CN101152261A - Application of phenyl ethyl alcohol glycosides and xylogen glycosides component in forsythia (fruit or leaf) - Google Patents
Application of phenyl ethyl alcohol glycosides and xylogen glycosides component in forsythia (fruit or leaf) Download PDFInfo
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Abstract
The invention relates to an application of the components of phenethyl alcohol glycoside and lignin glycoside inside forsythia (fruit or leaf) and belongs to the traditional Chinese medicine processing field. The invention considers the phenethyl alcohol glycoside and the lignin glycoside inside forsythia (fruit or leaf) as a general effective part to be used in the anti-inflammation, resisting bacterium and antivirus field, and the invention provides the application with a high efficient and nonpolluting method which is capable of the industrialized production that is the phenethyl alcohol glycoside and the lignin glycoside can be extracted from the forsythia leaf as well as from the forsythia fruit. The invention discovers that the components of the phenethyl alcohol glycoside and the lignin glycoside inside forsythia (fruit or leaf) has resisting effect towards a plurality of kinds of viruses and bacterium, such as the streptococcus pyogenes, the heamophilus influenza, the Escherichia coli, the staphylococcus epidermis, the deformed streptococcus, the pneumococcus, the deformed bacillus, the influenza virus, the respiratory syncytial virus etc., which lay a foundation for the components of the phenethyl alcohol glycoside and the lignin glycoside inside forsythia (fruit or leaf) to be applied to the clinic as the preparation.
Description
Technical field the present invention relates to a kind of application of phenethyl alcohol glycosides and lignan glycosides component from Fructus Forsythiae (fruit or leaf).The manufacture field that belongs to Chinese medicine.
Background technology Fructus Forsythiae Forsythia suspensa (Thunb.) Vahl is an Oleaceae plant Forsythia machaka, and China removes south China, and outside Tibet and the northwestward region-by-region, all there is distribution all the other each province, and is better with Shanxi product Fructus Forsythiae quality.Fructus Forsythiae is one of modal medical material in the Chinese medicine, and wherein fruit is the medicinal part of traditional medical material Fructus Forsythiae, and " 2005 editions records of Chinese pharmacopoeia Fructus Forsythiae mainly has heat-clearing and toxic substances removing, the effect of mass dissipating and swelling eliminating.The Chinese patent medicine preparation that with the Fructus Forsythiae is principal agent is increasing year by year, and for example: SHUANGHUANGLIAN ZHUSHEYE, SHUANGHUANGLIAN KOUFUYE etc. clinically are used for the treatment of the diseases such as fever and headache that flu causes more.
Traditional medicinal part of Fructus Forsythiae is the dry fruit of Fructus Forsythiae, and the aerial parts of Folium Forsythiae all over the mountains and plains or band leaf then goes out of use.Studies show that, the composition of Folium Forsythiae and fruit has concordance preferably, but the content of effective ingredient such as lignan glycosides and phenethyl alcohol glycosides etc. is than high in the fruit in the leaf, phillyrin content is higher than green grass or young crops far away and sticks up and stick up always in the leaf, its content is about about 40 times that stick up always, 3～4 times of sticking up of green grass or young crops, phillyrin content just are one of important indicators of weighing the Fructus Forsythiae quality of medicinal material.And also do not have technology that Folium Forsythiae is applied to pharmaceutical manufacturing at present, has only a patent (patent No.: 01122779.6 exercise question: a kind of forsythoside extraction process) Folium Forsythiae is applied to extract the Fructus Forsythiae ester glycoside monomer, the monomeric analgesic effect that waits pharmacological action well below phenethyl alcohol glycosides and lignan glycosides summation of Fructus Forsythiae ester glycoside is extracted the relevant patent report that phenethyl alcohol glycosides and lignan glycosides are applied to drug effect aspects such as analgesic, antiinflammatory, antibacterial, antiviral in still have no way of at present Folium Forsythiae or the Fructus Forsythiae.
