CN1965873B - Chinese medicinal extract having blood sugar-lowering activity, its preparation process, composition and use - Google Patents
Chinese medicinal extract having blood sugar-lowering activity, its preparation process, composition and use Download PDFInfo
- Publication number
- CN1965873B CN1965873B CN2006100920381A CN200610092038A CN1965873B CN 1965873 B CN1965873 B CN 1965873B CN 2006100920381 A CN2006100920381 A CN 2006100920381A CN 200610092038 A CN200610092038 A CN 200610092038A CN 1965873 B CN1965873 B CN 1965873B
- Authority
- CN
- China
- Prior art keywords
- extract
- balanophora
- plant
- glucose
- balaenoptera borealis
- 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.)
- Expired - Fee Related
Links
Images
Landscapes
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a hypoglycemic extract from a Balanophora L, a preparation method thereof, a drug combination containing the Balanophora L or the extract thereof, as well as use as drugs and health products of the Balanophora L or the extract thereof and the drug combination, especially the use for preparing drugs and health products which treat and prevent metabolic diseases relevant to the diabetes and complication thereof or the like.
Description
Technical field
The present invention relates to from Balanophora plant (Balanophora L) extraction can hypoglycemic extract, this preparation method of extract, contain the maybe pharmaceutical composition of this genus extract of Balanophora plant (Balanophora L), and Balanophora plant (Balanophora L) maybe should belong to extract and its pharmaceutical composition purposes as medicine, was particularly useful for preparing the medicine and the health product of the treatment metabolic disease relevant with prevent diabetes and complication thereof etc.
Background technology
Show that according to the WHO interrelated data prevalence of diabetes, disability rate and mortality rate and the general health extent of injury be the 3rd of row noninfectious, it has become after cardiovascular and cerebrovascular disease and tumor, the third-largest disease of serious threat human health.There are diabetics 1.3 hundred million people the world today, type 2 diabetes mellitus patient not more than 90% wherein, and also annual with 1% speed increase, expecting the year two thousand twenty 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 patient'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 be that hypoglycemia shock and weight increase, especially chlorpropamide, glibenclamide are more common, so the patient of overweight should not use this type of medicine.
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.Thing is not a phenformin because its serious adverse effects, and a lot of countries forbid.
The representative drugs that medicament of insulin sensitizer has gone on the market has thiazolidinediones medicines such as rosiglitazone.The thiazolidinediones medicine can directly strengthen type 2 diabetes mellitus patient's liver, muscle and the fatty 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 do not cause hypoglycemia.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 relevant unusual insulin secretion pattern of taking food obtain correcting simulation physiology insulin secretion.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.
The medicine that alpha-glucosidase inhibitor class medicine has gone on the market has 3 kinds of acarbose, Fu Gelibo sugar and miglitols.Along with Bayer acarbose (Acatbose) 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 at small intestinal, thereby acarbose become a line medicine of treatment diabetes, and further enlarges indication.
In Balanophoraceae (Balanophoraceae) the Balanophora plant (Balanophora L), medicinal crude drug is a Herba balanophorae japonicae (Balaenoptera borealis Lesson, Balanophora japonica Mak.), Balanophora involicrata Hook.f. (Balanophora inovolucrata Hook f.) and Herba Balanophorae polyandrae (Balanophorapolyandra Griff.).
Herba balanophorae japonicae (Balaenoptera borealis Lesson, Balanophora japonica Mak.), Balanophora involicrata Hook.f. (Balanophora inovolucrata Hook f.) and Herba Balanophorae polyandrae (Balanophorapolyandra Griff.) all are perennial parasitics meat herbaceous plant.Root stock is grown in underground, and is spherical in shape, and the surface has tubercle prominent.Scape is red or yellow, gives birth to loose spadix on it.Flower unisexuality, hermaphroditism or different strain, bloom August, is the different preface of male and female (inflorescence unisexuality) plant, and block rhizome is a plurality of to bunch up.All no chlorophylls.Stem is slim and frahile, and leaf is alternately to life or closely to life.One bract is arranged under the staminate inflorescence ellipse, male flower, and bract merges each other and forms many hexagonal potholes that are, and bears the male flower of tool stalk, tapel 3 radixes from the base portion of pothole.Female inflorescence is subsphaeroidal or oval, little clava inverted cone, and tip cuts shape, and long is wide 3～4 times; Female flower only give birth on the inflorescence main shaft.9-10 month result.The male flower of Balanophora involicrata Hook.f. has handle, and there is foliate tube sheath bag quilt at the scape middle part; And the male flower stockless of Balaenoptera borealis Lesson, the middle part of scape does not have a sheath.Be grown in the hillside sylvan life of height above sea level 1000--2500 rice, colonize on the root of xylophyta.
