CN101167799A - Scutellaria barbata total flavone and its application in preparing influenza virus resisting medicine - Google Patents
Scutellaria barbata total flavone and its application in preparing influenza virus resisting medicine Download PDFInfo
- Publication number
- CN101167799A CN101167799A CNA2007100472572A CN200710047257A CN101167799A CN 101167799 A CN101167799 A CN 101167799A CN A2007100472572 A CNA2007100472572 A CN A2007100472572A CN 200710047257 A CN200710047257 A CN 200710047257A CN 101167799 A CN101167799 A CN 101167799A
- Authority
- CN
- China
- Prior art keywords
- scutellariae barbatae
- herba scutellariae
- influenza virus
- total flavone
- total flavones
- 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 relates to total flavone of barbat skullcap and new usage in the preparation of anti-influenza virus drug, belonging to the field of traditional Chinese medicine. The total flavone of barbat skullcap of the invention is total flavone extract which is separated and extracted from the dry aerial part of barbat skullcap which belongs to labiatae scutellaria plant and grows in China. Tested by mass spectrum and 13C, 1H, the total flavone extract of barbat skullcap contains active chemical component 5, 7, 4'-tri-hydroxyl flavone (apigenin) of the above chemical structure. The total flavone extract is tested by in vitro cell model and in vivo animal model and proved to have strong activity of anti-influenza virus. The total flavone extract and active component apigenin can be further prepared into anti-influenza virus drug and the dosage forms can be capsules, tablets, granules, and injection and the like.
Description
Technical field
The invention belongs to the field of Chinese medicines, relate to a kind of anti-influenza virus medicament, be specifically related to Herba Scutellariae Barbatae total flavones and the new purposes in the preparation anti-influenza virus medicament thereof.
Background technology:
Herba Scutellariae Barbatae is the dry herb of Labiatae Scutellaria plant Scutellaria barbate, main product in Jiangsu of China, ground such as Jiangxi, Fujian, Guangdong, resource is abundanter.Its main component is flavone compound, diterpene and diterpene ginkgolide, polysaccharide, also has the necessary trace element of abundant human body etc.The tradition traditional Chinese medical science is thought Herba Scutellariae Barbatae property suffering, hardship, cold, goes into lung, liver, kidney, and effect heat-clearing and toxic substances removing, blood stasis dispelling diuresis cure mainly worm venom, the swollen toxic swelling of skin ulcer, infectious hepatitis, cirrhotic ascites, oedema due to nephritis, traumatic injury.Herba Scutellariae Barbatae is widely used in the traditional Chinese medical science, and composition and the pharmacologically active of relevant Herba Scutellariae Barbatae have had comparatively deep research.Discover that Herba Scutellariae Barbatae is showing certain effect aspect analgesic, anticancer, hepatoprotective, immunomodulating, antibacterial, anti-ageing the waiting for a long time.Employing mice oxter inoculated tumour cell methods such as Wang Gang have been measured the anti-tumor activity of Herba Scutellariae Barbatae ethanol extract, show that the Herba Scutellariae Barbatae ethanol extract has significant inhibitory effect to transplanted tumor, and dose-dependence (Wang Gang preferably arranged, Dong Mei, the research [J] of Herba Scutellariae Barbatae ethanol extract anti-tumor activity, modern combination of Chinese and Western medicine magazine, 2004,12:9).Xie Luokun etc. studies show that the Herba Scutellariae Barbatae ethanol extraction can obviously suppress human myeloid leukemia K562 cell proliferation, make the K562 cell morphology and biochemical characteristics that apoptosis has occur, propagation inhibition and apoptosis-induced effect to the K562 cell simultaneously has certain concentration dependent (Xie Luokun, Deng Tao, Herba Scutellariae Barbatae extract inducing leukemia K562 apoptosis [J], Wuhan University's journal (medicine), 2004,25 (2)).
The foreign study person finds, separates the Flavonoid substances that obtains and can effectively suppress methicillin-resistant staphylococcus aureus resistance (MRSA) from Herba Scutellariae Barbatae.
Take a broad view of report both domestic and external, there is no Herba Scutellariae Barbatae (Scutellaria barbate) dry aerial parts extractive of general flavone resisiting influenza virus drug effect and with the medicine of its preparation.
Summary of the invention
The purpose of this invention is to provide Herba Scutellariae Barbatae total flavones and the new purposes in the preparation anti-influenza virus medicament thereof.
