CN101502536A - Cedar total flavone as well as preparation method and medical use - Google Patents
Cedar total flavone as well as preparation method and medical use Download PDFInfo
- Publication number
- CN101502536A CN101502536A CNA2008100099986A CN200810009998A CN101502536A CN 101502536 A CN101502536 A CN 101502536A CN A2008100099986 A CNA2008100099986 A CN A2008100099986A CN 200810009998 A CN200810009998 A CN 200810009998A CN 101502536 A CN101502536 A CN 101502536A
- Authority
- CN
- China
- Prior art keywords
- cedar
- total flavones
- finished product
- preparation
- concentrated solution
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention belongs to the field of pharmaceutical technology and particularly relates to cedar total flavonoids, a preparation method and a use thereof. The method comprises the steps of taking fresh or dried cedar branches and leaves as medicinal materials, not crushing or crushing into the particle size of 10-60 meshes, extracting by 10 times-20 times of the weight of the medicinal materials of water and/or alcohol, filtering and concentrating extracting solution, processing concentrated solution by the solvent method to obtain a finished product of the cedar total flavonoids or separating the concentrated lsolution by macroporous resin, then concentrating and drying eluent to obtain the finished product of the cedar total flavonoids. The finished product of the cedar total flavonoids can be prepared into a variety of pharmaceutical dosage forms with pharmaceutically acceptable carriers or excipients, the content of extract of the cedar total flavonoids in each unit of dosage form is 5-1000mg, and the finished product of the cedar total flavonoids comprises cedar flavonoids, 8-hydroxy luteolin-O-beta-D-xylopyranoside, 8-hydroxy luteolin-O-beta-D-glucopyranosid and so on. The finished product of the cedar total flavonoids can be widely applied in anti-inflammatory, antipyretic, analgesic, anti-influenza virus, anti-hepatitis virus, anti-retrovirus including HIV, lowering blood pressure, lowering blood lipid and anti-thrombosis or the products which are related to the diseases.
Description
Technical field:
The invention belongs to medical technical field, be specifically related to Cedar total flavones and preparation method thereof and medical usage.
Background technology:
Flavone compound is a class flavochrome that extensively is present in the plant, its physiological function that presents is varied, comprise cardiovascular function, anti-oxidation function, arrhythmia function, the anticancer function of antitumor, antitussive and antiasthmatic function etc., have a wide range of applications in food and medicine industry.
Cedar [Sabina pingii (Cheng ex Ferre) Cheng et W.T.Wang var.Wilsonii (Rehd.) Cheng et L.K.Fu] is a Cupressaceae Sabina plant, be rich in the flavonoid chemical constituent, but do not see up to now, the report of relevant Cedar total flavones chemical constituent preparation method and medical usage thereof as yet.
Summary of the invention:
The objective of the invention is to fail to prepare the deficiency of Cedar total flavones in order to overcome prior art, for people provide a kind of Cedar total flavones and preparation method thereof and medical usage, specifically from Cedar, extract the method for total flavonoid composition, and the purposes of products obtained therefrom in antiinflammatory, analgesic, analgesia, antiviral (as influenza virus, hepatitis virus, comprise the retrovirus retrovirus of HIV etc.), blood pressure lowering, blood fat reducing, antithrombotic.
The objective of the invention is to realize by following technical proposals.
The preparation method of Cedar total flavones of the present invention, be to be medicinal raw material with aquatic foods product or dry product Cedar branch and leaf, without pulverizing or pulverizing is 10～60 order granularities, water and/or alcohol extraction through 10 times～20 times of medical material weight, extracting solution concentrates after filtration, concentrated solution is handled with solvent method and is obtained Cedar total flavones finished product or concentrated solution after macroporous resin separates, concentrate eluant, dry and obtain Cedar total flavones finished product, and with Cedar total flavones finished product with pharmaceutically acceptable carrier or excipient are prepared into various pharmaceutical dosage forms, the content of Cedar extractive of general flavone is 5～1000mg in its unit dosage forms, is preferably 10～100mg.Its technological process is as follows:
In the such scheme, described Cedar total flavones finished product is including but not limited to cupresuflavone, hypolaetin-O-β-xylopyranoside (8-hydroxyl luteolin-7-O-beta-D-xylopyranoside), Hypolaetin-O-β-glycoside (8-hydroxyl luteolin-7-O-beta-D-pyranglucoside).Structural formula is as follows:
Cupresuflavone hypolaetin-O-β-xylopyranoside Hypolaetin-O-β-glycoside cupresuflavone
In the such scheme, described Cedar total flavones finished product content is more than 30%.