This medical instrument has hemostasis, granulation promoting, analgesic effect.Among the peoplely be usually used in treating stomachache, epistaxis, woman month through haemophilia, dysentery and traumatic hemorrhage etc.Also can be used as tonic.Decoction can be separated drunk, and the levigation accent is controlled rectum with the Oleum Sesami external and deviate from.
The pharmacological action of Balanophora plant (Balanophora L) has been reported have anti-inflammatory and antalgic and deinebriating effect [1, Ruan Hanli, Chinese medicine academic periodical, 2003,21 (6): 910-911] [2, Rong Juquan, China's national folk medical magazine, 2003,65 (always): 347-349].
Obtaining chemical compound in the chemical constitution study of Balanophora plant (Balanophora L) has: β-XIANGSHU ester (the plain A of Balaenoptera borealis Lesson); palmityl lupene alcohol ester (the plain B of Balaenoptera borealis Lesson); acetic acid β-XIANGSHU ester; acetic acid lupene alcohol ester; β-amyrenone; lupenone and Palmic acid; (-)-lariciresinol; (-)-(+)-Pinoresinol [(-)-pinoresinol]; 1-O-coffee acyl-β-D-glucopyanosyl; 1-O-coffee acyl-(6-O-galloyl)-β-D-glucopyanosyl; 1-O-coffee acyl-(4-O-galloyl)-β-D-glucopyanosyl; gallic acid clerodolone clerodolone-3-O-(6-O-palmityl)-β-D-glucopyranoside; coniferin; methyl coniferin [3; Shen Xiaoling; Chinese herbal medicine; 1996; 27 (5): 259-260] [4; in the Xiaxin; Chinese herbal medicine; 2001; 32 (1:6-9)] [5; Liu Xikui; Yunnan plant research; 1998,20 (3): 369-373].
Summary of the invention
The object of the invention is to provide the extract that extracts from Balanophora plant (Balanophora L).
Another object of the present invention is to provide the method for this extract of preparation.
Another purpose of the present invention is to provide pharmaceutical composition, comprises carrier commonly used in Balanophora plant (Balanophora L), Balanophora plant (Balanophora L) extract and the pharmaceutical field.
Another purpose of the present invention is to provide Balanophora plant (Balanophora L) and/or Balanophora plant (Balanophora L) extract, or contains the application of compositions in preparation treatment and prevent diabetes and complication medicine thereof of Balanophora plant (BalanophoraL) and/or Balanophora plant (Balanophora L) extract.
Another purpose of the present invention is to provide Balanophora plant (Balanophora L) and/or Balanophora plant (Balanophora L) extract, or contains the application of compositions in preparation treatment and prevent diabetes and complication health product thereof of Balanophora plant (BalanophoraL) and/or extract.
Another purpose of the present invention is to provide Balanophora plant (Balanophora L) and/or Balanophora plant (Balanophora L) extract, or contains the application of compositions in preparation treatment and prevent diabetes correlated metabolism diseases medicine of Balanophora plant (BalanophoraL) and/or Balanophora plant (Balanophora L) extract.
Another purpose of the present invention is to provide Balanophora plant (Balanophora L) and/or Balanophora plant (Balanophora L) extract, or contains the application of compositions in preparation treatment and prevent diabetes correlated metabolism diseases health product of Balanophora plant (BalanophoraL) and/or Balanophora plant (Balanophora L) extract.
In order to finish the object of the invention, the present invention takes following technical scheme:
Balanophora plant (Balanophora L) crude drug drying and suitable pulverizing to increase the contact area of medical material and 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 alcohol compound 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.
After above-mentioned steps finishes, merging filtrate, filtrate is cooled off when normal pressure or decompression heating are concentrated into doubly volume of medical material weight 1-5 under dynamical state.The extraction solvent that uses is that alcohol compound 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.