Herba Scutellariae Barbatae total flavones of the present invention be from the dry aerial parts of my home-made Labiatae Scutellaria plant Herba Scutellariae Barbatae (the medical material Chinese: Herba Scutellariae Barbatae, Scutellariae barbaae, Herba) separation and Extraction obtains extractive of general flavone, through mass spectrum and
13C,
1H measures, confirm described Herba Scutellariae Barbatae total flavones extract contain effective chemical constituent 5,7,4 '-trihydroxyflavone (apigenin), its chemical constitution is as follows:
Described extractive of general flavone behind the animal model test, confirms that it has very strong anti-influenza virus activity in cell in vitro model and body.
Described extractive of general flavone can further prepare anti-influenza virus medicament, makes capsule, tablet, dosage forms such as granule and injection.Described active component apigenin also can be made into dosage forms such as capsule, tablet, granule and injection.
The specific embodiment
Embodiment 1
1) extract Herba Scutellariae Barbatae total flavones:
Get the Chinese crude drug Herba Scutellariae Barbatae, use the 50-80% alcohol extraction, concentrate petroleum ether extraction, D-101 macroporous resin on the aqueous portion, water and ethanol gradient elution are collected eluent, detect through magnesium powder/hydrochloric acid, collect the high part of flavones content, be concentrated into driedly that solid content is the effective site product, the effective site product yield reaches more than 1%, and wherein general flavone content surpasses 50%.Through biological activity assay, described total flavones has the activity of obvious suppression influenza virus.
Concrete extraction and result relate to:
Lixiviate: crude drug weight 1000 grams
Extractum 131 gram yields: 13.1%
Macroporous resin separates:
Weight 17.7 gram yields 1.77%
General flavone content 57.5% total flavones yield 1.0%.
2) structure is identified
Through mass spectrum and
13C,
1H measures, and confirms that extract Herba Scutellariae Barbatae total flavones of the present invention contains chemical constituent 5,7,4 '-trihydroxyflavone (apigenin), and its chemical constitution is as follows:
Through biological activity assay, described apigenin has the biological activity of good vitro inhibition influenza virus.
3) Herba Scutellariae Barbatae total flavones suppresses experiment to popular type cold virus
(1) 96 orifice plates are adopted in experiment, and cell is Testis et Pentis Canis passage cell (MDCK), and virus is H
1N
1Influenza A virus (from the Chinese Academy of Medical Sciences), every hole adds 100TCID
50Virus, 5%CO
237 ℃ of absorption added described extractive of general flavone, observation of cell pathological changes effect (CPE) after 72 hours after 2 hours.The result shows:
TC
50＝150μg/ml，EC
50＝37.5μg/ml，TI＝4。
(2) apigenin is external inhibited to popular type cold virus, and the result shows:
TC
50＝50μg/ml，EC
50＝8.5μg/ml，TI＝5.88。
(3) anti-influenza virus activity animal experiment in the Herba Scutellariae Barbatae total flavones body
Adopt the kunming mice (laboratory animal portion of Fudan University) of 17-18g, virus control group, ribavirin group (100mg/kg), heavy dose of group (45mg/kg), middle dosage group (11.5mg/kg), small dose group (2.8mg/kg) are set, every group of male and female half and half.Virus adopts FM strain (available from the Chinese Academy of Medical Sciences), 10TCID
50The virus of concentration infects with nasal drip, and viral infection is oral administration after 2 hours.Write down the dead mouse situation every day, continuous record 14 days.In addition, in infecting 4 mices of every group of dissection in the 5th day, its pneumonopathy range degree detects by an unaided eye.
Experimental result shows:
(1) Herba Scutellariae Barbatae total flavones can effectively reduce the pneumonopathy variable area behind the influenza infection.Compare with the virus control group, it is 63.16%, 46.28% and 27.27% that heavy dose of group (45mg/kg), middle dosage group (11.5mg/kg), small dose group (2.8mg/kg) reduce the pneumonopathy variable area; And ribavirin group (100mg/kg) reduces pneumonopathy variable area 50.41%.The Herba Scutellariae Barbatae total flavones of heavy dose of group can effectively reduce pneumonopathy variable area behind the viral infection.
Table 1 is the influence that Herba Scutellariae Barbatae total flavones reduces mouse lung pathological changes area.
(2) Herba Scutellariae Barbatae total flavones has the protective effect to mice life.Compare with the virus control group, heavy dose of group (45mg/kg), middle dosage group (11.5mg/kg), small dose group (2.8mg/kg) make the life of virus infected mice prolong 74.51%, 41.18% and 35.29%; And ribavirin (100mg/kg) makes the life of virus infected mice prolong 73.52%.Show that described Herba Scutellariae Barbatae total flavones extract has the very strong protective effect to mice life.