In the such scheme, during extraction used alcohol be methanol, ethanol, propanol, butanols, n-butyl alcohol, ethylene glycol, carbochain less than 32 alkanols, carbochain less than 32 enols, or their mixture.
In the such scheme, method therefor includes but not limited to reflux, percolation, ultrasonic, microwave extraction during extraction.
In the such scheme, described concentrated solution is handled with solvent method and is included but not limited to obtain Cedar total flavones finished product from n-butanol portion by the n-butanol extraction concentrated solution; Or the employing alcohol precipitating method, promptly add ethanol to concentration and reach by weight about 80% to concentrated solution, remove precipitation after leaving standstill cold preservation, obtain Cedar total flavones finished product.
Above-mentioned Cedar total flavones finished product also can be described as the Cedar extractive of general flavone.
In the such scheme, when concentrated solution separated through macroporous resin, described macroporous resin included but not limited to various nonpolar, low poles, Semi-polarity or polar macroporous adsorbent resin.
In the such scheme, when concentrated solution separated through macroporous resin, macroporous resin eluting solvent for use included but not limited to 3～5: 1 methanol or ethanol water of by volume, or the mixture of the ethyl acetate of different proportion, chloroform, ethanol, methanol, acetone.
In the such scheme, described dosage form comprises various regular dosage forms such as tablet, capsule, injection.
In the such scheme, its preparation formulation is a tablet, and every contained Cedar extractive of general flavone is 10～100mg.
In the such scheme, its preparation formulation is a capsule, and the content of the Cedar extractive of general flavone that every capsules is contained is 10～100mg.
In the such scheme, its preparation formulation is an injection, and the content of contained Cedar extractive of general flavone is 10～100mg in the per unit dosage form.
The medical usage of Cedar total flavones of the present invention, be meant that the Cedar total flavones can be used for antiinflammatory, analgesic, analgesia, resisiting influenza virus, hepatitis virus resisting, anti-retrovirus retrovirus, blood pressure lowering, blood fat reducing, the antithrombotic that comprises HIV, or with the product of these disease associations in use.
Advantage of the present invention is: provide and can expect to be used for antiinflammatory, analgesic, analgesia, antiviral (as influenza virus, hepatitis virus, comprise the retrovirus retrovirus of HIV etc.), blood pressure lowering, blood fat reducing, the Cedar total flavones of antithrombotic use and the preparation method of preparation thereof, its cost is low, process stabilizing, pharmacologically active is remarkable.
The specific embodiment:
Further specify the present invention below by embodiment, the present invention is not limited only to described embodiment.
Embodiment one
The preparation of Cedar total flavones: with aquatic foods product Cedar branch and leaf is medicinal raw material, gets Cedar medical material 1kg and is ground into 10 order powder, adds the water of 10 times of medical material weight, heating and refluxing extraction 3 times, each 2 hours, filter merge extractive liquid,, concentrating under reduced pressure reclaims solvent, to 1g crude drug/mL.Concentrated solution is added ethanol to 80% weight concentration of alcohol gradually, remove precipitation after leaving standstill cold preservation, drying under reduced pressure gets yellowish-brown Cedar total flavones powder 58.4g, contains the total flavones 43% that comprises cupresuflavone, hypolaetin-O-β-xylopyranoside, Hypolaetin-O-β-glycoside.
Embodiment two
The preparation of Cedar total flavones: with dry product Cedar branch and leaf is medicinal raw material, gets Cedar medical material 1kg and is ground into 60 order powder, and with the 50% ethanol water percolation extraction of 20 times of medical material weight, the extracting solution concentrating under reduced pressure reclaims solvent, to 1g crude drug/mL.With concentrated solution by activated D141 type (low pole) macroporous resin column of handling well, flavones ingredient in the concentrated solution is adsorbed by resin column, and discard effluent, distilled water flushing with 3 times of column volumes, discard effluent, continue with 5: 1 ethanol water of by volume (ethanol: eluting resin column water=5: 1), till the complete eluting of flavones ingredient quilt on being adsorbed in, and collection eluent, concentrating under reduced pressure, the dry yellowish-brown Cedar total flavones powder 55.7g that gets contains and comprises cupresuflavone, hypolaetin-O-β-xylopyranoside, Hypolaetin-O-β-glycoside etc. are at interior total flavones 51%.
Embodiment three
The preparation of Cedar total flavones: with dry product Cedar branch and leaf is medicinal raw material, gets Cedar medical material 1kg and is ground into 40 order powder, adds the methanol of 10 times of medical material weight, supersound extraction 3 times, each 20min filters merge extractive liquid,, concentrating under reduced pressure reclaim solvent, and thin up is to 1g crude drug/mL.Concentrated solution is passed through n-butanol extraction 3 times, and each 100ml merges n-butanol portion, and drying under reduced pressure gets Cedar total flavones yellowish-brown powder 40.3g, and its general flavone content is 56%.