The gained paste is carried out purification, and extracting method according to claim 8 is characterized in that, purification be by, solvent extraction, gel filtration, polyamide, macroporous resin, ion exchange resin or adsorpting column chromatography.The effective site that obtains.
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, refabrication becomes extractum or dry powder.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, 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 active component
As the inventive method Balanophora plant (Balanophora L) and/or Balanophora plant (Balanophora L) extract and pharmaceutically acceptable carrier.
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, nasal cavity, oral mucosa, skin, peritoneum or rectally etc., preferred oral administration.
Extract of the present invention or contain the route of administration of its pharmaceutical composition comprises drug administration by injection equally.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, hydrocarbon sodium and citric acid, calcium carbonate, polyoxyethylene sorbitol fatty acid ester, dodecyl sodium sulfate 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, as arabic gum, Tragacanth, gelatin, ethanol, 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, hydrocarbon sodium 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, 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 etc.Disintegrating agent is as agar powder, dry starch, alginate, dodecyl sodium sulfate, methylcellulose etc.For example for capsule is made in the administration unit, effective ingredient the present invention is carried thing mix, and the mixture that will obtain thus places hard gelatine capsule or soft capsule with above-mentioned various carriers.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 and hit liquid, can in injection preparation, add proper amount of sodium chloride, glucose or glycerol, in addition, can also add conventional cosolvent, buffer agent, PH regulator 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 0.001-100g/Kg body weight, is preferably the 0.01-50g/Kg body weight, most preferably is the 0.05-25g/Kg body weight.Above-mentioned dosage can the single dose form or is divided into severally, and for example the administration of two, three or four dosage modes is subject to administration doctor's clinical experience and comprises 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.
Description of drawings
Fig. 1. Balaenoptera borealis Lesson extract to the oral starch-bearing of normal mouse after the inhibitory action of blood sugar increasing
Fig. 2. Balaenoptera borealis Lesson extract is to the inhibitory action of the oral sucrose load of normal mouse back blood sugar increasing
Fig. 3. Balaenoptera borealis Lesson extract to the normal mouse glucose load after the influence of blood sugar increasing
Fig. 4. Balaenoptera borealis Lesson extract is to the influence of the plain tolerance of normal mouse islets
The specific embodiment
The concrete demonstration of following embodiment application of the present invention.But present embodiment does not limit the scope of application of the present invention.
Extract experiment
Embodiment 1. water are carried extract
Herba balanophorae japonicae (Balaenoptera borealis Lesson, Balanophora japonica Mak.) herb 100g with distilled water 500g hot reflux, extracts three times in (500ml water/time), the each extraction 1 hour, get water extract 26.0g behind the extracting solution concentrating under reduced pressure, be dissolved in the 50ml water, add ethanol and measure 70% (volume ratio) to containing alcohol, precipitation, filter, concentrated filtrate gets yellow powder shape solid 14.0g to doing.
The filtrate part is separated through macroporous resin column:
Filtrate part 14.0g uses the 50ml water dissolution, is added on the 100g macroporous resin column (S-8), and it is colourless to be washed till effluent with distilled water, and the reuse ethanol elution is colourless to effluent, and the ethanol elution partial concentration gets 7.5g.Macroporous resin is washed to effluent does not have alcohol (macroporous resin regeneration).
Embodiment 2. alcohol extraction extracts
Balanophora involicrata Hook.f. (Balanophora inovolucrata Hook f.) herb 2500g, use the 95%EtOH hot reflux, extract three times (10L 95%EtOH/ time), slowly be heated to boiling, the each extraction 1 hour, get 95%EtOH extract 532.0g behind the extracting solution concentrating under reduced pressure, be suspended in the 1500ml water, filter, filtrate adds ethyl acetate extraction three times (1500ml/ time), combining extraction liquid, decompression and solvent recovery gets yellow toner powder solid 210.0g.
Embodiment 3. ethyl acetate are carried extract
Herba Balanophorae polyandrae (Balanophora polyandra Griff.) herb 1000g uses petroleum ether 5000ml, is heated to backflow, extracts three times, extracts 1 hour at every turn, gets ligroin extraction 56.0g behind the extracting solution concentrating under reduced pressure; Use ethyl acetate 5000ml then, be heated to backflow, extract three times, extracted one hour at every turn, extracting solution merges, and decompression and solvent recovery gets ethyl acetate extraction position 173.0g.