Summary of the invention the objective of the invention is to phenethyl alcohol glycosides in the Fructus Forsythiae (fruit or leaf) and lignan glycosides as a total effective parts, be applied to antiinflammatory, antibacterial, antiviral field, and for this application provides a kind of efficient height, pollution-free and energy suitability for industrialized production promptly can also can be extracted the method for phenethyl alcohol glycosides and lignan glycosides from Folium Forsythiae from Fructus Forsythiae.Phenethyl alcohol glycosides and lignan glycosides possess anti-inflammatory efficacy in the Fructus Forsythiae (fruit or leaf), have the antiinflammatory action that detumescence is alleviated pain; Phenethyl alcohol glycosides and lignan glycosides component have the vitro inhibition effect to various bacteria as micrococcus scarlatinae, hemophilus influenza, Klebsiella Pneumoniae, escherichia coli, staphylococcus aureus, staphylococcus epidermidis, Streptococcus mutans, streptococcus pneumoniae, Bacillus proteus, Pseudomonas aeruginosa, enterococcus in the Fructus Forsythiae (fruit or leaf).In vivo test is the result show, phenethyl alcohol glycosides and lignan glycosides component are to staphylococcus aureus, streptococcus pneumoniae bacterial strain induced mice protective effect of infection in the Fructus Forsythiae (fruit or leaf); Phenethyl alcohol glycosides and lignan glycosides component are in the external effect that inhibition influenza virus, respiratory syncytial virus, adenovirus type III, Measles virus, coxsackie B 4 viruses and herpes simplex virus are arranged in the Fructus Forsythiae (fruit or leaf).The present invention shows that middle phenethyl alcohol glycosides of Fructus Forsythiae (fruit or leaf) and lignan glycosides have tangible antiinflammatory, antibiotic, antivirus action.
Drug action
1. antiinflammatory action
1). the effect of the rat paw edema model that phenethyl alcohol glycosides and lignan glycosides component on Carrageenan are brought out in the Fructus Forsythiae (fruit or leaf)
After rat divides into groups by body weight, in the right back sufficient plantar subcutaneous injection 1% carrageenin 0.1ml/ of rat only, cause scorching 5h pneumoretroperitoneum drug administration by injection, the dosage of phenethyl alcohol glycosides and lignan glycosides component in the Fructus Forsythiae (fruit or leaf) (following all be called for short " Fructus Forsythiae group ") is respectively 8g crude drug/kg, 4g crude drug/kg, 2g crude drug/kg, positive controls is SHUANGHUANLIAN group (64mg/kg), and blank group is the normal saline group.Measure sufficient sole of the foot volume respectively at different time, calculate the swelling degree, the results are shown in Table 1, Fig. 1.
Effect (ml, the n=10 of the rat paw edema model that phenethyl alcohol glycosides and lignan glycosides component on Carrageenan are brought out in table 1 Fructus Forsythiae (fruit or leaf)
)
| Group | Time (h) | The blank group | Positive controls (64mg/kg) | Fructus Forsythiae group (g/kg) | ||
| High dose (8) | Middle dosage (4) | Low dosage (2) | ||||
| Normally | 0 | 0.94±0.16 | 0.97±0.20 | 0.92±0.22 | 0.88±0.16 | 0.93±0.19 |
| After giving carrageenin | 0.5 1 2 4 5.5 7.5 9.5 11.5 | 1.40±0.23 1.50±0.15 1.63±0.16 1.76±0.13 1.72±0.12 1.59±0.19 1.64±0.23 1.42±0.15 | 1.50±0.29 1.54±0.25 1.82±0.24 1.86±0.28 1.69±0.33 1.60±0.25 1.52±0.28 1.44±0.30 | 1.42±0.24 1.54±0.25 1.71±0.15 1.85±0.27 1.55±0.23 1.54±0.18 1.55±0.17 1.40±0.16 | 1.38±0.18 1.44±0.22 1.65±0.16 1.64±0.18 1.42±0.19 ** 1.49±0.17 1.49±0.20 1.31±0.17 | 1.30±0.20 1.44±0.38 1.80±0.14 * 1.81±0.22 1.59±0.28 1.51±0.31 1.50±0.31 1.44±0.26 |
Annotate: give carrageenin administration after 5 hours; Compare with matched group
*P＜0.05
*P＜0.01
The result shows that phenethyl alcohol glycosides and lignan glycosides component have the effect of obvious suppression rat paw edema in the injection Fructus Forsythiae (fruit or leaf) in institute's amount of reagent scope, and effect lasts till 12h.Similar to SHUANGHUANLIAN positive controls (64mg/kg) effect.
2). phenethyl alcohol glycosides and lignan glycosides component xylol bring out the effect of mice ear model in the Fructus Forsythiae (fruit or leaf)
Animal is divided into 5 groups at random, blank group, SHUANGHUANLIAN positive controls, high, medium and low three the dosage groups of injection Fructus Forsythiae, and dosage sees Table 2, and method is pressed Vam Arman and Zhu Xiu beautiful woman improved method.Experimental result sees Table 2, Fig. 2.
Phenethyl alcohol glycosides and lignan glycosides component xylol bring out the effect (n=10) of mice ear model in table 2 Fructus Forsythiae (fruit or leaf)
Annotate: compare with the blank group
*P＜0.05
*P＜0.01
The result shows, the mice ear effect that phenethyl alcohol glycosides and lignan glycosides component have significant antagonism dimethylbenzene to bring out in the injection Fructus Forsythiae (fruit or leaf), with the blank group relatively have significant difference (
*P＜0.05), similar to SHUANGHUANLIAN positive controls (94mg/kg) effect.