Embodiment four
The preparation of Cedar total flavones: with dry product Cedar branch and leaf is medicinal raw material, gets the Cedar medical material 1kg of 1cm left and right sides segment, adds 60% ethanol of 10 times of medical material weight, microwave extraction 3 times, each 30min filters merge extractive liquid,, concentrating under reduced pressure reclaims solvent, to 1g crude drug/mL.With concentrated solution by activated D101 type (nonpolar) macroporous resin column of handling well, flavones ingredient in the concentrated solution is adsorbed by resin column, and discard effluent, distilled water flushing with 3 times of column volumes, discard effluent, and 3: 1 the ethanol water of usefulness by volume that continues (ethanol: eluting resin column water=4: 1), till the complete eluting of flavones ingredient quilt on being adsorbed in, and the collection eluent, concentrating under reduced pressure, the dry yellowish-brown Cedar total flavones powder 56.4g that gets.
Embodiment five
The preparation tablets that contains the Cedar extractive of general flavone
Prescription:
Become dosis refracta
Cedar extract (embodiment 1) 60g
Starch 50g
Dextrin 60g
Sucrose 10g
Magnesium stearate 2g
Make 1000
Method for making: above-mentioned prescription composition mixes, granulates according to the conventional formulation method and is pressed into tablet.
Embodiment six
Contain the capsule preparation of Cedar extractive of general flavone
Prescription:
Become dosis refracta
Cedar extractive of general flavone (embodiment 1) 60g
Lactose 60g
Dextrin 15g
Starch 45g
HMPC is an amount of
Make 1000
Method for making: above-mentioned prescription composition mixes, granulates according to the conventional formulation method and adorns capsule No. 2.
Embodiment seven
Contain the injection preparation of Cedar extractive of general flavone
Prescription:
Become dosis refracta
Cedar extractive of general flavone (embodiment 1) 25g
Tween 80 1.5g
NaCl 3g
Thimerosal 0.01g
Sodium carboxymethyl cellulose 5g
Water for injection adds to 1000ml
Method for making: above-mentioned prescription composition mixes, shakes up, filters and be packed as 5ml/ according to the conventional formulation method and props up, and sterilization promptly.
Embodiment eight
Cedar total flavones antiinflammatory action-xylol causes the influence of mice auricle swelling model
8.1 experimental technique adopts 50 of SPF level KM kind male mices, body weight 24g ± 2g, be divided into 5 groups at random by body weight, every group 10, be respectively model group (distilled water), positive controls (aspirin group 100mg/kg) and be subjected to reagent (50,25,10mg/kg) group, be administered once every day, for three days on end.After the last administration 1 hour, dimethylbenzene coating auris dextra, 1/ of 20 μ.Left side ear compares, and dislocation is put to death after 30 minutes, lays auricle with the 9mm card punch in left and right sides ear same area, weighs with ten thousand/balance, calculates auricle swelling degree, swelling rate and inhibitory rate of intumesce.Experimental data adopts the SPSS11.0 statistical software to carry out one factor analysis of variance.
8.2 experimental result
Table 8.1 Cedar total flavones xylol cause mice auricle swelling influence (n=10, X ± S, mg)
Annotate: compare with model group,
*P＜0.01.
Mice Auricle is smeared 30min behind the dimethylbenzene, smears the position and acute inflammatory reactions such as tangible redness occur, and as can be seen from the above table, its auricle edema rate is up to 172.9%.Cedar total flavones 50mg/kg, 25mg/kg dosage can obviously suppress the mice auricle swelling due to the dimethylbenzene, and its swelling degree, swelling rate and model group relatively have significant difference (P＜0.01).
8.3 brief summary Cedar total flavones can obviously suppress the mice caused by dimethylbenzene xylene auricle edema, prompting Cedar total flavones has the obvious suppression effect to acute inflammation.