Separate through macroporous resin at the ethyl acetate extraction position:
Filtrate part 173.0g uses the 1000ml water dissolution, filters, and filtrate is added on the 1000g macroporous resin column (S-8), and it is colourless to be washed till effluent with distilled water, and the reuse ethanol elution is colourless to effluent, and the ethanol elution partial concentration gets 113.0g.Macroporous resin is washed to effluent does not have alcohol (macroporous resin regeneration).
The pharmacologically active experiment:
Experimental example 1. Balaenoptera borealis Lesson extracts to the normal mouse starch-bearing after the inhibitory action of blood sugar increasing
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 (BAITANGPING, 10mg/kg) irritate stomach as the positive control drug group, all the other groups are irritated stomach with starch (3.0g/kg) with different each 20g crude drug of Balaenoptera borealis Lesson extract (SHG88, SHG89, SHG90)/kg body weight 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.Result's (Fig. 1, table 1) illustrates, Balaenoptera borealis Lesson extract can obviously suppress the rising of blood glucose behind the normal mouse starch-bearing under 20g crude drug/kg dosage, and area under the blood glucose curve (AUC) reduces.The Balaenoptera borealis Lesson extract action intensity difference of different parts.The effect of this result and alpha-glucosidase inhibitor Acarbose is similar.
Table 1. Balaenoptera borealis Lesson extract is to the influence of the AUC of normal mouse starch tolerance
*,
*, compare p＜0.05,0.01. with matched group
Experimental example 2. Balaenoptera borealis Lesson extracts are to the inhibitory action of normal mouse sucrose load back blood sugar increasing
Normal ICR male mice, be divided into 4 groups (n=10) at random, overnight fasting before the experiment, irritate stomach as the positive control drug group with sucrose (4.0g/kg) for one group, all the other groups are irritated stomach with sucrose with different each 20g crude drug of extract (SHG88, SHG89, SHG90)/kg body weight respectively, and 30min, 60min, 120min measure blood sugar concentration before irritating stomach and behind the filling stomach.Result's (Fig. 2, table 2) shows that Balaenoptera borealis Lesson extract obviously suppresses the rising of normal mouse sucrose load back blood glucose under 20g crude drug/kg dosage, move after the glycemic peaks, and area under the blood glucose curve (AUC) reduces.The Balaenoptera borealis Lesson extract action intensity difference of different parts.
Table 2. Balaenoptera borealis Lesson extract is to the influence of the AUC of normal mouse sucrose tolerance
*,
* *, compare p＜0.05,0.001. with matched group
Experimental example 3. Balaenoptera borealis Lesson extracts to the normal mouse glucose load after the influence of blood sugar increasing
Normal ICR male mice, be divided into 4 groups (n=10) at random, fasting is 2 hours before the experiment, irritating stomach with glucose (2.0g/kg) for one group organizes in contrast, all the other groups are respectively with glucose and different each 20g crude drug of Balaenoptera borealis Lesson extract (SHG88, SHG89, SHG90)/kg body weight continuous irrigation stomach 7 days, 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's (Fig. 3, table 3) illustrates, the Balaenoptera borealis Lesson extract extract obviously suppresses the rising of blood glucose behind the normal mouse oral glucose glucose load under 20g crude drug/kg dosage, and glycemic peaks reduces, and area under the blood glucose curve (AUC) reduces.Illustrate that Balaenoptera borealis Lesson extract not only has the activity that suppresses alpha-glucosidase, the effect that delay glucose absorbs, and also has the effect that promotes the normal mouse glucose metabolism.The Balaenoptera borealis Lesson extract action intensity difference of different parts.