Table 2 is Herba Scutellariae Barbatae total flavones protective effects to mice life.
Table 1
Table 2
| Medicine | Dosage | The The average survival time natural law (my god) | ||||||||
| Male | p | Female | p | Total | P | |||||
| Virus control | 5.0±1.0 | 5.1±1.2 | 5.1±1.0 | |||||||
| Ribavirin | 100mg/kg | 8.3±2.0 | 0.004 | 9.5±2.1 | 0.018 | 8.9±2.0 | 0.003 | |||
| Medicine | 45.0mg/kg | 8.5±3.0 | 0.006 | 9.3±2.6 | 0.001 | 8.9±2.7 | ＜0.001 | |||
| 11.5mg/kg | 6.8±0.8 | 0.002 | 7.5±0.5 | ＜0.001 | 7.2±0.7 | ＜0.001 | ||||
| 2.81mg/kg | 6.7±1.0 | 0.008 | 7.2±0.4 | 0.001 | 6.9±0.8 | ＜0.001 | ||||
| Ribavirin 4.4 | Life prolongs | |||||||||
| Male | Female | Total | ||||||||
| Prolong natural law 100mg/kg 86.27% | Prolong natural law 3.3 3.75 | Prolong natural law 66% 73.52% | ||||||||
| 45.0mg/kg | 3.5 | 70％ | 4.2 | 82.3％ | 3.8 | 74.51％ | ||||
| 41.18％ 35.29％ | Medicine | 11.5mg/kg | 1.8 | 36％ | 2.4 | 47.1％ | 2.1 | |||
| 2.81mg/kg | 1.7 | 34％ | 2.1 | 41.2％ | 1.8 | |||||
| IC 50 | 23.1mg/kg | 12.15mg/kg | 18.9mg/kg | |||||||
Embodiment 2
Get prepared Herba Scutellariae Barbatae total flavones extract 50 grams, pulverized 100 mesh sieves, add starch 3 gram mix homogeneously, add 10% starch slurry again and make soft material in right amount, 20 eye mesh screens are granulated, 60-70 ℃ of drying, cross 30 mesh sieve granulate, add hydroxypropyl cellulose 3 grams and the abundant mixing of magnesium stearate 1 gram, tabletting, film coating makes 1000.Every contains extractive of general flavone 50mg.
Embodiment 3
Get prepared Herba Scutellariae Barbatae total flavones extract 50 grams, pulverized 100 mesh sieves, add starch 3 grams, microcrystalline cellulose is an amount of, granulate with Diluted Alcohol, 20 eye mesh screens are granulated, 60-70 ℃ of drying, granulate, it is an amount of to add magnesium stearate, and fully mixing is inserted capsule promptly, 1000.
Embodiment 4
Get prepared Herba Scutellariae Barbatae total flavones extract 30 grams, pulverized 100 mesh sieves, add starch 300 grams, add 10% starch slurry and make granule in right amount, 60-70 ℃ of drying, packing.
Embodiment 5
Get prepared Herba Scutellariae Barbatae total flavones extract 50 grams, add an amount of water for injection, heating for dissolving, add 0.5% active carbon again and fully stir, boiled 20 minutes, filter, be cooled to room temperature, freezer spends the night, and adds the injection water to 1000ml, regulates pH to 7 with sodium bicarbonate, filtration sterilization, fill is sealed, and sterilization promptly gets injection.Specification is transferred 2ml, 10ml, 100ml.
Claims (4)
1. the Herba Scutellariae Barbatae total flavones extract is in the purposes of preparation in the anti-influenza virus medicament.
2. by the described purposes of claim 1, it is characterized in that described Herba Scutellariae Barbatae total flavones extract, prepare by following method: the dry aerial parts of getting Chinese crude drug Herba Scutellariae Barbatae scutellariae barbatae, use the 50-80% alcohol extraction, concentrate petroleum ether extraction, D-101 macroporous resin on the aqueous portion, water and ethanol gradient elution are collected eluent, detect through magnesium powder/hydrochloric acid, collect the high part of flavones content, be concentrated into dried, effective site, wherein general flavone content surpasses 50%.