Embodiment nine
Cedar total flavones refrigeration function-refrigeration function 9.1 experimental techniques that escherichia coli endotoxin is caused fever in rabbits were not done the adult healthy rabbit of any test, one-level, body weight 2.0kg～2.5kg, male and female dual-purpose.Before experiment, survey animal heat every day once, continuous three days.Experiment same day, measure animal heat 2 times, more than 0.5 hour, get 2 body temperature between 38.6 ℃～39.5 ℃ at interval, and 2 body temperature are no more than 0.3 ℃ of person and formally test (twice body temperature meansigma methods is basal body temperature).To screen 40 of qualified animals and be divided into 5 groups at random by basal body temperature, each 8, the male and female dual-purpose, be respectively model group (distilled water), positive controls (aspirin 100mg/kg) and be subjected to reagent group (200,100,50mg/kg), each organizes behind the gastric infusion 1 hour, press 250ng/kg dosage auricular vein injection escherichia coli endotoxin, measure injection back 1h, 2h, 3h, 4h and 6h body temperature respectively.Experimental data adopts the SPSS11.0 statistical software to carry out one factor analysis of variance.
9.2 experimental result
Table 9.1 Cedar total flavones is to the influence of fever in rabbits due to the escherichia coli endotoxin (n=8, X ± S, ℃)
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
As can be seen from the above table, rabbit body temperature promptly begins to rise behind the injection escherichia coli endotoxin, keeps 3-4 hour.Cedar total flavones 200mg/kg, 100mg/kg can obviously suppress the rising of rabbit body temperature, and each time point measuring more all has significant difference (P＜0.05 or P＜0.01) with model group.
9.3 brief summary Cedar total flavones has tangible refrigeration function to the caused fever in rabbits of escherichia coli endotoxin, prompting this product has analgesic effect of bringing down a fever.
Embodiment ten
Cedar total flavones analgesic activity-acetic acid twisting experiment
10.1 experimental technique adopts 50 of SPF level KM kind mices, male and female half and half, body weight 20g ± 2g, be divided into 5 groups at random by body weight, every group 10, be respectively model group (distilled water), positive controls (aspirin group 100mg/kg) and be subjected to reagent (200,100,50mg/kg) group, be administered once every day, for three days on end.After the last administration 1 hour, each treated animal lumbar injection 0.6% acetum 0.2ml/ only.Observe behind the injection acetum time (turn round body incubation period) and writhing response number of times that writhing response appears in each group in the 30min.Experimental data adopts the SPSS11.0 statistical software to carry out one factor analysis of variance.
10.2 experimental result
The influence of table 10.1 Cedar total flavones Dichlorodiphenyl Acetate induced mice writhing response (n=10, X ± S)
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
As can be seen from the above table, Cedar total flavones 200mg/kg, 100mg/kg give mouse stomach, once a day, and for three days on end, can obviously prolong due to the acetic acid turn round body incubation period and the body number of times is turned round in reduction, relatively have significant difference (P＜0.05 or P＜0.01) with model group.
10.3 brief summary Cedar total flavones can obviously prolong acetic acid induced mice writhing response turn round body incubation period and the body number of times is turned round in reduction, prompting Cedar total flavones has certain analgesic activity.
Embodiment 11
The Cedar total flavones is killed the test of A type cold virus
11.1 experimental technique Cedar total flavones is plain and A type cold virus (TCID
50=1.02 * 10
4/ ml) hatch 1 hour altogether after, with the antigenic amount of Influenza A Virus EIAKit (Precoated) kit measurement cold virus of Katara, thereby extrapolate the amount of A type cold virus.Killing rate (%)=100 * [1-(the OD value of the OD value of sample determination-culture fluid contrast)/(the OD value of the OD value of common cold venom contrast-culture fluid contrast)].
11.2 experimental result
Table 11.1 Detection of antigen method detects the killing action of 3 pairs of A types of Cedar total flavones sample cold virus
11.3 brief summary Cedar total flavones has the effect of directly killing to A type cold virus, when concentration is 0.10mg/ml, the direct killing rate of HIV virus has been reached more than 89%.
Embodiment 12
The activity of the external anti-hepatitis B of Cedar total flavones
12.1 the 2.2.1.5 cell of experimental technique culture expression antigen of hepatitis B virus adds the Cedar total flavones in cell conditioned medium liquid, continue to cultivate, after four days, change culture fluid, continue to cultivate three days, use hepatitis B surface antigen and the antigenic expression of e antigen measuring kit measurement then.Suppression ratio (%)=100 * [1-(the OD value of the OD value-culture fluid of sample determination)/(the OD value of the OD value-culture fluid of 2.2.1.5 cell contrast)], cell survival rate (%)=100 * (the OD value of the OD value-culture fluid of sample determination)/(the OD value of the OD value-culture fluid of 2.2.1.5 cell contrast).Vitro detection Cedar total flavones is to the effect of hepatitis B antigen express cell 2.2.1.5.