2. bacteriostasis
Phenethyl alcohol glycosides and lignan glycosides component have the vitro inhibition effect to various bacteria as micrococcus scarlatinae, hemophilus influenza, Klebsiella Pneumoniae, escherichia coli, staphylococcus aureus, staphylococcus epidermidis, Streptococcus mutans, streptococcus pneumoniae, Bacillus proteus, Pseudomonas aeruginosa, enterococcus in the Fructus Forsythiae (fruit or leaf).In vivo test is the result show, this component has protective effect to staphylococcus aureus, the infection of streptococcus pneumoniae bacterial strain induced mice;
1). the in-vitro antibacterial experiment
Adopt dish dilution method, antibacterial be inoculated in respectively in the plating medium of each self application, put 37 ℃ cultivate 12h after, from flat board, scrape and get lawn, with the physiological saline solution dilution, measure bacterial concentration with the Maxwell opacity tube, be mixed with 9 * 10
6The CFU/ml dilution of bacteria, from various antibacterial dilution tubes, get 0.05ml bacterium liquid respectively, dibbling does not contain on the contrast flat board of medicine in dull and stereotyped the reaching of each medicine, and observed result behind 37 ℃ of cultivation 24h is minimal inhibitory concentration with the contained antibiotic Cmin of no bacterial growth plate.Micrococcus scarlatinae, streptococcus pneumoniae and hemophilus influenza place 5%CO
2Cultivate the 24h observed result in the incubator.The results are shown in Table 3
Phenethyl alcohol glycosides and lignan glycosides component are to the outer MIC measurement result of 11 kinds of bacterial bodies in table 3 Fructus Forsythiae (fruit or leaf)
| Antibacterial | The strain number | Medicine | MIC scope (g/L) | MIC 50 (g/L) | MIC 90 (g/L) |
| Staphylococcus aureus staphylococcus epidermidis micrococcus scarlatinae streptococcus pneumoniae Streptococcus mutans enterococcus escherichia coli Klebsiella Pneumoniae Bacillus proteus Pseudomonas aeruginosa hemophilus influenza | 49 47 11 10 10 21 56 43 65 49 8 | Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN Fructus Forsythiae SHUANGHUANLIAN | 62.5～125 75～300 62.5～125 37.5～300 62.5～125 37.5～300 62.5～125 18.75～300 62.5～125 75～300 250～600 150～600 62.5～125 37.5～300 62.5～125 37.5～150 125～500 150～600 125～500 150～300 62.5～125 75～300 | 62.5 75 62.5 150 62.5 37.5 62.5 62.5 62.5 75 250 150 62.5 37.5 62.5 37.5 125 150 125 150 62.5 75 | 125 300 126 600 125 300 125 300 125 300 500 600 125 300 125 150 500 600 500 300 125 300 |
Extracorporeal bacteria inhibitor test shows, phenethyl alcohol glycosides and lignan glycosides component have tangible bacteriostasis to micrococcus scarlatinae, hemophilus influenza, Klebsiella Pneumoniae, escherichia coli, staphylococcus aureus, staphylococcus epidermidis, Streptococcus mutans, streptococcus pneumoniae in the Fructus Forsythiae (fruit or leaf), Bacillus proteus, Pseudomonas aeruginosa, enterococcus are had certain inhibitory action, but inhibitory action there is not above-mentioned antibacterial obvious.
2). antibacterial tests in the body
With the mice random packet, 10 every group, male and female are all used.Bacterium stock solution is diluted desired concn with yeast, and the bacterium liquid inductance that is equivalent to 100% minimum lethal dose through lumbar injection dyes mice.At once inject with the 6h pneumoretroperitoneum after infection, medicine liquid volume is 0.5ml.Observe 7d record dead mouse situation, calculate the ED of every kind of medicine with the Bliss method
50With 95% fiducial limit.
Phenethyl alcohol glycosides and lignan glycosides component see Table 4 and table 5 respectively to the endogenous protective result of the test of staphylococcus aureus S9811 strain and streptococcus pneumoniae 3011 infecting mouses in the Fructus Forsythiae (fruit or leaf).