3. by the described purposes of claim 1, it is characterized in that containing chemical constituent 5,7 in the described Herba Scutellariae Barbatae total flavones extract, 4 '-trihydroxyflavone, its chemical constitution is as follows:
4. by the purposes of claim 1, wherein said Herba Scutellariae Barbatae total flavones extract is made capsule, tablet, granule or injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200710047257A CN101167799B (en) | 2007-10-19 | 2007-10-19 | Scutellaria barbata total flavone and its application in preparing influenza virus resisting medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200710047257A CN101167799B (en) | 2007-10-19 | 2007-10-19 | Scutellaria barbata total flavone and its application in preparing influenza virus resisting medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101167799A true CN101167799A (en) | 2008-04-30 |
| CN101167799B CN101167799B (en) | 2012-09-05 |
Family
ID=39388647
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200710047257A Expired - Fee Related CN101167799B (en) | 2007-10-19 | 2007-10-19 | Scutellaria barbata total flavone and its application in preparing influenza virus resisting medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101167799B (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104644744A (en) * | 2014-10-21 | 2015-05-27 | 中山大学 | Scutellaria barbata extract as well as preparation method and application thereof |
| CN108703965A (en) * | 2018-06-26 | 2018-10-26 | 华东师范大学 | Application of the apiolin in preparing anti-influenza virus medicament |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100362008C (en) * | 2004-11-05 | 2008-01-16 | 王英锋 | Barbat skullcap general flavone preparation method and quality control method |
-
2007
- 2007-10-19 CN CN200710047257A patent/CN101167799B/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104644744A (en) * | 2014-10-21 | 2015-05-27 | 中山大学 | Scutellaria barbata extract as well as preparation method and application thereof |
| CN108703965A (en) * | 2018-06-26 | 2018-10-26 | 华东师范大学 | Application of the apiolin in preparing anti-influenza virus medicament |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101167799B (en) | 2012-09-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN107158063B (en) | Enteric-coated pellet prepared from honeysuckle effective part composition and preparation method thereof | |
| CN1754541A (en) | Steroid saponin pharmaceutical composition and its preparation method and uses | |
| CN102961439A (en) | Total flavone extract of Hyssopus officinalis, preparation method thereof and application thereof | |
| CN102961469B (en) | Traditional Chinese medicine dispersible tablet for treating upper respiratory infection, and preparation method and quality detection method thereof | |
| CN101011520A (en) | Method for preparing medicament containing trillium tschonoskii extractive and its application | |
| CN102068535A (en) | Immature bitter orange or bitter orange total flavonoids extract prepared by ethanol reflux and extraction and application thereof | |
| CN101023976B (en) | Medicine composition with anti-virus function | |
| CN101167799B (en) | Scutellaria barbata total flavone and its application in preparing influenza virus resisting medicine | |
| CN106729140B (en) | Compound preparation for treating influenza and preparation method thereof | |
| CN105037464A (en) | Plant flavone compounds, and preparation method and application thereof | |
| CN101028322B (en) | Use of Maoliefengdou extract for preparing anti-cancer medicine | |
| CN1775267A (en) | Kaikoujian extract, Its preparing method and use | |
| CN1817898A (en) | Use of anti-inflammatory medicine for scheelite total saponin and its saponin compound | |
| CN103405494B (en) | Bauhinia championii n-butyl alcohol extract and preparation method and application thereof | |
| CN104069344A (en) | Traditional Chinese medicine composition for treating cancer and preparation and preparation method thereof | |
| CN101134092A (en) | Traditional Chinese medicine compound preparations for treating respiratory disease and method for preparing the same | |
| CN105998041A (en) | Application of rosmarinic acid-4-O-beta-D-glucoside in preparing drug for preventing and treating flu | |
| CN1803179A (en) | Traditional Chinese medicine composition and its preparation method and quality control method | |
| CN102138957B (en) | Colocynth extract, and production method and application thereof | |
| CN104945460A (en) | Preparation method and applications of roxburic acid | |
| CN1165545C (en) | Method for separating and extracting total flavone from goldenrain tree plant and its application | |
| CN1460513A (en) | Jinlian Qingre capsule and its preparation method | |
| CN101816706B (en) | Chinese traditional medicament valid target composition for treating viral respiratory infection diseases | |
| CN111588742A (en) | Application of myrrh sesquiterpene extract in preparation of chronic obstructive pulmonary disease medicine | |
| CN104288223A (en) | Method for preparing total flavonoids of Chinese mosla herb and application of total flavonoids of Chinese mosla herb |
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: 20120905 Termination date: 20151019 |
|
| EXPY | Termination of patent right or utility model |