12.2 experimental result
The result of the test of the external surface antigen expression inhibiting effect to the 2.2.1.5 cell of table 12.1 Cedar total flavones
The external inhibiting result of the test of e antigen presentation of table 12.2 Cedar total flavones to the 2.2.1.5 cell
The result of the test of the external toxic action to the 2.2.1.5 cell of table 12.3 Cedar total flavones
12.3 brief summary Cedar total flavones can suppress the surface antigen and the antigenic expression of e of 2.2.1.5 cell.And, the Cedar total flavones is little to the toxicity of 2.2.1.5 cell in finite concentration, such as, Cedar total flavones sample 1 is 67.16% to the expression inhibiting rate of the surface antigen of 2.2.1.5 cell when 250 μ g/ml, is 72.03% to the antigenic expression inhibiting rate of the e of 2.2.1.5 cell, under this drug level, 2.2.1.5 the MTT result of cell is 0.804, and the MTT result of normal 2.2.1.5 cell is 1.229, cell survival rate reaches 65.08%.
Embodiment 13
The Cedar total flavones is killed the test of HIV
13.1 experimental technique Cedar total flavones element is used the amount of the HIV-1P24 kit measurement antigen P24 of Biomerieux after hatching 1 hour altogether with HIV virus (TCID50=1.78 * 105), thereby extrapolates the amount of HIV virus.Killing rate (%)=100 * [1-(the OD value of the OD value of sample determination-culture fluid contrast)/(the OD value of the OD value-culture fluid contrast of HIV virus liquid contrast)].
13.2 experimental result
Table 13.1 HIV-1P24 Detection of antigen method detects the killing action of Cedar total flavones to HIV
| Concentration (mg/ml) | The OD value of measuring | Killing rate (%) |
| 0.80 | 0.211 | 92.75 |
| 0.20 | 0.421 | 85.49 |
| 0.10 | 0.569 | 80.38 |
| 5% " 84 " disinfectant solution | 0.002 | |
| The contrast of HIV virus liquid | 2.896 | |
| The culture fluid contrast | 0.001 | |
| The test kit positive (80pg/ml) | 1.124 | |
| The test kit feminine gender | 0.011 |
13.3 brief summary Cedar total flavones has the effect of directly killing to HIV virus, when concentration is 0.10mg/ml, the direct killing rate of HIV virus has been reached more than 80%.
Embodiment 14
The activity of the reverse transcription of Cedar total flavones vitro inhibition HIV-1
14.1 experimental technique adds the reverse transcription titer in the solution of medicine is arranged, measure with the Retrosys reverse transcriptase activity test kit of Innovagen company then.Suppression ratio (%)=100 * [1-(the OD value of the OD value of sample determination-culture fluid contrast)/(the OD value of the OD value of reverse transcription titer contrast-culture fluid contrast)].
14.2 experimental result
The inhibiting result of the test of the external reverse transcriptase of table 14.1 Cedar total flavones to HIV-1
| Concentration (mg/ml) | The OD value of measuring | Suppression ratio (%) |
| 0.80 | 0.229 | 87.54 |
| 0.20 | 0.338 | 81.52 |
| 0.10 | 0.478 | 73.32 |
| The culture fluid contrast | 0.001 | |
| The contrast of reverse transcription titer | 1.789 |
14.3 brief summary Cedar total flavones has inhibitory action to the reverse transcriptase of HIV-1, when concentration is 0.10mg/ml, the inhibitory action of the reverse transcriptase of HIV-1 has been reached more than 73%.
Embodiment 15
The Cedar total flavones is to the protective effect of the cell that is subjected to HIV and infects
15.1 experimental technique HIV viral infection MT4 cell; in cell suspension, add the Cedar total flavones; continue to cultivate; after four days; measure the quantity of cell with mtt assay; the MT4 cell contrast of infecting with the HIV that does not add the Cedar total flavones, thus calculate of the protective effect of Cedar total flavones to the cell that is subjected to HIV and infects.The protected rate of cell (%)=100 * (cell+HIV+ medicinal liquid-cell+HIV)/(cell contrast-cell+HIV).
15.2 experimental result
Table 15.1 Cedar total flavones is to the result of the test of the protective effect of the cell that is subjected to HIV and infects
15.3 brief summary Cedar total flavones has the better protect rate to the cell that infected by HIV, when concentration was 0.10mg/ml, the protective rate of pair cell had reached 92.75%.
Embodiment 16
The Cedar total flavones is to the inhibitory action of the HIV in the cell that is subjected to the HIV infection
16.1 experimental technique HIV viral infection MT4 cell, in cell suspension, add the Cedar total flavones, continue to cultivate, after four days, change culture fluid, continue to cultivate three days, use the amount of the antigen P24 in each mixed culture supernatant of HIV-1P24 kit measurement of Biomerieux, thereby extrapolate the amount of HIV virus.Suppression ratio (%)=100 * [1-(the OD value of the OD value of sample determination-cell contrast)/(the OD value of the OD value of cell+HIV contrast-cell contrast)].
