneration).
Macroporous resin eluting part activated carbon column chromatography separates:
Get macroporous resin column water elution liquid part 15g water dissolution, go up 80 gram activated-charcoal columns (GH-2 type) and go up chromatography, the water eluting is collected 1,2,3-indantrione monohydrate alkaloid reactive moieties, this eluent of concentrating under reduced pressure to do the 3.8g eluate.
Embodiment 3. alcohol extraction extracts
1 kilogram on Rhizoma Melaleuca Viridiflora bark adds 6 times of amount 70% (volume ratio) ethanol, and soaked overnight or 4 hours slowly are heated to boiling, reflux filtration 1 hour; Overall process repeats secondary, merging filtrate, concentrating under reduced pressure, temperature 60-70 ℃, pressure 85-98KPa is concentrated into when not having ethanol fully, adds 1 kg of water and continues to be heated to boiling, the centrifugal insoluble matter of removing in cooling back, and add a small amount of washing insoluble matter three times, filtrate is merged concentrating under reduced pressure under temperature 60-70C, drying under reduced pressure (temperature 70-80 ℃, pressure 85-98Kpa) gets extract 106g then.
Pharmacological evaluation
The inhibitory action of 1 pair of α glucosidase activity of experimental example
The normal rat sacrificed by decapitation is got epimere jejunum mucosa, and after buffer homogenate, the high speed frozen centrifugation extracts the α glucosidase, and-20 ℃ of preservations are standby; Embodiment 1 extract with the preparation of the phosphate buffer of pH6.0 and be diluted to variable concentrations (as 10mg, 1mg, 0.1mg, 0.01mg, the 0.001mg/m1 crude drug), be substrate with sucrose, mensuration is to the inhibition percentage rate of sucrase active, according to suppressing the IC of percentage rate calculating to enzymatic activity
50Test of many times result shows that this extract is to the IC of enzymatic activity
50In 5 μ g-10 μ g/ml crude drug scopes.Illustrate that this extract has very strong α glucoside enzyme inhibition.
The influence of blood sugar increasing behind 2 pairs of normal mouse glucose loads of experimental example
Normal ICR male mice, be divided into 5 groups (n=10) at random, overnight fasting before the experiment, irritating stomach with glucose (2.0g/kg) for one group organizes in contrast, one group with glucose and Acarbose (BAITANGPING 10mg/kg) is irritated stomach as the positive control drug group, and all the other groups are respectively with extract (35mg/kg, 70mg/kg, 140mg/kg) the filling stomach of glucose and various dose, the determination of glucose oxidase blood sugar concentration is used in 30min, 60min, 120min blood sampling before irritating stomach and behind the filling stomach.Result (unlisted) shows that each dosed administration group and positive control drug Acarbose group compare zero difference at the blood glucose value of different time points with matched group.Further specifying this medicine treatment diabetes action target spot is to suppress the α glucosidase activity.
The inhibitory action of blood sugar increasing behind 3 pairs of normal mouse starch-bearings of experimental example
Normal ICR male mice, be divided into 5 groups (n=10) at random, overnight fasting before the experiment, irritating stomach with starch (3.0g/kg) for one group organizes in contrast, one group with starch and Acarbose (acarbose 10mg/kg) is irritated stomach as the positive control drug group, and all the other groups are irritated stomach with the starch (3.0g/kg) and the extract (35mg/kg, 70mg/kg, 140mg/kg) of various dose respectively, the determination of glucose oxidase blood sugar concentration is used in 30min, 60min, 120min blood sampling before irritating stomach and behind the filling stomach.Experimental result is seen Fig. 1 and table 1.
The influence of blood glucose area under curve behind the table 1. pair normal mouse starch-bearing
Group dosage (mg/kg) AUC (mg/dl.hr)
Matched group-435.1 ± 63.2
AUC is an area under curve; Compare * * * P＜0.001 with matched group
Presentation of results, extract can obviously suppress the rising of blood glucose behind the normal mouse starch-bearing under 35mg/kg, 70mg/kg, 140mg/kg dosage, move after the glycemic peaks, and area reduces under the blood glucose curve, and presents certain dose-effect relationship.
The inhibitory action of 4 pairs of normal mouse sucrose loads of experimental example back blood sugar increasing
Normal ICR male mice, be divided into 5 groups (n=10) at random, overnight fasting before the experiment, irritating stomach with sucrose (4.0g/kg) for one group organizes in contrast, irritate stomach as the positive control drug group with sucrose and Acarbose (10mg/kg) for one group, all the other groups are irritated stomach with the extract (10mg/kg, 20mg/kg, 40mg/kg) of sucrose and various dose respectively, and 30min, 60min, 120min measure blood sugar concentration before irritating stomach and behind the filling stomach.Experimental result is seen Fig. 2 and table 2.
