CN109260192A - Purposes of the qroxylin A in preparation prevention and treatment virus infection of respiratory system drug - Google Patents
Purposes of the qroxylin A in preparation prevention and treatment virus infection of respiratory system drug Download PDFInfo
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- CN109260192A CN109260192A CN201710586443.7A CN201710586443A CN109260192A CN 109260192 A CN109260192 A CN 109260192A CN 201710586443 A CN201710586443 A CN 201710586443A CN 109260192 A CN109260192 A CN 109260192A
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- qroxylin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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Abstract
The invention belongs to the field of Chinese medicines, are related to new application of the qroxylin A shown in following formula in pharmacy, and in particular to purposes of the qroxylin A in preparation prevention and treatment virus infection of respiratory system drug.The present invention is confirmed through whole animal model experiment, the qroxylin A infected by influenza infection induced mice acute lung injury has good therapeutic effect, the lung pathologies damage of viral mice with acute lung injury can be significantly improved, significantly improve mouse weight, significantly reduce mouse Lung Exponent and pulmonary lesion area, the therapeutic equivalence of its curative effect and the same dose of Scullcap total-flavonoids and aglycon baicalein, and its curative effect is significantly better than the same dose of scutellosides, can be further used for preparing new prevention and treatment virus infection of respiratory system drug.
Description
Technical field
The invention belongs to the field of Chinese medicines, are related to traditional Chinese medicine monomer qroxylin A in preparation and prevent and treat virus infection of respiratory system drug
In purposes.
Background technique
Data shows that virus infection of respiratory system infectiousness is strong, the death rate is high, sprawling is rapid, prevalence is extensive, easily causes big
Amount casualties, medical social security system are chaotic, property largely loses, and cause social fear etc..According to records, twentieth century is several
The atypical pneumonia (SARS) of secondary large-scale flu outbreak and outburst in 2003 causes serious consequence to society.It exhales
Desorption system virus infection can lead to body acute lung injury (ALI), and further development can be at acute respiratory distress syndrome
(ARDS), symptom is mainly shown as: the respiratory symptoms such as pharyngalgia, runny nose, nasal obstruction, cough and DOMS, fever, fear
The general reactions symptoms such as cold, headache, Nausea and vomiting, hyperpyrexia.Respiration system virus variation rapidly, is also easy to produce what height caused a disease
The appearance of strain and drug-resistant virus all makes virus infection of respiratory system be difficult to control.Influenza is the most common breathing system
System disease of viral infection, wherein influenza A virus is periodically broken out in crowd, and the most common influenza virus is H1N1
And H3N2.Although human knowledge's respiration system virus infection disease has last 100 years history, existing defence and treatment are exhaled
The medical science of desorption system virus infection (especially highly pathogenic respiration system virus) still seems very weak；Current anti-current
The susceptible generally existing a variety of toxic side effects of cytotoxic drug；Virus variation is rapid, and the vaccine research period is long, it is difficult to play in time effective
Protection effect.
Qroxylin A is the important flavone compound of one of baikal skullcap root, and it is anti-that research finds that qroxylin A has
Allergy, antitumor and anti-inflammatory etc. pharmacological activity.Baikal skullcap root is the common antipyretic and antidotal type Chinese medicine that " Chinese Pharmacopoeia " records, and is more
The dry root of year raw herbaceous plant radix scutellariae (Scutellaria baicalensis Georgi).Flavone compound is in radix scutellariae
Main chemical compositions and active constituent, mainly in the form of glycosides or aglycon exist, studies have found that Baical Skullcap root P.E, scutelloside
There is therapeutic effect to the chmice acute injury of lungs that influenza A virus induces with baicalein.But so far for qroxylin A to exhaling
There is not been reported for the treatment of desorption system disease of viral infection.
Status based on the prior art, the quasi- new application for providing qroxylin A in pharmacy of present inventor, specifically
It is related to purposes of the qroxylin A in preparation prevention and treatment virus infection of respiratory system drug.
Summary of the invention
The new application that the object of the present invention is to provide qroxylin As in pharmacy, and in particular to qroxylin A is anti-in preparation
Purposes in treating respiratory system virus infective medicament.
The molecular structure of qroxylin A of the present invention is as follows:
The present invention confirms that the qroxylin A infected by influenza infection induced mice is anxious through whole animal model experiment
Property injury of lungs has a good therapeutic effect, the therapeutic equivalence of curative effect and the same dose of Scullcap total-flavonoids and aglycon baicalein,
And its curative effect is significantly better than the same dose of scutellosides (P < 0.05), can be further used for preparing new prevention and treatment respiration system virus
Infection medicine.