16.2 experimental result
Table 16.1 Cedar total flavones is to the inhibitory action of the HIV in the cell that is subjected to the HIV infection
16.3 brief summary Cedar total flavones has inhibitory action to the HIV in the cell that is subjected to HIV and infects, and when concentration is 0.10mg/ml, the suppression ratio of HIV virus has been reached more than 76%.
Embodiment 17
The Cedar total flavones is to the inhibitory action of reverse transcriptase activity in the supernatant of the cell that is subjected to HIV and infects
17.1 experimental technique adds the Cedar total flavones with HIV viral infection MT4 cell in cell suspension, continue to cultivate, after four days, change culture fluid, continue to cultivate three days, with the reverse transcriptase activity in the Retrosys reverse transcriptase activity test kit mensuration cell conditioned medium liquid of Innovagen.Suppression ratio (%)=100 * [1-(the OD value of the OD value of sample determination-cell contrast)/(the OD value of the OD value of cell+HIV contrast-cell contrast)].
17.2 experimental result
Table 17.1 Cedar total flavones is to the inhibitory action of the reverse transcriptase activity in the cell that is subjected to the HIV infection
17.3 brief summary Cedar total flavones has inhibitory action to reverse transcriptase activity in the supernatant of the cell that is subjected to HIV and infects, when concentration is 0.10mg/ml, the suppression ratio of HIV virus has been reached more than 90%.
Embodiment 18
The Cedar total flavones is to the spontaneous hypertensive rat antihypertensive activity
18.1 totally 40 of experimental technique 16 all SHR in age (spontaneously hypertensive) rats are complete male.Utilize RM6200 bio signal acquisition system to measure the initial blood pressure of each animal, be divided into four groups at random by blood pressure with noinvasive tail platen press.Be respectively model group (normal saline); Positive controls (the sharp 10mg/kg of Top); Cedar total flavones low dose group (200mg/kg) and Cedar total flavones high dose group (400mg/kg).After 4 weeks of continuous oral administration, measure blood pressure with noinvasive tail platen press once more.Experimental data adopts the SPSS11.0 statistical software to handle.
18.2 experimental result
Table 18.1 Cedar total flavones to the influence of the systolic pressure of spontaneous hypertensive rat (n=10, X ± S, mmHg)
Annotate: * * represents to compare with model group P＜0.01; * P＜0.05 is compared in expression with model group.
18.3 each dosage group of brief summary Cedar total flavones all has obvious antihypertensive activity.
Embodiment 19
Cedar total flavones blood fat reducing activity
19.1 the experimental technique animal subject adopts the SD rat.Totally 50, male and female half and half, body weight 120-160g.Tried the rat ophthalmic corner of the eyes and got the every blood fat observation index of hematometry normal value.According to the TC level rat is divided into 5 groups: 1 normal feedstuff matched group; 1 hyperlipidemia model matched group (high fat group) and three dosage groups of Cedar total flavones (100mg/kg; 200mg/kg; 400mg/kg).Every group 10.After beginning test, except that the normal feedstuff matched group, all the other each groups are all used high lipid food feed (78.8% normal feedstuff, 1% cholesterol, 10% yolk powder, 10% Adeps Sus domestica and 0.2% Fel Sus domestica salt).Each rats in test groups per os is irritated stomach and is tried solution, and two matched groups are irritated stomaches and given normal saline, and irritate the stomach amount and be 1.0ml/100g once a day, 30d continuously, weighing once and is irritated the stomach amount according to the body weight adjustment weekly.Take a blood sample behind the fasting 16h when test is last extremely eventually and measure serum TC (T-CHOL), TG (triglyceride) content.Experimental data adopts the SPSS11.0 statistical software to handle.
19.2 experimental result
Table 19.1 Cedar total flavones to the influence of high-fat adiposity rat TC and TG (n=10, X ± S, mmol/L)
Annotate: * * represents to compare with model group P＜0.01; * P＜0.05 is compared in expression with model group.19.3 the brief summary result of the test shows that the Cedar total flavones can effectively reduce the intravital TC of high-fat adiposity rat, TG level.