Phenethyl alcohol glycosides and lignan glycosides component are to the endogenous protective experiment of infection of staphylococcus aureus mice in table 4 Fructus Forsythiae (fruit or leaf)
| Medicine | Dosage (g/kg) | Log10 dose | Number of animals (only) | Death toll (only) | Mortality rate (%) |
| Fructus Forsythiae SHUANGHUANLIAN normal saline | 0.76 0.38 0.19 0.095 0.047 0.600 | -0.1192 -0.4202 -0.7212 -1.0223 -1.3279 | 10 10 10 10 10 10 10 | 0 2 4 6 10 1 10 | 0 20.00 40.00 60.00 100.0 10.00 100.0 |
According to result of the test, adopt the Bliss software processes, ED
50For: 0.1550g/kg
Table 5 Fructus Forsythiae is to the endogenous protective test of pneumococcal infection mice
| Medicine | Dosage (g/kg) | Log10 dose | Number of animals (only) | Death toll (only) | Mortality rate (%) |
| Fructus Forsythiae SHUANGHUANLIAN normal saline | 0.76 0.38 0.19 0.095 0.047 0.60 | -0.1192 -0.4202 -0.7212 -1.0223 -1.3279 | 10 10 10 10 10 10 10 | 1 2 4 6 8 2 10 | 10.00 20.00 40.00 60.00 80.00 20.00 100.00 |
In vivo test is the result show, phenethyl alcohol glycosides and lignan glycosides component have significant protective effect, its ED to staphylococcus aureus, the infection of streptococcus pneumoniae bacterial strain induced mice in the Fructus Forsythiae (fruit or leaf)
50Be respectively 0.1552g/kg, 229.3737～421.3597g/kg with 95% fiducial limit; 0.1457g/kg, 301.3706～488.6162g/kg; 74g/kg.
3. antivirus action
1). phenethyl alcohol glycosides and lignan glycosides component are to the pathological changes caused by virus protective effect in the Fructus Forsythiae (fruit or leaf)
Infecting 30-100TCID
50The situation of 6 kinds of viruses under, phenethyl alcohol glycosides and lignan glycosides component are in the concentration range of 31.2g/L～3.90g/L in the Fructus Forsythiae (fruit or leaf), influenza virus, respiratory syncytial virus, adenovirus type III and Measles virus there is its cytopathic effect of obvious suppression, to Coxsackie B virus
4, herpes simplex virus I-type also has certain pathological changes caused by virus effect that delays, its effect the results are shown in Table 6 not as obvious to preceding four kinds of viruses.
Phenethyl alcohol glycosides and lignan glycosides component are to the pathological changes caused by virus effect in table 6 Fructus Forsythiae (fruit or leaf)
| Strain | Infective dose (TCID 50) | SHUANGHUANGLIAN 2.343g/L | Fructus Forsythiae 15.62g/L | The cell contrast | Virus control |
| Influenza FM 1 RSV AdV-3 MV | 100 30 100 30 | - - - ± | - - - - | - - - - | ++++ ++++ ++++ ++++ |
| CVB 3 HSV-I | 50 100 | ± - | ± + | - - | ++++ ++++ |
Annotate :-acellular pathological changes shown; ± be shown with and delay cytopathic effect; + show the cytopathy below 1/4; ++ show that 1/4～1/2 cell has pathological changes; The cell of +++show 1/2～3/4 has pathological changes; ++ ++ show that the cell more than 3/4 has pathological changes.
2). phenethyl alcohol glycosides and lignan glycosides component are to the influence of mice influenza virus property pneumonia in the Fructus Forsythiae (fruit or leaf)
Phenethyl alcohol glycosides and lignan glycosides component adopt the EXCEL statistical software to the result that influences of mice pneumonia in the Fructus Forsythiae (fruit or leaf), carry out two groups of mean T checks, see table 6 for details.In 0.12g/kg/d and above metering, have significant therapeutic effect, the results are shown in Table 7.
Phenethyl alcohol glycosides and lignan glycosides component are to the effect of mice influenza virus property pneumonia in table 7 Fructus Forsythiae (fruit or leaf)
The extraction processing method of phenethyl alcohol glycosides and lignan glycosides component is as follows in the Fructus Forsythiae (fruit or leaf):
1. the medicinal part of medical material is selected
Be used as fruit or Folium Forsythiae that the Fructus Forsythiae that extracts processing phenethyl alcohol glycoside and lignan glycosides component is meant Fructus Forsythiae among the present invention.
2. the roughing of medical material
Fructus Forsythiae: the Fructus Forsythiae that is used as medical material among the present invention can be Fructus Forsythiae fresh harvesting or exsiccant, Fructus Forsythiae can be directly as medical material, or can be ground into the powder of suitable size by common pulverizer, also can become superfine powder or become nano level powder by micronizing by nanometer collider pulverizing.The thickness of powder depends on dosage form and preparation technology's needs.
Folium Forsythiae: the Folium Forsythiae that is used as medical material among the present invention can be Folium Forsythiae fresh harvesting or exsiccant or band leaf aerial parts.Folium Forsythiae can be directly as medical material, or can be cut into the leaf silk of suitable size by microtome, or is ground into the powder of suitable size by common pulverizer, also can become superfine powder or become nano level powder by nanometer collider pulverizing by micronizing.The thickness of powder depends on dosage form and preparation technology's needs.The bright leaf of Fructus Forsythiae also can directly adopt the composition in the milling process extraction leaf, or pushes the extraction of squeezing the juice by adding an amount of water.