The present invention prepares qroxylin A by following methods:
Dry radix scutellariae medicinal materials are taken, with 80% ethyl alcohol heating and refluxing extraction, combined extract is concentrated under reduced pressure into no alcohol taste, leaching
Cream adds water to be suspended；The macroporous absorbent resin of the preprocessed mistake of suspension adsorbs, and successively uses distilled water, 80% ethanol elution, collects
Dry Scullcap total-flavonoid is concentrated under reduced pressure in ethanol eluate；It is characterized through UPLC, wherein including scutelloside, baicalein and mica
The flavones ingredients such as plain A.
The present invention has carried out qroxylin A for preventing and treating the experiment in vivo of viral acute lung injury:
The present invention has carried out whole animal model experiment to study qroxylin A to viral mice with acute lung injury
The influence of weight and lung pathologies damage:
After selecting 5 week old SPF male BALB/c mouses, vein to give propofol injection anesthesia, collunarium infects influenza disease
Malicious mouse lung adapted strain establishes chmice acute model of lung injury, and wherein Normal group gives viral dilution, presses after 2h after infection
The drug of group oral administration gavage various concentration；
Experimental result shows that the qroxylin A can significantly mitigate the pathology damage of mouse lung, mitigates acute lung damage
Wound；Therapeutic effect and the same dose of Scullcap total-flavonoids and baicalein are suitable, but be substantially better than the same dose of scutellosides (P <
0.05)。
It is verified by experiments, qroxylin A involved in the present invention can prepare the drug of new treatment virus infection of respiratory system.
Detailed description of the invention
Fig. 1: influence of the qroxylin A to viral mice with acute lung injury weight.
Fig. 2: the influence that qroxylin A changes viral mice with acute lung injury lung pathologies.
Specific embodiment
Embodiment 1 prepares Scullcap total-flavonoid and qroxylin A
Dry radix scutellariae medicinal materials 1.2Kg is taken, three times with 80% ethyl alcohol heating and refluxing extraction, for the first time with 10 times of amount solvent extractions
2h, second and third time with 8 times of amount solvent extraction 1.5h, merge extracting solution three times, are concentrated under reduced pressure into no alcohol taste, obtain medicinal extract and add respectively
Water is suspended；The pretreated AB-8 macroporous absorbent resin absorption of suspension, successively with the distilled water of 3 times of bed volumes, 6 times of column beds
80% ethanol elution of volume collects ethanol eluate, and dry Scullcap total-flavonoid, yield 25.48% is concentrated under reduced pressure；Using super
High performance liquid chromatography (UPLC), characterizes Scullcap total-flavonoid obtained, and it includes flavone compound scutellosides, radix scutellariae
Element and qroxylin A, content are respectively 51.79%, 3.78% and 0.57%.
Therapeutic effect of 2 qroxylin A of embodiment to influenza A virus induction acute lung injury
5 week old SPF male BALB/c mouse 48 is selected, is randomly divided into 6 groups (A, B, C, D, E, F groups): A group by weight
For Normal group, B group is model group, C, D, E and F group respectively 100mg/kg Scullcap total-flavonoid, scutelloside, baicalein and
Qroxylin A, every group 8；All mouse tail vein injection propofol injection 0.026ml/10g, under mouse anesthesia state
Collunarium infects 30 μ l of H1N1 virus, and each 15 μ l of left and right nose, wherein Normal group gives viral dilution；Group is pressed after infecting 2h
The oral drug for giving various concentration, 0.1ml/10g are administered 4 days, and A, B group give 0.5%CMC-Na；Last time administration is for 24 hours
Afterwards, i.e., the 4th day (after 96h) materials；Conventional treatment mouse takes full lung, observes pulmonary lesion situation, with the progress of pulmonary lesion area
Lung scoring, and record, after lung weighing, superior lobe of right lung is taken to steep formalin, the observation for pathological section；
The changes of weight used in the present invention is that whether there is or not protective effects to viral mice with acute lung injury for evaluation drug
One macro-indicators；Normally group mouse spirit is good, and Quick off the mark is strong, and hair is glossy, and breathing, diet is normal, and weight is certainly
So increase；Other groups of mouse start to fall ill after infection three days, show as the inability that is slow in action, and breathing has some setbacks, and chilly is cold,
It can be clearly felt that mouse temperature rapid drawdown, feed are reduced with holding, weight drastically reduces；By the daily weight of mouse divided by sense
Dye same day weight draws changes of weight curve up to changes of weight rate, with the daily changes of weight rate of mouse, as the result is shown (as schemed
Shown in 1), the 4th day fall maximum of model group mouse body weight, and the fall of mouse weight after drug is given certain
It decreases in degree, compares other administration groups, it is maximum that scutelloside (100mg/kg) organizes weight loss amplitude；
Lung Exponent is the ratio of the lung weight and weight of mouse, and value is bigger to illustrate that lung lesion degree is more serious；With normal group
It compares, model group mouse Lung Exponent and lung scoring are significantly raised；It is aobvious to give mouse Lung Exponent and injury of lungs scoring after qroxylin A
Writing reduces, and compared with scutelloside group (100mg/kg), qroxylin A (100mg/kg) can significantly reduce viral acute lung injury
Mouse lung scores (as shown in table 1).