Table 3. Balaenoptera borealis Lesson extract is to the influence of the AUC of normal mouse glucose tolerance
*, compare p＜0.05. with matched group
Experimental example 4. Balaenoptera borealis Lesson extracts are to the influence of the plain tolerance of normal mouse islets
Normal ICR male mice is divided into 4 groups (n=10) at random, irritates stomach with water for one group and organizes in contrast, and all the other groups were irritated stomach continuous 10 days with each 20g crude drug of different Balaenoptera borealis Lesson extract (SHG88, SHG89, SHG90)/kg body weight respectively.Fasting is 2 hours before the experiment, and subcutaneous injection insulin 0.4U/kg with 30min, the 60min blood sampling of injection back, uses the determination of glucose oxidase blood sugar concentration before injection.Result's (Fig. 4, table 4) explanation, the Balaenoptera borealis Lesson extract extract obviously strengthens the reactivity of normal mouse subcutaneous injection insulin under 20g crude drug/kg dosage, compare with corresponding matched group, the blood glucose value of each time point obviously reduces, and area under the blood glucose curve (AUC) reduces.Illustrate that Balaenoptera borealis Lesson extract has the effect of certain increase normal mouse to insulin sensitivity.The Balaenoptera borealis Lesson extract action intensity difference of different parts.
Table 4. Balaenoptera borealis Lesson extract is to the influence of the AUC of the plain tolerance of normal mouse islets
*,
*, compare p＜0.05,0.01. with matched group
Experimental example 5. Balaenoptera borealis Lesson extracts are to the inhibitory action of Protein-tyrosine-phosphatase 1b (PTP1b)
Protein-tyrosine-phosphatase 1b (PTP1b) is one of important regulatory factor in the insulin signaling conducting system.A plurality of factors in the insulin signaling conducting system are that the protein tyrosine phosphatase by its molecule activates, and make its dephosphorylation and inactivation through the PTP1b effect again, thereby keep the balance of insulin signaling conducting system.Therefore, PTP1b is considered to one of novel targets of euglycemic agent.We obtain PTP1b albumen with the method for gene recombinaton, and the Balaenoptera borealis Lesson extract of observing 100 μ g/ml in vitro tests can obviously suppress the activity (table 5) of PTP1b.The Balaenoptera borealis Lesson extract action intensity difference of different parts.The result of experimental example 4,5 illustrates that all Balaenoptera borealis Lesson extract has insulin-sensitizing effect.
Table 5. Balaenoptera borealis Lesson extract is to the inhibitory action (n=3) of Protein-tyrosine-phosphatase 1b (PTP1b)
Experimental example 6. Balaenoptera borealis Lesson extracts are to the influence of normal mouse blood sugar
Normal ICR male mice, random packet (n=10), matched group is irritated stomach with water every day, all the other groups respectively with different Balaenoptera borealis Lesson extract (SHG21, SHG88, SHG89, SHG90) each 5,20,20,20g crude drug/kg body weight irritated stomach continuous 7-10 days.Non-fasting (no-fasting) blood glucose (being equivalent to post-prandial glycemia) is measured in experiment that morning 8:30 blood sampling.Experiment fasting on the same day 2.5 hours, and after administration, measure (fasting) blood glucose on an empty stomach before the blood sampling in 2 hours.Use the determination of glucose oxidase blood sugar concentration.As a result SHG21, SHG88, SHG89 and SHG90 make respectively animal the meansigma methods of non-fasting (no-fasting) blood glucose reduced by 27,23,16 and 6%; Make the meansigma methods of its empty stomach (fasting) blood glucose reduce by 25,19,7,0%.Balaenoptera borealis Lesson extract is described under 5-20g crude drug/kg dosage, the certain reduction normal mouse empty stomach and the effect of post-prandial glycemia is arranged, the Balaenoptera borealis Lesson extract action intensity difference of different parts.
Experimental example 7. Balaenoptera borealis Lesson extracts are to the influence of alloxan induced hyperglycemia mice blood glucose
ICR male mice tail vein injection alloxan 75mg/kg, measuring blood sugar of blood extracting behind the 72h.Blood glucose＞200mg/dl person is the hyperglycemia mice, and according to the blood sugar level of animal grouping (n=10).Matched group is irritated stomach with water every day, and the administration group was irritated stomach continuous 10 days with the Balaenoptera borealis Lesson extract SHG21 of 5g crude drug/kg body weight.Experiment that morning 8:30 gets blood, measures non-fasting (no-fasting) blood glucose (being equivalent to post-prandial glycemia).Experiment fasting on the same day 2.5 hours, and measure (fasting) blood glucose on an empty stomach before after administration, getting blood in 2 hours.Use the determination of glucose oxidase blood sugar concentration.The result shows that Balaenoptera borealis Lesson extract SHG21 can make the meansigma methods of non-fasting (no-fasting) blood glucose of alloxan induced hyperglycemia mice reduce by 42% under 5g crude drug/kg dosage; Make its meansigma methods reduction by 34% of (fasting) blood glucose on an empty stomach.Illustrate that Balaenoptera borealis Lesson extract has the effect of certain reduction alloxan induced hyperglycemia mice blood glucose.