Embodiment 20
Cedar total flavones function of promoting blood circulation to disperse blood clots-collagen protein-epinephrine is brought out the inhibitory action that the mice thrombus in vivo forms
20.1 experimental technique adopts 50 of SPF level NIH kind mices, male, body weight 24g ± 2g, be divided into 5 groups at random by body weight, every group 10, be respectively model group (distilled water), positive controls (aspirin group 20mg/kg) and be subjected to reagent (50,25,10mg/kg) group, be administered once every day, for three days on end.After the last administration 1 hour, the derivant that mixes of mouse tail vein injection collagen protein (225 μ g/ only) and epinephrine (9 μ g/ only) was observed the recovery number of mice hemiplegia in the 15min, and the calculating medicine is to mouse brain thrombosis protective rate.Experimental data adopts the SPSS11.0 statistical software to carry out chi-square analysis.
20.2 experimental result
Table 20.1 Cedar total flavones brings out the influence that the mice thrombus in vivo forms to collagen protein-epinephrine
Annotate: compare with model group,
*P＜0.05,
*P＜0.01.
As can be seen from the above table, Cedar total flavones 50mg/kg, 25mg/kg give mouse stomach, once a day, and for three days on end, can obviously improve the recovery rate that collagen protein-epinephrine brings out the mouse brain hemiplegia, relatively have significant difference (P＜0.05 or P＜0.01) with model group.
20.3 brief summary Cedar total flavones can obviously improve the recovery rate that collagen protein-epinephrine brings out the mouse brain hemiplegia, prompting Cedar total flavones has anti thrombotic action.
Claims (10)
1. the preparation method of a Cedar total flavones, it is characterized in that being is medicinal raw material with aquatic foods product or dry product Cedar branch and leaf, without pulverizing or pulverizing is 10～60 order granularities, water and/or alcohol extraction through 10 times～20 times of medical material weight, extracting solution concentrates after filtration, concentrated solution is handled with solvent method and is obtained Cedar total flavones finished product or concentrated solution after macroporous resin separates, concentrate eluant, drying and obtain Cedar total flavones finished product.
2. the preparation method of Cedar total flavones according to claim 1, it is characterized in that it being with pharmaceutically acceptable carrier or excipient are prepared into various pharmaceutical dosage forms with described Cedar total flavones finished product, the content of Cedar extractive of general flavone is 5～1000mg in its unit dosage forms, and described dosage form comprises tablet, capsule, injection.
The preparation method of 3 Cedar total flavones according to claim 1, it is characterized in that described alcohol be meant methanol, ethanol, propanol, butanols, n-butyl alcohol, ethylene glycol, carbochain less than 32 alkanols, carbochain less than a kind of of 32 enols or their mixture.
4. the preparation method of Cedar total flavones according to claim 1 is characterized in that described extracting method is reflux, percolation, ultrasonic, microwave extraction.
5. the preparation method of Cedar total flavones according to claim 1 is characterized in that described concentrated solution is handled with solvent method to be meant and to obtain Cedar total flavones finished product from n-butanol portion by the n-butanol extraction concentrated solution; Or the employing alcohol precipitating method, promptly add ethanol to concentration and reach by weight about 80% to concentrated solution, remove precipitation after leaving standstill cold preservation, obtain Cedar total flavones finished product.
The preparation method of 6 Cedar total flavones according to claim 1 is characterized in that described macroporous resin is meant various nonpolar, low poles, Semi-polarity or polar macroporous adsorbent resin.
7. the preparation method of Cedar total flavones according to claim 1, it is characterized in that described concentrated solution is when macroporous resin separates, macroporous resin eluting solvent for use is 3～5: 1 methanol or an ethanol water of by volume, or the mixture of the ethyl acetate of different proportion, chloroform, ethanol, methanol, acetone.
8. the preparation method of Cedar total flavones according to claim 2, it is characterized in that it being that described Cedar total flavones finished product and acceptable carrier pharmaceutically or excipient are prepared into various pharmaceutical dosage forms, the content of Cedar total flavones finished product is 10～100mg in its unit dosage forms.
9. Cedar total flavones finished product, it is characterized in that in the described Cedar total flavones finished product that including but not limited to cupresuflavone, hypolaetin-O-β-xylopyranoside (8-hydroxyl luteolin-7-O-beta-D-xylopyranoside), Hypolaetin-O-β-glycoside (8-hydroxyl luteolin-7-O-beta-D-pyranglucoside), structural formula is as follows:
The Cedar general flavone content is more than 30% in the described Cedar total flavones finished product.