3. the extracting method of medical material
Is Folium Forsythiae of the present invention or Fructus Forsythiae extract by above-mentioned various Folium Forsythiae or Fructus Forsythiae medical material through the resulting total lignin glycosides of extraction separation purification and total phenethyl alcohol glycosides.Extract also refers to further to separate with total phenethyl alcohol glycoside apoplexy due to endogenous wind and the single chemical constituent that obtains from total lignin glycosides.Folium Forsythiae of the present invention or Fructus Forsythiae extract are meant and adopt water extraction, decoction and alcohol sedimentation technique, alcohol extracting method, ethanol extract from water precipitation, percolation, supercritical carbon dioxide extraction method, macroporous adsorbent resin method, ethyl acetate or resulting Folium Forsythiae of n-butyl alcohol heat reflow method or Fructus Forsythiae extract, also comprise squeezing the juice of bright leaf, and concentrate, dry thing.
1). water extraction: the technology that water extraction of the present invention is produced Folium Forsythiae or Fructus Forsythiae extract is meant that powder with blade, leaf silk, coarse powder or the Fructus Forsythiae of Folium Forsythiae is under the condition more than 50 ℃, percentage by weight by medical material and water is 1: 6-1: 35 extracting in waters are more than 0.5 hour, extracting solution merges, promptly.
2). alcohol extracting method: the technology that alcohol extracting method of the present invention is produced Folium Forsythiae or Fructus Forsythiae extract is meant that powder with Folium Forsythiae blade, leaf silk, coarse powder or Fructus Forsythiae is under the condition more than 50 ℃, by medical material and alcoholic acid percentage by weight is 1: 6-1: 35 added the 50%-95% ethanol extraction more than 0.5 hour, extracting solution merges, behind the decompression recycling ethanol, promptly.
3). decoction and alcohol sedimentation technique: the technology that decoction and alcohol sedimentation technique of the present invention is produced Folium Forsythiae or Fructus Forsythiae extract is meant that powder with Folium Forsythiae blade, leaf silk, coarse powder or Fructus Forsythiae is under the condition more than 50 ℃, percentage by weight by medical material and water is 1: 6-1: 35 extracting in waters are more than 0.5 hour, extracting solution merges, be condensed into thick paste, add ethanol to remove macromolecule impurity, add alcoholic acid amount and be 50%-95% for contain the alcohol amount to medicinal liquid, staticly settle, filter, behind the alcohol deposit fluid decompression recycling ethanol, promptly.
4). ethanol extract from water precipitation: the technology that ethanol extract from water precipitation of the present invention is produced Folium Forsythiae or Fructus Forsythiae extract is meant that powder with Folium Forsythiae blade, leaf silk, coarse powder or Fructus Forsythiae is under the condition more than 50 ℃, by medical material and alcoholic acid percentage by weight is 1: 6-1: 35 added the 50%-95% ethanol extraction more than 0.5 hour, extracting solution merges, behind the decompression recycling ethanol, staticly settle, filter, medicinal liquid promptly.
5). alcohol percolation method: the technology that percolation of the present invention is produced Folium Forsythiae or Fructus Forsythiae extract is meant in the percolator of packing into after the powder moistening with Folium Forsythiae blade, leaf silk, coarse powder or Fructus Forsythiae, by medical material and alcoholic acid percentage by weight is 1: 6-1: 35 add the 50%-95% ethanol percolation, percolate merges, behind the decompression recycling ethanol, medicinal liquid promptly.
6). the technology that supercritical carbon dioxide extraction method of the present invention is produced Folium Forsythiae or Fructus Forsythiae extract is meant packs the powder of Folium Forsythiae blade, leaf silk, coarse powder or Fructus Forsythiae in the extraction kettle into, with supercritical carbon dioxide extraction method (can add an amount of entrainer, pH value regulator as required) effective ingredient in the medical material is extracted, decompress(ion) is removed carbon dioxide again, residue is collected, promptly.
4. initial gross separation
The macroporous adsorbent resin method:
The Folium Forsythiae or the Fructus Forsythiae extract of gained can obtain initial gross separation through macroporous adsorbent resin method of the present invention again after above-mentioned arbitrary method is extracted.The technology that macroporous adsorbent resin legal system of the present invention is got Folium Forsythiae extract or Fructus Forsythiae extract is meant the Folium Forsythiae extracting solution or the Fructus Forsythiae extracting solution of said method gained, through macroporous adsorptive resins absorption effective ingredient, discard effluent, continue with 10%-95% ethanol elution macroporous adsorptive resins, till making absorption effective ingredient thereon by complete eluting, behind the eluent decompression recycling ethanol, promptly.