Influence result of 1 qroxylin A of table to mouse pneumonia
P < 0.001 compared with model group * P < 0.01 compared with model group, * * *；
#P < 0.05 compared with scutelloside group
Lung Exponent=(mouse lung weight/mouse weight) × 100%
Pathological examination results show normally to organize alveolar clear-cut, there is more complete alveolar structure, no oozing phenomenon, base
This no inflammation；Model group pathological section shows that alveolar wall obviously thickens, alveolar collapse deformation, a large amount of leukocyte recruitments, and inflammation is tight
Weight；100mg/kg Scullcap total-flavonoid, baicalein and qroxylin A administration group can be seen that clearly alveolar profile, have
Whole alveolar structure, no severe haemorrhage phenomenon, inflammatory symptom significantly mitigate；100mg/kg scutelloside group alveolar wall partial thickening,
The inflammatory phenomenas such as inflammatory cell infiltration are mitigated, it can be seen that clearly alveolar profile (as described in Figure 2).
The present invention our experiments show that, the qroxylin A has apparent therapeutic effect, energy to viral acute lung injury
The lung pathologies damage for significantly improving viral mice with acute lung injury, significantly improves mouse weight, significantly reduces mouse lung and refers to
Several and pulmonary lesion area；Scutelloside is the main compound in radix scutellariae, and existing research shows that virus can be effectively relieved in scutelloside
Property acute lung injury, but experimental result of the present invention confirm, therapeutic effect of the qroxylin A to viral acute lung injury
Significantly better than scutelloside, the qroxylin A can prepare new prevention and treatment virus infection of respiratory system drug.
Claims (4)
1. purposes of the qroxylin A shown in following formula in preparation prevention and treatment virus infection of respiratory system drug,
2. by purposes described in claim, which is characterized in that the qroxylin A mitigates influenza infection induced mice
Acute lung injury.
3. by purposes described in claim, which is characterized in that the qroxylin A mitigates caused by influenza infection
The pathology damage of mouse lung.
4. by purposes described in claim, which is characterized in that the qroxylin A is prepared by following methods,
Dry radix scutellariae medicinal materials are taken, three times with 80% ethyl alcohol heating and refluxing extraction, for the first time with 10 times of amount solvent extraction 2h, second,
Merged extracting solution three times with 8 times of amount solvent extraction 1.5h respectively three times, be concentrated under reduced pressure into no alcohol taste, obtain medicinal extract and water is added to be suspended；It is mixed
Suspension pretreated AB-8 macroporous absorbent resin absorption, successively with the distilled water of 3 times of bed volumes, 6 times of bed volumes
80% ethanol elution collects ethanol eluate, and dry Scullcap total-flavonoid, yield 25.48% is concentrated under reduced pressure；Using ultra high efficiency liquid
Phase chromatography (UPLC), characterizes Scullcap total-flavonoid obtained, and it includes flavone compound scutelloside, baicalein and thousand
Layer paper factor A, content is respectively 51.79%, 3.78% and 0.57%.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710586443.7A CN109260192A (en) | 2017-07-18 | 2017-07-18 | Purposes of the qroxylin A in preparation prevention and treatment virus infection of respiratory system drug |
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| CN201710586443.7A CN109260192A (en) | 2017-07-18 | 2017-07-18 | Purposes of the qroxylin A in preparation prevention and treatment virus infection of respiratory system drug |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117462571A (en) * | 2023-06-28 | 2024-01-30 | 扬子江药业集团江苏龙凤堂中药有限公司 | Pharmaceutical composition and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106860471A (en) * | 2015-12-13 | 2017-06-20 | 复旦大学 | A kind of purposes of AhR receptor proteins inhibitor in antiviral drugs is prepared |
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2017
- 2017-07-18 CN CN201710586443.7A patent/CN109260192A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106860471A (en) * | 2015-12-13 | 2017-06-20 | 复旦大学 | A kind of purposes of AhR receptor proteins inhibitor in antiviral drugs is prepared |
Non-Patent Citations (2)
| Title |
|---|
| S HEROLD等: "Influenza virus-induced lung injury: pathogenesis and implications for treatment", 《EUROPEAN RESPIRATORY JOURNAL》 * |
| 郑艳红: "两种不同规格黄芩提取物制备工艺及质量标准研究", 《中国优秀硕士学位论文全文数据库 医药卫生科技辑》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117462571A (en) * | 2023-06-28 | 2024-01-30 | 扬子江药业集团江苏龙凤堂中药有限公司 | Pharmaceutical composition and application thereof |
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