Above-mentioned 7 pharmacological evaluation show that Balanophora plant (Balanophora L) extract has the activity of certain inhibition alpha-glucosidase, animal polysaccharide and disaccharidase load back blood glucose rise and peak is reduced and after move, area reduces under the blood glucose curve; Have certain insulin-sensitizing effect, make animal increase the reduction amplitude of insulin-induced blood glucose, area reduces under the blood glucose curve; PTP1B is shown certain inhibitory action; Have and promote the body glucose metabolism, make the animal glucose load after the blood glucose rise and peak reduce, area reduces under the blood glucose curve; In addition, also have certain reduction normal and the fasting glucose of alloxan induced hyperglycemia mice and the effect of non-fasting blood glucose.These effects all are of value to the improvement of diabetic sugar metabolism, lipid metabolic disorder, are particularly useful for preparing the medicine and the health product of the treatment metabolic disease relevant with prevent diabetes and complication thereof etc.
Claims (1)
1. the application of Balaenoptera borealis Lesson (Balanophora japonica Mak.) in preparation treatment and prevent diabetes and complication medicine thereof.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2006100920381A CN1965873B (en) | 2005-06-07 | 2006-06-07 | Chinese medicinal extract having blood sugar-lowering activity, its preparation process, composition and use |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200510074850.7 | 2005-06-07 | ||
| CN200510074850 | 2005-06-07 | ||
| CN2006100920381A CN1965873B (en) | 2005-06-07 | 2006-06-07 | Chinese medicinal extract having blood sugar-lowering activity, its preparation process, composition and use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1965873A CN1965873A (en) | 2007-05-23 |
| CN1965873B true CN1965873B (en) | 2011-04-20 |
Family
ID=38074966
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2006100920381A Expired - Fee Related CN1965873B (en) | 2005-06-07 | 2006-06-07 | Chinese medicinal extract having blood sugar-lowering activity, its preparation process, composition and use |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1965873B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107459548A (en) * | 2017-08-29 | 2017-12-12 | 云南养尊堂生物科技有限公司 | A kind of method that extraction from dioecious balanophora herb prepares Balaenoptera borealis Lesson element |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107753531B (en) * | 2017-10-18 | 2020-06-23 | 三峡大学 | Wenwang-herba violae extract and application thereof in preparing anti-cancer drugs |
| CN107890468B (en) * | 2017-12-15 | 2020-02-21 | 天津大学 | Use of 1, 3, 6-tri-O- (E) -caffeoyl- β -D-glucopyranose |
| CN108771690B (en) * | 2018-08-23 | 2021-10-29 | 嘉应学院 | A Balanophora japonica L extract with blood sugar or blood lipid reducing effect, and its preparation method and application |
| CN111302943A (en) * | 2018-12-11 | 2020-06-19 | 沈阳药科大学 | Phenolic acid compound and preparation method and application thereof |
| CN115068486A (en) * | 2021-03-15 | 2022-09-20 | 中国医学科学院药物研究所 | Application of boswellic acid compounds as LTB4 receptor inhibitors |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1279980A (en) * | 2000-06-23 | 2001-01-17 | 杨辉栋 | Health-care medicine for sobering up and eliminating alcoholism |
-
2006
- 2006-06-07 CN CN2006100920381A patent/CN1965873B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1279980A (en) * | 2000-06-23 | 2001-01-17 | 杨辉栋 | Health-care medicine for sobering up and eliminating alcoholism |
Non-Patent Citations (8)
| Title |
|---|
| Akihiro HOSOKAWA et al..A New Lignan from Balanophora abbreviata and Inhibition ofLipopolysaccharide (LPS)-induced Inducible Nitric OxideSynthase (iNOS) Expression.Chem. Pharm. Bull52 10.2004,52(10),1265-1267. |