5. purification
Folium Forsythiae extract that initial gross separation obtains or Fructus Forsythiae extract need can reach the preparation requirement through the following steps purification.
1). ethyl acetate heat reflow method of the present invention is produced Folium Forsythiae or the Fructus Forsythiae extract that the technology of phenethyl alcohol glycosides and lignan glycosides component in the Fructus Forsythiae (fruit or leaf) is meant the said method gained, through adsorbing materials such as kieselguhr absorption effective ingredient, percentage by weight by kieselguhr (or other adsorbing materials) and ethyl acetate is 1: 6-1: 45 added ethyl acetate extraction more than 0.5 hour, extracting solution merges, reclaim ethyl acetate, promptly.
2). n-butyl alcohol heat reflow method of the present invention is produced Folium Forsythiae or the Fructus Forsythiae extract that the technology of phenethyl alcohol glycosides and lignan glycosides component in the Fructus Forsythiae (fruit or leaf) is meant the said method gained, through adsorbing materials such as kieselguhr absorption effective ingredient, percentage by weight by kieselguhr (or other adsorbing materials) and n-butyl alcohol is 1: 6-1: 45 added n-butanol extraction more than 0.5 hour, extracting solution merges, reclaim n-butyl alcohol, promptly.
The invention has the advantages that middle phenethyl alcohol glycosides of a Fructus Forsythiae (fruit or leaf) and lignan glycosides component are as a total effective parts, be applied to antiinflammatory, antibacterial, antiviral field, and for the first time find that it has inhibitory action to multiple virus, antibacterial, be applied to clinical laying the foundation for from now on phenethyl alcohol glycosides in the Fructus Forsythiae (fruit or leaf) and lignan glycosides component being made preparation.The invention has the advantages that to this application provides a kind of efficient high the method for middle phenethyl alcohol glycosides of pollution-free and energy suitability for industrialized production Fructus Forsythiae (fruit or leaf) and lignan glycosides component.Extraction process is with low cost, and is safe and effective, and production technology is simple, is suitable for pharmaceutical factory large-scale production.
Description of drawings
The rat paw edema action effect curve that phenethyl alcohol glycosides and lignan glycosides component on Carrageenan are brought out in Fig. 1 Fructus Forsythiae (fruit or leaf)
Phenethyl alcohol glycosides and lignan glycosides component xylol bring out the action effect figure of mice ear model in Fig. 2 Fructus Forsythiae (fruit or leaf)
The specific embodiment
Embodiment 1:
Get Folium Forsythiae or Fructus Forsythiae 1000g, clean removing impurity, after the drying, be ground into 5-60 purpose powder with pulverizer, add 20 liters in water, decoct and extracted merge extractive liquid, three times in 1 hour, promptly get Folium Forsythiae or Fructus Forsythiae water extract, the water extract directly by AB-8 type macroporous adsorptive resins absorption effective ingredient, discards effluent, continues and uses 70% ethanol elution, collect 70% ethanol elution 200ml, concentrating under reduced pressure is used the 0.15g diatomite adsorption, mixes thoroughly, behind the bone dry, add ethyl acetate 30ml, decoct and extract merging filtrate three times, the reclaim under reduced pressure ethyl acetate promptly gets phenethyl alcohol glycosides and lignan glycosides in the Fructus Forsythiae (fruit or leaf).Phenethyl alcohol glycosides and lignan glycosides component are used for the experiment of the rat paw edema model effect that on Carrageenan brings out in this Fructus Forsythiae (fruit or leaf), obtain the results are shown in Table 1.
Embodiment 2:
Get Folium Forsythiae or Fructus Forsythiae 1000g, clean, after the drying, be ground into 5-60 purpose powder with pulverizer to remove impurity, add 20 liters of 80% ethanol, decoct and extracted 2 hours, filter, decompression filtrate recycling ethanol behind the concentrate drying, promptly gets Folium Forsythiae or Fructus Forsythiae ethanol extraction.Ethanol extraction, water-soluble, by AB-8 type macroporous adsorptive resins absorption effective ingredient, discard effluent, continue and use 70% ethanol elution, collect 70% ethanol elution 200ml, concentrating under reduced pressure, use the 0.15g diatomite adsorption, stir evenly bone dry after, add n-butyl alcohol 30ml, decoct and extract three times, merging filtrate, the reclaim under reduced pressure n-butyl alcohol promptly gets phenethyl alcohol glycosides and lignan glycosides in the Fructus Forsythiae (fruit or leaf).Phenethyl alcohol glycosides and lignan glycosides component are used for the experiment that xylol brings out the effect of mice ear model in this Fructus Forsythiae (fruit or leaf), obtain the results are shown in Table 2.