10. the medical usage of Cedar total flavones finished product according to claim 9, it is characterized in that being meant Cedar total flavones finished product at antiinflammatory, analgesic, analgesia, resisiting influenza virus, hepatitis virus resisting, anti-retrovirus retrovirus, blood pressure lowering, blood fat reducing, the antithrombotic that comprises HIV, and with the product of these disease associations in application.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100099986A CN101502536B (en) | 2008-02-10 | 2008-02-10 | Cedar total flavone as well as preparation method and medical use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100099986A CN101502536B (en) | 2008-02-10 | 2008-02-10 | Cedar total flavone as well as preparation method and medical use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101502536A true CN101502536A (en) | 2009-08-12 |
| CN101502536B CN101502536B (en) | 2012-05-02 |
Family
ID=40974997
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008100099986A Active CN101502536B (en) | 2008-02-10 | 2008-02-10 | Cedar total flavone as well as preparation method and medical use |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101502536B (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101744830B (en) * | 2008-06-17 | 2012-09-05 | 上海医药工业研究院 | Flavonoid compound and application of plant extract containing same |
| CN104398542A (en) * | 2014-10-30 | 2015-03-11 | 厦门大学 | Method for extracting and purifying flavones from plants containing flavones |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1299675C (en) * | 2004-05-24 | 2007-02-14 | 南京大学 | Composition of cupresulflavone and its preparation |
-
2008
- 2008-02-10 CN CN2008100099986A patent/CN101502536B/en active Active
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101744830B (en) * | 2008-06-17 | 2012-09-05 | 上海医药工业研究院 | Flavonoid compound and application of plant extract containing same |
| CN104398542A (en) * | 2014-10-30 | 2015-03-11 | 厦门大学 | Method for extracting and purifying flavones from plants containing flavones |
| CN104398542B (en) * | 2014-10-30 | 2017-11-07 | 厦门大学 | A kind of method of the extraction and purification flavones from the plant containing flavones |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101502536B (en) | 2012-05-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10624938B2 (en) | Total flavone extract of flower of abelmoschus manihot L. medic and preparation method thereof | |
| CN103768534B (en) | A kind of Chinese medicine composition with antitumor activity | |
| CN102114044A (en) | Artificially processed bear bile powder and preparation method thereof | |
| CN101313927A (en) | Southernwood total flavone, method for preparing its composition and medicine uses thereof | |
| CN101904839B (en) | Application of imperatorin in preparing medicament for preventing and treating hepatitis or liver injury | |
| CN102370695B (en) | Qinglongyi active extract, its preparation method and its application | |
| WO2015192758A1 (en) | Anti-tumor pharmaceutical application of pentacyclic triterpene saponin compounds of szechuan melandium root | |
| CN104435034A (en) | PNS (panax notoginseng saponins) and preparation method thereof | |
| CN102134192A (en) | Preparation method for extracting chlorogenci acid from honeysuckle and application of honeysuckle extract | |
| CN102579559B (en) | Bauhinia championii ethyl acetate extract, n-butyl alcohol extract, and preparation methods and applications thereof | |
| US20030054047A1 (en) | Pharmaceutical composition for the treatment of viral infection | |
| US9629385B2 (en) | Dietary composition containing cistanche deserticola polysaccharide with inhibitory effects on colon cancer | |
| CN101502536B (en) | Cedar total flavone as well as preparation method and medical use | |
| CN107753823B (en) | Traditional Chinese medicine composition for treating or preventing hand-foot-and-mouth disease | |
| CN103272016A (en) | Traditional chinese medicine composition | |
| CN103191175B (en) | Diarrhoea-stopping traditional Chinese medicine composition, capsule and application thereof | |
| RU2651750C2 (en) | Application of albizzia chinensis extract in preparation of medicine for treatment of gastric ulcer | |
| CN103816147A (en) | Novel pharmaceutical uses of garcinolic acid, neogambogic acid and composition of garcinolic acid and neogambogic acid | |
| CN102961443B (en) | Rhizoma menispermi antineoplastic extract, Preparation method and use | |
| Guan et al. | Study on anti-tumor effect of Solanum lyratum Thunb. extract in S180 tumor-bearing mice | |
| WO2018188548A1 (en) | Traditional chinese medicine composition with hypoglycemic effect | |
| CN104069149A (en) | Method for processing traditional Chinese medicine decoction piece by using bear gall as matrix | |
| CN103263492A (en) | Traditional chinese medicine extract | |
| CN102670656B (en) | Chinese medicinal enteric capsules for treating medium-term and advanced tumors and chronic hepatitis B and preparation method for capsules | |
| CN101607009B (en) | Pharmaceutical composition for treating cold |
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 | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20190517 Address after: Fourth Floor, Women's and Children's Activity Center, Changdu West Road, Tibet Autonomous Region, 854000 Patentee after: Enway Pharmaceutical Co., Ltd. Address before: No. 28 Pioneering Road, Chengdu High-tech Industrial Development Zone, Sichuan 610041 Patentee before: Xue Yongxin |
|
| TR01 | Transfer of patent right |