| Akihiro HOSOKAWA et al..A New Lignan from Balanophora abbreviata and Inhibition ofLipopolysaccharide (LPS)-induced Inducible Nitric OxideSynthase (iNOS) Expression.Chem. Pharm. Bull52 10.2004,52(10),1265-1267. * |
| 沈小玲等.筒鞘蛇菰的化学成分.中草药27 5.1996,27(5),259-260. |
| 沈小玲等.筒鞘蛇菰的化学成分.中草药27 5.1996,27(5),259-260. * |
| 腾荣伟等.蛇菰的化学成分.云南植物研究22 2.2000,22(2),225-233. |
| 腾荣伟等.蛇菰的化学成分.云南植物研究22 2.2000,22(2),225-233. * |
| 黄代才.鹿仙草临床运用辑验.中国民族民间医药杂志 40.1999,(40),276. |
| 黄代才.鹿仙草临床运用辑验.中国民族民间医药杂志 40.1999,(40),276. * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107459548A (en) * | 2017-08-29 | 2017-12-12 | 云南养尊堂生物科技有限公司 | A kind of method that extraction from dioecious balanophora herb prepares Balaenoptera borealis Lesson element |
| CN107459548B (en) * | 2017-08-29 | 2019-11-29 | 云南养尊堂生物科技有限公司 | A method of extraction prepares Balaenoptera borealis Lesson element from dioecious balanophora herb |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1965873A (en) | 2007-05-23 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1965873B (en) | Chinese medicinal extract having blood sugar-lowering activity, its preparation process, composition and use | |
| CN102526165A (en) | Rhodiola effective fractions, preparation method, drug composition and uses thereof | |
| CN102526164A (en) | Traditional Chinese medicine composition for preventing insulin resistance and related metabolic syndrome thereof | |
| CN103342726B (en) | The preparation method of a kind of blood sugar lowering camellia flavonoid and application thereof | |
| CN1326814C (en) | Process for preparing Erigeron breviscapus active component | |
| CN101601780A (en) | The application of Chinese violet in anti-diabetic and control correlated metabolism diseases | |
| CN101961366A (en) | Preparation method of malan straw extract, malan straw product, pharmaceutical composition and application thereof | |
| CN106668348A (en) | Pharmaceutical composition for treating diabetic retinopathy | |
| CN100486606C (en) | Total sennoside extract for treating constipation and its extraction process | |
| CN102579530A (en) | Preparation method of aralia taibaiensis total saponin having diabetes mellitus resisting effect and medicament | |
| CN101433598A (en) | Uses of giant knotweed for preventing and treating insulin resistance and related metabolic diseases thereof | |
| CN103845634A (en) | Application of Cymbopogon plant extractive as insulin sensitizing medicine | |
| CN101428055A (en) | Uses of rhodiola rosea plants in medicament for preventing and treating diabetes and adiposis | |
| CN101120969A (en) | Medicine for treating diabetes and its complications and preparing method thereof | |
| CN107875350B (en) | A Chinese medicinal composition for treating diabetes | |
| CN101974011A (en) | New compound methyl brevicate with medical activity | |
| CN101766676B (en) | Extract of Albizia chinensis (Osbeck) Merr, preparation method, combination and purpose thereof | |
| CN101428054A (en) | Uses of rhodiola rosea in preventing and treating insulin resistance, and correlated metabolism diseases | |
| CN104436022A (en) | Hemsleya-macrosperma-containing traditional Chinese medicine composition for treating diabetes mellitus | |
| CN104622987B (en) | A kind of pharmaceutical composition for treating chronic hepatitis liver cirrhosis and application | |
| CN102462726B (en) | The extracting and developing of Rhizoma Melaleuca Viridiflora total alkaloids and polyhydroxylated alkaloid compound and purposes | |
| CN101974010B (en) | New compound erigeron breviscapus acid with officinal activity | |
| CN106074736A (en) | A kind of pharmaceutical composition treating cerebral thrombosis and preparation method thereof | |
| CN1283271C (en) | Sinowilsonia henryi extract and its prepn process, composition and use | |
| CN100998587A (en) | Application of 5-hydroxy furfurol for preparing medicine |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20110420 Termination date: 20150607 |
|
| EXPY | Termination of patent right or utility model |