Embodiment 3:
Get Folium Forsythiae or Fructus Forsythiae 1000g, clean removing impurity, after the drying, be ground into 5-200 purpose powder with pulverizer, add 10 liters in water, decoct and extracted 2 hours, extracting solution is condensed into thick paste, and adding ethanol is 70% to making medicinal liquid contain the alcohol amount, staticly settle, filter, behind the decompression filtrate recycling ethanol, concentrate, drying promptly gets Folium Forsythiae or Fructus Forsythiae water extracting alcohol hypostasis.The water extract-alcohol precipitation extract, water-soluble, by AB-8 type macroporous adsorptive resins absorption effective ingredient, discard effluent, continue and use 70% ethanol elution, collect 70% ethanol elution 200ml, concentrating under reduced pressure is used the 0.15g diatomite adsorption, mixes thoroughly, behind the bone dry, add ethyl acetate 30ml, decoct and extract merging filtrate three times, the reclaim under reduced pressure ethyl acetate promptly gets phenethyl alcohol glycosides and lignan glycosides in the Fructus Forsythiae (fruit or leaf).Phenethyl alcohol glycosides and lignan glycosides component are used for the experiment to the outer MIC mensuration of 11 kinds of bacterial bodies in this Fructus Forsythiae (fruit or leaf), obtain the results are shown in Table 3.
Embodiment 4:
Get Folium Forsythiae or Fructus Forsythiae 1000g, clean removing impurity, after the drying, be ground into 5-200 purpose powder with pulverizer, add 10 liters of 80% ethanol, decoct and extracted 2 hours, filter, behind the decompression filtrate recycling ethanol, add water to 50 liters, staticly settle, filter, filtrate concentrates, and drying promptly gets Folium Forsythiae or Fructus Forsythiae alcohol extracting-water precipitating thing.The alcohol extracting-water precipitating extract directly by AB-8 type macroporous adsorptive resins absorption effective ingredient, discards effluent, continue and use 70% ethanol elution, collect 70% ethanol elution 200ml, concentrating under reduced pressure, use the 0.15g diatomite adsorption, mix thoroughly, behind the bone dry, add ethyl acetate 30ml, decoct and extract three times, merging filtrate, the reclaim under reduced pressure ethyl acetate promptly gets phenethyl alcohol glycosides and lignan glycosides in the Fructus Forsythiae (fruit or leaf).Phenethyl alcohol glycosides and lignan glycosides component are used for the endogenous protective experiment to the infection of staphylococcus aureus mice in this Fructus Forsythiae (fruit or leaf), obtain the results are shown in Table 4.
Embodiment 5:
Get Folium Forsythiae or Fructus Forsythiae 1000g, clean to remove impurity, after the drying, be ground into 5-200 purpose powder with pulverizer, pack into after the moistening in the percolator, 50% ethanol 6L percolation, percolate merges, behind the decompression recycling ethanol, residue is collected, concentrate, drying promptly gets Folium Forsythiae or Fructus Forsythiae percolation extract.Percolation extract, water-soluble, by AB-8 type macroporous adsorptive resins absorption effective ingredient, discard effluent, continue and use 70% ethanol elution, collect 70% ethanol elution 200ml, concentrating under reduced pressure, use the 0.15g diatomite adsorption, stir evenly bone dry after, add n-butyl alcohol 30ml, decoct and extract three times, merging filtrate, the reclaim under reduced pressure n-butyl alcohol promptly gets phenethyl alcohol glycosides and lignan glycosides in the Fructus Forsythiae (fruit or leaf).Phenethyl alcohol glycosides and lignan glycosides component are used for the experiment to the pathological changes caused by virus effect in this Fructus Forsythiae (fruit or leaf), obtain the results are shown in Table 6.
Embodiment 6:
Get Folium Forsythiae or Fructus Forsythiae 1000g, clean to remove impurity, after the drying, be ground into 5-200 purpose powder with pulverizer, in the extraction kettle of packing into, fed supercritical carbon dioxide extraction 3 hours, decompress(ion) is removed carbon dioxide, and residue is collected, and concentrates, drying promptly gets Folium Forsythiae or Fructus Forsythiae supercritical extract.Supercritical extract, water-soluble, by AB-8 type macroporous adsorptive resins absorption effective ingredient, discard effluent, continue and use 70% ethanol elution, collect 70% ethanol elution 200ml, concentrating under reduced pressure, use the 0.15g diatomite adsorption, stir evenly bone dry after, add n-butyl alcohol 30ml, decoct and extract three times, merging filtrate, the reclaim under reduced pressure n-butyl alcohol promptly gets phenethyl alcohol glycosides and lignan glycosides in the Fructus Forsythiae (fruit or leaf).Phenethyl alcohol glycosides and lignan glycosides component are used for the experiment to the effect of mice influenza virus property pneumonia in this Fructus Forsythiae (fruit or leaf), obtain the results are shown in Table 7.