The influence of table 2. pair normal mouse sucrose load back blood glucose area under curve
Group dosage (mg/kg) AUC (mg/dl/hr)
Matched group-362.7 ± 45.7
AUC is an area under curve; Compare * * * P＜0.001 with matched group
The result shows that extract obviously suppresses the rising of normal mouse sucrose load back blood glucose under 10mg/kg, 20mg/kg, 40mg/kg dosage, move after the glycemic peaks, and area reduces under the blood glucose curve, and presents dose-effect relationship preferably.
Above-mentioned 4 pharmacological evaluation show, the Rhizoma Melaleuca Viridiflora extract specific inhibition α glucosidase of energy also has very strong activity, move after making animal polysaccharide and disaccharidase load back blood glucose rise and peak reduce also, area reduces under the blood glucose curve, be of value to the improvement of diabetic sugar metabolism, lipid metabolic disorder, can be used for the treatment of diabetes and impaired glucose tolerance.
Claims (18)
1, the application of Rhizoma Melaleuca Viridiflora (suregade glomerulata (BL.)) in the preparation alpha-glucosidase inhibitor.
2, the application of Rhizoma Melaleuca Viridiflora (suregade glomerulata (BL.)) in the preparation hypoglycemic medicine.
3, the application of Rhizoma Melaleuca Viridiflora (suregade glomerulata (BL.)) in the preparation slimming medicine.
4, the extracting method of a kind of plant Rhizoma Melaleuca Viridiflora (suregade glomerulata (BL.)) extract is characterized in that, crude drug Rhizoma Melaleuca Viridiflora (suregade glomerulata (BL.)) is used solvent extraction, and merge extractive liquid, concentrates, and carries out purification again.
5, extracting method according to claim 4 is characterized in that, described solvent is selected from the mixture of water, alcohols or water and alcohols.
6, extracting method according to claim 4, it is characterized in that, when using water extraction, when being concentrated into medical material weight 1-5 times volume, add alcohol, make its alcohol that contains reach the concentration of 40-80% (volume ratio) and staticly settle, filter or the centrifugal insoluble matter of removing, filtrate merging further is condensed into paste.
7, extracting method according to claim 5 is characterized in that, described alcohol is methanol, ethanol, isopropyl alcohol, butanols or its mixture.
8, extracting method according to claim 4 is characterized in that, described being extracted as in temperature carried out for the scope from 20 ℃ to the solvent refluxing temperature.
9, extracting method according to claim 4 is characterized in that, purification is by macroporous resin, ion exchange resin or adsorpting column chromatography.
10, extracting method according to claim 4 is characterized in that, the eluant during purification is water or ammonia.
11, extracting method according to claim 9 is characterized in that, ion exchange resin is a cationic resin.
12, extracting method according to claim 11 is characterized in that, cationic resin is a sulfonic resin.
13, extracting method according to claim 9 is characterized in that, described adsorpting column chromatography comprises silica gel, aluminium oxide, cellulose, polyamide, activated carbon.
14, a kind of Rhizoma Melaleuca Viridiflora (suregadeglomerulata (BL.)) extract of method extraction as claimed in claim 4.
15, a kind of pharmaceutical composition is characterized in that, comprises medicine effective dose, the Rhizoma Melaleuca Viridiflora extract and/or Rhizoma Melaleuca Viridiflora and the pharmaceutically acceptable carrier that extract as the method as claimed in claim 4 of active component.
16, the application of Rhizoma Melaleuca Viridiflora (suregade glomerulata (the BL.)) extract of method extraction as claimed in claim 4 in the preparation alpha-glucosidase inhibitor.
17, the application of Rhizoma Melaleuca Viridiflora (suregade glomerulata (the BL.)) extract of method extraction as claimed in claim 4 in the preparation hypoglycemic medicine.
18, the application of Rhizoma Melaleuca Viridiflora (suregade glomerulata (the BL.)) extract of method extraction as claimed in claim 4 in the preparation slimming medicine.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102462726A (en) * | 2010-11-04 | 2012-05-23 | 中国医学科学院药物研究所 | Extraction, separation and application of suregada glomerulate total alkaloid and polyhydroxy alkaloid compounds |
| CN111647095A (en) * | 2020-06-30 | 2020-09-11 | 华润三九医药股份有限公司 | Polysaccharide of fraxinus chinensis, preparation method and application thereof |
-
2002
- 2002-12-05 CN CN 02155523 patent/CN1283271C/en not_active Expired - Lifetime
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102462726A (en) * | 2010-11-04 | 2012-05-23 | 中国医学科学院药物研究所 | Extraction, separation and application of suregada glomerulate total alkaloid and polyhydroxy alkaloid compounds |
| CN102462726B (en) * | 2010-11-04 | 2016-03-09 | 中国医学科学院药物研究所 | The extracting and developing of Rhizoma Melaleuca Viridiflora total alkaloids and polyhydroxylated alkaloid compound and purposes |
| CN111647095A (en) * | 2020-06-30 | 2020-09-11 | 华润三九医药股份有限公司 | Polysaccharide of fraxinus chinensis, preparation method and application thereof |
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