Claims (6)
1. the present invention relates to the application of middle phenethyl alcohol glycosides of a kind of Fructus Forsythiae (fruit or leaf) and lignan glycosides component, it is characterized in that: phenethyl alcohol glycosides and lignan glycosides component have antiinflammatory, antibacterial, antivirus action in the described Fructus Forsythiae (fruit or leaf).
2. the application of phenethyl alcohol glycosides and lignan glycosides component in a kind of Fructus Forsythiae according to claim 1 (fruit or leaf) is characterized in that: described antiinflammatory action is meant the mice ear effect that middle phenethyl alcohol glycosides of Fructus Forsythiae (fruit or leaf) and lignan glycosides component have inhibition rat paw edema and antagonism dimethylbenzene to bring out.
3. the application of phenethyl alcohol glycosides and lignan glycosides component in a kind of Fructus Forsythiae according to claim 1 (fruit or leaf), it is characterized in that: described bacteriostasis is meant that middle phenethyl alcohol glycosides of Fructus Forsythiae (fruit or leaf) and lignan glycosides component to various bacteria, have the vitro inhibition effect as micrococcus scarlatinae, hemophilus influenza, Klebsiella Pneumoniae, escherichia coli, staphylococcus aureus, staphylococcus epidermidis, Streptococcus mutans, streptococcus pneumoniae, Bacillus proteus, Pseudomonas aeruginosa, enterococcus.In vivo test is the result show, this component has protective effect to staphylococcus aureus, the infection of streptococcus pneumoniae bacterial strain induced mice.
4. the application of phenethyl alcohol glycosides and lignan glycosides component in a kind of Fructus Forsythiae according to claim 1 (fruit or leaf), it is characterized in that: described antivirus action is meant that phenethyl alcohol glycosides and lignan glycosides component are in the concentration range of 31.2g/L～3.90g/L, to influenza virus, respiratory syncytial virus, adenovirus type III, Measles virus, Coxsackie B virus in the Fructus Forsythiae (fruit or leaf)
4, herpes simplex virus I-type has and suppresses its cytopathic effect.
5. the application of phenethyl alcohol glycosides and lignan glycosides component in a kind of Fructus Forsythiae according to claim 1 (fruit or leaf), it is characterized in that: described antivirus action is meant that middle phenethyl alcohol glycosides of Fructus Forsythiae (fruit or leaf) and lignan glycosides component are in 0.12g/kg/d and above metering, to mice influenza virus property pneumonia therapeutical effect.
6. the present invention relates to the application of middle phenethyl alcohol glycosides of a kind of Fructus Forsythiae (fruit or leaf) and lignan glycosides component, it is characterized in that: its extract is phenethyl alcohol glycosides and a lignan glycosides component in the Fructus Forsythiae (fruit or leaf), in the Fructus Forsythiae (fruit or leaf) phenethyl alcohol glycosides and lignan glycosides component be meant from the Folium Forsythiae powder or/and the Folium Forsythiae extract separation and purification to total lignin glycosides, total caffeoyl phenethyl alcohol glycosides, also can be meant further from total lignin glycosides, total caffeoyl phenethyl alcohol glycoside apoplexy due to endogenous wind and separate and the single chemical constituent that obtains; Concrete extracting mode is: water extraction, decoction and alcohol sedimentation technique, alcohol extracting method, ethanol extract from water precipitation, percolation, supercritical carbon dioxide extraction method, macroporous adsorbent resin method and ethyl acetate (n-butyl alcohol) kieselguhr heat reflow method.
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| CNA2007101213274A CN101152261A (en) | 2007-09-04 | 2007-09-04 | Application of phenyl ethyl alcohol glycosides and xylogen glycosides component in forsythia (fruit or leaf) |
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| CNA2007101213274A CN101152261A (en) | 2007-09-04 | 2007-09-04 | Application of phenyl ethyl alcohol glycosides and xylogen glycosides component in forsythia (fruit or leaf) |
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| CN105287610A (en) * | 2014-06-27 | 2016-02-03 | 石家庄以岭药业股份有限公司 | Application of forsythiaside I and preparation method thereof |
| CN104027401A (en) * | 2014-07-07 | 2014-09-10 | 河南太龙药业股份有限公司 | Shuanghuanglian medicine combination used for virus resisting, heat clearing and inflammation diminishing of children and preparing method thereof |
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| CN105560257A (en) * | 2016-01-05 | 2016-05-11 | 李春华 | Novel drug for treating bacterial infection |
| CN108776222A (en) * | 2018-06-14 | 2018-11-09 | 吉林省农业科学院 | Gongzhuling mycin bacteriostatic activity detection method and application |
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